Rezolute, Inc. announced that the Company has initiated a Phase 2 proof-of-concept study for RZ402, a plasma kallikrein inhibitor (PKI) being developed as an oral therapy for the treatment of Diabetic Macular Edema (DME). The current standard of care for DME is anti-vascular growth factor (anti-VEGF) injections into the eye, requiring repeated administration over recurring periods of time to preserve vision, with significant treatment burden and occasional serious side effects. The invasive route of administration, coupled with inadequate responsiveness in some patients, leads to overall undertreatment and suboptimal vision outcomes in DME patients.

The Phase 2 study is a multi-center, randomized, double-masked, placebo-controlled, parallel-arm study to evaluate the safety, efficacy, and pharmacokinetics of RZ402 administered as monotherapy over a 12-week treatment period in participants with DME who are naïve to or have received limited anti-VEGF injections. The study population will include DME patients with mild to moderate Non-Proliferative Diabetic Retinopathy (NPDR), Central Subfield Thickness (CST) of =320 µm (or corresponding values), and Best-Corrected Visual Acuity (BCVA) of =78 Early Treatment Diabetic Retinopathy Study (ETDRS) letters (=20/25 on Snellen chart). Patients who have previously received more than three anti-VEGF injections prior to the study will be excluded.

Eligible participants will be randomized equally, to one of three RZ402 active treatment arms at doses of 50, 200, and 400 mg, or a placebo control arm, and will receive study drug once daily for 12 weeks, before completing a four-week follow-up. The study is expected to enroll approximately 100 patients overall, across approximately 25 investigational sites in the United States. The principal endpoints of the trial include the change in CST, as measured by Spectral Domain Ocular Coherence Tomography (SD-OCT), the change in visual acuity by ETDRS scale, the repeat dose pharmacokinetics of RZ402 in patients with DME, and the safety and tolerability of RZ402.