Drug intelligence / Profile preview

levcromakalim

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Intravenous (used Experimentally), Oral (investigated)
01

Overview

Levcromakalim is the active enantiomer of cromakalim and functions as an ATP-sensitive potassium (KATP) channel opener. It acts primarily as a vasodilator by activating KATP channels in vascular smooth muscle, leading to membrane hyperpolarization and relaxation of the vessel wall. This mechanism underlies its antihypertensive effects and has also been explored for asthma and gastric ulcer treatment. In clinical research, intravenous levcromakalim is notable for its ability to reliably induce migraine attacks in susceptible individuals—both with and without aura—making it a valuable tool in experimental headache studies. The drug’s action on KATP channels may also increase extracellular potassium concentrations in neural tissues, potentially triggering cortical spreading depression or activating the trigeminovascular system involved in migraine pathophysiology[1][2][3][4][5][7][8].

Other names
(-)-cromakalimlemakalim
02

Targets

SUR2B (Sulfonylurea receptor 2B)KCNJ11 (Atp-sensitive inward rectifier potassium channel 11)SUR2A (ATP-binding cassette sub-family C member 9)

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