On December 8, 2023, the latest announcement on the official website of the State Food and Drug Administration (NMPA) of China showed that tepotinib tablets have been officially approved in China. According to public information,Tepotinib is an oral MET inhibitor and is the world's first MET inhibitor. It has previously been approved for marketing in Japan and the U.S. for patients with non-small cell lung cancer (NSCLC) harboring MET exon 14 (metex14) skips.
Non-small cell lung cancer (NSCLC) is a common type of lung cancer, accounting for about 85% of lung cancer cases, while the MEDEX14 skipping mutation is a metastatic NSCLC-specific genetic variant, and the clinical proportion of patients with METex14 skipping spikes in the Chinese non-small cell lung cancer (NSCLC) population is about 09%-2.0%, and in pulmonary sarcomatoid carcinoma, the proportion is as high as 13%-22%.
The met14 exon skipping spike is closely related to the prognosis of patients with non-small cell lung cancer (NSCLC), and lung cancer patients with this mutation tend to have a higher degree of malignancy and shorter survival. Because the metex14 skipping variant is relatively rare in lung cancer, there are limited options for patients with this variant.
Tepotinib is an oral, targeted anti-cancer** drug. Approximately 3-4% of patients with non-small cell lung cancer (NSCLC) will experience MET exon 14 skips. As a MET inhibitor, tepotinib is able to inhibit the aberrant activity of MET protein. Therefore, when tepotinib is used in metastatic non-small cell lung cancer carrying the metex14 skipping variant, which can block the MET signaling pathway and inhibit the proliferation and spread of cancer cells, thereby delaying the progression of the disease and improving the survival rate of patients.
In a phase II, open-label, multi-cohort study of tepotinib 500 mg in patients with metex14 skipping variants, and efficacy and safety were evaluated in predefined subgroups based on age, prior ** (chemotherapy and immune checkpoints) inhibitors and brain metastases, intracranial activity was assessed using a special retrospective analysis using the Response Assessment of Neuro-Tumor Brain Metastases (RANO-BM) criteria. Among those involved in the trial,:The observed objective response rate (ORR) was 447%。The objective response rate (ORR) was 48 for patients aged < 75 and 75 years, respectively8% and 397%。
Treatment-naïve patients showed consistent efficacy compared to those who had previously received **;Median duration of response: 108 vs. 111 month. Of the 15 patients analyzed by RANO-BM (12 of whom had received radiation**), 13 achieved intracranial disease control;Five of the seven patients with measurable brain metastases experienced partial intracranial reactions. As a result, we can see that tepotinib showed meaningful activity in subgroups of different ages, prior to**, and brain metastases, with a manageable safety profile and few discontinuations.
The approval of tepotinib provides a much-needed targeted** option for patients with advanced non-small cell lung cancer (NSCLC) with MET exon 14 skipping alterations
References: 1**Wait. Expert consensus on NSCLC targeting of met14 exon skipping mutations. Chinese Journal of Lung Cancer. 2023；26(06):416-428.
2.lex,sakaih,felipe,veillonr,garassinomc,raskinj,cortotab,viteris,mazieresj,smitef,thomasm,iamswt,chobc,kimhr,yangjc,chenym,pateljd,bestvinacm,parkk,griesingerf,johnsonm,gottfriedm,britschgic,heymachj,sikoglue,berghoffk,schumacherkm,brunsr,ottog,paikpk.efficacyandsafetyinpatientswithmetexon14skippingnsclc:outcomesinpatientsubgroupsfromthevisionstudywithrelevanceforclinicalpractice.clincancerres.2022mar15；28(6):1117-1126.doi:10.1158/1078-0432.ccr-21-2733.pmid:34789481；pmcid:pmc9365370.
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