Drug intelligence / Profile preview

tepotinib + paclitaxel

Development stage
Phase 2
Lead developer
Merck KGaA
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Tepotinib + paclitaxel is an investigational combination therapy consisting of tepotinib, a highly selective small molecule inhibitor of the MET receptor tyrosine kinase, and paclitaxel, a microtubule-stabilizing chemotherapeutic agent. This combination is being studied primarily for the treatment of advanced gastric and gastroesophageal junction carcinomas (AGC/GEJC) with MET amplification or MET exon 14 alterations. Tepotinib targets aberrant MET signaling pathways involved in tumor growth and survival, while paclitaxel disrupts cell division by stabilizing microtubules. Preclinical studies suggest that this combination may be particularly effective in tumors with specific MET gene alterations or phosphorylation status[2]. Clinical trials are ongoing to determine the maximal tolerated dose and efficacy as second-line therapy in these patient populations[1][3][4][6].

02

Targets

MET (Mesenchymal-epithelial transition factor receptor)TUBB (Tubulin (alpha and beta subunits))

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