Drug intelligence / Profile preview

nerispirdine hydrochloride

Development stage
Discontinued
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

Nerispirdine hydrochloride (HPP 432) is an investigational small molecule drug developed by Sanofi (formerly Aventis) for the treatment of multiple sclerosis (MS). It is a novel analogue of 4-aminopyridine (dalfampridine) that acts as a use-dependent blocker of both axonal voltage-gated potassium (K+) channels and neuronal voltage-gated sodium (Na+) channels. By inhibiting K+ channels, nerispirdine aims to restore nerve impulse conduction in demyelinated axons, thereby improving motor functions such as walking speed. The addition of Na+ channel blockade is intended to provide neuroprotective effects and mitigate the proconvulsant activity typically associated with pure K+ channel blockers. The compound also enhances the release of acetylcholine at the neuromuscular junction. Nerispirdine reached Phase 2 clinical development, including a 14-week randomized, double-blind, placebo-controlled trial in Spain evaluating doses of 50 mg, 100 mg, and 200 mg in MS patients with walking disability, but development was subsequently discontinued.

Other names
nerispirdinenerispirdine hydrochloride
02

Targets

KCNH2 (Voltage-gated potassium channel subfamily H member 2)KCNA1 (Voltage-gated potassium channel subfamily A member 1)NaV (Voltage-gated sodium channels)KCNA2 (Voltage-gated potassium channel subfamily A member 2)

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