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pralsetinib + selpercatinib
- Development stage
- Unknown
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Pralsetinib and selpercatinib are selective RET tyrosine kinase inhibitors (TKIs) used to treat patients with RET gene alterations, particularly in non-small cell lung cancer (NSCLC) and thyroid cancer. Both drugs received FDA accelerated approval in 2020 based on the pivotal ARROW trial (pralsetinib) and LIBRETTO-001 trial (selpercatinib). They work by selectively inhibiting RET by competing with ATP for binding at the adenosine triphosphate-binding site, preventing RET phosphorylation and downstream signaling. Both drugs have demonstrated efficacy against brain metastases and share similar mechanisms of action, though with different safety profiles.
- Brand names
- GavretoRetevmo
02
Targets
JAK2 (Janus kinase 2)NTRK1 (Tropomyosin-related receptor kinase A)FLT3 (Fms related receptor tyrosine kinase 3)PDGFRB (Platelet-derived growth factor receptor beta)FGFR3 (Fibroblast growth factor receptor 3)JAK1 (Janus kinase 1)NTRK3 (Tropomyosin receptor kinase C)FGFR2 (Keratinocyte growth factor receptor)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)DDR1 (Discoidin domain receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)
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