Benzinga | May 4, 2021 12:33PM EDT

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

* Rezolute Inc (NASDAQ: 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.