OncoPharm Tepotinib
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Feb 4, 2021 The podcast dives into the recent FDA approval of tepotinib for metastatic non-small cell lung cancer. It provides an engaging comparison with capmatinib, highlighting differences in pharmacology and dosing. The hosts discuss side effects and ongoing research, offering insights into the efficacy of these treatments. Overall, the conversation sheds light on how these therapies fit into patient care and what this means for the future of lung cancer treatment.
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MET Exon 14 Skipping Mutation
- Tepotinib and capmatinib both target MET exon 14 skipping mutation in metastatic NSCLC.
- This mutation causes exon 14 skipping, leading to an abnormally active MET protein.
Capmatinib's Stronger MET Affinity
- Capmatinib shows greater selectivity and stronger affinity for C-Met with lower IC50 than tepotinib.
- This difference may or may not be clinically significant.
pKa Influences Absorption Timing
- Capmatinib has acidic pKa (~0.9) leading to higher solubility in acidic gastric environment.
- Tepotinib has basic pKa (~9.5) leading to delayed absorption mainly in the small intestine and requires food for better bioavailability.