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Item 1. Business

2026-03-16 compared with 2025-03-26 · 211 added, 124 removed, 318 unchanged (51% of the section changed)

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We were incorporated in the state of Delaware on January 3, 2011.

During 2015, HealthCare Pharmaceuticals Pty Ltd.

(“HCP Australia”) was formed and is our wholly owned subsidiary.

On December 10, 2015, we entered into a merger agreement with GITR Inc.

(“GITR”), an entity under common control, whereby a wholly owned subsidiary was merged with GITR and the surviving name of the wholly owned subsidiary was GITR Inc.

On August 29, 2016, we entered into a merger agreement with Macrocure Ltd.

(“Macrocure”), a publicly held, clinical-stage biotechnology company based in Petach Tikva, Israel.

In connection with the merger, Macrocure became our wholly owned subsidiary and we applied to be listed on the Nasdaq Global Market.

Nasdaq approved the listing, and trading in our common stock commenced on January 24, 2017, under the trading symbol “LPTX.” On February 1, 2017, Macrocure’s name was changed to Leap Therapeutics Ltd.

In 2020, Leap Therapeutics Ltd.

was dissolved.

On December 15, 2021, Leap Securities Corp.

was formed and is our wholly owned subsidiary.

On January 17, 2023, we entered into a merger agreement with Flame Biosciences, Inc., a privately held, biotechnology corporation (“Flame”), whereby Flame became a wholly owned subsidiary under the name Flame Biosciences, LLC.

We are a biopharmaceutical company developing novel biomarker-targeted antibody therapies designed to treat patients with cancer by inhibiting fundamental tumor-promoting pathways, targeting cancer-specific cell surface molecules, and harnessing the immune system to attack cancer cells.

Our strategy is to identify, acquire, and develop molecules that will rapidly translate into high impact therapeutics that generate durable clinical benefit and enhanced patient outcomes.

Our lead clinical stage drug candidate is sirexatamab (DKN-01), a monoclonal antibody that inhibits Dickkopf-related protein 1 (“DKK1”).

We are currently studying sirexatamab in a clinical trial in patients with colorectal cancer.

We also have a preclinical program to develop a proprietary monoclonal antibody that we call FL-501.

FL-501 works by inhibiting the GDF-15 protein.

We intend to apply our extensive experience identifying and developing transformational products to build a pipeline of programs that have the potential to change the practice of cancer medicine.

Cancer is the general name for a group of more than 100 diseases in which cells grow and divide out of control.

Over 16 million people in the United States have cancer.

The National Cancer Institute (“NCI”) estimated that over 2.0 million people developed cancer and that nearly 612,000 people died of cancer in 2024.

While progress has been made from the War on Cancer to the Human Genome Project, and despite advances in early detection and new cancer cell targeted treatments, cancer generally remains an incurable disease.

Our wholly owned subsidiaries as of December 31, 2025 include HealthCare Pharmaceuticals Pty Ltd.

(“HCP Australia”), Leap Securities Corp., Flame Biosciences LLC, and Leap Therapeutics, Inc.

Prior to October 2025, we devoted substantially all of our resources to development efforts related to biomarker-targeted antibody therapies designed to treat patients with cancer.

Our clinical stage program is sirexatamab (DKN-01), a monoclonal antibody that inhibits Dickkopf-related protein 1, or DKK1, for the treatment of colorectal cancer patients.

We also have a preclinical antibody program, FL-501, that is designed to treat cachexia-related indications.

In October 2025, we announced a $58.88 million private placement, led by Winklevoss Capital, and the intent to initiate a digital asset treasury strategy.

Immediately following the financing, we initiated a strategy to deploy a portion of our capital raised that is not required to provide working capital for our ongoing operations to accumulate digital assets, focused on Zcash.

Zcash is a protocol and blockchain network of connected devices all over the world, working together to validate transactions and maintain the Zcash ledger.

ZEC is the monetary unit, or coin, of Zcash.

Zcash allows for transactional privacy, providing users with options for fully shielded transactions in which the sender, recipient, and amount are encrypted.

On November 12, 2025, we changed our name from “Leap Therapeutics, Inc.” to “Cypherpunk Technologies Inc.” and changed our trading symbol from “LPTX” to “CYPH”.

We were renamed to Cypherpunk to reflect the strategic focus on acquiring ZEC, participating in the development of Zcash, and the values of privacy and liberty.

Our ongoing biotechnology research and development operations are conducted under a wholly-owned subsidiary named “Leap Therapeutics, Inc.”.

We are a privacy technology company implementing a digital asset treasury strategy anchored by Zcash and, through our subsidiary Leap, are developing novel therapies for patients with cancer.

Overview of Cypherpunk

Cypherpunk is a privacy technology company.

Our mission is to advance technologies that guarantee privacy for all humans on the internet.

Our vision is a future where technology defends self-sovereignty and secures human freedom.

We are not a typical digital asset treasury company.

While we hold digital assets as part of our strategy, our core business is identifying, developing, investing in, and, where appropriate, acquiring or building privacy-enhancing technologies.

Our initial and primary focus is the Zcash ecosystem, which we believe represents the most mature implementation of private digital money.

Over time, we intend to assemble a portfolio of complementary privacy technologies that, together, are designed to secure privacy for individuals across the digital economy.

We believe that privacy is a precondition for the meaningful exercise of individual freedoms, including freedom of speech, thought, and association.

As digital systems expand and personal data generation accelerates, we believe demand for privacy-preserving infrastructure will grow and that the companies and protocols best positioned to provide it will capture significant long-term value.

There are public companies focused on delivery, social networking, search, payments, and entertainment, among other sectors.

To our knowledge, there is no publicly traded company whose core mission is the advancement of privacy technology.

We intend to fill that gap.

Our strategy is to combine disciplined capital allocation with active investment in privacy infrastructure, positioning the Company to benefit from what we believe is a structural increase in global demand for privacy-preserving technologies as digital surveillance capabilities expand and the volume of personal data generated continues to grow.

Privacy Strategy

We are focused on identifying, developing, and investing in privacy-enhancing technologies that address the growing global demand for data protection, digital autonomy, and secure communications.

We believe that privacy is an increasingly vital component of the digital economy and that technologies enabling responsible data protection, user control, and cryptographic security will play a critical role in future digital infrastructure.

We intend to execute a broad corporate strategy designed to make Cypherpunk a globally recognized leader in the privacy field.

We believe that demand for privacy-enhancing technologies will increase as digital systems expand and data generation accelerates.

Our objective is to position Cypherpunk as a disciplined capital allocator and strategic partner in this sector, supporting innovation while maintaining a focus on sustainable value creation and risk management.

Zcash Overview

Zcash is a cryptographic digital asset that operates on a decentralized, open-source blockchain network known as the Zcash Network.

The network consists of a distributed group of independent computers that collectively maintain and validate a shared transaction ledger.

No central authority owns, controls, or operates the Zcash Network;

instead, its infrastructure and rules are maintained through consensus among network participants.

Transactions on the Zcash Network are recorded on a publicly accessible blockchain.

ZEC functions as the native unit of value on the network and may be used to transfer value between users, pay transaction fees, or facilitate exchange for fiat currencies or other digital assets through trading platforms or private transactions.

Zcash was launched in 2016 using a modified version of the Bitcoin codebase, with a fixed maximum supply of 21 million coins.

Its distinguishing technical feature is the use of zero-knowledge proofs (zk-SNARKs), which allow transactions to be validated by the network without revealing the sender, receiver, or transaction amount.

This cryptographic approach has been adopted or referenced by other blockchain projects, including Ethereum and Solana.

The Zcash protocol has undergone several upgrades since launch, including the introduction of Halo 2, a recursive proof system that eliminates the need for trusted setup ceremonies.

Since inception, Zcash has processed tens of millions of transactions and has generally ranked among the larger privacy-focused digital assets by market capitalization.

Privacy-Preserving Transaction Features

Zcash was developed to advance blockchain technology.

A core feature of the Zcash Network is optional privacy:

the protocol supports both transparent transfers, which disclose transaction data in a manner similar to many other blockchains like Bitcoin, and privacy-preserving transfers that allow users to selectively disclose information associated with a transaction.

Privacy on Zcash is enabled through zero-knowledge cryptography which can conceal transaction amounts and counterparties while still permitting network validation.

Transactions using these privacy features are commonly referred to as “shielded” transactions.

As of December 31, 2025 approximately 31% of all ZEC was shielded.

Since the launch of the Zcash Network in 2016, the amount of shielded ZEC has been consistently growing suggestive of utility and adoption of Zcash’s advantage to other blockchain networks without enhanced privacy, such as Bitcoin.

Zcash History, Network Development, and Governance

Zcash was launched on October 28, 2016 by scientists, advisers, and engineers affiliated with Electric Coin Company (“ECC”) (formerly the Zcash Company) as a new blockchain network based on the Bitcoin codebase but designed with enhanced privacy functionality.

Rather than created through a true network fork, Zcash was independently launched using a modified version of Bitcoin’s underlying software architecture.

As a result, ownership of bitcoin did not confer ownership of ZEC at the time of launch.

From its launch through early 2026, ECC played a significant role in supporting protocol research and development, including advancing scalability and usability improvements and contributing to upgrades that became part of the primary Zcash client implementation.

This development model was broadly comparable to the role played by core developer communities in other open-source blockchain ecosystems, although ultimate adoption of changes depended on the decentralized network.

Ongoing development of the Zcash protocol is supported by a combination of open-source contributors and organizations that propose, review, and implement software updates.

Changes to the protocol are adopted only if accepted by the broader network, and participants may choose whether to implement proposed upgrades.

The protocol has been upgraded over time to improve the usability, efficiency, and security of shielded transactions.

In January 2026, all employees of ECC resigned from their positions following a governance dispute with the board of Bootstrap, the nonprofit organization that had overseen ECC.

The former ECC team, led by former CEO Josh Swihart, subsequently announced the formation of a new company, Zcash Open Development Lab (ZODL) to continue Zcash protocol development.

In connection with this transition, the Bootstrap board authorized the transfer of the Zashi wallet technology and related intellectual property to the new entity, and announced an orderly wind-down of ECC.

Certain digital assets, including the Z.cash domain and the official Zcash social media accounts, were transferred to the Zcash Foundation.

In February 2026, ZODL released an update to the Zashi wallet and renamed the wallet Zodl.

ZODL aims to make Zcash easier to use, with continued development of the wallet as well as supporting Zcash at the protocol level.

We believe that Zodl represents critical privacy infrastructure and will support the adoption of Zcash and demand for ZEC.

On March 9, 2026, ZODL announced a financing of over $25 million with investments from a16z, Winklevoss Capital, Coinbase, Paradigm, Chapter One, David Friedberg, Balaji Srinivasan, and others.

We invested $5 million in ZODL as part of our commitment to the Zcash ecosystem and the team with the leading Zcash wallet and development expertise.

Zcash Decentralization and Mining

Zcash functions on a distributed network architecture that allows participants to transact directly without reliance on centralized authorization, clearing entities, or custodial intermediaries.

The issuance of ZEC and the validation of transactions are governed by protocol-defined rules embedded in the network software rather than by discretionary actions of any organization.

No single entity controls or operates the Zcash Network.

Prices for ZEC are not fixed or managed by any party and instead emerge from trading activity across digital asset marketplaces and from negotiated transactions between counterparties.

Transaction integrity on the Zcash Network is maintained through a computational consensus process in which independent participants, known as miners, compete to confirm transfers and record them in sequential data structures, known as blocks.

These blocks collectively form the Zcash blockchain, which serves as a continuously updated record of confirmed network activity.

To generate a block, miners compete by performing computational work defined by the protocol, selecting unconfirmed transactions and proposing a valid block for network acceptance.

Transaction data is propagated across the network, evaluated under consensus rules, and permanently recorded once accepted.

Only one miner succeeds in adding each block, and the protocol dynamically adjusts mining difficulty to maintain consistent block timing as total network hash power fluctuates.

Miners are economically incentivized through protocol-defined rewards, consisting of newly issued ZEC and transaction fees associated with the transactions included in a block.

New blocks are produced at an average interval of approximately 1.25 minutes, with block rewards allocated probabilistically based on the relative computing power contributed by individual miners or mining pools.

Once validated by network nodes, the block is appended to the blockchain, and the associated reward is issued to the successful miner.

This process governs transaction finality and represents the sole mechanism through which new ZEC is introduced into circulation.

ZEC Transactions

The Zcash Network accommodates both standard transactions that disclose details on the blockchain and privacy-focused transactions that limit public visibility of transaction information.

Users who interact directly with the network typically do so through a “wallet”, which generates cryptographic credentials and enables the sending and receipt of ZEC.

Each wallet is controlled by private keys, and possession of the relevant private key is required to authorize transfers;

loss or compromise of those keys may result in permanent loss of access to the associated ZEC.

Privacy-enabled Zcash transfers employ zero-knowledge cryptographic methods which allow transactions to be validated without revealing transaction amounts or counterparties.

These mechanisms enable the network to confirm authorization and prevent double spending while preserving confidentiality.

In addition to on-chain transfers, some ZEC ownership changes occur off-chain, such as internal ledger movements within exchanges or custodial platforms.

Because these off-chain activities are not recorded on the blockchain, they are not protected by the protocol’s consensus mechanisms and may expose participants to additional counterparty and operational risks.

Maximum Supply and Halving Schedule

The Zcash protocol establishes a fixed maximum supply of 21 million ZEC, which are introduced into circulation over time through block rewards.

New ZEC is issued as part of the mining process at regular intervals.

The block subsidy is reduced by 50% at predetermined intervals, commonly referred to as “halvings,” which occur based on block height rather than calendar date and are designed to slow the rate of new issuance over time.

Since its launch, Zcash has undergone multiple halving events.

The first occurred in November 2020, reducing the block reward from 6.25 ZEC to 3.125 ZEC.

The second halving occurred in November 2024, further reducing the block reward to 1.5625 ZEC.

Future halvings are expected to occur at approximately four-year intervals thereafter based on the current network hash rate, with each event continuing to reduce the rate of new ZEC issuance until the maximum supply is reached.

The market price of ZEC is determined by supply and demand for ZEC among buyers and sellers and the overall utility of the Zcash Network, and is typically quoted in fiat currencies or relative to other digital assets on trading platforms.

Centralized exchanges generally publish real-time pricing and volume data that serve as common market reference points.

ZEC may also be traded through over-the-counter arrangements or private transactions, which are typically less transparent than exchange-based trading.

As of December 31, 2025, the following exchanges have been registered as money services businesses with FinCEN, and have state money transmitter licensing:

Coinbase, Kraken, Binance.US, and Gemini Space Station, which is an affiliate of our largest stockholder, Winklevoss Capital.

However, there are several additional exchanges that trade ZEC including:

KuCoin, Binance (Global), OKX, Bitget and Gate.io.

Our ZEC Digital Asset Treasury Holdings

Our investment thesis for ZEC rests on two premises.

First, Zcash is built on the same sound monetary principles as Bitcoin:

a fixed supply of 21 million coins, open-source development, and decentralized consensus, but adds privacy-preserving transaction capabilities through zero-knowledge cryptography.

We view Bitcoin as a store of value and Zcash as private digital money:

one protects value across time, the other protects privacy in daily transactions.

Second, we believe that the market has not yet priced in the growing structural demand for financial privacy.

Transaction data reveals patterns of life:

location, associations, habits, and financial capacity.

As data collection and surveillance capabilities expand, we expect demand for privacy-preserving financial infrastructure to increase.

Zcash, as the most technically mature privacy-preserving blockchain with a fixed monetary supply, is, in our view, well-positioned to capture a meaningful share of that demand.

As of March 11, 2026, we held a total of 294,743.10 ZEC, at an average purchase price of $335.89, representing approximately 1.76% of the total circulating supply of the Zcash Network.

Our stated objective is to accumulate holdings representing at least 5% of the total circulating supply over time.

This objective is subject to change, and we may suspend, reduce, or modify acquisition activity at any time based on our assessment of market conditions, capital availability, and strategic priorities.

Competition Related to our Cypherpunk Business

The privacy technology, cryptocurrency, and digital asset treasury industries are characterized by continuing technological advancement and significant competition.

Our digital asset treasury strategy involves, from time to time and subject to market conditions, acquiring ZEC using proceeds from offerings of equity securities or other capital raising transactions.

While we believe that our focus on privacy technologies and the Zcash Network provides us with competitive advantages, we compete for capital with, among others:

Exchange Traded Products, such as Grayscale Zcash Trust;

other digital assets with a larger market value than ZEC, such as bitcoin;

digital asset treasury companies focused on other digital assets, such as Strategy Inc.;

digital asset exchanges that sell ZEC directly to investors;

traditional financial firms that have entered into the digital assets market;

and other entities that pursue strategies to accumulate or gain exposure to digital assets.

In addition, numerous venture capital firms have established investment strategies around privacy technologies and digital assets, including a16z crypto.

Many of the entities against which we may compete for capital or for investment in or development of privacy technologies have significantly greater financial resources and expertise than we do.

This competition could adversely affect the availability and cost of capital for our ZEC purchases and our privacy technology strategy, and thereby could affect the market price of our securities.

Government Regulation Related to our Cypherpunk Business

Congress and a number of U.S.

federal and state agencies (including FinCEN, the Treasury Department Office of Foreign Assets Control (“OFAC”), SEC, CFTC, the Financial Industry Regulatory Authority (“FINRA”), the Consumer Financial Protection Bureau (“CFPB”), the Department of Justice, the Department of Homeland Security, the Federal Bureau of Investigation, the U.S.

Internal Revenue Service, a bureau of the U.S.

Department of the Treasury (the “IRS”), the Office of the Comptroller of the Currency, the Federal Deposit Insurance Corporation, the Federal Reserve and state financial institution and securities regulators) have been examining, among other issues:

digital asset market structure and regulation, and a bill known as the Digital Assset Market Clarity Act of 2025 is currently under consideration in Congress;

and the operations of digital asset networks and digital asset users, with particular focus on the extent to which digital assets can be used to launder the proceeds of illegal activities, evade sanctions or fund criminal or terrorist enterprises and the safety and soundness of trading platforms and other service providers that hold or custody digital assets for users.

Various foreign jurisdictions have, and may continue to, in the near future, adopt laws, regulations or directives that affect the Zcash Network and its users.

For example, beginning on July 1, 2027, regulations in the European Union will prohibit transactions involving anonymous wallets and privacy-focused digital assets such as ZEC.

There remains significant uncertainty regarding foreign governments’ future actions with respect to the regulation of digital assets, particularly digital assets with privacy features such as Zcash.

Such laws, regulations or directives may conflict with those of the United States and may negatively impact the acceptance of ZEC by users, merchants, and service providers outside the United States and may therefore impede the growth or sustainability of the Zcash ecosystem in the United States and globally, or otherwise negatively affect the value of the ZEC that we hold in our treasury.

Drug Development Through Our Leap Therapeutics Subsidiary

Our subsidiary, Leap, is a biopharmaceutical company developing novel biomarker-targeted antibody therapies designed to treat patients with cancer and other diseases with high unmet medical need.

Our lead program is sirexatamab (DKN-01), a monoclonal antibody that inhibits Dickkopf-related protein 1 (“DKK1”).

We recently completed a Phase 2 study of sirexatamab in patients with colorectal cancer.

We also have a preclinical program to develop a monoclonal antibody inhibiting the GDF-15 protein, known as FL-501.

FL-501 has potential to treat patients with a broad variety of difficult-to-treat diseases such as:

cancer cachexia, hyperemesis gravidarum and pregnancy-related nausea and vomiting, and many others associated with aging and frailty.

Market Opportunity

Colorectal Cancer

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Mutations in the pathways modulated by DKK1, such as APC, and activation of the Wnt pathway are highly prevalent in CRC patients.

CRCs belonging to the consensus molecular subtype 2 (“CMS2”) are specifically characterized by hyperactivation of Wnt signaling.

CMS2 is most seen in cancers in the distal colon and rectum.

For patients who have non-microsatellite instability-high (“MSI-H”) colorectal cancer, and who do not have a specific mutation that can be targeted

with approved therapies, outcomes are extremely poor for patients who have progressed on first-line therapy.

A clinical trial of the antibody bevacizumab in combination with chemotherapy generated a response rate of approximately 5% and PFS of 5.7 months.

In 2024, according to company estimates, there were roughly 45,000 and 265,000 first-line treated patients and roughly 30,000 and 160,000 second-line treated patients for advanced CRC in the United States and top 7 non-US markets, respectively.

We estimate that roughly 50% of second-line treated patients did not receive first-line anti-VEGF therapy.

We also estimate that the relevant DKK1-high population would be 25% of second-line CRC patients.

For patients who have microsatellite stable (“MSS”) colorectal cancer, and who do not have a specific mutation that can be targeted with approved therapies, outcomes are extremely poor for patients who have progressed on first-line therapy.

A clinical trial of the antibody bevacizumab in combination with chemotherapy generated a response rate of approximately 5% and PFS of 5.7 months in second-line patients.

Our Product and Clinical Studies

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DKK1 also has a role in suppressing the immune system from effectively targeting and clearing the cancer.

Published data, including from The Cancer Genome Atlas (“TCGA”) and real world evidence from our collaboration with Tempus, indicate that DKK1 levels are significantly higher or have an important high DKK1 population in many cancers, including esophagogastric cancer (“EGC”), non-small cell lung cancer (“NSCLC”), endometrial cancer, CRC, and pancreatic cancer.

Published data, including from The Cancer Genome Atlas (“TCGA”) and real world evidence from our collaboration with Tempus, indicate that DKK1 levels are significantly higher or have an important high DKK1 population in many cancers, including esophagogastric cancer, non-small cell lung cancer, endometrial cancer, CRC, and pancreatic cancer.

In addition, elevated DKK1 is associated with worse overall survival or time to treatment discontinuation for patients with CRC and several other cancers.

Researchers have shown that when the DKK1 protein is added in certain animal models, the cancer grows larger.

Publications have also demonstrated a role for DKK1 in maintaining an environment around a tumor that suppresses the immune system’s ability to clear the tumor and to prevent metastasis.

DKK1 has been shown to activate the suppressive effects of myeloid–derived suppressor cells (“MDSC”).

Other published data has shown that metastatic tumor cells with stem cell-like features avoid the immune system by overexpressing DKK1 and secreting it out of the cell.

Secreted DKK1 can then down-regulate certain molecules on tumor cells known as natural killer cell activating ligands, that would activate the immune system, causing these cancer cells to remain invisible to natural killer cells (“NK cells”) and evade the immune system.

We have also identified DKK1 as being involved with the activity of T regulatory cells that can suppress anti-tumor T lymphocytes (“T cells”).

Through these multiple activities, research has shown that DKK1 helps protect the cancer cells from being targeted by the immune system.

Preclinical studies that we and others have conducted demonstrated that using an anti-DKK1 antibody can lead to clinical benefits in xenograft cancer models.

The anti-DKK1 antibody is believed to shift cell signaling in multiple cell types, thereby resulting in an anti-tumor immune effect.

In these models, researchers demonstrated that an anti-DKK1 antibody allowed the immune system to recognize and attack the cancer cells.

We believe that the more selective and local the activity is to the tumor, the more likely a drug will be safe and well tolerated and a potential combination partner to other anti-cancer drugs.

Further, our preclinical and clinical data suggests that sirexatamab upregulates PD-L1, suggestive of synergy in combination with an anti-PD1/PD-L1 therapy.

Sirexatamab is a high affinity, neutralizing monoclonal antibody targeting DKK1.

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The FDA granted orphan drug designation to sirexatamab for the treatment of gastric and gastroesophageal junction cancer.

In addition, on September 24, 2020, the FDA granted Fast Track designation to sirexatamab in combination with BeiGene’s tislelizumab for the treatment of patients with gastric and gastroesophageal junction adenocarcinoma whose tumors express high DKK1, following disease progression on or after prior fluoropyrimidine- and platinum- containing chemotherapy and if appropriate, human epidermal receptor growth factor (HER2)/neu-targeted therapy.

We are currently developing sirexatamab in a clinical trial in patients with colorectal cancer and have also conducted clinical trials in patients with gastric/gastroesophageal junction cancer and endometrial cancer patients.

In addition, on September 24, 2020, the FDA granted Fast Track designation to sirexatamab in combination with tislelizumab for the treatment of patients with gastric and gastroesophageal junction adenocarcinoma whose tumors express high DKK1, following disease progression on or after prior fluoropyrimidine- and platinum- containing chemotherapy and if appropriate, human epidermal receptor growth factor (HER2)/neu-targeted therapy.

We are currently developing sirexatamab in patients with CRC and have also conducted clinical trials in patients with gastric/gastroesophageal junction cancer and with endometrial cancer.

Colorectal Cancer

Mechanism of Action and Preclinical Data

We have evaluated sirexatamab in multiple preclinical CRC models.

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Treatment with sirexatamab can result in tumor regressions as a monotherapy and can overcome 5-FU-resistance to have further activity in combination with 5-FU chemotherapy.

We believe that these 5-FU-resistant models are reflective of the second-line CRC population currently being recruited in the DeFianCe clinical study.

Supportive of anti-angiogenic activity, preclinical models have also shown fewer and smaller blood vessels in response to sirexatamab treatment, and an additive effect of sirexatamab + bevacizumab at reducing xenograft tumor size.

DeFianCe Study –Second Patients Combination with bevacizumab and chemotherapy

The DeFianCe study is a Phase 2, randomized, open-label, multicenter study of DKN-01 in combination with standard of care bevacizumab and chemotherapy in patients with advanced microsatellite stable (“MSS”) CRC who have received one prior systemic therapy.

Part A of the study enrolled 33 patients.

Based on the results of these first 33 patients, the study expanded into a 188-patient randomized controlled trial against bevacizumab and standard of care chemotherapy.

The primary objective is progression-free survival (“PFS”).

Secondary objectives include overall response rate (“ORR”), duration of response (“DoR”), and overall survival (“OS”), including in the exploratory populations of patients with high DKK1 and who have had no prior anti VEGF therapy.

In January 2025, we presented updated ORR and PFS data from Part A of DeFianCe.

We believe that these 5-FU-resistant models are reflective of the second-line CRC population.

We believe that sirexatamab also work through an anti-angiogenic mechanism of action, preclinical models have also shown fewer and smaller blood vessels in response to sirexatamab treatment, and an additive effect of sirexatamab in combination with bevacizumab at reducing xenograft tumor size.

DeFianCe Study –Second-Line Patients in combination with bevacizumab and chemotherapy

The DeFianCe study is a Phase 2, randomized, open-label, multicenter study of sirexatmab (DKN-01) in combination with standard of care bevacizumab and chemotherapy in patients with advanced microsatellite stable (“MSS”) CRC who have received one prior systemic therapy.

Part A of the study enrolled 33 patients as a single arm trial.

Based on the results of these first 33 patients, the study expanded into Part B, a 188-patient randomized controlled trial against bevacizumab and standard of care chemotherapy.

Part A – Single Arm

In January 2025, we presented ORR and PFS data from Part A of DeFianCe.

In the 27 response-evaluable patients, the ORR was 33% and the disease control rate (“DCR”) was 93%.

Of these responding patients, the median DoR experienced was 9.92 months.

The 21 patients with CRC originating on the left side of the colon or rectum experienced an ORR of 38%, a DCR of 100%, and median PFS of 8.64 months.

In the 15 patients who had never received prior bevacizumab, the ORR was 53%, the DCR was 93%, and their median PFS was 8.05 months.

On March 26, 2025, we reported updated preliminary clinical data from Part B of the randomized and controlled DeFianCe Study.

Part B – Randomized Controlled Trial

In October 2025, we presented final clinical data from Part B at the European Society for Medical Oncology (ESMO) Congress 2025.

In patients with high circulating DKK1 plasma levels (upper quartile as measured by the SomaLogic SomaScan platform, n=44), the sirexatamab experimental arm has improved ORR, by both investigator-assessment (“IA”) and blinded independent central review (“BICR”), PFS, and OS compared to the control arm:

Experimental Arm

Patients remaining on study drug

PFS K-M curve in DKK1-high upper quartile patients

OS K-M curve in DKK1-high upper quartile patients

● In patients with high circulating DKK1 plasma levels (upper median as measured by the SomaLogic SomaScan platform, n=88), the sirexatamab experimental arm has improved ORR, by both IA and BICR, PFS, and OS compared to the control arm:

Experimental Arm

Patients remaining on study drug

In patients who had not received prior anti-VEGF therapy (n=95), the sirexatamab experimental arm (n=49) has improved ORR, PFS and OS compared to the Control Arm:

Experimental Arm

Patients remaining on study drug

Across the intent-to-treat (ITT) population with second-line MSS CRC (n=188), the sirexatamab experimental arm had improved ORR compared to the control arm, with PFS and OS still to mature due to the high number of patients remaining on study drug:

● Across the intent-to-treat (ITT) population with second-line MSS CRC (n=188), the sirexatamab experimental arm had higher ORR and longer PFS compared to the control arm, although this did not reach the pre-defined statistical signficance:

Experimental Arm

Patients remaining on study drug

DKK1 levels correlated with increasing clinical benefit in those patients receiving DKN-01 compared to Control patients in the control arm who did not.

In addition, patients in the experimental arm with lung metastases had an ORR advantage relative to patients with lung metastases in the control arm (36% vs 13%, n=90) and patients in the experimental arm with liver metastases had an ORR

advantage relative to patients with liver metastases in the control arm (37% vs 28%, n=136).

Prior immunotherapies have been shown to typically perform poorly in treating patients with lung metastases or liver metastases.

Gastric / Gastroesophageal Junction Cancer

DisTinGuish Study - Part C –– First Line Randomized Controlled Trial combination with tislelizumab and SOC chemotherapy

In collaboration with BeiGene, we conducted P205, the DisTinGuish study, a three-part Phase 2 study of DKN-01 in combination with tislelizumab in patients with inoperable, locally advanced, gastric and gastroesophageal junction adenocarcinoma (“GEA”).

Part C of the DisTinGuish study enrolled 170 first-line, HER2-negative GEA patients.

Patients were randomized to receive either DKN-01 in combination with tislelizumab and SOC chemotherapy or to receive tislelizumab and SOC chemotherapy.

The primary objective was to determine the effect of adding DKN-01 on the endpoint of median PFS in DKK1-high patients (defined as DKK1 TPS > 20) and in all patients.

Secondary objectives of Part C included OS and ORR as measured by RECIST v1.1 in DKK1-high and all patients.

Enrollment began in October 2022 and was completed in December 2023.

In January 2025, we reported results of Part C.

While demonstrating activity in biomarker populations, the study did not generate a clear positive signal and we believe the study will be negative on the primary PFS endpoints when it completes, resulting in the decision not to move forward with Phase 3 studies in gastric cancer.

Across the Intent-to-Treat (“ITT”) population (n=170), patients treated with sirexatamab plus tislelizumab and chemotherapy (experimental arm, n=85) had a confirmed ORR of 52% by both IA and BICR, while patients treated with tislelizumab and chemotherapy alone (control arm, n=85) had a confirmed ORR of 56% by IA and 42% by BICR.

By BICR, patients in the experimental arm with DKK1-high tumors (n=22) had a confirmed ORR of 59%, compared to 36% in the control arm (n=22) and patients in the experimental arm with PD-L1-negative tumors (n=18) had a confirmed ORR of 44% compared to 32% in the control arm (n=19).

In the ITT population, preliminary median PFS in the experimental arm was 9.72 months by BICR and 7.66 months by IA compared to 11.99 months by BICR and 10.41 months by IA in the control arm.

The median PFS for tislelizumab plus chemotherapy in the Phase 3 Rationale-305 study was 6.9 months (95% CI:

In the DKK1-high population, preliminary median PFS in the experimental arm was 7.72 months by BICR and 7.43 months by IA compared to 7.79 months by BICR and 11.14 months by IA in the control arm.

The hazard ratio for PFS by BICR was 0.68, representing a trend in favor of the experimental arm in the overall time to event analysis.

Sirexatamab plus tislelizumab and chemotherapy was well tolerated, without additive toxicity to the standard of care.

FL-501 is a potential best in class monoclonal antibody in preclinical development that targets growth and differentiation factor 15 (GDF15), which is a cytokine that is produced at elevated levels in response to various stresses, including chronic inflammation, obesity, cardiovascular diseases, cancers, and chemotherapy treatment.

DKK1 levels correlated with increasing clinical benefit in those patients receiving sirexatamab compared to patients in the control arm who had poorer outcomes and shorter survival as DKK1 levels increased.

High GDF15 expression is associated with cachexia including loss of appetite, nausea and weight loss, and is also a validated target with a successful randomized clinical trial from Pfizer.

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In preclinical cachexia models, FL-501 increased body weight and restored muscle mass.

In addition, we are interested in the role of GDF15 in promoting an immunosuppressive tumor micro-environment, much like DKK1, and the broad range of cancers including gastric, colorectal, pancreatic and prostate, where elevated GDF15 also correlates with poor prognosis.

FL-501 is being developed through a collaboration agreement with Adimab.

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We expect to use trademark protection for our products as they are marketed.

We exclusively license from Eli Lilly and Company (“Lilly”), rights under 25 issued patents and 2 pending patent applications, all of which belong to the same patent family.

We exclusively license from Eli Lilly and Company (“Lilly”), rights under 26 issued patents and 1 pending patent application, all of which belong to the same patent family.

The patents and applications in this patent family are directed to the composition of matter and use of sirexatamab, and include (i) one issued U.S.

Patent, (ii) issued patents in the following jurisdictions:

Argentina, Australia, Brazil, Canada, China, Eurasia, Europe, Gulf Cooperation Council, India, Israel, Japan, Lebanon, Macao, Mexico, New Zealand, Pakistan, Singapore, South Africa, Taiwan, Ukraine, Hong Kong and South Korea and (iii) pending applications in the following jurisdictions:

Venezuela and Thailand.

Argentina, Australia, Brazil, Canada, China, Eurasia, Europe, Gulf Cooperation Council, India, Israel, Japan, Lebanon, Macao, Mexico, New Zealand, Pakistan, Singapore, South Africa, Taiwan, Ukraine, Hong Kong, Thailand and South Korea and (iii) a pending application in Venezuela.

The base 20-year term for patents in this family would expire in 2030.

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Patent term extensions for delays in marketing approval may also extend the terms of patents in this family.

We own one issued U.S.

Patent, granted patents in Japan, Korea, Mexico, and Israel and pending applications directed to the use of a biomarker in patients receiving DKN-01 therapy in the following jurisdictions:

Australia, Brazil, Canada, China, Europe, Hong Kong, India, Israel, Japan, Korea, Mexico, New Zealand, Russia, Singapore and the United States.

We own two issued U.S.

Patents, granted patents in Australia, Japan, Korea, Mexico, and Israel and pending applications directed to the use of a biomarker in patients receiving DKN-01 therapy in the following jurisdictions:

Brazil, Canada, Europe and Hong Kong,.

The issued U.S.

Patent and any additional patents that may issue in the United States based on the pending U.S.

Application will expire in 2037, absent any terminal disclaimer, patent term adjustment due to administrative delays by the United States Patent and Trade Office (“USPTO”) or patent term extension under the Drug Price Competition and Patent Term Restoration Act of 1984, referred to as the Hatch-Waxman Act or Hatch-Waxman Amendment, and provided that all required maintenance fee payments are timely paid.

The Japanese Patent and any other patents that may issue in foreign jurisdictions will likewise expire in 2037, provided that all required annuities are timely paid.

Patents will expire in 2037, absent any terminal disclaimer, patent term adjustment due to administrative delays by the United States Patent and Trade Office (“USPTO”) or patent term extension under the Drug Price Competition and Patent Term Restoration Act of 1984, referred to as the Hatch-Waxman Act or Hatch-Waxman Amendment, and provided that all required maintenance fee payments are timely paid.

The non-USPatents and any other patents that may issue in foreign jurisdictions will likewise expire in 2037, provided that all required annuities are timely paid.

We also own two additional patent families both directed to the treatment of cancer using DKN-01 in specific subpopulations of patients.

In the first patent family, the patient subpopulation is defined by its DKK-1 expression level.

Applications are pending in the following jurisdictions:

the United States of America, China, Japan, South Korea, Australia, New Zealand, Canada, Hong Kong, Mexico, Brazil, Israel, Europe and Singapore.

A patent has granted in South Korea and applications are pending in the following jurisdictions:

the United States of America, China, Australia, Canada, Hong Kong, Mexico, Brazil, Israel and Europe.

In the second patent family, the patient subpopulation is defined as harboring a specific genetic mutation.

Applications are pending in the following jurisdictions:

the United States of America, China, Japan, South Korea, Australia, New Zealand, Canada, Hong Kong, Mexico, Brazil, Israel, Europe and Singapore.

the United States of America, South Korea, Australia, Canada, Hong Kong, Mexico, Brazil, Israel and Europe.

Any patents that may issue in the United States based on the applications in these two patent families will expire in 2040, absent any terminal disclaimers, patent term adjustment due to administrative delays at the USPTO or patent term extension under the Hatch-Waxman Act, and provided that all required maintenance fee payments are timely paid.

Any patents that may issue in foreign jurisdictions will likewise expire in 2040, provided that all required annuities are timely paid.

The Korean Patent and any other patents that may issue in foreign jurisdictions will likewise expire in 2040, provided that all required annuities are timely paid.

We also own another patent family directed to the treatment of colorectal cancer using combination therapy comprising sirexatamab and additional therapeutic agents.

Applications are pending in the following jurisdictions:

the United States of America, China, Japan, South Africa, South Korea, Australia, New Zealand, Canada, Mexico, Brazil, Israel, Europe and Singapore.

the United States of America, China, Japan, South Korea, Australia, New Zealand, Canada, Mexico, Brazil, Hong Kong, Israel and Europe.

Any patent that may issue in the United States based on the pending U.S.

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Any patents issued in foreign jurisdictions will likewise expire in 2043.

We also own two U.S.

Provisional applications directed to the treatment of colorectal cancer using combination therapy comprising sirexatamab and additional therapeutic agents in specific subpopulations of patients.

If non-Provisional patent applications claiming the benefit of the first filed pending U.S.

Provisional patent application referenced above are filed in 2025, any patent that may issue from such applications will expire no earlier than 2045 absent any terminal disclaimer.

We also own one pending international patent application filed under the Patent Cooperation Treaty (“PCT”) directed to the treatment of colorectal cancer using combination therapy comprising sirexatamab and additional therapeutic agents in specific subpopulations of patients.

The PCT is an international patent law treaty that provides a unified procedure for filing a single initial patent application to seek patent protection for an invention simultaneously in each of the member states.

Although a PCT Application is not itself examined and cannot issue as a patent, it allows the applicant to seek protection in any of the member states through national phase applications.

Any patents that may issue in the United States based on the PCT application will expire no earlier than 2045 absent any terminal disclaimer.

Any patents issued in foreign jurisdictions will likewise expire in 2045.

We also own a pending U.S.

Provisional application directed to, among other things, FL-501 (a monoclonal antibody that inhibits GDF-15).

If non-Provisional patent applications (e.g., a regular U.S.

application, a PCT Application or direct foreign applications) claiming the benefit of the U.S.

Provisional application are filed in 2026, any patents that may issue in the United States will expire no earlier than 2046 absent any terminal disclaimer.

Any patents issued in foreign jurisdictions will likewise expire in 2046.

The base term of a U.S.

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Lilly may terminate the agreement (i) upon our material breach of the Lilly Agreement upon ninety (90) days written notice to us, unless we cure such breach or violation during such ninety day period or (ii) if we challenge, or materially assist any third person to challenge, the validity or enforceability of the licensed intellectual property that is the subject of the Lilly Agreement upon thirty (30) days written notice to us, unless we cure such breach or violation during such thirty (30) day period.

be required to grant to Lilly an irrevocable, non-exclusive, perpetual, fully paid up license under all patent rights developed or acquired by us during the term of the Lilly Agreement that relate to the Lilly licensed intellectual property, (iv) subject to certain limitations, we will be required to grant to Lilly an irrevocable, non-exclusive, perpetual, fully paid up license to the results of data from all preclinical and clinical studies of any compound or product covered by the Lilly Agreement, (v) subject to certain limitations, we will be required to take all steps necessary to permit Lilly to commence marketing product covered by the Lilly Agreement, and (vi) we will be required to assign or re-assign to Lilly all Lilly patents covered by the Lilly Agreement and that were assigned by Lilly to us.

If Lilly terminates the Lilly Agreement or if we terminate the Lilly Agreement without cause, (i) all rights under the licensed intellectual property rights will terminate and immediately and automatically revert to Lilly, (ii) any sublicense will be assigned by us to Lilly so that such sublicense becomes a direct license between Lilly and such sublicensee, (iii) subject to certain limitations, we will be required to grant to Lilly an irrevocable, non-exclusive, perpetual, fully paid up license under all patent rights developed or acquired by us during the term of the Lilly Agreement that relate to the Lilly licensed intellectual property, (iv) subject to certain limitations, we will be required to grant to Lilly an irrevocable, non-exclusive, perpetual, fully paid up license to the results of data from all preclinical and clinical studies of any compound or product covered by the Lilly Agreement, (v) subject to certain limitations, we will be required to take all steps necessary to permit Lilly to commence marketing product covered by the Lilly Agreement, and (vi) we will be required to assign or re-assign to Lilly all Lilly patents covered by the Lilly Agreement and that were assigned by Lilly to us.

If we terminate the Lilly Agreement for material breach by Lilly or Lilly’s bankruptcy, the licenses will remain in full force and effect and we will remain liable for the payment of all royalty obligations under the Lilly Agreement.

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The Adimab Agreement also contains certain standard representations and warranties and certain standard confidentiality and indemnification provisions.

Competition Related to our Leap Therapeutics Business

The biotechnology and pharmaceutical industries are characterized by continuing technological advancement and significant competition.

While we believe that our product candidates, technology, knowledge, experience and scientific resources provide us

with competitive advantages, we face competition from major pharmaceutical and biotechnology companies, academic institutions, governmental agencies and public and private research institutions, among others.

While we believe that our product candidates, technology, knowledge, experience and scientific resources provide us with competitive advantages, we face competition from major pharmaceutical and biotechnology companies, academic institutions, governmental agencies and public and private research institutions, among others.

Any product candidates that we successfully develop and commercialize will compete with existing therapies and new therapies that may become available in the future.

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In addition, manufacturers of biopharmaceutical products participating in Medicaid and Medicare are required to comply with mandatory price reporting, discount, and rebate requirements.

The processes for obtaining regulatory approvals in the United States and in foreign countries, along with subsequent compliance with applicable statutes and

regulations, require the expenditure of substantial time and financial resources.

The processes for obtaining regulatory approvals in the United States and in foreign countries, along with subsequent compliance with applicable statutes and regulations, require the expenditure of substantial time and financial resources.

The following is a summary of the primary government regulations applicable to our business.

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● Phase 2 — Controlled studies are conducted in limited subject populations with a specified disease or condition to evaluate preliminary efficacy, identify optimal dosages, dosage tolerance and schedule, possible adverse effects and safety risks, and expanded evidence of safety.

● Phase 3 — These adequate and well-controlled clinical trials are undertaken in expanded subject populations, generally at geographically dispersed clinical trial sites, to generate enough data to provide statistically significant evidence of clinical efficacy and safety of the product for approval, to establish the overall risk-benefit profile of the product, and to

provide adequate information for the labeling of the product.

Typically, two Phase 3 trials are required by the FDA for product approval.

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The FDA also may require submission of a risk evaluation and mitigation strategy, or REMS, to ensure that the benefits of the biologic outweigh the risks.

The REMS plan could include medication guides, physician communication plans, and elements to assure

safe use, such as restricted distribution methods, patient registries, or other risk minimization tools.

The REMS plan could include medication guides, physician communication plans, and elements to assure safe use, such as restricted distribution methods, patient registries, or other risk minimization tools.

An assessment of the REMS must also be conducted at set intervals.

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In some cases, a Fast Track product may be eligible for accelerated approval or priority review.

On September 24, 2020, the FDA granted Fast Track designation to DKN-01 for the treatment of patients with gastric and gastroesophageal junction adenocarcinoma whose tumors express high

DKK1, following disease progression on or after prior fluoropyrimidine- and platinum- containing chemotherapy and if appropriate, human epidermal receptor growth factor (HER2)/neu targeted therapy.

On September 24, 2020, the FDA granted Fast Track designation to DKN-01 for the treatment of patients with gastric and gastroesophageal junction adenocarcinoma whose tumors express high DKK1, following disease progression on or after prior fluoropyrimidine- and platinum- containing chemotherapy and if appropriate, human epidermal receptor growth factor (HER2)/neu targeted therapy.

The FDA may give a priority review designation to products that are intended to treat serious conditions and, if approved, would provide significant improvements in the safety or effectiveness of the treatment, diagnosis, or prevention of serious conditions.

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Such actions may include refusal to approve pending applications, license suspension or revocation, withdrawal of an approval, imposition of a clinical hold or termination of clinical trials, warning letters, untitled letters, cyber letters, modification of promotional materials or labeling, provision of corrective information, imposition of post-market requirements including the need for additional testing, imposition of distribution or other restrictions under a REMS, product recalls, product seizures or detentions, refusal to allow imports or exports, total or partial suspension of production or distribution, FDA debarment, injunctions, fines, consent decrees, corporate integrity agreements, debarment from receiving government contracts, new orders under existing contracts, exclusion from participation in federal and state healthcare programs, restitution, disgorgement, or civil or criminal penalties, including fines and imprisonment, and result in adverse publicity, among other adverse consequences.

Other Regulation

Other Regulation Related to our Leap Therapeutics Business

In addition to any FDA restrictions on marketing and promotion of drugs and devices, other federal and state laws restrict our business practice including, without limitation, anti-kickback and false claims laws, data privacy and security laws, as well as transparency laws regarding payment or other items of value provided to healthcare providers.

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We are also governed by other federal, state and local laws of general applicability, such as laws regulating working conditions, employment practices, as well as environmental protection.

Research and Development Expenses

Research and Development Expenses Related to Our Leap Therapeutics Business

Our total research and development expenses were $25.7 million and $57.2 million, during the years ended December 31, 2025 and 2024, respectively.

See Part II — Item 7 — “Management’s Discussion and Analysis of Financial Condition and Results of Operations” of this Annual Report on Form 10-K for additional details regarding our research and development activities.

As of December 31, 2024, we had 52 full-time employees, including 41 in research and development and 11 in general and administrative roles.

We have 2 employees who have an M.D., 12 employees who have a Ph.D., 1 employee who has a JD, and 18 employees with a master’s degree.

As of December 31, 2025, we had 6 full-time employees.

None of our employees are represented by a labor union or subject to a collective bargaining agreement.

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We make these reports available as soon as reasonably practicable after they are filed with or furnished to the SEC.

The information contained on, or that can be accessed through our

website is not a part of or incorporated by reference into this Annual Report on Form 10-K.

The information contained on, or that can be accessed through our website is not a part of or incorporated by reference into this Annual Report on Form 10-K.

We will also provide to any person without charge, upon request, a copy of any of the foregoing materials.

Any such request must be made in writing to us at:

Leap Therapeutics, Inc.

Cypherpunk Technologies Inc.

c/o Investor Relations, 47 Thorndike Street, Suite B1, Cambridge, MA 02141.

Compared sentence by sentence after normalising whitespace, quotation marks, case and digits, so re-formatting and restated figures do not read as changed language. Wording changes appear as one removal and one addition. The current filing and the prior one are authoritative.

What changed 10-K

Item 1. Business