Skin pigmentation and pharmacokinetics of melanotan-I in humans

Sydney O. Ugwu, James Blanchard, Robert T. Dorr, Norman Levine, Christine Brooks, Mac E. Hadley, Mikel Aickin, Victor J. Hruby

Research output: Contribution to journalArticlepeer-review

36 Scopus citations


A comparative pharmacokinetic trial was performed with a superpotent synthetic melanotropic peptide, [Nle4-D-Phe7]-α-MSH1-13 (melanotan-I or MT-I) given by three routes of administration. Plasma levels were measured by RIA and tanning was quantitated using serial reflectometry. Doses of 0.16 mg kg-1 were administered intravenously (IV) and orally (PO), and doses from 0.08 to 0.21 mg kg-1 subcutaneously (SC), in a randomized crossover fashion to three male volunteers over five consecutive days for 2 weeks (ten doses). The results indicate that the SC dose is completely bioavailable compared to the IV dose. No detectable drug levels were observed following PO dosing. The plasma half-lives following SC dosing ranged from 0.07 to 0.79 h for the absorption phase and from 0.8 to 1.7 h for the β-phase. Clearance ranged from 0.12 to 0.19 L kg-1 h-1 and 3.9% or less of the dose was recovered in the urine. Side-effects were minimal, consisting of occasional gastrointestinal upset and facial flushing. Significant tanning of the forehead, arms, and neck was noted following IV or SC dosing. This effect peaked at 1 week following drug administration but was still present 3 weeks after completing the ten-dose regimen. It is concluded that SC administration is an efficacious method of delivering melanotan-I.

Original languageEnglish (US)
Pages (from-to)259-269
Number of pages11
JournalBiopharmaceutics and Drug Disposition
Issue number3
StatePublished - Apr 1997


  • humans
  • melanotan-I
  • pharmacokinetics
  • pigmentation

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science
  • Pharmacology (medical)


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