The article, titled, "An open-label, single-dose, randomized, parallel-group study of the safety and relative bioavailability of topical sildenafil cream vs oral sildenafil in healthy male adults," discusses findings from the study evaluating a higher and lower dose of topical Sildenafil Cream applied to the penis with and without condom use compared with a 50 mg oral dose of sildenafil. Access the full publication here.

"We are a women’s health company, and that remains at the center of everything we do. One of Daré Bioscience’s core strengths is our ability to apply sophisticated formulation and drug-delivery science to well-understood active ingredients in ways designed to address important gaps in care," said Sabrina Martucci Johnson, President and Chief Executive Officer of Daré Bioscience. "These peer-reviewed results are exciting because they demonstrate the potential power of that approach. Topical dosing is targeted and has been shown to result in substantially lower systemic exposure than an oral dose of sildenafil. This study in men provided additional clinical insight into our proprietary topical Sildenafil Cream formulation and expanded the evidence supporting its differentiated delivery profile. We believe that knowledge ultimately strengthens the scientific foundation of our work in women’s sexual health while also supporting the broader potential of Daré Bioscience’s formulation."

The open-label, randomized study enrolled 62 healthy men who received a single dose of either 36 mg or 71 mg of sildenafil in topical cream, with or without condom use, or a 50 mg oral dose of sildenafil in tablet form. The study evaluated safety and systemic pharmacokinetics of sildenafil and its active metabolite, N-desmethyl sildenafil.

The study treatments were well tolerated, with all 14 treatment-emergent adverse events reported during the study characterized as mild. Seven of the 14 events occurred in five participants who received oral sildenafil. There were no serious adverse events, severe adverse events, deaths or discontinuations due to treatment-emergent adverse events.

Importantly, Daré Bioscience’s proprietary topical Sildenafil Cream resulted in substantially lower systemic exposure to sildenafil compared with the oral sildenafil group. Mean maximum plasma concentrations for sildenafil following topical administration (all four Sildenafil Cream dosing groups) ranged from 969 to 1,274 pg/mL, compared with 238,000 pg/mL for the oral sildenafil group. Relative bioavailability of sildenafil following topical administration (all four Sildenafil Cream dosing groups) ranged from 2.55% to 3.20%, suggesting a much lower systemic exposure as compared with the oral sildenafil group.

At the 71 mg topical dose, mean maximum plasma concentration of sildenafil was approximately 187-fold lower than following the 50 mg oral dose, while systemic exposure measured by AUClast and AUCinf was approximately 33-fold and 34-fold lower, respectively. 71 mg sildenafil in 2 grams of cream was the dose tested in a subsequent Phase 2b study of Sildenafil Cream, 3.6% in premenopausal women for treatment of female sexual arousal disorder.

"These Phase 1 findings provide important clinical evidence regarding the potential safety and pharmacokinetic profile of topical Sildenafil Cream in men," said David Friend, PhD, Chief Scientific Officer of Daré Bioscience. "The substantially lower systemic exposure observed with topical administration is consistent with the rationale for localized delivery of sildenafil and supports continued development of our investigational Sildenafil Cream, 3.6% as a potential differentiated approach for arousal concerns."

The study was designed as a safety and pharmacokinetic evaluation in healthy men without erectile dysfunction and therefore did not assess efficacy or erectile response. The publication adds to the clinical evidence supporting continued development of Daré Bioscience's proprietary Sildenafil Cream, 3.6% formulation, which has been evaluated in women with female sexual arousal disorder.

While Daré Bioscience remains solely focused on advancing solutions for women’s health, the Company believes that a broader body of clinical evidence around its proprietary formulations can provide valuable scientific insights that ultimately strengthen the foundation for its work in women’s sexual health. The Phase 1 study in men provided additional clinical evidence characterizing the behavior of the proprietary Sildenafil Cream, 3.6% formulation and Daré Bioscience’s localized drug-delivery approach using sildenafil, a well-characterized active pharmaceutical ingredient. Sildenafil Cream, 3.6% has been clinically evaluated in women with female sexual arousal disorder, the clinically analogous condition to erectile dysfunction in men.