On January 19, 2021 Veru Inc. (NASDAQ: VERU), an oncology biopharmaceutical company with a focus on developing novel medicines for the management of prostate and breast cancer, reported the online publication of an article in Nature Medicine, Volume 27, Issue 2, February, 2021, entitled: "The Androgen Receptor is a Tumor Suppressor in Estrogen Receptor-Positive Breast Cancer" (View Source or DOI # 10.1038/s41591-020-01168-7) by an international team headed by Drs (Press release, Veru, JAN 19, 2021, View Source [SID1234574197]). Theresa Hickey and Wayne Tilley at the University of Adelaide in collaboration with scientists at the Garvan Institute of Medical Research in Australia.

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In the Nature Medicine publication, Dr. Hickey and colleagues provide scientific evidence supporting a new discovery in breast cancer demonstrating that the androgen receptor acts like a tumor suppressor. Using human cell line and patient derived breast cancer models, they demonstrate that androgen receptor activation by androgens and enobosarm, a selective androgen receptor agonist, had potent antitumor activity in all ER positive breast cancer preclinical models tested including those that have become resistant to estrogen receptor targeted endocrine therapy as well as CDK 4/6 inhibitors, which are standard of care treatments for advanced, ER+ breast cancer. Further, enobosarm, by activating the androgen receptor, has demonstrated antitumor activity in both estrogen receptor targeted endocrine therapy resistant and CDK4/6 inhibitor resistant metastatic human breast cancer models. In contrast, androgen receptor inhibitors, like enzalutamide, had no effect. This study clears up the confusion in the scientific field regarding the role that the androgen receptor is playing in ER+ breast cancer.

"We provide compelling new experimental evidence that androgen receptor activating drugs, like enobosarm, can be more effective than existing (e.g., Tamoxifen) or new (e.g., Palbociclib) standard-of-care treatments and, in the case of the latter, can be combined to enhance growth inhibition. Moreover, enobosarm as a selective androgen receptor activating agent lacks the undesirable masculinizing side effects of natural androgens and has potential additional clinical benefits in women including promotion of bone, muscle and physical function, and mental health," said Professor Wayne Tilley, Director of the Dame Roma Mitchell Cancer Research Laboratories, and Associate Professor Theresa Hickey, Head of the Breast Cancer Group, who led the Nature Medicine study.

"This important new work establishes that the androgen receptor is a tumor suppressor and that enobosarm, as an AR targeted agent, has anti-tumor activity not only in AR+ ER+ metastatic breast cancer that has become resistant to estrogen receptor targeted endocrine and CDK4/6 inhibitor treatments, but also that enobosarm in combination with a CDK4/6 inhibitor (e.g. Palbociclib) restores CDK4/6 inhibitor sensitivity in ER+ breast cancer that has become resistant to CDK4/6 inhibition," said Mitchell Steiner, M.D., Chairman, President and Chief Executive Officer of Veru. "I would like to congratulate Dr. Tilley and his international team for this landmark study which provides deep scientific evidence for the novel therapeutic approach Veru has taken to address estrogen receptor targeted endocrine therapy and CDK4/6 inhibitor resistance in patients with AR+ ER+ metastatic breast cancer. We are excited to be advancing enobosarm, our AR activating targeted agent, into a Phase 3 registration ARTEST clinical trial scheduled for next quarter."

Enobosarm is an oral, first-in-class, new chemical entity, selective androgen receptor targeting agonist that activates the androgen receptor in AR+ER+HER2- metastatic breast cancer without unwanted masculinizing side effects and has potentially beneficial effects including increase in muscle mass and physical function and the promotion of bone strength and healing. Enobosarm is the first new class of targeted endocrine therapy for advanced breast cancer in decades. Last quarter the FDA agreed to the ARTEST Phase 3 registration clinical trial design to evaluate the efficacy and safety of enobosarm, a selective androgen receptor targeted agent, versus physician’s choice of either exemestane or tamoxifen as an active comparator for the treatment of metastatic ER+/HER2- breast cancer in approximately 240 patients who have failed a nonsteroidal aromatase inhibitor (anastrozole or letrozole), fulvestrant, and a CDK4/6 inhibitor. The primary endpoint is radiographic progression-free survival.