molecules of the month


oral melanocortin-4 receptor antagonist

Ph. I candidate

focused screen of 28K library for MC4R activity

J. Med. Chem., February 19, 2023

Pfizer Inc., Groton, CT

PF-07258669, oral melanocortin-4 receptor antagonist, Ph. I candidate, PFIZER INC., GROTON, CT
6 mins read

MC4R antagonism to help gain weight. PF-07258669 is a melanocortin-4 receptor (MC4R) antagonist intended to help increase weight gain, in contrast to MC4R agonists which have been studied extensively in the industry for weight loss (and have notable side effects such as priapism). The peptidic MC4R agonist, setmelanotide, for example, was approved in 2020 for the treatment of obesity. An MC4R antagonist like PF-07258669 could instead be helpful for treating cachexia, a metabolic disorder that results in weight and muscle loss associated with advanced cancer and the late stages of other major chronic illnesses. It has been estimated to affect 9 million patients in the industrialized world, including 50-80% of cancer patients. The standard of care according to current clinical…

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