An evaluation of the pharmacokinetic and pharmacodynamic effects of bremelanotide administered by intranasally and subcutaneously in healthy male and female volunteers — VialBase Research

Summary

Phase 1/2 pharmacokinetic and pharmacodynamic study of bremelanotide (PT-141) administered via intranasal and subcutaneous routes in healthy men and women. The study established dose-response relationships and demonstrated sexual arousal effects in both sexes.

Key Findings

• Bremelanotide produced dose-dependent erectile responses in healthy men
• Genital arousal responses also observed in female participants
• Both intranasal and subcutaneous routes were effective
• Subcutaneous route showed more predictable pharmacokinetics
• Intranasal development was later abandoned due to blood pressure concerns
• Established the 1.75 mg subcutaneous dose used in phase 3 trials

Methodology

Phase 1/2, randomized, double-blind, placebo-controlled, crossover studies in 48 healthy volunteers (men and women). Bremelanotide administered at multiple doses via intranasal spray or subcutaneous injection. Erectile response (RigiScan in men), genital blood flow (in women), pharmacokinetic sampling, and safety assessments.

Limitations

• Healthy volunteers — not patients with sexual dysfunction
• Intranasal route ultimately abandoned (phase 3 used SC only)
• Small sample sizes per dosing group
• Short-duration pharmacodynamic assessments
• Female endpoints limited by measurement technology at the time

Relevance to Content

Establishes PT-141’s dual-sex efficacy — important for content positioning beyond “female Viagra.” The route-of-administration evolution (nasal → injectable) is relevant for practical content. The dose-finding data informs clinical dosing discussions. Useful for science-forward content about PT-141’s mechanism and development.

See Also

• Parent compound: PT-141