Narges K Tafreshi, Christopher J Tichacek, Darpan N Pandya, Michael L Doligalski, Mikalai M Budzevich, HyunJoo Kil, Nikunj B Bhatt, Nancy D Kock, Jane L Messina, Epifanio E Ruiz, Nella C Delva, Adam Weaver, William R Gibbons, David C Boulware, Nikhil I Khushalani, Ghassan El-Haddad, Pierre L Triozzi, Eduardo G Moros, Mark L McLaughlin, Thaddeus J Wadas, David L Morse
New effective therapies are greatly needed for metastatic uveal melanoma, which has a very poor prognosis with a median survival of less than 1 y. The melanocortin 1 receptor (MC1R) is expressed in 94% of uveal melanoma metastases, and a MC1R-specific ligand (MC1RL) with high affinity and selectivity for MC1R was previously developed. Methods: The 225 Ac-DOTA-MC1RL conjugate was synthesized in high radiochemical yield and purity and was tested in vitro for biostability and for MC1R-specific cytotoxicity in uveal melanoma cells, and the lanthanum-DOTA-MC1RL analog was tested for binding affinity...
August 2019: Journal of Nuclear Medicine