Drug intelligence / Profile preview

selpercatinib + ranitidine

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of **selpercatinib**, a selective small molecule RET tyrosine kinase inhibitor used for RET-driven cancers, and **ranitidine**, a histamine H2-receptor antagonist used primarily for reducing gastric acid secretion. Selpercatinib inhibits RET and other kinases to prevent tumor growth; ranitidine acts by reversibly inhibiting the histamine H2-receptors of gastric parietal cells, thereby suppressing gastric acid production. This combination is not marketed as a fixed-dose product but refers to co-administration of both drugs, which is clinically relevant because ranitidine (an H2 antagonist) can reduce selpercatinib's serum concentration, likely by raising gastric pH and altering selpercatinib absorption[2][3]. Selpercatinib is developed for RET fusion-positive cancers (e.g., non-small cell lung cancer, medullary thyroid cancer, other RET fusion solid tumors)[1][2]. Ranitidine is developed and marketed for treatment of peptic ulcer disease and gastroesophageal reflux disease.

02

Targets

RET (Rearranged during transfection receptor tyrosine kinase)FGFR3 (Fibroblast growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)HRH2 (Histamine H2 Receptor)VEGFR3 (Vascular endothelial growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)

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