PT-141

Bremelanotide · Vyleesi

PT-141 (bremelanotide) is a synthetic melanocortin receptor agonist and the first centrally acting peptide approved by the FDA for a sexual dysfunction indication — marketed as Vyleesi (Palatin Technologies / AMAG Pharmaceuticals) for hypoactive sexual desire disorder (HSDD) in premenopausal women. Unlike phosphodiesterase-5 inhibitors such as sildenafil, which act peripherally through vascular smooth muscle relaxation, PT-141 acts centrally via melanocortin MC3R and MC4R receptors in the hypothalamus to modulate sexual motivation and arousal pathways — a mechanistically distinct approach that is effective regardless of vascular status. Pivotal Phase 3 RCTs in premenopausal women with HSDD demonstrated statistically significant improvements in satisfying sexual events and desire scores versus placebo, establishing the clinical evidence base for FDA approval in 2019. PT-141 dosage: the FDA-approved dose is 1.75mg administered as a single subcutaneous injection in the abdomen using an auto-injector device, approximately 45 minutes before anticipated sexual activity; it should not be used more than once per 24 hours or more than 8 times per month per prescribing guidance. Compounded PT-141 — available through licensed compounding pharmacies — is prepared in various concentrations for use under physician supervision. PT-141 nasal spray formulations have been investigated as an alternative delivery route, though the approved form is subcutaneous injection. PT-141 for men: while FDA approval is limited to premenopausal women with HSDD, PT-141 is used off-label in men for sexual dysfunction, including cases where PDE5 inhibitors are insufficient or contraindicated; the central mechanism of action is not sex-specific. Side effects: the most common adverse effect is nausea (reported in approximately 40% of subjects in pivotal trials), followed by flushing, headache, and transient hyperpigmentation with repeated use. A transient increase in blood pressure is observed in the first hour post-injection; PT-141 is contraindicated in patients with uncontrolled hypertension or cardiovascular disease. PT-141 (Vyleesi) is FDA-approved and requires a prescription; compounding pharmacy access also requires a prescription. Providers offering PT-141 consultations — including telehealth platforms — can be found in the PeptideBase directory. [Women's health addendum] Bremelanotide (marketed as Vyleesi) is FDA-approved specifically for hypoactive sexual desire disorder (HSDD) in premenopausal women, based on Phase 3 RECONNECT trial data; systematic review characterizes the clinical benefit as modest, with nausea/flushing as common adverse effects and cardiovascular contraindications (uncontrolled hypertension, known cardiovascular disease). It is not evidenced or approved for menopausal indications, and prescribing information directs use of contraception with discontinuation if pregnancy is suspected — there is no human pregnancy safety data supporting continued use.