Drug intelligence / Profile preview

PF-03882845

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

PF‑03882845 is a potent and selective non-steroidal mineralocorticoid receptor antagonist developed by Pfizer. It is an orally bioavailable small molecule designed to block the mineralocorticoid receptor (MR) without significant activity on androgen, estrogen alpha, or glucocorticoid receptors. Unlike traditional steroidal MR antagonists such as eplerenone and spironolactone, PF‑03882845 is a pyrazoline derivative with high selectivity for MR and minimal off-target effects. Preclinical studies demonstrated that it provides renal protection in models of aldosterone-mediated renal disease and diabetic nephropathy by reducing albuminuria and markers of fibrosis more potently than eplerenone while presenting a lower risk for hyperkalemia. Clinical development for diabetic nephropathy was terminated for strategic reasons[1][2][4][6].

Other names
(3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydrobenzo[g]indazole-7-carboxylic acidcompound 2compound2compound-2
02

Targets

MR (Mineralocorticoid receptor)

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