Department of Investigational Cancer Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, TX, USA.
Department of Investigational Cancer Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, TX, USA; Pharmacy Clinical Programs, The University of Texas MD Anderson Cancer Center, Houston, TX, USA.
Cell Rep Med. 2023 Dec 19;4(12):101332. doi: 10.1016/j.xcrm.2023.101332.
The US Food and Drug Administration (FDA) approval of the selective RET inhibitors selpercatinib and pralsetinib has led to a paradigm change in the treatment of RET-altered lung and thyroid cancers through a higher response rate and a more tolerable safety and toxicity profile than multi-kinase inhibitors. Recently, selpercatinib has received a tissue-agnostic FDA approval for all RET-fusion-positive cancers, and pralsetinib has shown pan-cancer activity as well. Given the anticipated increase in the use of both drugs across multiple tumor types, it is crucial to recognize the possible side effects and approaches for their optimal management in order to maximize the clinical benefit for treated patients. In this review, we underscore potential toxicities associated with selective RET inhibitors and discuss strategies to mitigate them.
美国食品和药物管理局 (FDA) 批准了选择性 RET 抑制剂塞尔帕替尼和普拉替尼，这导致 RET 改变的肺癌和甲状腺癌的治疗发生了范式转变，其反应率更高，安全性和毒性特征更可耐受，优于多激酶抑制剂。最近，塞尔帕替尼因其对所有 RET 融合阳性癌症的组织不可知的 FDA 批准，普拉替尼也显示出泛癌活性。鉴于这两种药物在多种肿瘤类型中的预期使用增加，认识到它们可能的副作用以及优化管理的方法对于最大限度地提高治疗患者的临床获益至关重要。在这篇综述中，我们强调了与选择性 RET 抑制剂相关的潜在毒性，并讨论了减轻这些毒性的策略。
