Chemistry:Opakalim
Opakalim (INN, USAN; developmental code names BHV-7000, BPN-25203, and KB-3061) is a highly selective Kv7.2 and Kv7.3 potassium channel opener which is under development for the treatment of bipolar disorders, epilepsy, partial epilepsies, major depressive disorder, erythromelalgia, pain, infantile spasms, and mood disorders.[1][2][3][4] It is taken orally.[1] The drug was originated by Channel Biosciences and was under development by Biohaven Pharmaceuticals or Biohaven Therapeutics.[1][2] As of April 2026, it is in phase 2/3 clinical trials for bipolar disorders, epilepsy, and partial epilepsies, phase 2 trials for major depressive disorder, and phase 1 trials for erythromelalgia and pain, whereas no recent development has been reported for infantile spasms and mood disorders.[1][2] A phase 2 trial for major depressive disorder failed to meet its primary efficacy endpoint, resulting in focus more on epilepsy instead.[3]
Mechanism of Action
Opakalim is a potent and selective opener of the heteromeric Kv7.2/7.3 potassium channels responsible for generating the M-current, responsible for stablising the neural membrane potential and controlling repetitive firing. Activation of the Kv7.2/7.3 channels enhances the M-current, leading to hyperpolarisation of the neural membrane and a higher action potential threshold. This reduces neuronal hyperexcitability, an underlying cause of seizures. [5] The high selectivity of Opakalim and its minimal activity on GABA-A receptors is thought to contribute to its low incidence of somnolence observed in clinical trials, a common side effect of many anti-seizure medications that also modulate GABAergic neurotransmission.
See also
- List of investigational bipolar disorder drugs
- List of investigational antidepressants
- List of investigational analgesics
- Azetukalner
- Flupirtine
- Retigabine
References
- ↑ 1.0 1.1 1.2 1.3 "Biohaven Pharmaceuticals". 15 April 2026. https://adisinsight.springer.com/drugs/800056133.
- ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on Opakalim with Synapse". 2 April 2026. https://synapse.patsnap.com/drug/2228dba9608d4014ab45e40815d85a71.
- ↑ 3.0 3.1 "Potassium channel agonists emerging as treatment options for focal epilepsy: are we breaking new ground?". Expert Opinion on Emerging Drugs: 1–8. May 2026. doi:10.1080/14728214.2026.2675274. PMID 42153277.
- ↑ "Expanding the toolkit: An update on the evolution of new therapies for Lennox-Gastaut Syndrome". Seminars in Pediatric Neurology 56. December 2025. doi:10.1016/j.spen.2025.101242. PMID 41371876.
- ↑ "An In-depth Technical Guide to Opakalim (BHV-7000): A Novel Kv7.2/7.3 Potassium Channel Activator". https://pdf.benchchem.com/15590/An_In_depth_Technical_Guide_to_Opakalim_BHV_7000_A_Novel_Kv7_2_7_3_Potassium_Channel_Activator.pdf.
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