A novel DOTA-alpha-melanocyte-stimulating hormone analog for metastatic melanoma diagnosis.

Froidevaux S, Calame-Christe M, Tanner H, Sumanovski L, Eberle AN

Journal of nuclear medicine : official publication, Society of Nuclear Medicine1 Dec 2002Cited by 54 (Europe PMC)

PMID12468522PepBankPUB-12468522

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 study5

No result from this study comes from a test of the peptide.

Studies that did not test the peptide alone5

In this study, Melanotan I (afamelanotide) was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Melanotan I (afamelanotide).

01AnimalNot a test of Melanotan I (afamelanotide) aloneAnimal study (in vivo)Pharmacokinetics
In B16F1 melanoma-bearing mice, (111)In-DOTA-NDP-MSH showed high MC1R-mediated uptake by melanoma, similar to (111)In-DOTA-MSH(oct).
In plain wordsIn mice with melanoma, radiolabeled DOTA-NDP-MSH accumulated strongly in the tumor.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableMelanoma uptake of (111)In-DOTA-NDP-MSH
Study
mousen: not reported in source
B16F1 melanoma-bearing mice
Outcome group
Pharmacokinetics · Cancer
Source sentences
Summary
In B16F1 melanoma-bearing mice, both (111)In-DOTA-NDP-MSH and (111)In-DOTA-MSH(oct) exhibited high MC1R-mediated uptake by melanoma, which differed by a factor of only 1.5 at 4 h after injection.
1 context sentence(design, population, supporting numbers)
Summary · context
The resulting DOTA conjugates were evaluated in vitro for their MC1R-binding affinity and melanogenic activity in isolated mouse B16F1 cells and in vivo for their biodistribution in mouse models of primary and metastatic melanoma after labeling with (111)In.
In this study, Melanotan I (afamelanotide) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan I (afamelanotide).
Report a problemFND-1246852202
02AnimalNot a test of Melanotan I (afamelanotide) aloneAnimal study (in vivo)Pharmacokinetics
In mice, the kidneys were the main route of excretion of (111)In-DOTA-NDP-MSH, with somewhat lower kidney values than (111)In-DOTA-MSH(oct).
In plain wordsIn mice, radiolabeled DOTA-NDP-MSH left the body mainly through the kidneys, with lower kidney levels than the octapeptide analog.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableKidney excretion of (111)In-DOTA-NDP-MSH
Study
mousen: not reported in source
B16F1 melanoma-bearing mice
Outcome group
Pharmacokinetics · Kidney and urinary
Source sentences
Summary
The main route of excretion for both radioconjugates was the kidneys, whereby (111)In-DOTA-MSH(oct) led to somewhat higher kidney values than did (111)In-DOTA-NDP-MSH.
1 context sentence(design, population, supporting numbers)
Summary · context
The resulting DOTA conjugates were evaluated in vitro for their MC1R-binding affinity and melanogenic activity in isolated mouse B16F1 cells and in vivo for their biodistribution in mouse models of primary and metastatic melanoma after labeling with (111)In.
In this study, Melanotan I (afamelanotide) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan I (afamelanotide).
Report a problemFND-1246852203
03AnimalNot a test of Melanotan I (afamelanotide) aloneAnimal study (in vivo)Pharmacokinetics
In mice, (111)In-DOTA-NDP-MSH was much more poorly cleared from nonmalignant tissues, including bone, than (111)In-DOTA-MSH(oct).
In plain wordsIn mice, radiolabeled DOTA-NDP-MSH stayed longer in healthy tissues, including bone, than the octapeptide analog.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableClearance from nonmalignant tissues including bone
Study
mousen: not reported in source
B16F1 melanoma-bearing mice
Outcome group
Pharmacokinetics · Musculoskeletal
Source sentences
Summary
In contrast, the latter was much more poorly cleared from other nonmalignant tissues, including bone, the most radiosensitive organ.
1 context sentence(design, population, supporting numbers)
Summary · context
The resulting DOTA conjugates were evaluated in vitro for their MC1R-binding affinity and melanogenic activity in isolated mouse B16F1 cells and in vivo for their biodistribution in mouse models of primary and metastatic melanoma after labeling with (111)In.
In this study, Melanotan I (afamelanotide) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan I (afamelanotide).
Report a problemFND-1246852204
04AnimalNot a test of Melanotan I (afamelanotide) aloneAnimal study (in vivo)Pharmacokinetics
In mice, the tumor-to-bone uptake ratio 4 h after injection of (111)In-DOTA-NDP-MSH was 4.9, lower than 53.9 for (111)In-DOTA-MSH(oct).
In plain wordsIn mice, radiolabeled DOTA-NDP-MSH gave a much lower tumor-to-bone ratio than the octapeptide analog.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableTumor-to-bone ratio 4 h after injection
Study
mousen: not reported in source
B16F1 melanoma-bearing mice
Outcome group
Pharmacokinetics · Cancer
Measurements
tumor-to-bone ratio
4.9 ratio
(111)In-DOTA-NDP-MSH, 4 h
Source sentences
Summary
Therefore, (111)In-DOTA-MSH(oct) displayed higher uptake ratios of tumor to nontarget tissue (e.g., tumor-to-bone ratio 4 h after injection was 4.9 for (111)In-DOTA-NDP-MSH and 53.9 for (111)In-DOTA-MSH(oct)).
1 context sentence(design, population, supporting numbers)
Summary · context
The resulting DOTA conjugates were evaluated in vitro for their MC1R-binding affinity and melanogenic activity in isolated mouse B16F1 cells and in vivo for their biodistribution in mouse models of primary and metastatic melanoma after labeling with (111)In.
In this study, Melanotan I (afamelanotide) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan I (afamelanotide).
Report a problemFND-1246852205
05LabNot a test of Melanotan I (afamelanotide) aloneIn vitro (cells)Activity measurement
In vitro, the DOTA conjugate of NDP-MSH bound the MC1R with an IC50 of 0.25 nmol/L, with higher potency than DOTA-MSH(oct).
In plain wordsIn lab tests, the DOTA-linked NDP-MSH bound strongly to the melanoma receptor MC1R, more strongly than the new octapeptide analog.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableMC1R binding affinity of DOTA-NDP-MSH
Study
mousen: not reported in source
isolated B16F1 mouse cells
Outcome group
Receptor activity and mechanism · Pharmacology
Measurements
IC50
0.25 nmol/L
DOTA-NDP-MSH, MC1R
Source sentences
Summary
DOTA-MSH(oct) was shown to bind with high affinity (inhibitory concentration of 50% [IC(50)] = 9.21 nmol/L) to the MC1R, although with lower potency than does DOTA-NDP-MSH (IC(50) = 0.25 nmol/L).
1 context sentence(design, population, supporting numbers)
Summary · context
The resulting DOTA conjugates were evaluated in vitro for their MC1R-binding affinity and melanogenic activity in isolated mouse B16F1 cells and in vivo for their biodistribution in mouse models of primary and metastatic melanoma after labeling with (111)In.
In this study, Melanotan I (afamelanotide) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan I (afamelanotide).
Report a problemFND-1246852201

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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