Activity and bioavailability of tepotinib for leptomeningeal metastasis of NSCLC with MET exon 14 skipping mutation

Cancer Communications

article

Hisashi Tanaka¹  Kageaki Taima¹  Tomonori Makiguchi¹  Junichi Nakagawa²  Takenori Niioka²  Sadatomo Tasaka¹ 

[1] Department of Respiratory Medicine, Hirosaki University Graduate School of Medicine;Department of Pharmacy, Hirosaki University Hospital

关键词: cerebrospinal fluid;    IC50;    leptomeningeal metastasis;    MET exon 14 skipping mutation;    non-small cell lung carcinoma;    performance status;    pharmacokinetics;    tepotinib;   

DOI  :  10.1002/cac2.12124

学科分类：社会科学、人文和艺术（综合）

来源: Springer

【 摘 要 】

Tepotinib is a key drug for cancer patients with mesenchymal-epithelial transition receptor tyrosine kinase proto-oncogene (MET) exon 14 skipping mutation. However, its bioavailability in the cerebrospinal fluid (CSF) in humans has not been fully elucidated. Moreover, information about the efficacy of tepotinib in patients with leptomeningeal metastasis is limited. Here, we present the case of a 56-year-old man who was diagnosed with lung adenocarcinoma with MET exon 14 skipping mutation. He was urgently hospitalized due to leptomeningeal metastasis. We administered tepotinib 500 mg/day as the second-line therapy and observed improvement in leptomeningeal metastasis and performance status. The tepotinib concentrations reached 1,648 ng/mL in the plasma and 30.6 ng/mL in the CSF, with a penetration rate (CSF/plasma) of 1.83%. These demonstrate tepotinib could achieve a high rate of central nervous system transition and could be effective against leptomeningeal metastasis.

【 授权许可】

CC BY|CC BY-NC-ND