Department of Pharmacy, Second Affiliated Hospital of Naval Medical University, 200003, Shanghai, China.
Institute of Basic Medicine and Cancer (IBMC), Zhejiang Cancer Hospital, Chinese Academy of Sciences, Hangzhou, Zhejiang, 310022, China.
Eur J Clin Pharmacol. 2024 Jun;80(6):827-838. doi: 10.1007/s00228-024-03626-4. Epub 2024 Mar 14.
Since the first experimentally proven tyrosine kinase inhibitor (TKI) imatinib was introduced in the clinical setting, TKIs have attracted widespread attention because of their remarkable therapeutic effects and improvement of survival rates. TKIs are small-molecule, multi-target, anti-cancer agents that target different tyrosine kinases and block downstream signaling.
However, with in-depth research on TKI drugs, the adverse reactions-for example, thyroid dysfunction-have become a concern and thus have attracted the attention of numerous researchers. Thyroid dysfunction, especially hypothyroidism, that occurs in high incidence during TKI therapy has a close relationship with treatment efficacy, but the mechanism of TKI-induced thyroid dysfunction is obscure.
This review discusses the epidemiology, possible mechanisms, and clinical significance of hypothyroidism in cancer patients treated with TKI.
自首个经实验证实的酪氨酸激酶抑制剂(TKI)伊马替尼引入临床应用以来,由于其显著的治疗效果和生存率的提高,TKI 引起了广泛关注。TKI 是小分子、多靶点的抗癌药物,针对不同的酪氨酸激酶并阻断下游信号。
然而,随着对 TKI 药物的深入研究,不良反应(例如甲状腺功能障碍)已成为关注点,因此引起了众多研究人员的关注。TKI 治疗期间发生的甲状腺功能障碍,尤其是甲状腺功能减退症,发生率较高,与治疗效果密切相关,但 TKI 诱导甲状腺功能障碍的机制尚不清楚。
本文讨论了接受 TKI 治疗的癌症患者中甲状腺功能减退症的流行病学、可能的机制和临床意义。