NOW ENROLLING PHASE III sunRIZE TRIAL In the study of congenital hyperinsulinism

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We take novel approaches to defined disease pathways and leverage our metabolic expertise to develop therapies that have the potential to overcome the shortcoming of current standards of care by significantly improving clinical outcomes for patients.

ProgramINDPhase 1Phase 2Phase 3
RZ358    |
Congenital hyperinsulinism
Orphan designation in US and EU
Pediatric Rare Disease designation in US
 
DrugStage
RZ358    |
Orphan designation in US and EU
Pediatric Rare Disease designation in US
Congenital hyperinsulinism
Phase 3

RZ358

REZ-SGFX-358

Congenital hyperinsulinism (CHI) is a rare pediatric genetic disorder characterized by excessive production of insulin by the pancreas. If left untreated, elevated insulin levels can cause extreme hypoglycemic (low blood sugar) events, increasing the risk of neurologic and developmental complications, including persistent feeding problems, learning disabilities, recurrent seizures, brain damage or even death.

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. Rezolute believes that RZ358 is ideally suited as a potential therapy for conditions characterized by excessive insulin levels and is developing it to treat the hyperinsulinism and low blood sugar characteristic of diseases such as congenital hyperinsulinism (CHI). 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.

Publications

NEJM Letter to the Editor: Anti–Insulin Receptor Antibody for Malignant Insulinoma and Refractory Hypoglycemia

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Treatment Of Severe Refractory Hypoglycemia Due To Malignant Insulinoma With A Novel Anti-Insulin Receptor Antibody

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Clinical Studies

Rezolute recently revealed results from the Phase 2b study. View Results

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ProgramINDPhase 1Phase 2Phase 3
RZ358    |
Tumor-Associated Hyperinsulinism (taHI)
Expanded Access Program
 
DrugStage
RZ358    |
Expanded Access Program
Tumor-Associated Hyperinsulinism (taHI)
Phase 2

RZ358

Insulinomas can cause hypoglycemia through the excessive secretion of insulin with subsequent activation of the insulin receptor (insulin-mediated HI). Insulinomas are the most common type of functional pancreatic neuroendocrine tumor and tend to be small and challenging to diagnose. There are approximately 10,000-15,000 patients in the US living with Insulinoma, of which approximately 10 percent have malignant/unresectable tumors requiring chronic treatment to control their HI.

RZ358 has been shown to counteract excessive insulin action downstream, at the insulin-receptor on target organs. The unique mechanism of action of RZ358 makes the therapy a potential universal treatment for any form of hyperinsulinism, including taHI resulting from insulinoma. Given the unmet need in taHI as well as the potential therapeutic benefit of RZ358 as demonstrated by the cases under the expanded access program (EAP) as well as the efficacy demonstrated in previous clinical experience in cHI,  Rezolute plans to evaluate RZ358 in an IND-opening late-stage (registrational) clinical trial as a new development program and second rare disease indication.


ProgramINDPhase 1Phase 2Phase 3
RZ402   |
Diabetic Macular Edema
 
DrugStage
RZ402   |
Diabetic Macular Edema
Phase 2

RZ402

REZ-SGFX-402_Diseased
REZ-SGFX-402_Treated

Diabetic retinopathy (DR) affects approximately one third of adults with diabetes and is the leading cause of vision loss in the working age population. Diabetic Macular Edema (DME) is a severe vision-threatening complication of DR characterized by swelling of the retina and thickening of the macula, the part of the eye that is responsible for high-resolution vision. Anti-vascular growth factor (anti-VEGF) injections into the eye are the current standard of care for DME, requiring continued administration over long periods of time to preserve vision. Due to their invasive route of administration and occasional serious side effects, there is a tendency to delay treatment until later in the disease course, and long-term compliance with eye injection regimens can be difficult for patients. Coupled with inadequate responsiveness in some patients, this leads to overall undertreatment and suboptimal vision outcomes in DME patients.

The contact-activation kallikrein-kinin system promotes increased vascular permeability and inflammation via key downstream mediators, including bradykinin, and activation of the intrinsic pathway of coagulation. Pathophysiologic upregulation of this system has been linked to a variety of diseases which are characterized by vascular dysfunction, including diabetic macular edema.

RZ402 is a small molecule selective and potent plasma kallikrein inhibitor (PKI) being developed as a potential oral therapy for the chronic treatment of diabetic macular edema (DME). By inhibiting the formation of kallikrein, RZ402 is designed to block downstream bradykinin production and the pro-inflammatory, pro-coagulant, and fluid-leakage contact-activation cascade.

RZ402 has been shown to reduce and prevent retinal vascular leakage in animal models by 80-90%.

Publications

Plasma Kallikrein Mediates Angiotensin II Type 1 Receptor–Stimulated Retinal Vascular Permeability

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Nonclinical safety and pharmacology of RZ402, a plasma kallikrein inhibitor, for the treatment of diabetic macular edema as a daily oral therapy

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Clinical Trials

RZ402, our oral PKI in development for DME, recently announced results from the Phase 1b study. View Results

RZ402, our oral PKI in development for DME, recently announced results from the Phase 1b study. View Results
Rezolute initiated a Phase 2a study in December 2022, with announcement of top line data planned for early 2024.

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