Drug intelligence / Profile preview

ABT-639

Development stage
Phase 2
Lead developer
AbbVie
Modality
Small Molecules
Administration
Oral
01

Overview

ABT-639 is a peripherally acting, highly selective T-type calcium channel (CaV3.2) blocker developed by AbbVie for the treatment of neuropathic pain, including painful diabetic neuropathy and neuralgia. It is an orally bioavailable small molecule that selectively binds to and blocks the CaV3.2 isoform of low voltage-gated T-type calcium channels in peripheral sensory neurons, thereby inhibiting neuronal hyperexcitability and nociceptive signaling. Preclinical studies demonstrated robust antinociceptive activity in animal models without significant effects on psychomotor or hemodynamic function. In clinical trials up to phase II, ABT-639 did not show significant analgesic efficacy over placebo in patients with neuropathic pain but was well tolerated[1][3][4][5][6].

Other names
(R)-4-Chloro-2-fluoro-N-(2-fluorophenyl)-5-(octahydropyrrolo[1,2-a]pyrazine-2-carbonyl)benzenesulfonamideABT-639 free baseABT639 free baseABT 639 free base
02

Targets

CACNA1B (Voltage-dependent N-type calcium channel subunit alpha-1B)CACNA1H (T-type voltage-gated calcium channel 3.2)CACNA1G (T-type Calcium Channel Protein Subunit Alpha-1G)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)

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