Description

Product Summary – PT-141 11mg

Field	Details
Product Name	PT-141
Category	Synthetic peptide; melanocortin receptor (MC1R & MC4R) agonist.
Length	7 amino acids (cyclic heptapeptide analog of α-MSH)
Amino Acid Sequence	Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-OH (cyclic lactam structure; N-terminal acetylation, D-Phe substitution improves stability)
Molecular Formula	C₅₀H₆₈N₁₄O₁₀
Molecular Weight	≈ 1025.2 Da
Form & Purity	Lyophilized powder or pre-filled auto-injector; ≥95% purity (HPLC, vendor spec).
Storage	Store at controlled room temperature (20–25 °C) in original packaging; protect from light. Do not freeze.
Key Mechanisms	– Activates central melanocortin receptors (MC3R/MC4R) in the hypothalamus → increases dopaminergic signaling linked to sexual desire – Unlike PDE5 inhibitors, it acts via CNS pathways rather than vascular nitric oxide pathways – Improves sexual desire and reduces distress in HSDD
Research / Clinical Use Cases	– Approved: HSDD in premenopausal women (FDA 2019) – Investigational: Male erectile dysfunction (shown efficacy independent of nitric oxide), antidepressant-induced sexual dysfunction, potential metabolic roles
Common AEs / Safety Signals	– Nausea, flushing, headache, vomiting, injection-site reactions – Temporary increase in blood pressure and decrease in heart rate; contraindicated in uncontrolled hypertension or cardiovascular disease – Hyperpigmentation of skin and gums with chronic use (due to MC1R activation)
Contraindications / Warnings	– Pregnancy (category not established; avoid use) – Uncontrolled hypertension, known cardiovascular disease – Caution in patients with a risk of syncope or those prone to nausea/vomiting
Regulatory / Compliance	– FDA approved (2019, brand Vyleesi®) for premenopausal women with HSDD – Not approved for men (though studied in ED) – Prescription-only; limited to specific indications

Mechanism of Action PT-141

PT-141 is a non-selective receptor agonist, but its functional potency is biased towards the MC4R, which is the principal subtype of MCR implicated in prosexual effects. PT-141 binds to MC4R and activates it, triggering the intracellular signaling cascades. [1]

Sexual Health Effects

Preclinical and translational data describe the localized action of PT-141 in the specific CNS areas, including the medial preoptic area (mPOA) and components of the mesolimbic reward system that regulate sexual motivation and behavior. Animal data explain that PT-141 activates the neurons in the hypothalamus to enhance the domain release, which in turn hypothetically improves the sexual motivation.

The MCR signaling, triggered by PT-141, also interacts with other neurotransmitters, such as nitric oxide signaling, which has a role in genital vasodilation and erection. Preclinical studies found that PT-141 caused the cross-talk of serotonergic and glutamatergic, which led to a change in the excitatory/inhibitory balance between the sexual motivational network.

PT-141 acts centrally and modulates the autonomic output to enhance the parasympathetic outflow and NO synthase activity in the cavernosal efferent pathways. Animal models describe the ability of PT-141 to produce an erection and show synergistic effects when combined with a peripheral agent like a PDE-5 inhibitor. [3]

Latest Research on HSDD & PT-141

Most recent evidence shows that PT-141 supports boosting sexual desire and reducing issues in women with HSDD. Brain scans strengthen that it affects how the brain processes sexual signals. But not everyone agrees that the data is substantial; some reports note missing information, higher side effects, and lower long-term preference for the drug. [4]

Tolerability and Safety Considerations of PT-141

Generally well tolerated in approved use
The most common adverse events can be nausea, flushing, headache, and a transient increase in blood pressure.
Contraindicated in patients with uncontrolled hypertension or cardiovascular disease.
No significant risk of skin cancer observed (unlike some other melanocortin analogs), but long-term data remain limited.
FDA-approved; safety established mainly in short-term, on-demand dosing.

Citations

Zhang, H., Chen, L. N., Yang, D., Mao, C., Shen, Q., Feng, W., Shen, D. D., Dai, A., Xie, S., Zhou, Y., Qin, J., Sun, J. P., Scharf, D. H., Hou, T., Zhou, T., Wang, M. W., & Zhang, Y. (2021). Structural insights into ligand recognition and activation of the melanocortin-4 receptor. Cell research, 31(11), 1163–1175. https://doi.org/10.1038/s41422-021-00552-3
Molinoff, P. B., Shadiack, A. M., Earle, D., Diamond, L. E., & Quon, C. Y. (2003). PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences, 994, 96–102. https://doi.org/10.1111/j.1749-6632.2003.tb03167.x
King, S. H., Mayorov, A. V., Balse-Srinivasan, P., Hruby, V. J., Vanderah, T. W., & Wessells, H. (2007). Melanocortin Receptors, Melanotropic Peptides, and Penile Erection. Current Topics in Medicinal Chemistry, 7(11), 1098. https://pmc.ncbi.nlm.nih.gov/articles/PMC2694735/
Kingsberg, S. A., Clayton, A. H., Portman, D., Williams, L. A., Krop, J., Jordan, R., Lucas, J., & Simon, J. A. (2019). PT-141 for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials. Obstetrics and Gynecology, 134(5), 899–908. https://doi.org/10.1097/AOG.0000000000003500

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