Rezolute Presents Data on RZ358 in Post-Gastric Bypass Hypoglycemia at ENDO 2021

Rhea-AI Summary

Rezolute, Inc. (RZLT) announced positive results from its Phase 2a study of RZ358 for post-gastric bypass hypoglycemia at ENDO 2021. The study demonstrated a significant over 50% improvement in hypoglycemia, achieving near-normal glucose levels. RZ358 was safe, well-tolerated, and did not induce hyperglycemia. The pharmacokinetic model supports the potential effectiveness of RZ358 in future trials, including those for congenital hyperinsulinism. Rezolute is advancing RZ358, which has received Orphan Drug Designation in multiple regions.

Positive

• Phase 2a study results show over 50% improvement in hypoglycemia.
• RZ358 was safe and well tolerated with no serious adverse reactions.
• Pharmacokinetic model supports future clinical trials.
• RZ358 received Orphan Drug Designation in the US and EU.

Negative

• None.

REDWOOD CITY, Calif., March 22, 2021 (GLOBE NEWSWIRE) -- Rezolute, Inc. (“Rezolute” or “the Company”) (Nasdaq: RZLT) today presented positive results of a Phase 2a study of RZ358 in patients with post-gastric bypass hypoglycemia (PGBH), as well as results of a pharmacologic model of the drug candidate, at the Endocrine Society’s Annual Meeting, ENDO 2021, held virtually from March 20 through March 23. The study objective was met, with a clinically significant improvement in hypoglycemia by more than 50%, translating to near normalization of average glucose levels. Furthermore, a population-based PK-PD model characterized the observed drug concentrations and quantified the exposure-response relationship.

“These results in patients with post-gastric bypass hypoglycemia, as well as the broader program-based pharmacologic modeling we’ve presented today, provide further confirmation of RZ358’s unique mechanism of action and therapeutic potential, which by design is highly suited to address hypoglycemia caused by hyperinsulinemia,” said Brian Roberts, MD, senior vice president of clinical development at Rezolute. “We have also generated a quantitative and predictive model of RZ358 behavior, which will prove valuable in the planning and execution of our late-stage clinical development programs with RZ358, including our study in congenital hyperinsulinism.”

About the Phase 2a Study

The presentation, titled “Single and repeat-dose study of RZ358 in Patients with Post-Gastric Bypass Hypoglycemia (PGBH): Results of Population PK/PD Modeling,” reported the results of a Phase 2a, open-label, single ascending (3, 6, and 9 mg/kg) and repeat dose (3 mg/kg/week for 4 weeks) study of IV RZ358 in 16 patients with PGBH. Serial measurements of RZ358 concentrations as well as biomarkers and continuous glucose monitoring (CGM) were performed for up to 6 weeks. The results showed that RZ358 was safe and well tolerated with no serious adverse reactions or discontinuations. RZ358 led to a sustained improvement of at least 50% in time in target blood glucose range (70-180 mg/dL), translating to near normalization of average daily glucose values. Consistent with its mechanism of action, RZ358 did not cause hyperglycemia.

Using pooled observations from the Company’s clinical studies with RZ358, a final 3-compartmental population PK model and empirical PK-PD model generally described the observed PGBH study exposures and glucose response. Pharmacokinetic simulations showed that model-predicted efficacious target concentrations can be readily achieved with RZ358 dosing regimens that are currently being evaluated in clinical trials and which meet the candidate’s target product profile.

Ann Arbor Pharmacometrics Group (A2PG) conducted the PK/PD modeling referenced above.

About RZ358
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. 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 congenital HI. As RZ358 acts downstream from the beta cells, it has the potential to be universally effective at treating congenital HI caused by any of the underlying genetic defects.

RZ358 received Orphan Drug Designation in the United States and European Union as well as Pediatric Rare Disease Designation in the US. Rezolute is currently evaluating RZ358 in the RIZE trial, a Phase 2b clinical trial in patients with congenital hyperinsulinism.

About Rezolute, Inc.
Rezolute is advancing targeted therapies for rare, metabolic, and life-threatening diseases. Its lead product candidate, RZ358, is in Phase 2b development as a potential treatment for congenital hyperinsulinism (HI), a rare pediatric endocrine disorder. Its pipeline also includes RZ402, an orally available plasma kallikrein inhibitor in Phase 1 development as a potential treatment for diabetic macular edema. For more information, visit www.rezolutebio.com or follow us on Twitter.

Forward-Looking Statements
This release, like many written and oral communications presented by Rezolute, Inc. and our authorized officers, may contain certain forward-looking statements regarding our prospective performance and strategies within the meaning of Section 27A of the Securities Act and Section 21E of the Securities Exchange Act of 1934, as amended. We intend such forward-looking statements to be covered by the safe harbor provisions for forward-looking statements contained in the Private Securities Litigation Reform Act of 1995 and are including this statement for purposes of said safe harbor provisions. Forward-looking statements, which are based on certain assumptions and describe future plans, strategies, and expectations of the Company, are generally identified by use of words such as "anticipate," "believe," "estimate," "expect," "intend," "plan," "project," "seek," "strive," "try," or future or conditional verbs such as "could," "may," "should," "will," "would," or similar expressions. Our ability to predict results or the actual effects of our plans or strategies is inherently uncertain. Accordingly, actual results may differ materially from anticipated results. Readers are cautioned not to place undue reliance on these forward-looking statements, which speak only as of the date of this release. Except as required by applicable law or regulation, Rezolute undertakes no obligation to update these forward-looking statements to reflect events or circumstances that occur after the date on which such statements were made.

Media Contact
Amy Jobe, Ph.D.
LifeSci Communications
+1 315 879 8192
ajobe@lifescicomms.com

Investor Contact
Corey Davis, Ph.D.
LifeSci Advisors
+1 212 915 2577
cdavis@lifesciadvisors.com

FAQ

What were the results of the Phase 2a study of RZ358 presented by Rezolute?

The Phase 2a study showed over a 50% improvement in hypoglycemia in patients, achieving near-normal glucose levels.

Did RZ358 demonstrate any safety concerns during the Phase 2a study?

RZ358 was reported as safe and well-tolerated with no serious adverse reactions.

What designations has RZ358 received?

RZ358 has received Orphan Drug Designation in the United States and European Union.

What is the mechanism of action for RZ358?

RZ358 is a monoclonal antibody that modifies insulin's binding to maintain glucose levels, addressing hyperinsulinemia.

What is the next step for Rezolute after the Phase 2a study results?

Rezolute is evaluating RZ358 in the RIZE trial, a Phase 2b clinical trial for congenital hyperinsulinism.