Drug intelligence / Profile preview

PF-00446687

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

PF-00446687 is a potent and selective small molecule agonist of the melanocortin 4 receptor (MC4R), developed by Pfizer for the treatment of erectile dysfunction. It is brain penetrant and acts as a non-peptide agonist with high selectivity for MC4R. In clinical studies up to phase II for erectile dysfunction in men, a single oral dose of 200 mg showed similar effectiveness to 100 mg sildenafil; lower doses were ineffective. The drug demonstrated that selective targeting of MC4R can produce aphrodisiac effects comparable to older peptide-based melanocortin receptor agonists but with fewer side effects due to its selectivity[1][2][3][7].

Other names
862281-92-3UNII-63P236Z73IUNII63P236Z73IUNII 63P236Z73IMethanone, ((3S,4R)-4-(2,4-difluorophenyl)-1-(1,1-dimethylethyl)-3-pyrrolidinyl)((3R,5S)-4-hydroxy-3,5-dimethyl-4-phenyl-1-piperidinyl)-
02

Targets

MC4R (Melanocortin 4 receptor)

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