Porwal Mayur, Kumar Arvind, Rastogi Vaibhav, Maheshwari Kamal Kishore, Verma Anurag
Department of Pharmacology, Teerthanker Mahaveer College of Pharmacy, Teerthanker Mahaveer University, Moradabad, 244001, Uttar Pradesh, India.
Drug Design Laboratory, School of Pharmaceutical Sciences, IFTM University, Moradabad, 244001, Uttar Pradesh, India.
Curr Drug Res Rev. 2023 Mar 8. doi: 10.2174/2589977515666230308125238.
Odevixibat is synthesized through chemical modification of Benzothiazepine's structure. It is a tiny chemical that inhibits the ileal bile acid transporter and is used to treat a variety of cholestatic illnesses, including progressive familial intrahepatic cholestasis (PFIC). For cholestatic pruritus and liver disease development, bile acid transporter inhibition is a unique treatment strategy. Odevixibat reduces enteric bile acid reuptake. Oral odevixibat was also studied in children with cholestatic liver disease. Odevixibat received its first approval in the European Union (EU) in July 2021 for the treatment of PFIC in patients aged 6 months, followed by approval in the USA in August 2021 for the treatment of pruritus in PFIC patients aged 3 months. Bile acids in the distal ileum can be reabsorbed by the ileal sodium/bile acid cotransporter, a transport glycoprotein. Odevixibat is a sodium/bile acid co-transporter reversible inhibitor. An average 3 mg once-daily dose of odevixibat for a week resulted in a 56% reduction in the area under the curve of bile acid. A daily dose of 1.5 mg resulted in a 43% decrease in the area under the curve for bile acid. Odevixibat is also being evaluated in many countries for the treatment of other cholestatic illnesses, including Alagille syndrome and biliary atresia. This article reviews the updated information on odevixibat with respect to its clinical pharmacology, mechanism of action, pharmacokinetics, pharmacodynamics, metabolism, drug-drug interactions, pre-clinical studies, and clinical trials.
奥地维西巴特是通过对苯并噻氮䓬结构进行化学修饰合成的。它是一种微小的化学物质，可抑制回肠胆汁酸转运体，用于治疗多种胆汁淤积性疾病，包括进行性家族性肝内胆汁淤积症（PFIC）。对于胆汁淤积性瘙痒和肝脏疾病的发展，抑制胆汁酸转运体是一种独特的治疗策略。奥地维西巴特可减少肠道胆汁酸的重吸收。口服奥地维西巴特也在患有胆汁淤积性肝病的儿童中进行了研究。奥地维西巴特于2021年7月在欧盟（EU）首次获批用于治疗6个月及以上患者的PFIC，随后于2021年8月在美国获批用于治疗3个月及以上PFIC患者的瘙痒。远端回肠中的胆汁酸可被回肠钠/胆汁酸共转运体（一种转运糖蛋白）重吸收。奥地维西巴特是一种钠/胆汁酸共转运体可逆抑制剂。每天平均3毫克的奥地维西巴特剂量持续一周，可使胆汁酸曲线下面积减少56%。每日剂量1.5毫克可使胆汁酸曲线下面积减少43%。奥地维西巴特也正在许多国家进行评估，用于治疗其他胆汁淤积性疾病，包括阿拉吉列综合征和胆道闭锁。本文综述了奥地维西巴特在临床药理学、作用机制、药代动力学、药效学、代谢、药物相互作用、临床前研究和临床试验方面的最新信息。
