On February 22, 2022 (local time), Rezolute, Inc., a U.S. bio-venture in which Handok and Genexine are the largest shareholders, announced a major positive outcome during the U.S. Phase Ib multiple-dose escalation (MAD) study for RZ402. This outcome reconfirms that RZ402 may be orally administered once daily. Rezolute plans to start the Phase II clinical trial in the second half of this year.

RZ402, which is being developed by Rezolute, is a plasma kallikrein inhibitor for the treatment of diabetic macular edema. It is being developed as an oral treatment to overcome the limitations of existing injections. Handok invested in Genexine and Rezolute in 2019, when it also became their largest shareholder. In 2020, it obtained commercialization rights in Korea for RZ402.

In the results of the recently completed Phase Ib multiple-dose escalation study, RZ402 provided evidence it was safer and more tolerable, even at higher doses, than in the previous single-dose escalation study. In addition, no serious drug or other side effects were reported.

“RZ402 is an oral treatment that overcomes the limitations of existing injections and can become a new paradigm in the treatment of diabetic macular edema. Treating patients faster can lead to better clinical outcomes and prevent vision loss, especially in people suffering from diabetic macular edema,” said Dr. Raj Agrawal, M.D., Vice President of Rezolute. He added, “New treatment options are needed as half of the people with diabetic macular edema are burdened with ocular injections, which are VEGF inhibitory drugs, without particular effect.”

“We are delighted to be able to see meaningful results from analysis of the plasma kallikrein activity of RZ402 in people. RZ402 showed a strong efficacy in suppressing retinal inflammation and retinal vascular leakage, which are the main features of diabetic macular edema in animal models. In addition, this study exceeded the target concentration, which confirmed the potential of RZ402 in the treatment of diseases related to the Kinin-kallikrein system, including diabetic macular edema,” said Dr. Brian Roberts, M.D., Senior Vice President and Head of Clinical Development at Rezolute.

Rezolute, which develops targeted therapeutics for rare and metabolic diseases, was listed on the NASDAQ in 2020. Major items in the R&D pipeline include RZ358 for the treatment of congenital hyperinsulinemia, a rare pediatric endocrine disease, and RZ402, an oral plasma kallikrein inhibitor for the treatment of diabetic macular edema. Handok holds commercialization rights for these two products in Korea. Rezolute plans to present the final outcomes of the RZ402 clinical trial so far at this year’s conference.