US 12,440,570 B2
Conjugation of MCR1 ligand with cytotoxic drugs for treating skin cancer
Minying Cai, Tucson, AZ (US); Victor J. Hruby, Tucson, AZ (US); and Yang Zhou, Tucson, AZ (US)
Assigned to ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA, Tucson, AZ (US)
Filed by ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA, Tucson, AZ (US)
Filed on Jan. 19, 2022, as Appl. No. 17/579,237.
Application 17/579,237 is a continuation in part of application No. PCT/US2020/042769, filed on Jul. 20, 2020.
Claims priority of provisional application 62/876,536, filed on Jul. 19, 2019.
Prior Publication US 2022/0143196 A1, May 12, 2022
Int. Cl. A61K 47/55 (2017.01); A61K 9/00 (2006.01); A61K 47/54 (2017.01); A61K 47/64 (2017.01); A61P 35/00 (2006.01)
CPC A61K 47/55 (2017.08) [A61K 9/0014 (2013.01); A61K 47/545 (2017.08); A61K 47/64 (2017.08); A61P 35/00 (2018.01)] 16 Claims
 
1. A pharmaceutical composition comprising a ligand-drug conjugate comprising a peptide ligand bound to a drug moiety, wherein the ligand-drug conjugate is according to the formula: L-A-B-D, wherein L is the peptide ligand, A is a spacer derived from aminohexanoic acid, B is a cleavable linker, and D is the drug moiety, wherein the peptide ligand is according to the formula:
Ac-Nle-c[Asp-His-Taa-Arg-Trp-Lys]-NH2 (SEQ ID NO: 89), or is a derivative that has at least 50% homology to SEQ ID NO: 89, wherein Taa is DPhe or DNal(2′).