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osimertinib + pralsetinib
- Development stage
- Preclinical
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A combination therapy consisting of osimertinib (a third-generation EGFR tyrosine kinase inhibitor) and pralsetinib (a selective RET tyrosine kinase inhibitor). This combination is primarily used to overcome resistance to osimertinib monotherapy in EGFR-mutated non-small cell lung cancer (NSCLC) patients who have acquired RET fusions, particularly ANK3-RET fusion. The combination has demonstrated durable responses exceeding 12 months in clinical cases, even with dose adjustments to manage overlapping toxicities.
02
Targets
DDR1 (Discoidin domain receptor 1)EGFR (Epidermal growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FLT3 (Fms related receptor tyrosine kinase 3)ERBB2 (Erb-b2 receptor tyrosine kinase 2)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)PDGFRB (Platelet-derived growth factor receptor beta)RET (Rearranged during transfection receptor tyrosine kinase)NTRK1 (Tropomyosin-related receptor kinase A)NTRK3 (Tropomyosin receptor kinase C)VEGFR2 (Vascular endothelial growth factor receptor 2)
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