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Published on: January 7, 2019
Peptide-targeted radionuclide therapy for melanoma
1College of Pharmacy, University of New Mexico, 2502 Marble NE, MSC09 5360, Albuquerque, NM 87131, USA. ymiao@salud.unm.edu
Abstract:
Melanocortin-1 receptor (MC1-R) and melanin are two attractive melanoma-specific targets for peptide-targeted radionuclide therapy for melanoma. Radiolabeled peptides targeting MC1-R/melanin can selectively and specifically target cytotoxic radiation generated from therapeutic radionuclides to melanoma cells for cell killing, while sparing the normal tissues and organs. This review highlights the recent advances of peptide-targeted radionuclide therapy of melanoma targeting MC1-R and melanin. The promising therapeutic efficacies of 188Re-(Arg(11))CCMSH (188Re-[Cys(3,4,10), D-Phe(7),Arg(11)]-alpha-MSH(3-13)), 177Lu- and 212Pb-labeled DOTA-Re(Arg(11))CCMSH (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-[ReO-(Cys(3,4,10), D-Phe(7), Arg(11))]-alpha-MSH(3-13)) and 188Re-HYNIC-4B4 (188Re-hydrazinonicotinamide-Tyr-Glu-Arg-Lys-Phe-Trp-His-Gly-Arg-His) in preclinical melanoma-bearing models demonstrate an optimistic outlook for peptide-targeted radionuclide therapy for melanoma. Peptide-targeted radionuclide therapy for melanoma will likely contribute in an adjuvant setting, once the primary tumor has been surgically removed, to treat metastatic deposits and for treatment of end-stage disease. The lack of effective treatments for metastatic melanoma and end-stage disease underscores the necessity to develop and implement new treatment strategies, such as peptide-targeted radionuclide therapy.
Insights
Peptide-targeted radionuclide therapy shows promise for melanoma by targeting MC1-R and melanin. This approach delivers radiation specifically to melanoma cells, offering a new strategy for metastatic and end-stage disease.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging and Therapy
Background:
- Melanoma treatment remains challenging, especially for metastatic and end-stage disease.
- Melanocortin-1 receptor (MC1-R) and melanin are melanoma-specific targets.
- Peptide-targeted radionuclide therapy offers a strategy for targeted cytotoxic radiation delivery.
Purpose of the Study:
- To review recent advances in peptide-targeted radionuclide therapy for melanoma.
- To highlight therapeutic strategies targeting MC1-R and melanin.
- To discuss the potential of this therapy for various stages of melanoma.
Main Methods:
- Review of preclinical studies on radiolabeled peptides targeting MC1-R and melanin.
- Evaluation of specific peptide conjugates such as 188Re-(Arg(11))CCMSH, 177Lu- and 212Pb-labeled DOTA-Re(Arg(11))CCMSH, and 188Re-HYNIC-4B4.
- Assessment of therapeutic efficacies in preclinical melanoma models.
Main Results:
- Radiolabeled peptides targeting MC1-R/melanin demonstrate selective delivery of radiation to melanoma cells.
- Promising therapeutic efficacies observed in preclinical models with agents like 188Re-(Arg(11))CCMSH and others.
- The approach shows potential for sparing normal tissues and organs.
Conclusions:
- Peptide-targeted radionuclide therapy targeting MC1-R and melanin presents an optimistic outlook for melanoma treatment.
- This therapy is a potential adjuvant treatment for metastatic deposits after primary tumor removal.
- It offers a necessary new strategy for end-stage melanoma patients lacking effective options.
