Rezolute, Inc, with Handok and Genexine as its largest shareholders, announced the results of a Phase II(a) clinical trial of RZ358, a candidate substance for new drugs, on patients with post-gastric bypass hypoglycemia (PGBH) at ENDO 2021 on March 22, 2021.

The clinical trial results showed meaningful improvement in low blood sugar levels among more than 50% of patients in the trial, and average blood sugar levels were almost normalized, thereby satisfying research goals. In addition, the drug concentration and exposure-reaction relationship were also confirmed through the collective pharmacokinetics and pharmacodynamics model.

According to Brian Roberts, Rezolute’s Head of Clinical Development., “This clinical trial confirmed the mechanism of action unique to RZ358, the candidate substance for new drugs, and its possibility as a treatment. This signifies that there is a possibility RZ358 can treat low blood sugar levels caused by hyperinsulinism.” He added, “The data produced using the pharmacokinetics and pharmacodynamics model will be a significant help in research on congenital hyperinsulinism and planning and implementing pivotal clinical trials for RZ358.”

The presentation was made under the title “A Single and Repeat-Dose Study of RZ358 in Patients with Post-Gastric Bypass Hypoglycemia (PGBH)”. It reported the results of single ascending (3, 6, and 9 mg/kg) and repeated doses (3 mg/kg/week for four weeks) of RZ358 in a study. Serial measurements of RZ358 concentrations as well as biomarkers and continuous glucose monitoring (CGM) were performed. The results showed that RZ358 was safe and well tolerated with no serious adverse reactions. 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.

RZ358 is an intravenously administered human monoclonal antibody that binds to a unique site on the insulin receptors throughout the body. It is being developed to treat excessive insulin levels, such as hyperinsulinism and low blood sugar levels. RZ358 received Orphan Drug Designation in the United States and European Union as well as Pediatric Rare Disease Designation. Rezolute is currently evaluating RZ358 in patients with congenital hyperinsulinism in the RIZE trial, a Phase IIb clinical trial.

Rezolute is a U.S. bio-venture developing targeted treatments for rare diseases and metabolic illnesses and was listed on the Nasdaq in 2020. Major R&D pipelines include RZ358, currently in Phase IIb clinical trials and a treatment for the rare pediatric endocrine disease of congenital hyperinsulinism, and RZ402, an oral plasma kallikrein inhibitor for the treatment of diabetic macular edema (DME) that is currently in Phase I clinical trials. Handok and Genexine jointly invested in Rezolute in 2019 to become its largest shareholders. Handok reinforced its drugs pipeline for diabetes and rare diseases by acquiring domestic commercialization rights for RZ402 and RZ358 in 2020.