Department of Pharmacy, Kyushu University Hospital, 3-1-1 Maidashi, Higashi-ku, Fukuoka, 812-8582, Japan.
Department of Clinical Pharmacology and Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka, 812-8582, Japan.
Clin Pharmacokinet. 2024 Jul;63(7):945-964. doi: 10.1007/s40262-024-01392-1. Epub 2024 Jul 16.
Letermovir is a newly developed antiviral agent used for the prophylaxis of human cytomegalovirus infections in patients undergoing allogeneic hematopoietic cell transplantation. This novel anti-cytomegalovirus drug, used for the prophylaxis of cytomegalovirus reactivation until approximately 200 days after transplantation, effectively reduces the risk of clinically significant cytomegalovirus infection. No human counterpart exists for the terminase complex; letermovir is virus specific and lacks some toxicities previously observed with other anti-cytomegalovirus drugs, such as cytopenia and nephrotoxicity. The absolute bioavailability of letermovir in healthy individuals is estimated to be 94% based on a population-pharmacokinetic analysis. In contrast, oral administration of letermovir to patients undergoing hematopoietic cell transplantation results in lower exposure than that in healthy individuals. Renal or hepatic impairment does not influence the intrinsic clearance of letermovir. Co-administration of letermovir may alter the plasma concentrations of other drugs, including itself, as it acts as a substrate and inhibitor/inducer of several drug-metabolizing enzymes and transporters. In particular, attention should be paid to the drug-drug interactions between letermovir and calcineurin inhibitors or azole antifungal agents, which are commonly used in patients undergoing hematopoietic cell transplantation. This article reviews and summarizes the clinical pharmacokinetics and pharmacodynamics of letermovir, focusing on patients undergoing hematopoietic cell transplantation, healthy individuals, and specific patient subsets.
来特莫韦是一种新开发的抗病毒药物,用于异体造血细胞移植患者人巨细胞病毒感染的预防。这种新型抗巨细胞病毒药物用于预防巨细胞病毒再激活,直到移植后约 200 天,可有效降低临床显著巨细胞病毒感染的风险。终止酶复合物在人体内没有对应的物质;来特莫韦是病毒特异性的,缺乏以前观察到的其他抗巨细胞病毒药物的一些毒性,如血细胞减少症和肾毒性。基于群体药代动力学分析,健康个体中来特莫韦的绝对生物利用度估计为 94%。相比之下,造血细胞移植患者口服来特莫韦的暴露量低于健康个体。肾或肝损伤不影响来特莫韦的内在清除率。来特莫韦的联合给药可能会改变其他药物的血浆浓度,包括它本身,因为它是几种药物代谢酶和转运体的底物和抑制剂/诱导剂。特别是,应注意来特莫韦与钙调神经磷酸酶抑制剂或唑类抗真菌药物之间的药物相互作用,这些药物在接受造血细胞移植的患者中通常联合使用。本文综述和总结了来特莫韦的临床药代动力学和药效学,重点关注接受造血细胞移植的患者、健康个体和特定患者亚组。