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Veru announced that it has enrolled the first patient in its Phase 2 clinical trial of VERU-100, a novel, proprietary gonadotropin-releasing hormone antagonist decapeptide, three-month subcutaneous depot injection formulation, for the treatment of hormone sensitive advanced prostate cancer. The Phase 2 clinical trial is an open label, multicenter, dose finding study evaluating the efficacy and safety of subcutaneous injected doses of VERU-100 in 35 men with hormone sensitive advanced prostate cancer. The primary efficacy endpoint is percent of men that reach castrate levels of total testosterone by Day 28 and maintain castrate testosterone levels beyond 90 days. The secondary endpoint is the percent of men that reach less than 20 ng/dL of total testosterone levels by Day 28 that are maintained at less than 20 ng/dL through Day 91.

Veru announced additional clinical results from the Phase 2 study demonstrating that the anticancer benefits of enobosarm, a selective androgen receptor (AR) targeting agent, were related to the presence and amount of AR expression in breast cancer tissue in subjects with AR+ER+ HER2- metastatic breast cancer, will be presented at the American Society of Clinical Oncology 2021 Annual Meeting being held June 4-8, 2021. Highlights of presentation: In preclinical studies, AR has been established as a tumor suppressor in breast cancer. Clinically, AR is expressed in up to 90% of breast cancers and targeting AR with enobosarm, an oral selective AR agonist, would be a major new endocrine therapy for metastatic breast cancer. The positive G200802 Phase 2 clinical study in 136 heavily pretreated women with AR+ER+HER2- metastatic breast cancer who progressed following CDK4/6 inhibitor and/or estrogen blocking agent treatment confirmed that the AR is commonly expressed in breast cancer tissue and when activated by enobosarm is acting in these patients as a tumor suppressor. In the overall Phase 2 study, the presence and the amount of AR receptor expression in breast cancer tissue correlated with a beneficial antitumor response. The best overall target lesion reduction of greater than30% occurred only in subjects who were AR+. In a post-hoc analysis of 84 women who had AR+ER+HER2- metastatic breast cancer, measurable disease, and centrally confirmed AR status at study entry, an AR positivity threshold of greater than or equal to 40% in breast cancer tissue distinguished patients that responded to enobosarm in both dose arms. AR positivity greater than or equal to 40% was common as 52% of subjects in study met this threshold. Focusing on the 9mg cohort, the dose selected for the Phase 3 ARTEST study, the best objective tumor response rate was 48% for greater than or equal to 40% AR positivity versus 0% for less than40% AR positivity. Similarly, the clinical benefit rate was 79% for greater than or equal to 40% AR positivity versus 18% for less than40% AR positivity. The median radiographic progression free survival was 5.5 month for greater than or equal to 40% AR positivity versus 2.75 months for less than40% AR positivity. Enobosarm was very well tolerated without masculinizing side effects, increases in hematocrit, or liver toxicity. Conclusions from Phase 2 study: Enobosarm, a selective AR agonist, targets AR, a tumor suppressor, in AR+ ER+ HER2- metastatic breast cancer; Objective tumor responses to enobosarm monotherapy require the presence and a threshold level of AR expression in heavily pretreated AR+ ER+ HER2- metastatic breast cancer; AR may be used as a biomarker to identify patients with AR+ ER+ HER2- metastatic breast cancer that are most likely to respond to enobosarm; Enobosarm treatment was well tolerated as an endocrine therapy without masculinizing side effects, increases in hematocrit, or liver toxicity; Targeting the AR tumor suppressor pathway to be studied prospectively in a 3rd line metastatic setting in the Phase 3 ARTEST registration clinical trial of enobosarm monotherapy versus active control for the treatment of AR+ER+HER2- metastatic breast cancer patients who have failed a nonsteroidal aromatase inhibitor, fulvestrant, and a CDK4/6 inhibitor.

Veru announced the presentation of the Phase 1b/2 clinical trial update of sabizabulin, an oral cytoskeleton disruptor which in prostate cancer also disrupts androgen receptor transport, to treat men with metastatic castration resistant prostate cancer who failed at least one androgen receptor targeting agent, at the American Society of Clinical Oncology 2021 Annual Meeting being held June 4-8, 2021. The Phase 1b/2 clinical study was designed as a dynamic study with an initial 3+3 standard safety study component followed by an expanded study with increases in dose and schedule. The Phase 1b/2 clinical trial enrolled 80 men and is ongoing with patients in both the Phase 1b and 2 components still on study. Highlights of the study presentation are as follows: Sabizabulin oral daily dosing was well tolerated, and the most common adverse events, being mostly Grade 1 and 2, were diarrhea, fatigue, nausea, and decrease in appetite. There was no evidence of clinically relevant neutropenia or neurotoxicity. Safety profile was similar to that reported in package inserts for androgen receptor targeting agents, abiraterone and enzalutamide. Clinically meaningful and durable evidence of objective tumor responses were observed in patients on 63mg oral daily dosing schedule: In the ITT population with measurable disease, the ORR was 20.7%.