Drug intelligence / Profile preview

CP-609754

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

Overview

CP-609754 is a quinolinone derivative that functions as a potent and reversible farnesyltransferase inhibitor with potential anticancer activity. It inhibits farnesyl protein transferase, an enzyme that mediates the farnesylation of RAS, potentially inhibiting the RAS pathway. The compound demonstrated in vivo antitumor activity against 3T3 H-ras (61L) tumors. It was originally developed for the treatment of patients with Ras-positive cancer but was later licensed to Link Medicine for the treatment of neurodegenerative diseases. Under the codename LNK-754, it was investigated in mouse models of Parkinson's disease and Alzheimer's disease, where positive results were demonstrated.

Other names
6-[(R)-(4-chlorophenyl)(hydroxy)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-ethynylphenyl)-1-methyl-1,2-dihydroquinolin-2-one
02

Targets

FTase (Protein Farnesyltransferase)

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