PT-141 (Bremelanotide)

Brand names: Vyleesi®

Mechanism of action: Melanocortin-4 receptor (MC4R) agonist; Acts on central nervous system pathways involved in sexual arousal; Does not act directly on the vascular system, unlike PDE5 inhibitors

Approved indications: Acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women

Proposed indications: Erectile dysfunction (off-label); Female sexual arousal disorder; Libido enhancement (general)

Reported dosing range*: Greater than 7 mg, intranasal (investigational, off-label use in men)

Outside the approved HSDD indication (1.75 mg subcutaneous as-needed), earlier development-stage trials studied this compound (then called PT-141) for erectile dysfunction in men via intranasal administration, finding a statistically significant erectile response at doses greater than 7 mg (Diamond LE et al. (2004). Double-Blind, Placebo-Controlled Evaluation of the Safety, Pharmacokinetic Properties and Pharmacodynamic Effects of Intranasal PT-141, a Melanocortin Receptor Agonist, in Healthy Males and Patients With Mild-to-Moderate Erectile Dysfunction. International Journal of Impotence Research). Note this is a different route (intranasal, not subcutaneous) and different dose than the approved HSDD indication. Not FDA-approved for use in men or in postmenopausal women.

*General range reported in available research or other sources -- not an individualized recommendation. Actual use should be supervised by a qualified provider.

Administration: Subcutaneous injection — As needed, prior to anticipated sexual activity

Compare with: Melanotan II

Evidence rating: ⭐⭐⭐⭐☆ (Approved for a specific indication) — Strong randomized controlled trial support for its approved indication (female HSDD); evidence for off-label uses like erectile dysfunction is more limited.

Landmark trials: RECONNECT Study 1 and Study 2 (Phase 3) — Supported FDA approval for HSDD in premenopausal women.

Common side effects: Nausea, Flushing, Injection-site reactions, Headache

Serious risks: Transient increases in blood pressure; Focal hyperpigmentation of the skin, including face and gingiva, has been reported with repeated use and may persist after discontinuation; Safety of combination use with other HSDD therapies has not been established

Drug interactions: May transiently raise blood pressure — use caution with other agents affecting blood pressure.

Monitoring: Blood pressure, particularly with repeated use

Legal status: Prescription required. This is an FDA-approved medication for a specific indication (HSDD in premenopausal women) — available only through a licensed prescriber. Off-label use in other populations (e.g., men, postmenopausal women) is not FDA-approved. Dosing is determined by your prescriber and is not provided here.

Regulatory status: FDA Approved (premenopausal women, HSDD) • Not approved for other populations

Contraindications: Uncontrolled hypertension; Known cardiovascular disease; Pregnancy; Hypersensitivity to bremelanotide or formulation components

Pregnancy & breastfeeding: Not recommended during pregnancy. Safety during breastfeeding has not been established.

Dhillon S, Keam SJ. (2019). Bremelanotide: First Approval. Drugs, 79, 1599–1606. https://doi.org/10.1007/s40265-019-01187-w Clayton AH, Kingsberg SA, Portman D, et al. (2022). Safety profile of bremelanotide across the clinical development program. Journal of Women's Health.