关键词: 5-HT2C Bexicaserin (LP352) antiseizure medication (ASM) developmental and epileptic encephalopathies (DEE) drug-resistant epilepsy (DRE) serotonin

Mesh : Humans Anticonvulsants / therapeutic use pharmacology Animals Serotonin 5-HT2 Receptor Agonists / therapeutic use pharmacology Epilepsy / drug therapy Spasms, Infantile / drug therapy

来  源:   DOI:10.1080/14656566.2024.2373350

Abstract:
UNASSIGNED: Developmental epileptic encephalopathies (DEEs) pose significant challenges due to their refractory nature and limited treatment options. Despite advancements in genetic understanding, effective therapies targeting underlying pathophysiology are lacking. Serotoninergic dysfunction has been implicated in epilepsy, sparking interest in serotonin as a therapeutic target.
UNASSIGNED: This article explores the potential of bexicaserin, a selective 5-HT2C receptor agonist, as an adjunctive antiseizure medication in DEEs. Bexicaserin is thought to modulate GABAergic neurotransmission, suppressing central hyperexcitability. Preclinical studies demonstrate its efficacy across various seizure models. Clinical trials, including the Pacific Study, reveal promising results in reducing motor seizures. However, challenges such as adverse effects and treatment discontinuation underscore the need for further investigation.
UNASSIGNED: The efficacy of 5-HT2C serotoninergic agonists, validated in preclinical and clinical studies, highlights serotonin\'s role in DEEs. Bexicaserin offers new therapeutic possibilities, potentially synergizing with existing antiseizure medications. Polypharmacotherapy, targeting distinct pathways, may enhance therapeutic outcomes. Monitoring pharmacological interactions and addressing central nervous system comorbidities are crucial for optimizing treatment strategies. Further research is needed to elucidate bexicaserin\'s mechanisms and potential antiepileptogenic effects.
摘要:
发展性癫痫性脑病(DEE)由于其难治性和有限的治疗选择而面临重大挑战。尽管基因理解有了进步,缺乏针对基础病理生理学的有效疗法。血清素能功能障碍与癫痫有关,激发了人们对5-羟色胺作为治疗靶标的兴趣。
本文探讨了墨西哥的潜力,选择性5-HT2C受体激动剂,作为DEE的辅助抗癫痫药物。Bexicaserin被认为可以调节GABA能神经传递,抑制中枢过度兴奋。临床前研究证明其在各种癫痫发作模型中的功效。临床试验,包括太平洋研究,揭示了减少运动性癫痫发作的有希望的结果。然而,不良反应和停止治疗等挑战强调了进一步调查的必要性.
5-HT2C5-羟色胺能激动剂的疗效,在临床前和临床研究中验证,突出5-羟色胺在DEE中的作用。Bexicaserin提供了新的治疗可能性,可能与现有的抗癫痫药物协同作用。综合药物治疗,靶向不同的途径,可以提高治疗效果。监测药理学相互作用和解决中枢神经系统合并症对于优化治疗策略至关重要。需要进一步的研究来阐明bexicaserin的机制和潜在的抗癫痫作用。
公众号