Sacha T, Szczepanek E
Department of Hematology, Jagiellonian University Medical College, Cracow, Poland.
J Physiol Pharmacol. 2021 Jun;72(3). doi: 10.26402/jpp.2021.3.02. Epub 2021 Nov 19.
Ponatinib (Iclusig®, Takeda/Incyte) is a third-generation highly-potent-pan-inhibitor of tyrosine kinases, active in all single resistance ABL kinase mutations including the T315l mutation. It is approved to treat of chronic myeloid leukemia (CML) in every phase of disease-resistant or intolerant to second-generation tyrosine kinase inhibitors (2GTKIs) and for whom imatinib is not clinically appropriate as well as for patients with T315I mutation. The drug is also indicated for Ph+ acute lymphoblastic leukemia (ALL). The approved starting dose for ponatinib is 45 mg once daily. Available data revealed ponatinib dose-dependent increased risk of cardiovascular toxicity. There is still no consensus about the optimal, initial dose of ponatinib and its management during therapy. It is crucial to start treatment with the risk-adjusted dose and assess the benefit-risk profile of ponatinib dosing. Evaluation of dosing modification should be considered during treatment, mainly if toxicity occurs. Our study summarizes current knowledge and recommendations about the choice of starting dose of ponatinib and management of ponatinib dosing during the treatment.
波纳替尼(Iclusig®,武田/因赛特)是一种第三代强效泛酪氨酸激酶抑制剂,对包括T315I突变在内的所有单耐药ABL激酶突变均有活性。它被批准用于治疗对第二代酪氨酸激酶抑制剂(2GTKIs)耐药或不耐受且伊马替尼临床应用不合适的各阶段慢性髓性白血病(CML)患者以及T315I突变患者。该药物也适用于Ph+急性淋巴细胞白血病(ALL)。波纳替尼的批准起始剂量为每日一次45毫克。现有数据显示波纳替尼的心血管毒性风险呈剂量依赖性增加。关于波纳替尼的最佳初始剂量及其治疗期间的管理仍未达成共识。以风险调整剂量开始治疗并评估波纳替尼给药的获益风险状况至关重要。治疗期间应考虑评估剂量调整,主要是在出现毒性时。我们的研究总结了关于波纳替尼起始剂量选择及其治疗期间给药管理的当前知识和建议。