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Cyclic heptapeptide

Melanotan II — evidence

What has been published, classified by the kind of document it is. This is not a protocol, not a score, and not a recommendation for use.

Evidence overview

3 records in this file

  • CLINICAL TRIAL1
  • REVIEW1
  • REGULATORY1

Research areas. Human pigmentation pharmacology; Melanocortin development history; United States compounding.

Publication span. 1996–2026.

What we know

  • A 1996 pilot Phase I study explored pigmentation and tolerability in volunteers. No FDA-approved product followed.
  • It is the C-terminal amide; bremelanotide is the free-acid analogue and is approved.
  • FDA's withdrawn-nomination entry cites case reports of serious adverse events.

Editorial reading of the records below, labelled as Therapept analysis. How records are built

What remains uncertain

  • A contemporary controlled safety database. Case reports are a concern list, not an incidence rate.

Regulatory notes

No FDA-approved product

  • No approved drug product exists in Drugs@FDA.
  • Listed on FDA's table of bulk substances nominated for compounding and withdrawn by the nominator.
  • FDA's published entry references case reports of serious adverse events, including melanoma, posterior reversible encephalopathy syndrome, sympathomimetic toxidrome and priapism.
  • Not named on the WADA 2026 Prohibited List.

Regulatory status describes how a substance is classified. It is not a safety assessment of any particular material.

Studies and documents

  1. REGULATORY2026Regulatory listing

    FDA table of bulk drug substances nominated for compounding and subsequently withdrawn

    U.S. Food and Drug AdministrationFDA compounding communications

    Objective
    To record FDA's published compounding position.
    Endpoint investigated
    Compounding classification and cited case reports

    Nomination withdrawn. FDA's published entry references case reports of serious adverse events, including melanoma, posterior reversible encephalopathy syndrome, sympathomimetic toxidrome and priapism. Melanotan II is the C-terminal amide; bremelanotide is the free acid.

    Limitations. Case reports cited by FDA are not a randomised trial. They are a regulatory concern list.

    FDA — Certain bulk drug substances for use in compounding may present significant safety risksReviewed 12 September 2026

  2. REVIEW2006Narrative review

    Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization

    Hadley ME, Dorr RTPeptides

    Objective
    To review melanocortin peptide development, including melanotan-II and related analogues.
    Endpoint investigated
    Development history of melanocortin peptides

    Historical review of melanocortin peptide therapeutics by authors involved in the early programme. Distinguishes development paths that later produced an approved drug (bremelanotide) from melanotan-II, which did not.

    Limitations. Author-involved narrative. Does not replace later FDA materials on unapproved melanotan-II.

    DOI 10.1016/j.peptides.2005.01.029Hadley and Dorr, Peptides (2006)Reviewed 12 September 2026

  3. CLINICAL TRIAL1996Pilot Phase I study

    Evaluation of melanotan-II, a superpotent cyclic melanotropic peptide in a pilot phase-I clinical study

    Dorr RT, Lines R, Levine N, et al.Life Sciences

    Population
    Small adult volunteer cohort in a Phase I tanning study
    Objective
    To explore pigmentation and tolerability of melanotan-II in a pilot human study.
    Endpoint investigated
    Pigmentation and acute tolerability in a pilot cohort

    Early human Phase I work on melanotan-II as a melanocortin peptide, reporting pigmentation and adverse effects in a small volunteer study. It is historical pharmacology, not an approved-product trial. No FDA-approved product exists.

    Limitations. Pilot n; 1996 methods; not a contemporary safety database. Subsequent FDA compounding materials cite case reports of serious adverse events for this unapproved substance.

    DOI 10.1016/0024-3205(96)00160-9Dorr et al., Life Sci (1996)Reviewed 12 September 2026

Last reviewed 3 September 2026 · Compiled by Therapept Editorial · How these records are built