Tepotinib hydrochloride for the treatment of non-small cell lung cancer.

• Z.-X. Wu ^[1] ; J. Li ^{[1] [2]} ; S. Dong ^[3] ; L. Lin ^[4] ; C. Zou ^[3] ; Z.-S. Chen ^[1]
  1. [1] Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John’s University, Queens, New York, USA
  2. [2] Department of Otolaryngology-Head and Neck Surgery, Zhongnan Hospital of Wuhan University, Wuhan, China
  3. [3] Key Laboratory of Medical Electrophysiology of Education Ministry, School of Pharmacy, Southwest Medical University, China and Shenzhen Public Service Platform on Tumor Precision Medicine and Molecular Diagnosis, Southern University of Science and Technology, Shenzhen, Guangdong, China
  4. [4] Cell Research Center, Shenzhen Bolun Institute of Biotechnology, Shenzhen, China

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• Localización: Medicamentos de actualidad = Drugs of today, ISSN 1699-3993, Vol. 57, Nº. 4, 2021, págs. 265-275
• Idioma: inglés
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• Resumen

  • Non-small cell lung cancer (NSCLC) is one of the most devastating cancers with high mortality worldwide. By inhibiting the activity of specific molecular targets in the cancer cells, tyrosine kinase inhibitors (TKIs) have become a standard treatment in combating NSCLC. Tepotinib hydrochloride is an orally bioavailable, mesenchymal-epithelial transition (MET) TKI developed mainly for selected NSCLC patients with METex14 skipping mutations. Tepotinib demonstrated durable clinical response in phase II clinical trials, which led to its approval for use in Japan and breakthrough therapy designation and accelerated approval in the U.S. These progresses highlighted tepotinib as a promising candidate for NSCLC patients. This review summarizes the pharmacological profile of tepotinib, preclinical studies and landmark clinical trials of tepotinib. In addition, we share our perspectives on the future direction of tepotinib as a novel anticancer drug.