Daré Bioscience Announces Publication of Phase 1/2 Pharmacokinetic, Safety & Pharmacodynamic Data for a Potential New Hormone-Free Treatment for Vulvovaginal Atrophy

Daré Bioscience, Inc. recently announced the publication of results of its Phase 1/2 clinical study of DARE-VVA1, a proprietary, investigational formulation of tamoxifen for intravaginal administration to treat vulvovaginal atrophy (VVA) in women without the use of hormones. The journal article, Pharmacokinetics, safety and preliminary pharmacodynamic evaluation of DARE-VVA1: a soft gelatin capsule containing tamoxifen for the treatment of vulvovaginal atrophy, was published online and will appear in Climacteric, the official journal of the International Menopause Society. The randomized, double-blind, placebo-controlled study was designed to evaluate the pharmacokinetics, safety and pharmacodynamics of DARE-VVA1 in postmenopausal participants with moderate to severe VVA.

“We are excited to have this peer-reviewed article published in the International Menopause Society’s journal, Climacteric, and share our findings with the broader women’s health community,” said Andrea Thurman, MD, Medical Director for Daré Bioscience and lead author of the journal article. “The data from the study demonstrated safety and tolerability of our investigational product DARE-VVA1, as well as showed an improvement in vaginal cytology parameters and the bothersome vaginal symptoms commonly associated with VVA.”

Daré is developing DARE-VVA1 as a new hormone-free treatment option to address moderate to severe VVA. If successful, DARE-VVA1 has the potential to be an important therapeutic for the treatment of VVA for women currently or previously treated for hormone-receptor positive (HR+) breast cancer and for other women who would like a vaginal, non-hormonal option for VVA treatment.

Globally, breast cancer is the most frequently diagnosed cancer type, accounting for over two million cases each year. Approximately 4 million US women have a history of invasive breast cancer, and of all breast cancer diagnoses in US women, it is estimated that more than 68% are HR+. VVA prevalence in postmenopausal breast cancer survivors is estimated at 42% to 70%.

“The unmet need for an effective non-hormonal treatment for VVA caused by anti-cancer endocrine therapy in patients diagnosed with HR+ breast cancer is undeniable. The current lineup of estrogen-based therapies, commonly used to treat VVA in non-cancer patients, can be challenging for both HR+ breast cancer patients and their providers as the use of estrogen products, in any form, is often contraindicated for the HR+ breast cancer patient population,” said Sabrina Martucci Johnson, President and Chief Executive Officer of Daré Bioscience. “If we are successful, vaginally-administered, hormone-free DARE-VVA1 will offer patients and providers an important new treatment option to address one of the most common vaginal side effects associated with breast cancer therapy.”

The journal article is available online: https://doi.org/10.1080/13697137.2023.2211763

In November 2022, Daré announced positive topline results from the Phase 1/2 clinical study of DARE-VVA1.

Daré is conducting activities to support submission of an Investigational New Drug (IND) application and initiation of a Phase 2 clinical study of DARE-VVA1.

VVA is an inflammation and thinning of the vaginal epithelium due to the reduction in levels of circulating estrogen. Typical symptoms include vaginal dryness, itching, burning, and painful intercourse, adversely impacting quality of life. VVA is a common condition in postmenopausal women and women with, or with a history of, HR+ breast cancer. Many breast cancer survivors experience menopausal symptoms irrespective of age as a direct consequence of their cancer treatment. Breast cancer patients treated with aromatase inhibitors refer to VVA as one of the most unpleasant side effects of treatment. The prevalence of VVA in postmenopausal breast cancer patients is estimated to be between 42% and 70%.

Commonly used therapies for VVA are estrogen based and are often contraindicated in HR+ breast cancer patients, or patients with a genetic predisposition or history of familial disease, because of the concern that estrogen use will promote recurrence or occurrence of disease.

DARE-VVA1 is an investigational, proprietary formulation of tamoxifen for intravaginal administration. Daré is developing DARE-VVA1 as a hormone-free alternative to estrogen-based therapies for the treatment of moderate to severe VVA. Tamoxifen is a well-known and well-characterized selective estrogen receptor modulator (SERM) that has been prescribed by oncologists for decades for the treatment of breast cancer. Tamoxifen has unique properties that produce different effects (estrogen agonist or estrogen antagonist) in different types of tissues. In breast tissue, tamoxifen acts as an estrogen antagonist, meaning that it can inhibit estrogen’s effect and hence why it may be effective in treating HR+ breast cancer. In contrast, in other tissues such as vaginal tissues, tamoxifen has been reported to elicit an estrogen-like response. This has the potential to have a favorable effect on vaginal cytology. Studies of tamoxifen conducted over the last 40 years have documented its estrogen-like effects on vaginal epithelium. Localized tamoxifen therapy such as DARE-VVA1 thus has the potential to counter the physiologic changes that lead to VVA without introducing estrogen back into the system.

Daré Bioscience is a biopharmaceutical company committed to advancing innovative products for women’s health. The company’s mission is to identify, develop and bring to market a diverse portfolio of differentiated therapies that prioritize women’s health and well-being, expand treatment options, and improve outcomes, primarily in the areas of contraception, vaginal health, reproductive health, menopause, sexual health and fertility.

Daré’s first FDA-approved product, XACIATO™ (clindamycin phosphate) vaginal gel, 2% is a lincosamide antibacterial indicated for the treatment of bacterial vaginosis in female patients 12 years of age and older, which is under a global license agreement with Organon. XACIATO is a clear, colorless, viscous gel, to be administered once intravaginally as a single dose. Daré’s portfolio also includes potential first-in-category candidates in clinical development: Ovaprene, a novel, hormone-free monthly intravaginal contraceptive whose US commercial rights are under a license agreement with Bayer; Sildenafil Cream, 3.6%, a novel cream formulation of sildenafil to treat female sexual arousal disorder utilizing the active ingredient in Viagra; and DARE-HRT1, a combination bio-identical estradiol and progesterone intravaginal ring for menopausal hormone therapy. For more information, visit www.darebioscience.com.