Drug intelligence / Profile preview

perhexiline

Development stage
Phase 3
Lead developer
Heart Metabolics
Modality
Small Molecules
Administration
Oral
01

Overview

Perhexiline is a coronary vasodilator and antianginal agent used primarily for the management of severe or refractory angina pectoris. It acts by inhibiting mitochondrial carnitine palmitoyltransferase-1 (CPT-1) and to a lesser extent CPT-2, shifting myocardial metabolism from fatty acids to glucose utilization. This increases ATP production for the same oxygen consumption and enhances myocardial efficiency. The drug is well absorbed orally (>80%) and is highly protein bound (>90%). Its use has been limited by its narrow therapeutic index and risk of adverse effects such as neuropathy and hepatitis in poor metabolizers due to CYP2D6 polymorphisms. Therapeutic drug monitoring is recommended to minimize toxicity[1][5][7].

Brand names
PexsigPexid
Other names
Perhexilene2-(2,2-Dicyclohexylethyl)piperidinePerhexilinaPerhexilinum
02

Targets

SLC7A1 (Cationic amino acid transporter 1)CPT2 (Carnitine O-palmitoyltransferase 2)

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