What changed in this filing

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Item 1. Business

2021-09-15 compared with 2020-10-13 · 215 added, 142 removed, 11 unchanged (97% of the section changed)

2 unchanged sentences

Company ”, “

us ”) is advancing targeted therapies for metabolic

diseases with serious unmet needs.

On October 9, 2020, we completed

a private placement of equity securities that resulted in net proceeds to the Company of approximately $37.6 million.

October 7, 2020, our Board of Directors approved a one share for 50 shares reverse stock split of our $0.001 par

value Common Stock (the “Reverse Stock Split”).

The Reverse Stock Split was previously approved by stockholders

at our annual meeting on October 23, 2019 and was effective at 5:00 Eastern time on October 9, 2020.

first day of trading after the Reverse Stock Split was on October 13, 2020.

In connection with the Reverse Stock Split,

proportionate adjustments were made to increase the per share exercise prices and decrease the number of shares of Common

Stock issuable upon exercise of stock options and warrants whereby approximately the same aggregate price is required to be

paid for such securities upon exercise as had been payable immediately preceding the Reverse Stock Split.

In addition, any

fractional shares that would otherwise be issued as a result of the Reverse Stock Split were rounded up to the nearest whole

All references in this Annual Report to the number of shares of Common Stock and the related per share amounts have

been retroactively adjusted to give effect to the Reverse Stock Split.

Also during September 2020, we made

adjustments to the composition of our Board of Directors, which included appointing Philippe Fauchet as an independent director.

Our Board now consists of a majority of independent directors.

As of the date of this Annual Report, we

continue to work diligently toward our goal of having our shares of Common Stock listed on the Nasdaq Capital Market.

completion of the private placement and execution of the Reverse Stock Split, and board composition adjustments discussed above,

we believe that we currently meet all of Nasdaq’s initial listing standards.

We are currently engaged in active discussions

with the staff of Nasdaq with the objective to promptly complete the uplisting.

However, no assurance can be provided that we will

be successful in this regard.

us ”) is a clinical-stage biopharmaceutical company developing

transformative therapies for metabolic diseases related to chronic glucose imbalance.

In October 2020 we completed a private placement

of equity securities that resulted in net proceeds to the Company of approximately $37.4 million.

Also in October 2020, our Board of Directors (our

Board of Directors ”

or our “

Board ”) approved a one share for every fifty shares reverse stock split

of our common stock (the “

Reverse Stock Split ”).

The Reverse Stock Split was previously approved by shareholders at

our annual meeting on October 23, 2019 and was effective at 5:00 PM EST on October 9, 2020.

The first day of trading after the Reverse

Stock Split was on October 13, 2020.

In connection with the Reverse Stock Split, proportionate adjustments were made to increase the per

share exercise prices and decrease the number of shares of common stock issuable upon exercise of stock options and warrants whereby approximately

the same aggregate price is required to be paid for such securities upon exercise as had been payable immediately preceding the Reverse

In addition, any fractional shares that would otherwise be issued as a result of the Reverse Stock Split were rounded up

to the nearest whole share.

All references in this Annual Report to the number of shares of common stock and the related per share amounts

have been retroactively adjusted to give effect to the Reverse Stock Split.

In September 2020, we made adjustments to the

composition of our Board of Directors, which included appointing Philippe Fauchet as an independent director.

Furthermore, in March 2021,

our Board of Directors appointed Dr.

Kreher and Dr.

Wladimir Hogenhuis as independent directors.

Our board consists of a majority

of independent directors.

In November 2020, our application to the Nasdaq

Capital Markets was approved and we began trading on this market under the “RZLT”

In December 2020, we entered into an Equity Distribution

Agreement (“

EDA ”) with Oppenheimer & Co.

Inc., pursuant to which we may offer and sell, from time to time, shares

of the our common stock, par value $0.001 per share, having an aggregate offering price of up to $50.0 million.

August 2021, we sold 138,388 shares of our common stock pursuant to the EDA at an average price per share of $10.78 for net proceeds of

approximately $1.5 million.

In April 2021, we entered into a Loan and Security

Agreement (the “

Loan Agreement ”) with SLR Investment Corp.

SLR ”) and certain other lenders (the

Lenders ”) that provided for total borrowings up to $30.0 million in three tranches.

The initial tranche of funding

for $15.0 million was received in April 2021.

Under the Loan Agreement, we are required to maintain a restricted cash balance of at least

$5.0 million beginning no later than December 31, 2021.

The second tranche for $7.5 million is available upon our request by January 2022,

and the third tranche for $7.5 million is available upon our request by September 2022.

Access to the additional borrowings under the

second and third tranches is subject to our ability by the requested funding date to raise cumulative equity or subordinated debt financing

of $35.0 million and $70.0 million, respectively, and the achievement of certain clinical milestones related to RZ358 and RZ402.

permitted to make interest-only payments on each term loan at least through May 1, 2023, and the maturity date is on April 1, 2026.

In June 2021, we merged with and into our wholly

owned subsidiary, Rezolute Nevada Merger Corporation, a Nevada corporation (“

Merger Sub ”), pursuant to an Agreement

and Plan of Merger, dated as of June 18, 2021 (the “

Reincorporation Merger Agreement ”), between us and Merger Sub,

with Merger Sub as the surviving corporation (the “

Reincorporation Merger ”).

At the effective time of the Reincorporation

Merger (the “

Effective Time ”), the Merger Sub was renamed “Rezolute, Inc.”

and succeeded to the assets,

continued our business and assumed our rights and obligations by operation of law.

The Reincorporation Merger Agreement was approved by

our shareholders at the 2021 annual meeting of our shareholders held on May 26, 2021.

Summary of Clinical Assets

Our lead clinical asset, RZ358, is an antibody

therapy in Phase 2b development as a potential treatment for congenital hyperinsulinism (“CHI”), an ultra-rare pediatric

genetic disorder.

In February 2020, we announced the

initiation of the RZ358-606 Phase 2b study (“RIZE”) globally at multiple study centers.

Prior to COVID-19, we had planned

to complete the RIZE study by the middle of calendar year 2021.

March 2020, we paused the RIZE study as a result of the COVID-19 pandemic.

As the COVID-19 pandemic abates in different

regions, we are resuming clinical activities including trial site initiations.

We believe that patient enrollment will recommence

by the end of October 2020.

Further, if we can begin enrolling patients on this timeframe, we believe we will be able to complete

the RIZE study in the second half of calendar year 2021.

addition, in the first half of calendar year 2020, we had positive interactions with the U.S.

Food and Drug Administration (“FDA”).

In June 2020, we announced that FDA granted us Rare Pediatric Disease (“RPD”) designation for RZ358, which qualifies

us to receive a priority review voucher upon marketing approval of the drug in CHI.

Such a voucher could be redeemed to receive

a priority review of a subsequent marketing application for any drug candidate in any disease indication.

Further, we submitted

the RIZE protocol to FDA which allows us to expand the study to clinical sites in the United States.

We believe that patient enrollment

may commence in the United States in the first quarter of calendar year 2021.

Our next program, RZ402, is an investigational

new drug (“IND”) application-ready oral therapy, targeting diabetic macular edema (“DME”).

Prior to COVID-19

we were planning to file the IND with the FDA in the third quarter of calendar year 2020, followed by the initiation and completion

of a Phase 1 study this calendar year.

However, as a result of the present uncertainties associated with COVID-19 pandemic, we

have deferred filing the IND.

We anticipate initiating the clinical trial for RZ402 prior to the end of the first quarter of calendar

CHI is an ultra-rare pediatric genetic

disorder characterized by excessive production of insulin by the pancreas.

CHI is caused by mutations in about a dozen known genes

associated with pancreatic beta cells and their secretion of insulin.

If untreated, it can lead to dangerously low blood sugar

Rezolute’s lead candidate, RZ358, is an antibody in Phase 2b development that is designed to prevent severe, persistent

low blood sugar in patients with CHI.

RZ358 is an intravenously administered

human monoclonal antibody that binds to a unique site on the insulin receptor found across effector cells throughout the body in

Our lead clinical asset, RZ358, is an

antibody therapy in Phase 2b development as a potential treatment for congenital hyperinsulinism (“

HI ”), an

ultra-rare pediatric genetic disorder.

In February 2020, we announced the initiation of the RZ358-606 Phase 2b study

RIZE ”) globally at multiple study centers.

Prior to COVID-19, we had planned to complete the RIZE study by the

middle of calendar year 2021.

In March 2020, we paused the RIZE study as a result of the COVID-19 pandemic.

In January 2021, as the

COVID-19 pandemic began to abate in different regions, we resumed clinical activities including trial site initiations and patient

Subject to COVID-19 conditions, we are expecting to substantially complete enrollment in the RIZE study by the end of

calendar year 2021 and have top-line data in the first quarter of calendar year 2022.

In addition, in the first half of calendar year

2020, we had positive interactions with the U.S.

Food and Drug Administration (“

FDA ”).

In June 2020, we announced that

FDA granted us Rare Pediatric Disease (“

RPD ”) designation for RZ358, which qualifies us to receive a priority review

voucher (“PRV”) upon marketing approval of the drug in HI.

Such a voucher could be redeemed to receive a priority review of

a subsequent marketing application for any drug candidate in any disease indication.

Further, we submitted the RIZE protocol to FDA which

allows us to expand the study to clinical sites in the United States.

Our second clinical asset, RZ402, is a selective

and potent plasma kallikrein inhibitor (“

PKI ”) being developed as a potential oral therapy for the chronic treatment

of diabetic macular edema (“

DME ”).

RZ402 is currently in Phase 1 development.

In January 2021, we dosed the first subject

in the Phase 1a study, and in May 2021, we announced positive topline results whereby single dose oral administration of RZ402 resulted

in plasma concentrations that substantially exceeded target pharmacologically-active drug levels, demonstrating the potential for once

daily dosing.

RZ402 was generally safe and well-tolerated at all doses tested, without dose-limiting toxicities.

In August 2021, we announced

the initiation in the Phase 1b multiple-ascending dose study and planned to be completed by the first quarter of calendar year 2022.

favorable results are also obtained in the Phase 1b study, we expect to advance developmental activities toward a Phase 2a proof-of-concept

study during the second half of calendar year 2022.

HI is an ultra-rare pediatric genetic disorder

characterized by excessive production of insulin by the pancreas.

If untreated, the elevated insulin levels in these patients can induce

extreme hypoglycemia (low blood sugar) events, increasing the risk of neurological and developmental complications, including persistent

feeding problems, learning disabilities, recurrent seizures, brain damage or even death.

There are no approved therapies for HI and the

current standard of care treatments are suboptimal.

In some cases, pancreatic surgery is a treatment option, but this approach is invasive

and may require repeat surgeries.

Our lead candidate, RZ358, is an intravenously

administered human monoclonal antibody that binds to a unique site (allosteric) on the insulin receptor throughout the body, such as in

the liver, fat, and muscle.

This action allows RZ358 to counteract the effects of elevated insulin in the body.

Its unique allosteric

mechanism of action is reversible, depends on both insulin levels and blood sugar levels in a dose-dependent manner, and enables

patients to achieve normal levels of insulin and glucose.

Therefore, we believe that RZ358 is ideally suited as a potential therapy

for conditions characterized by excessive insulin production and it is being developed to treat hyperinsulinemia and prevent low

blood sugar for diseases such as CHI.

As RZ358 acts downstream from the beta cells, across effector cells in the liver, fat, and

muscle, it may be universally effective at treating CHI caused by any of the underlying genetic defects.

The RIZE study is a multi-center, open-label,

repeat-dose Phase 2b study of RZ358 in four sequential dosing cohorts of patients with CHI who are at least two years old and have

residual low blood sugar (<70 mg/dL) that is inadequately controlled on existing therapies.

In addition to safety and pharmacokinetic

evaluations, continuous glucose monitoring (“CGM”) and self-monitored blood glucose will be utilized to evaluate several

glycemic efficacy endpoints.

The primary endpoint is the time within a glucose target range of 70-180 mg/dL by CGM during weeks

4 and 8 of treatment compared to baseline.

DME is a severe complication of diabetes

marked by progressive vision loss and blindness.

Consistently high blood sugar levels can cause diabetic retinopathy, a complication

characterized by damage to the blood vessels in the eye and fluid leakage into the light-sensitive tissue known as the retina.

The accumulation of fluid may lead to DME, or swelling of the macula, the part of the retina responsible for sharp, straight-ahead

Currently available treatments for DME involve frequent burdensome injections into the eye or invasive laser surgery.

Rezolute is developing RZ402, a small molecule

plasma kallikrein inhibitor (“PKI”) for use in DME.

As a once-daily oral investigational therapy, RZ402 is designed

to improve compliance and treatment outcomes for patients with DME.

Elevated plasma levels of the enzyme kallikrein have been associated

with increased inflammation, vessel leakage and excess blood vessel growth in the eyes of patients with DME.

Genetic and pharmacologic

knockout of plasma kallikrein have been shown to protect against vascular endothelial growth factor (“VEGF”) induced

retinal blood vessel leakage in murine models without damaging long-term effects.

is a bioavailable small molecule inhibitor of plasma kallikrein that has shown the potential to prevent the onset of and reverse

vascular leakage in a dose-dependent manner in multiple rodent models of whole body and retinal vascular leakage.

Target plasma

concentrations were exceeded for 24 hours following oral dosing of RZ402 in monkeys and dogs, supporting the potential for once

daily dosing in humans.

Rezolute has completed a pre-IND meeting with the FDA and the IND-enabling toxicology studies in preparation

for filing an IND.

We face competition from pharmaceutical

and biotechnology companies, academic institutions, governmental agencies, and private research organizations in recruiting and

retaining highly qualified scientific personnel and consultants and in the development and acquisition of technologies.

There are a handful of companies developing

therapies for CHI that are potential competitors to RZ358.

Zealand Pharma is one such company.

There are a handful of companies developing

oral therapies for diabetic macular edema that are potential competitors to the plasma kallikrein inhibitor therapy, KalVista Pharmaceuticals being one such company.

The antibody modifies insulin's binding and signaling to maintain glucose levels in a normal range which counteracts

the effects of elevated insulin in the body.

Therefore, we believe that RZ358 is ideally suited as a potential therapy for conditions

characterized by excessive insulin levels, and it is being developed to treat the hyperinsulinism and low blood sugar characteristic of

diseases such as HI.

As RZ358 acts downstream from the beta cells, it has the potential to be universally effective at treating HI caused

by any of the underlying genetic defects.

RZ358 received Pediatric Rare Disease Designation

as well as Orphan Drug Designation in the U.S.

and European Union.

RZ358 is currently in Phase 2b development (the RIZE study,

The RIZE study is a multi-center, open-label, repeat-dose Phase 2b study of RZ358 in four sequential dosing cohorts of patients

with HI who are at least two years old and have residual low blood sugar (<70 mg/dL) that is inadequately controlled on existing therapies.

In addition to safety and pharmacokinetic evaluations, continuous glucose monitoring (“CGM”) and self-monitored blood glucose

will be utilized to evaluate several glycemic efficacy endpoints.

The primary endpoint is the time within a glucose target range of 70-180

mg/dL by CGM after week 8 of treatment compared to baseline.

DME is a vascular complication of diabetes and

a leading cause of blindness in the U.S.

and elsewhere.

Chronic exposure to high blood sugar levels can lead to inflammation, cell damage,

and the breakdown of blood vessel walls.

Specifically, in DME, blood vessels behind the back of the eye become porous and permeable leading

to the unwanted infiltration of fluid into the macula.

This fluid leakage creates distorted vision and left untreated, blindness.

Currently available treatments for DME

involve frequent burdensome anti-vascular growth factor (anti-VEGF) injections into the eye or invasive laser surgery.

designed to be a once daily oral therapy for the treatment of DME.

Unlike the anti-VEGF therapies, RZ402 targets the

Kallikrein–Kinin System in order to address inflammation and vascular leakage.

We believe that systemic exposure through oral

delivery is critical to target the microvasculature behind the back of the eye.

Further, as an oral therapy, RZ402 has the potential

to substantially change the therapeutic paradigm for patients suffering with DME by providing a convenient, self-administered

treatment option to encourage patients to initiate therapy sooner, adhere to prescribed treatment guidelines, and improve overall

We face competition from pharmaceutical and biotechnology

companies, academic institutions, governmental agencies, and private research organizations in recruiting and retaining highly qualified

scientific personnel and consultants and in the development and acquisition of technologies.

There are a handful of companies developing therapies

for HI that are potential competitors to RZ358.

Crinetics Pharmaceuticals Inc is one such company.

There are a handful of companies developing oral

therapies for DME that are potential competitors to the PKI therapy, KalVista Pharmaceuticals

being one such company.

Government Regulation

Regulation by governmental authorities

Regulation by governmental authorities in the

and other countries is a significant factor in the development, manufacture and marketing of pharmaceutical products.

All of our potential products will require regulatory approval by governmental agencies prior to commercialization.

In particular,

pharmaceutical therapies are subject to rigorous preclinical testing and clinical trials and other pre-market approval requirements

by the FDA and regulatory authorities in foreign countries.

Various federal, state and foreign statutes and regulations also govern

or influence the manufacturing, safety, labeling, storage, record keeping and marketing of such products.

We are also subject to various federal,

state, and local laws, regulations and recommendations relating to safe working conditions;

potential products will require regulatory approval by governmental agencies prior to commercialization.

In particular, pharmaceutical

therapies are subject to rigorous preclinical testing and clinical trials and other pre-market approval requirements by the FDA and regulatory

authorities in foreign countries.

Various federal, state and foreign statutes and regulations also govern or influence the manufacturing,

safety, labeling, storage, record keeping and marketing of such products.

We are also subject to various federal, state,

and local laws, regulations and recommendations relating to safe working conditions;

laboratory and manufacturing practices;

the experimental use of animals;

and the use and disposal of hazardous or potentially hazardous substances, including radioactive

compounds and infectious disease agents, used in connection with our research, development and manufacturing.

the experimental

use of animals;

and the use and disposal of hazardous or potentially hazardous substances, including radioactive compounds and infectious

disease agents, used in connection with our research, development and manufacturing.

Research and Development

We incurred approximately $14.5 million

and $19.1 million in research and development expenses for the fiscal years ended June 30, 2020 and 2019, respectively.

further discussion of activities related to our RZ358 and RZ402 product candidates, please refer to the discussion above.

discussion of our research and development expenses, please refer to the discussion under the caption Results of Operations

under Item 7 of this Annual Report.

As of June 30, 2020, we had 23 full-time

employees, all of whom have experience with pharmaceutical, biotechnology or medical product companies.

None of our employees or

contractors are covered by collective bargaining agreements.

We incurred approximately $15.0 million and $14.5

million in research and development expenses for the fiscal years ended June 30, 2021 and 2020, respectively.

For further discussion of

activities related to our RZ358 and RZ402 product candidates, please refer to the discussion above.

For further discussion of our research

and development expenses, please refer to the discussion under the caption Results of Operations under Item 7 of this Annual Report.

Human Capital Management

As of June 30, 2021, we had 26 employees, of which

19 employees were engaged in research and development, manufacturing, clinical operations and quality activities and 7 employees in general

administrative functions.

Of the 26 employees, all were located in the United States.

We have a number of employees who hold advanced

degrees, such as a Ph.D.

None of our employees are covered by a collective bargaining agreement, and we have experienced no work

stoppages nor are we aware of any employment circumstances that are likely to disrupt work at any

of our facilities .

As part of our measures to attract and retain personnel, we provide a number of benefits to our full-time employees,

including health insurance, life insurance, retirement plans, paid holiday and vacation time.

We believe that we maintain good relations

with our employees.

Diversity and Inclusion

Diversity and inclusion are priorities for us.

We believe that a rich culture of inclusion and diversity enables us to create, develop and fully leverage the strengths of our workforce.

Human Resources, Hiring and Professional

The development, attraction and retention of employees

is critical to our success.

We work diligently to attract the best talent from a diverse range of sources in order to meet the current

and future demands of our business.

We leverage both formal and informal programs to identify, foster and retain top talent.

Our Code of Business Conduct and Ethics ensures

that our conduct of business is consistent with the highest standards of business ethics.

Our Code of Business Conduct and Ethics serves

as a critical tool to help employees recognize and report unethical conduct, while preserving our culture of excellence.

Our Board of Directors, management and staff are provided with training regarding our Code of Business Conduct and Ethics.

Corporate Information

were incorporated in Delaware in 2010.

We maintain executive offices located at 201 Redwood Shores Parkway, Suite 315, Redwood

City, CA 94065 and our phone number is (650) 206-4507.

We were incorporated in Delaware in 2010 and

re-incorporated in Nevada in June 2021.

We maintain an executive office located at 201 Redwood Shores Parkway, Suite 315, Redwood City,

CA 94065 and our phone number is (650) 206-4507.

Our website is located at www.rezolutebio.com .

The information

contained in, or that can be accessed through, our website is not part of, and is not incorporated into this document.

The information contained in,

or that can be accessed through, our website is not part of, and is not incorporated into this document.

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