Rezolute, Inc., a US bio-venture with Handok and Genexine as its largest shareholders, acquired approval from the US Food and Drug Administration (FDA) for the Investigational New Drug (IND) of RZ402 on December 3, 2020 and will enter first-in-human Phase I clinical trials in the first quarter of 2021.

RZ402 is an oral plasma kallikrein inhibitor for the treatment of diabetic macular edema (DME). In a prevention and treatment model for rodents, it was found to reduce DME retinal inflammation and retinal vascular leakage by 80% or more. In pre-clinical trials, RZ402’s safety profile was confirmed by single and repeated injections within the dose range. Results of the animal study helped to overcome the limits of current DME treatment, which requires injections directly into the vitreous body, and confirmed RZ402’s potential as an oral treatment.

“Treatment of DME has progressed remarkably with the emergence of VEGF-inhibiting treatment, but some patients are uncomfortable with the fact that it is in the form of injections. RZ402 is expected to resolve this problem as it uses a daily intake method,” said Brian Roberts, Head of Clinical Development at Rezolute. He added, “In the animal studies conducted so far, we have confirmed positive data on the efficacy and safety of RZ402 in the treatment of DME. In particular, IND approval is a core phase in which we can confirm the potential of RZ402 as an oral treatment, and we plan to launch the clinical trial Phase I during the first quarter of 2021.”

Rezolute spearheads development of innovative treatments for rare diseases. In addition to RZ358, a treatment for congenital hyperinsulinism for which clinical trial Phase IIb is underway in Europe and the United States, preclinical trials of RZ402 have been completed successfully, and the drug will soon enter the clinical trial phase, thereby strengthening Rezolute’s R&D pipeline. 

RZ358 is a monoclonal antibody and first-in-class treatment for congenital hyperinsulinism that binds to a unique site on the insulin receptors throughout the body. In June earlier this year, it was designated as a treatment for a rare pediatric disease (RPD) by the US FDA. It is currently undergoing RIZE study, which is clinical trial Phase IIb, and topline data will be available in the first half of 2021.

In October this year, Rezolute received an investment of USD 41 million from leading investment companies CAM Capital, Federated Hermes Kaufmann, Surveyor Capital, and BVF Partners, and it was listed on the Nasdaq later in November. Handok and Genexine jointly invested in Rezolute in 2019 to become its largest shareholders. Handok reinforced its drug pipeline for diabetes and rare diseases by acquiring domestic commercialization rights for RZ402 and RZ358 in September 2020.