Drug intelligence / Profile preview

(3R,5S)-31c

Development stage: Preclinical
Lead developer: Johnson & Johnson
Modality: Small Molecules
Administration: Oral

Overview

(3R,5S)-31c is a brain-penetrant and selective triple T-type calcium channel blocker. It was developed through optimization from a racemic hit, resulting in improved physicochemical properties, solubility, and metabolic stability. The compound has demonstrated promising efficacy in the WAG/Rij-rat model of generalized nonconvulsive absence-like epilepsy, indicating its potential as a novel antiepileptic drug. It also showed an IC50 on CYP3A4 of 23–31 nM.

Other names: (3R,5S)-N,1-Dibenzyl-3,5-dimethyl-1,2,3,5-tetrahydro-4H-pyrido[3,4-e][1,4]diazepine-4-carboxamide

Targets

CACNA1H (T-type voltage-gated calcium channel 3.2)CACNA1G (T-type Calcium Channel Protein Subunit Alpha-1G)CACNA1I (Voltage-dependent T-type calcium channel subunit alpha-1I)

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