Skin pigmentation and pharmacokinetics of melanotan-I in humans.

Ugwu SO, Blanchard J, Dorr RT, Levine N, Brooks C, Hadley ME, Aickin M, Hruby VJ

Biopharmaceutics & drug disposition1 Apr 1997Cited by 28 (Europe PMC)

PMID9113347DOI10.1002/(sici)1099-081x(199704)18:3<259::aid-bdd20>3.0.co;2-xPepBankPUB-09113347

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Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study10

10 results from studies that gave the peptide. 10 results from people.

01HumanRandomized controlled trialPharmacokinetics
In three male volunteers, the subcutaneous melanotan I dose was completely bioavailable compared with the intravenous dose.
In plain wordsIn three men, melanotan I given under the skin reached the blood fully, compared with an injection into a vein.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableSubcutaneous bioavailability versus intravenous
Study
n = 3
Comparator
Intravenous dose
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.08 to 0.21 mg/kg · subcutaneous · 5 consecutive days for 2 weeks (ten doses)As given in this study (human).
Source sentences
Summary
The results indicate that the SC dose is completely bioavailable compared to the IV dose.
1 context sentence(design, population, supporting numbers)
Summary · context
Doses of 0.16 mgkg-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).
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02HumanRandomized controlled trialPharmacokinetics
In three male volunteers, no drug levels were detectable after oral melanotan I.
In plain wordsIn three men, no melanotan I could be detected in the blood after taking it by mouth.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicablePlasma levels after oral dosing
Study
n = 3
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.16 mg/kg · oral · 5 consecutive days for 2 weeks (ten doses)As given in this study (human).
Source sentences
Summary
No detectable drug levels were observed following PO dosing.
1 context sentence(design, population, supporting numbers)
Summary · context
Doses of 0.16 mgkg-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).
Report a problemFND-0911334702
03HumanRandomized controlled trialPharmacokinetics
After subcutaneous melanotan I, the plasma half-life of the absorption phase ranged from 0.07 to 0.79 h.
In plain wordsAfter melanotan I under the skin, the absorption half-life in blood ranged from 0.07 to 0.79 hours.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableAbsorption-phase plasma half-life after subcutaneous dosing
Study
n = 3
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.08 to 0.21 mg/kg · subcutaneous · 5 consecutive days for 2 weeks (ten doses)As given in this study (human).
Measurements
Absorption-phase half-life
0.07 to 0.79 h
subcutaneous
Source sentences
Summary
The plasma half-lives following SC dosing ranged from 0.07 to 0.79 h for the absorption phase
1 context sentence(design, population, supporting numbers)
Summary · context
Doses of 0.16 mgkg-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).
Report a problemFND-0911334703
04HumanRandomized controlled trialPharmacokinetics
After subcutaneous melanotan I, the plasma half-life of the beta-phase ranged from 0.8 to 1.7 h.
In plain wordsAfter melanotan I under the skin, the later half-life in blood ranged from 0.8 to 1.7 hours.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableBeta-phase plasma half-life after subcutaneous dosing
Study
n = 3
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.08 to 0.21 mg/kg · subcutaneous · 5 consecutive days for 2 weeks (ten doses)As given in this study (human).
Measurements
Beta-phase half-life
0.8 to 1.7 h
subcutaneous
Source sentences
Summary
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 beta-phase.
1 context sentence(design, population, supporting numbers)
Summary · context
Doses of 0.16 mgkg-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).
Report a problemFND-0911334704
05HumanRandomized controlled trialPharmacokinetics
Clearance of melanotan I ranged from 0.12 to 0.19 L kg-1 h-1.
In plain wordsMelanotan I was cleared from the body at a rate of 0.12 to 0.19 litres per kilogram per hour.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableClearance
Study
n = 3
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.08 to 0.21 mg/kg · subcutaneous · 5 consecutive days for 2 weeks (ten doses)As given in this study (human).
Measurements
Clearance
0.12 to 0.19 L kg-1 h-1
subcutaneous
Source sentences
Summary
Clearance ranged from 0.12 to 0.19 L kg-1 h-1
1 context sentence(design, population, supporting numbers)
Summary · context
Doses of 0.16 mgkg-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).
Report a problemFND-0911334705
06HumanRandomized controlled trialPharmacokinetics
At most 3.9% of the melanotan I dose was recovered in the urine.
In plain wordsNo more than 3.9% of the melanotan I dose was found in urine.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableUrinary recovery of the dose
Study
n = 3
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.08 to 0.21 mg/kg · subcutaneous · 5 consecutive days for 2 weeks (ten doses)As given in this study (human).
Measurements
Urinary recovery
≤ 3.9%
dose
Source sentences
Summary
3.9% or less of the dose was recovered in the urine.
1 context sentence(design, population, supporting numbers)
Summary · context
Doses of 0.16 mgkg-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).
Report a problemFND-0911334706
07HumanRandomized controlled trialSafety outcome
In three male volunteers, side effects of melanotan I were minimal and included occasional gastrointestinal upset.
In plain wordsIn three men, melanotan I caused minimal side effects, including occasional stomach upset.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableGastrointestinal upset
Study
n = 3
Outcome group
Adverse events · Gastrointestinal
Studied dose
0.08 to 0.21 mg/kg · intravenous, oral, subcutaneous · 5 consecutive days for 2 weeks (ten doses)As given in this study (human).
Source sentences
Summary
Side-effects were minimal, consisting of occasional gastrointestinal upset and facial flushing.
1 context sentence(design, population, supporting numbers)
Summary · context
Doses of 0.16 mgkg-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).
Report a problemFND-0911334707
08HumanRandomized controlled trialSafety outcome
In three male volunteers, side effects of melanotan I were minimal and included facial flushing.
In plain wordsIn three men, melanotan I caused minimal side effects, including facial flushing.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableFacial flushing
Study
n = 3
Outcome group
Adverse events · Skin and wound
Studied dose
0.08 to 0.21 mg/kg · intravenous, oral, subcutaneous · 5 consecutive days for 2 weeks (ten doses)As given in this study (human).
Source sentences
Summary
Side-effects were minimal, consisting of occasional gastrointestinal upset and facial flushing.
1 context sentence(design, population, supporting numbers)
Summary · context
Doses of 0.16 mgkg-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).
Report a problemFND-0911334708
09HumanRandomized controlled trialEfficacy outcome
In three male volunteers, significant tanning of the forehead, arms and neck followed intravenous or subcutaneous melanotan I.
In plain wordsIn three men, melanotan I given into a vein or under the skin was followed by clear tanning of the forehead, arms and neck.
Peptide
Melanotan I (afamelanotide)
Outcome
IncreaseTanning of forehead, arms and neck
Study
n = 3
Outcome group
Pigmentation · Skin and wound
Studied dose
0.16 mg/kg IV; 0.08 to 0.21 mg/kg SC · intravenous or subcutaneous · 5 consecutive days for 2 weeks (ten doses)As given in this study (human).
Source sentences
Summary
Significant tanning of the forehead, arms, and neck was noted following IV or SC dosing.
2 context sentences(design, population, supporting numbers)
Summary · context
tanning was quantiated using serial reflectometry.
Summary · context
Doses of 0.16 mgkg-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).
Report a problemFND-0911334709
10HumanRandomized controlled trialEfficacy outcome
In three male volunteers, the tanning effect peaked at 1 week after drug administration and was still present 3 weeks after the ten-dose regimen ended.
In plain wordsIn three men, the tan from melanotan I peaked after 1 week and was still there 3 weeks after the last dose.
Peptide
Melanotan I (afamelanotide)
Outcome
IncreaseTime course of tanning
Study
n = 3
Outcome group
Pigmentation · Skin and wound
Studied dose
0.16 mg/kg IV; 0.08 to 0.21 mg/kg SC · intravenous or subcutaneous · 5 consecutive days for 2 weeks (ten doses)As given in this study (human).
Source sentences
Summary
This effect peaked at 1 week following drug administration but was still present 3 weeks after completing the ten-dose regimen.
1 context sentence(design, population, supporting numbers)
Summary · context
Doses of 0.16 mgkg-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).
Report a problemFND-0911334710

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
13 Oct 2026, 21:44 UTC
Study results updated
Version 1
13 Oct 2026, 16:31 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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