Rezolute's Plasma Kallikrein Inhibitor Shows Encouraging Action In Diabetic Macular Edema Study

Rezolute Inc RZLT has announced positive topline results from Phase 1a clinical study evaluating RZ402 to treat diabetic macular edema (DME).
Single-dose oral administration of RZ402 resulted in plasma concentrations that substantially exceeded target pharmacologically active drug levels, demonstrating the potential for once-daily dosing.
The study enrolled 30 subjects in three planned sequential dose-level cohorts of 25 mg, 100 mg, and 250 mg.
Single doses of RZ402 resulted in dose-dependent increases in systemic exposure. Plasma concentrations of RZ402 exceeded the 3.5 ng/mL target concentration that was pharmacologically active in animal models for 24 hours after receipt of the 25 mg starting dose, and by over 20 and more than 5-fold at maximum concentration and 24 hours after dosing, respectively, at the highest dose tested.
RZ402 was generally safe and well-tolerated at all doses tested, without dose-limiting toxicities.
The company is planning a Phase 1b multiple ascending dose study, expected to initiate in the third quarter of this year.
RZ402 is a selective and potent plasma kallikrein inhibitor (PKI). By inhibiting kallikrein formation, RZ402 is designed to block downstream bradykinin production and the pro-inflammatory, pro-coagulant, and fluid-leakage contact-activation cascade.
Price Action: RZLT shares are up 3.32% at $7.46 during the market session on the last check Tuesday.