Preclinical evaluation of MC1R targeted radiopharmaceuticals using the ^203/212Pb theranostic pair.

Scaffidi-Muta JM, Boucher D, Li KC, Liu F, Tieu W, Abell AD

European journal of medicinal chemistry17 Sept 2026

PMID42762593DOI10.1016/j.ejmech.2026.119341PepBankPUB-42762593

Publisher page PubMedAsk about this study

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 study6

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

Studies that did not test the peptide alone6

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 B16 melanoma-bearing mice, [203Pb]Pb-9, a derivative of NDP-MSH, showed high tumour uptake relative to the other tested compounds.
In plain wordsIn mice with melanoma, a compound made from NDP-MSH reached the tumour more than the other compounds tested.
Peptide
Melanotan I (afamelanotide)
Outcome
IncreaseTumour uptake of [203Pb]Pb-9
Study
mousen: not reported in source
B16 melanoma-bearing mice
Comparator
Other tested compounds
Outcome group
Pharmacokinetics · Cancer
Source sentences
Summary
A subsequent biodistribution study in B16 melanoma bearing mice revealed a high tumour uptake of [²⁰³Pb]Pb-9 relative to the other tested compounds
1 context sentence(design, population, supporting numbers)
Summary · context
Competition binding assays identified compound 9, a derivative of the potent MC1R agonist NDP-MSH, as possessing sub-nanomolar binding affinity for MC1R and a high selectivity against the closely related melanocortin 4 receptor.
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-4276259303
02AnimalNot a test of Melanotan I (afamelanotide) aloneAnimal study (in vivo)Pharmacokinetics
In B16 melanoma-bearing mice, [203Pb]Pb-9, a derivative of NDP-MSH, had the lowest hepatic and splenic uptakes of the series.
In plain wordsIn mice with melanoma, a compound made from NDP-MSH built up in liver and spleen less than the other compounds tested.
Peptide
Melanotan I (afamelanotide)
Outcome
DecreaseHepatic and splenic uptake of [203Pb]Pb-9
Study
mousen: not reported in source
B16 melanoma-bearing mice
Comparator
Other tested compounds
Outcome group
Pharmacokinetics · Cancer
Source sentences
Summary
whilst simultaneously possessing the lowest hepatic and splenic uptakes of the series.
1 context sentence(design, population, supporting numbers)
Summary · context
Competition binding assays identified compound 9, a derivative of the potent MC1R agonist NDP-MSH, as possessing sub-nanomolar binding affinity for MC1R and a high selectivity against the closely related melanocortin 4 receptor.
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-4276259304
03AnimalNot a test of Melanotan I (afamelanotide) aloneAnimal study (in vivo)Pharmacokinetics
In B16 melanoma-bearing mice, organ uptake of [203Pb]Pb-9, a derivative of NDP-MSH, was by far the most specific for the tumour.
In plain wordsIn mice with melanoma, a compound made from NDP-MSH went mainly to the tumour.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableTumour specificity of organ uptake of [203Pb]Pb-9
Study
mousen: not reported in source
B16 melanoma-bearing mice
Outcome group
Pharmacokinetics · Cancer
Source sentences
Summary
Organ uptake of [²⁰³Pb]Pb-9 was accordingly by far the most specific for the tumour
1 context sentence(design, population, supporting numbers)
Summary · context
Competition binding assays identified compound 9, a derivative of the potent MC1R agonist NDP-MSH, as possessing sub-nanomolar binding affinity for MC1R and a high selectivity against the closely related melanocortin 4 receptor.
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-4276259305
04AnimalNot a test of Melanotan I (afamelanotide) aloneAnimal study (in vivo)Pharmacokinetics
In healthy mice, [203Pb]Pb-9, a derivative of NDP-MSH, showed low accumulation in normal organs.
In plain wordsIn healthy mice, a compound made from NDP-MSH built up little in normal organs.
Peptide
Melanotan I (afamelanotide)
Outcome
DecreaseAccumulation of [203Pb]Pb-9 in normal organs
Study
mousen: not reported in source
healthy mice
Outcome group
Pharmacokinetics · Cancer
Source sentences
Summary
its low accumulation in normal organs confirmed in a subsequent biodistribution study in healthy mice.
1 context sentence(design, population, supporting numbers)
Summary · context
Competition binding assays identified compound 9, a derivative of the potent MC1R agonist NDP-MSH, as possessing sub-nanomolar binding affinity for MC1R and a high selectivity against the closely related melanocortin 4 receptor.
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-4276259306
05LabNot a test of Melanotan I (afamelanotide) aloneOther designActivity measurement
In competition binding assays, compound 9, a derivative of NDP-MSH, had sub-nanomolar binding affinity for MC1R.
In plain wordsIn lab tests, a compound made from NDP-MSH bound very tightly to the MC1R receptor.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableMC1R binding affinity of compound 9
Study
n: not reported in source
competition binding assay
Outcome group
Receptor activity and mechanism · Cancer
Source sentences
Summary
Competition binding assays identified compound 9, a derivative of the potent MC1R agonist NDP-MSH, as possessing sub-nanomolar binding affinity for MC1R
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-4276259301
06LabNot a test of Melanotan I (afamelanotide) aloneOther designActivity measurement
In competition binding assays, compound 9, a derivative of NDP-MSH, showed high selectivity against the closely related melanocortin 4 receptor.
In plain wordsIn lab tests, a compound made from NDP-MSH bound much less to a related receptor, MC4R.
Peptide
Melanotan I (afamelanotide)
Outcome
Not applicableMC1R selectivity over MC4R
Study
n: not reported in source
competition binding assay
Outcome group
Receptor activity and mechanism · Cancer
Source sentences
Summary
Competition binding assays identified compound 9, a derivative of the potent MC1R agonist NDP-MSH, as possessing sub-nanomolar binding affinity for MC1R and a high selectivity against the closely related melanocortin 4 receptor.
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-4276259302

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.

Publication types

Journal Article

Keywords

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