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Gafapixant is a P2X3 receptor antagonist that has demonstrated the reduction of cough in patients with refractory chronic cough (RCC). Taste disturbance is the most frequent adverse event by gefapixant (approximately 60-70%).

Gefapixant（也称为 AF-219 和 MK-7264）是一种新型、有效、口服生物活性 P2X3 受体 (P2X3R) 拮抗剂，具有镇咳作用，可用于慢性咳嗽。 它抑制 P2X3R，与重组 hP2X3 同源三聚体相比，IC50 约为 30 nM，而 hP2X2/3 异源三聚体受体的 IC50 为 100-250 nM。 通过抑制含有 P2X3 的受体的 ATP 激活来治疗疼痛，预示着一种令人兴奋的疼痛管理新方法，而 Afferent 的项目标志着一类新型药物的先锋，准备探索这种方法，以满足疼痛管理中未满足的重大需求。

Trial MK -7264 043, NCT04193202, 2019 002308 42; A Phase 3b Randomized, Double-blind, Placebo Controlled, Multicenter Study to Evaluate the Efficacy and Safety of Gefapixant in Adult Participants With Recent Onset Chronic Cough Phase III Location(s): EU (including the UK), Canada, United States and other countries

2019年12月10日 · Experimental: Gefapixant Participants will receive gefapixant at a dose of 45 mg administered as an oral tablet twice daily for 12 weeks. Placebo Comparator: Placebo Participants will receive placebo matching gefapixant, administered as an oral tablet twice daily for 12 weeks. Primary Outcome Measures:1.

2017年5月22日 · Hypogeusia, reduced ability to taste, was reported in 1.6. placebo, 7.5 mg, 20 mg, and 50 mg of MK-7264, respectively. One patient. discontinued due to taste-related adverse events. No patients in the 7.5. mg and 20 mg groups discontinued due to taste-related adverse events. Laboratories. “We look forward to further discussions with regulatory.

MK-7264 is a reversible and selective P2X3 and P2X2/3 antagonist, exerting allosteric antagonism via preferential activity at closed channels. Its efficacy in rat models supports its clinical investigation for chronic sensitisation conditions.

MK-7264 （英語： Gefapixant）是一种 磺胺 类药物，作为 嘌呤 P2X受体 P2RX3 （英语：P2RX3） 的 拮抗剂，可用于治疗 慢性咳嗽 （英语：chronic cough）[1][2][3]。 ^ Muccino D, Green S. Update on the clinical development of gefapixant, a P2X3 receptor antagonist for the treatment of refractory chronic cough. Pulmonary Pharmacology & Therapeutics. June 2019, 56 ( …

The purpose of this study is to evaluate the efficacy and safety of gefapixant in participants with recent onset chronic cough (duration \>8 weeks after onset of cough symptoms) for \<12 months and a diagnosis of refractory or unexplained chronic cough. …

MK-7264首次给药前8周内献血或失血≥1个单位（约300 mL）。 访视1时尿妊娠试验呈阳性的WOCBP。 如果尿妊娠试验呈阳性或无法确认为阴性，则要求其进行血清妊娠试验。 需要接受不符合方案第6.5节规定的合并治疗。 曾接受MK-7264治疗。 目前正参与或在参与当前研究前30天内曾参与研究性化合物或器械的干预性临床研究。 筛选时存在显著异常的实验室检测（参见第8.3.6节和第8.3.7节），包括： a. 碱性磷酸酯酶、丙氨酸氨基转移酶（ALT、SGPT）、天冬氨酸氨基 …