Institute of Clinical Pharmacology, Anhui Medical University, Hefei, China; Key Laboratory of Anti-Inflammatory and Immune Medicine, Ministry of Education, Hefei, China; Anhui Collaborative Innovation Centre of Anti-Inflammatory and Immune Medicine, Hefei, China.
Institute of Clinical Pharmacology, Anhui Medical University, Hefei, China; Key Laboratory of Anti-Inflammatory and Immune Medicine, Ministry of Education, Hefei, China; Anhui Collaborative Innovation Centre of Anti-Inflammatory and Immune Medicine, Hefei, China.
Life Sci. 2021 Mar 1;268:118907. doi: 10.1016/j.lfs.2020.118907. Epub 2021 Jan 8.
The ATP-binding cassette (ABC) and solute carrier (SLC) transporter families consist of common drug transporters that mediate the efflux and uptake of drugs, respectively, and play an important role in the absorption, distribution, metabolism and excretion of drugs in vivo. Rheumatoid arthritis (RA) is an autoimmune disease characterized by erosive arthritis, and there are many RA patients worldwide. Methotrexate (MTX), the first-choice treatment for RA, can reduce the level of inflammation, prevent joint erosion and functional damage, and greatly reduce pain in RA patients. However, many patients show resistance to MTX, greatly affecting the efficacy of MTX. Many factors, such as irrational drug use and heredity, are associated with drug resistance. Considering the effect of drug transporters on drugs, many studies have compared the expression of drug transporters in drug-resistant and drug-sensitive patients, and abnormal transporter expression and transport activity have been found in patients with MTX resistance. Thus, drug transporters are involved in drug resistance. This article reviews the effects of transporters on the efficacy of MTX in the treatment of RA.
三磷酸腺苷结合盒（ABC）和溶质载体（SLC）转运蛋白家族由常见的药物转运蛋白组成，分别介导药物的外排和摄取，在药物的体内吸收、分布、代谢和排泄中发挥重要作用。类风湿关节炎（RA）是一种以侵蚀性关节炎为特征的自身免疫性疾病，全世界有许多 RA 患者。甲氨蝶呤（MTX）是 RA 的首选治疗药物，可降低炎症水平，防止关节侵蚀和功能损害，极大地减轻 RA 患者的疼痛。然而，许多患者对 MTX 表现出耐药性，这极大地影响了 MTX 的疗效。许多因素，如不合理的用药和遗传，与耐药性有关。鉴于药物转运体对药物的影响，许多研究比较了耐药和敏感患者的药物转运体表达情况，发现 MTX 耐药患者的转运体表达和转运活性异常。因此，药物转运体参与了耐药性。本文综述了转运体对 MTX 治疗 RA 疗效的影响。
