PT-141 Pharmacokinetics
PT-141 half-life, absorption, routes of administration, and clearance.
Absorption, Distribution, and Elimination
Following subcutaneous injection of the FDA-approved 1.75 mg dose (Vyleesi), PT-141 demonstrates rapid absorption with predictable kinetics. • Subcutaneous Tmax is approximately 1 hour, with peak plasma concentrations reached reliably across the 1.75 mg clinical dose range. • Terminal elimination half-life is approximately 2.7 hours — substantially shorter than the 24-hour duration of clinical effect, indicating that receptor-mediated central signaling persists well beyond systemic peptide clearance. • Bioavailability following subcutaneous administration has not been published as an absolute figure in the FDA label, but the consistent dose-response relationship across Phase 3 trials confirms reliable systemic exposure from the SC route.
Physicochemical and PK profile
- Molecular Formula
- C50H68N14O10
- Molecular Weight
- 1025.18 g/mol
- CAS Number
- 189691-06-3
- Half-Life
- 2.7 hours
- Sequence
- Ac-Nle-cyclo(Asp-His-D-Phe-Arg-Trp-Lys)-OH
- Solubility
- Soluble in water
- Storage
- Store at controlled room temperature or refrigerated.
References
- Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder · Kingsberg SA, et al. · 2019
- Kingsberg SA, et al. Bremelanotide for the treatment of hypoactive sexual desire disorder: two randomized phase 3 trials. Obstet Gynecol. 2019;134(5):899-908. · Kingsberg SA, Clayton AH, Portman D, Williams LA, Krop J, Jordan R, Lucas J, Simon JA · 2019
- Safety Profile of Bremelanotide Across the Clinical Development Program. · Clayton AH, Kingsberg SA, Portman D et al. · 2022
- The neurobiology of bremelanotide for the treatment of hypoactive ... · Pfaus JG, Sadiq A, Spana C, Clayton AH · 2022
- Clayton AH, et al. Long-term safety and efficacy of bremelanotide for hypoactive sexual desire disorder. Obstet Gynecol. 2019;134(5):909-917. · Simon JA, Kingsberg SA, Portman D, Williams LA, Krop J, Jordan R, Lucas J, Clayton AH · 2019
- Prespecified and Integrated Subgroup Analyses from the RECONNECT Phase 3 Studies of Bremelanotide. · Simon JA, Kingsberg SA, Portman D et al. · 2022
- [PDF] Vyleesi (bremelanotide) - accessdata.fda.gov
- Diamond LE, et al. An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist. J Sex Med. 2006;3(4):628-38. · Diamond LE, Earle DC, Heiman JR, Rosen RC, Perelman MA, Harning R · 2006
- Safarinejad MR. Salvage of sildenafil failures with bremelanotide: a randomized, double-blind, placebo controlled study. J Urol. 2008;179(3):1066-71. · Safarinejad MR, Hosseini SY · 2008
- Long-Term Safety and Efficacy of Bremelanotide for Hypoactive Sexual Desire Disorder. · Simon JA, Kingsberg SA, Portman D et al. · 2019
- Bremelanotide - LiverTox - NCBI Bookshelf - NIH
- Molinoff PB, et al. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci. 2003;994:96-102. · Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY · 2003
- Bremelanotide: First Approval - PubMed · Dhillon S, Keam SJ · 2019