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Home European Commission Approves TEPMETKO® (tepotinib) as First Oral MET Inhibitor for Advanced NSCLC with METex14 Skipping Alterations

European Commission Approves TEPMETKO® (tepotinib) as First Oral MET Inhibitor for Advanced NSCLC with METex14 Skipping Alterations

Feb 20, 2022 03:23 CST Updated 03:23
Merck Group

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The European Union (German: Europäische Union; French: Union européenne), abbreviated as the EU, is headquartered in Brussels, the capital of Belgium. It evolved from the European Communities and originally had six founding member states: Germany, France, Italy, the Netherlands, Belgium, and Luxembourg. The Union currently has 28 member states and 24 official languages.In December 1991, the European Council meeting in Maastricht adopted the Treaty on European Union, commonly known as the Maastricht Treaty. On November 1, 1993, the Maastricht Treaty officially entered into force, marking the formal establishment of the European Union. In 2012, the EU was awarded the Nobel Peace Prize.Donald Tusk serves as President of the European Council, and Antonio Tajani is President of the European Parliament. Jean-Claude Juncker, former Prime Minister of Luxembourg, is President of the European Commission.The EU’s treaties have been amended multiple times, and its operations are governed by the Treaty of Lisbon. Politically, all member states are democracies (according to The Economist’s 2008 Democracy Index). Economically, it constitutes the world’s second-largest economic entity (with Germany, France, and Italy being members of the G8). Militarily, the vast majority of EU member states are also members of the North Atlantic Treaty Organization (NATO).


News on February 19, 2022 /BioValleyBIOON/ -- Merck KGaA recently announced that the European Commission (EC) has approved the targeted anticancer drug Tepmetko (tepotinib): This drug is a highly selective, once-daily oral MET inhibitor, used as a monotherapy for the treatment of adult patients with advanced non-small cell lung cancer (NSCLC) who have previously received immunotherapy and/or platinum-based chemotherapy, require systemic therapy, and carry MET exon 14 skipping alterations (METex14 skipping).

It is estimated that lung cancer is the second most common cancer in Europe and the leading cause of cancer-related deaths, resulting in 388,000 deaths in 2018. Alterations in the MET signaling pathway, including METex14 skipping alterations, are found in 3%-4% of NSCLC cases, which are associated with advanced disease and poor prognosis.

Tepmetko is the world's first approved oral MET inhibitor for the treatment of patients with advanced NSCLC carrying MET gene alterations.Tepmetko was approved in Japan in March 2020 and in the United States in February 2021 for the treatment of NSCLC patients with METex14 skipping alterations. In Japan, Tepmetko has been granted Orphan Drug Designation (ODD) and SAKIGAKE Designation (Innovative Medicine). In the United States, Tepmetko has been granted Orphan Drug Designation (ODD) and Breakthrough Therapy Designation (BTD).

Tepmetko is also available in the United States.FDAThe first once-daily oral MET inhibitor approved for the treatment of patients with metastatic NSCLC harboring METex14 skipping alterations. September 2020,NovartisTargeted anticancer drug Tabrecta (capmatinib)Approved, isFDAThe first approved MET inhibitor for the treatment of adult patients with metastatic NSCLC harboring METex14 skipping alterations.Tepmetko and Tabrecta are both approved for: patients who have not previously received treatment (first-line) and patients who have previously received treatment (treated). In terms of medication,Tepmekto is taken orally once daily, while Tabrecta is taken orally twice daily.

This EU approval is based on data from the pivotal Phase 2 VISION study (NCT02864992). This is the largest clinical study to date in patients with metastatic NSCLC harboring METex14 skipping alterations, in which a total of 275 patients with METex skipping alterations (median age: 72.6 years) received Tepmetko treatment.

The main analysis data were previously published in the international top medical journal, The New England Journal of Medicine (NEJM): As of January 1, 2020, a total of 152 patients had received Tepmetko treatment, and 99 patients had undergone at least 9 months of follow-up.In the pooled biopsy group, the objective response rate (ORR) by independent review was 46%, and the median duration of response (DOR) was 11.1 months.。The ORR in the liquid biopsy group of 66 patients was 48%.、The ORR was 50% in 60 patients from the tissue biopsy group.All 27 patients achieved positive results with both methods. Additionally, Tepmetko demonstrated consistent and durable responses in both treatment-naïve patients (first-line group) and previously treated patients (post-treatment group).

Globally, lung cancer is the most common type of cancer and the leading cause of cancer-related deaths, with 2 million new cases diagnosed and 1.7 million deaths each year. Currently, three types of MET signaling pathway alterations (including METex14 skipping mutations, MET amplification, and MET protein overexpression) have been identified across various types of cancers, which are associated withTumorThe invasive behavior and poor clinical prognosis are related. It is estimated that MET signaling pathway alterations occur in 3-5% of NSCLC cases.

Tepotinib is an orally available MET kinase inhibitor discovered internally by Merck. It potently and highly selectively inhibits oncogenic signaling driven by MET (gene) alterations — including METex14 skipping mutations, MET amplification, and MET protein overexpression — with the potential to improve treatment outcomes for patients with aggressive tumors carrying these specific MET alterations. Beyond NSCLC, Merck is also actively evaluating tepotinib in combination with novel therapies for otherTumorIndications.

September 2019, United StatesFDAGranted tepotinib Breakthrough Therapy Designation (BTD) for the treatment of patients with metastatic NSCLC harboring METex14 skipping alterations whose disease has progressed following platinum-based chemotherapy.

Currently, Merck is also conducting another study, INSIGHT 2 (NCT03940703), to evaluate the combination of tepotinib and the tyrosine kinase inhibitor (TKI) osimertinib for EGFR-mutated, MET-amplified, locally advanced or metastatic NSCLC patients with acquired resistance to prior EGFR TKI therapy. (Bioon.com)