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阿达木单抗用于治疗类风湿关节炎的临床前发现与开发。

Preclinical discovery and development of adalimumab for the treatment of rheumatoid arthritis.

作者信息

Pelechas Eleftherios, Voulgari Paraskevi V, Drosos Alexandros A

机构信息

Rheumatology Clinic, Department of Internal Medicine, Medical School, University of Ioannina, Ioannina, Greece.

出版信息

Expert Opin Drug Discov. 2021 Mar;16(3):227-234. doi: 10.1080/17460441.2021.1846516. Epub 2020 Nov 18.

Abstract

: Rheumatoid arthritis (RA) is an autoimmune disease that is characterized by progressive joint disorders with significant pain and stiffness. In the past, RA was a difficult -to-treat ailment, but nowadays with the advent of biologics and better treatment strategies, disease remission is an achievable goal. Tumor necrosis factor α (TNFα) inhibitors were the first category of biologics to emerge with adalimumab being the first fully human TNFα.: the authors provide an overview of the historical events that led to the discovery of TNFα inhibitors and more specifically the drug adalimumab. Several key trials are presented regarding the safety of the drug as well as its successful journey, but there is also a narrative description of the drug's future after patent expiration.: Adalimumab is a fully human TNFα inhibitor with a fairly rapid onset of action. It has a generally good safety and efficacy profile. Clinicians must be aware of the possible side effects and treat them in a timely manner or discontinue the drug where appropriate. Due to the success of the bio-originator adalimumab, a multitude of biosimilars have emerged but not, thus far, for all of the indications of the bio-originator.

摘要

类风湿性关节炎(RA)是一种自身免疫性疾病,其特征为进行性关节紊乱,伴有显著疼痛和僵硬。过去,类风湿性关节炎是一种难以治疗的疾病,但如今随着生物制剂的出现和更好的治疗策略,疾病缓解已成为一个可以实现的目标。肿瘤坏死因子α(TNFα)抑制剂是最早出现的一类生物制剂,阿达木单抗是首个完全人源化的TNFα抑制剂。作者概述了导致TNFα抑制剂尤其是药物阿达木单抗发现的历史事件。介绍了几项关于该药物安全性及其成功历程的关键试验,但也有对该药物专利到期后未来情况的叙述性描述。阿达木单抗是一种完全人源化的TNFα抑制剂,起效相当迅速。其总体安全性和疗效良好。临床医生必须了解可能的副作用,并及时进行处理或在适当情况下停用该药物。由于生物原研药阿达木单抗的成功,众多生物类似药已出现,但迄今为止,并非针对生物原研药的所有适应症。

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