Melanocortin receptor agonists
Bremelanotide (PT-141) 30 mg/pen (total content)
CAS Number47
Basic Info
| CAS Number | 189691-06-3 — free / 1607799-13-2 — acetate |
|---|---|
| Active Ingredient | Bremelanotide (development code PT-141), a synthetic cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone (α-MSH); available as the free base (CAS 189691-06-3) or acetate salt (CAS 1607799-13-2) |
| Dosage Form | Pen (lyophilised, dual chamber) |
| Specification & Packaging | Strength: 30 mg/pen (total content) Pack: Dual-chamber pen (lyophilised + diluent) Group: 05 Item No.: 47 |
Storage & Common Excipients
| Storage Conditions | 2–8 °C, protected from light (lyophilised powder); **do not freeze**; use immediately after reconstitution and do not store. Follow the label |
|---|---|
| Common Excipients | The dual-chamber pen contains the lyophilised drug with excipients such as mannitol and a diluent chamber of sterile water or saline; preservative-free. Confirm against COA |
Product Introduction
A melanocortin-receptor (MC3R/MC4R) agonist. The reference product Vyleesi (bremelanotide nasal spray) was approved by the FDA in June 2019 for **premenopausal women** with acquired, generalised hypoactive sexual desire disorder (HSDD). The entries here are **injector-pen presentations (dual-chamber lyophilised powder plus diluent)**, a compounded/research presentation with a different route; PT-141 has long circulated as a research compound
Therapeutic Use
**Approved**: acquired, generalised HSDD in premenopausal women (nasal presentation). **Unapproved / investigational**: erectile dysfunction in men (a major development direction, including combination with PDE5 inhibitors) and female sexual dysfunction. The injection route and the specific products in this list have no approved indication and represent research / compliance-risk use
Mode of Action
A cyclic heptapeptide with the sequence Ac-Nle-Asp-His-D-Phe-Arg-Trp-Lys (D-Phe is chiral; it differs from Melanotan-II at the C-terminus, free carboxylic acid versus primary amide). It agonises central MC3R/MC4R to enhance sexual desire and motivation — a mechanism distinct from the peripheral vasodilation of PDE5 inhibitors, hence potential benefit when combined with a PDE5 inhibitor. It acts in both sexes, but the approved indication is limited to premenopausal women
Administration & Monitoring
Nasal administration as specified in the approved label (no additional monitoring required); the injection route must follow the research protocol. Monitor blood pressure and heart rate (MC-receptor agonism can raise blood pressure), pigmentation (MC1R, seen in about 1% of subjects) and nausea; monitor blood pressure and syncope risk when combined with a PDE5 inhibitor
Important Safety Information
Prescription medicine (US). Contraindicated in known or suspected cardiovascular disease, uncontrolled hypertension, uncontrolled psychiatric disorders (especially depression with suicidal or self-harm history) and bipolar disorder. **The product may raise blood pressure, particularly when combined with PDE5 inhibitors.** The injection route has no approved indication and represents unauthorised use. It carries abuse and diversion risk (it has been misused in non-consensual sexual scenarios, prompting legislation and regulatory action internationally)
Adverse Reactions
Headache and nausea (most common); increased blood pressure; upper-airway and sinus discomfort (nasal presentation); local skin reactions (injection route); hyperpigmentation (about 1%, MC1R activation); mood or psychiatric symptoms (rare)
Important Risks
Raised blood pressure, with hypotension/syncope when combined with PDE5 inhibitors; psychiatric/neuropsychiatric risk (potential mood effects of MC-receptor agonism); abuse and illegal-use/criminal-use risk; absence of long-term safety data for the injection route
Contraindications
Hypersensitivity; uncontrolled hypertension; known or suspected cardiovascular disease or cerebrovascular event; uncontrolled depression, bipolar disorder or any history of suicide or self-harm; pregnancy (no approved indication); use in another person without their consent is unlawful
Special Populations
The approved population is **premenopausal** women; there is no approved indication in postmenopausal women; use in men is off-label; contraindicated in children and adolescents; limited data in those over 65; insufficient data in hepatic or renal impairment
Usage Limitations
Prescription medicine, **strictly limited to the approved indication (premenopausal women with HSDD, nasal route) and the populations and routes defined in the label**. The injection route and long-acting pen presentations have no approved indication and must not be used for any purpose such as sexual assault. Controlled-substance peptide regulations apply; no resale or repackaging
Anti-Doping Testing
**Bremelanotide is not on the WADA Prohibited List.** However, because it acts on the α-MSH pathway and MC1R activation can alter skin pigmentation, it may raise questions during testing. Any athlete use should be proactively declared and supported by a TUE to avoid an adverse finding
Product Quality Testing
Identification (peptide mapping/MS, mass by MS), assay and purity (reverse-phase HPLC), cyclisation integrity, endotoxin, sterility, lyophilisate appearance, reconstitution time and clarity, fill volume, pen mechanism and dose accuracy, in-use stability, stability; COA
Inquiry / Request for information
We will respond within 24 hours. Customized synthesis is supported.