Drug intelligence / Profile preview

selpercatinib + rosuvastatin

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

Overview

Selpercatinib + rosuvastatin is a **combination of two small molecule drugs**. **Selpercatinib** is a selective RET kinase inhibitor approved for use in specific cancers with RET gene alterations, including non-small cell lung cancer (NSCLC), medullary thyroid cancer, and other RET fusion-positive solid tumors. It acts by inhibiting aberrant RET signaling, thereby blocking tumor growth and proliferation. **Rosuvastatin** is a statin (HMG-CoA reductase inhibitor) primarily used to treat hypercholesterolemia by inhibiting hepatic cholesterol synthesis, which reduces LDL cholesterol. This specific combination does not represent a clinical product, but the pair has been studied in healthy subjects to assess drug-drug interactions: selpercatinib inhibits the transporter BCRP (breast cancer resistance protein), leading to increased plasma concentrations of rosuvastatin when administered together[1][2].

02

Targets

ABCG2 (Breast cancer resistance protein)RET (Rearranged during transfection receptor tyrosine kinase)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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