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Imatinib sunitinib and pazopanib: From flat‐fixed dosing towards a pharmacokinetically guided personalized dose

机译:伊马替尼舒尼替尼和帕唑帕尼:从固定剂量给药到药代动力学指导的个性化剂量

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摘要

Tyrosine kinase inhibitors (TKIs) are anti‐cancer drugs that target tyrosine kinases, enzymes that are involved in multiple cellular processes. Currently, multiple oral TKIs have been introduced in the treatment of solid tumours, all administered in a fixed dose, although large interpatient pharmacokinetic (PK) variability is described. For imatinib, sunitinib and pazopanib exposure‐treatment outcome (efficacy and toxicity) relationships have been established and therapeutic windows have been defined, therefore dose optimization based on the measured blood concentration, called therapeutic drug monitoring (TDM), can be valuable in increasing efficacy and reducing the toxicity of these drugs.
机译:酪氨酸激酶抑制剂(TKIs)是针对酪氨酸激酶的抗癌药物,酪氨酸激酶是参与多个细胞过程的酶。目前,尽管描述了较大的患者间药代动力学(PK)变异性,但已在实体瘤的治疗中引入了多种口服TKI,全部以固定剂量给药。对于伊马替尼,已经建立了舒尼替尼和帕唑帕尼的暴露-治疗结果(疗效和毒性)之间的关系,并定义了治疗窗口,因此,根据测得的血药浓度优化剂量(称为治疗药物监测(TDM))可能对提高疗效具有重要意义。并降低这些药物的毒性。

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