Drug intelligence / Profile preview

everolimus + imatinib

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

A combination therapy of **everolimus**, a mammalian target of rapamycin (mTOR) inhibitor, and **imatinib**, a tyrosine kinase inhibitor that targets KIT, ABL, and PDGFR-A/B kinases. This combination has been investigated primarily for advanced renal cell carcinoma and gastrointestinal stromal tumors (GIST) resistant to imatinib. Everolimus inhibits mTORC1-mediated cell growth and proliferation, while imatinib blocks receptor tyrosine kinases including PDGFR, potentially reducing cell survival and angiogenesis[1][3][5]. The rationale for the combination is dual blockade of mTOR-driven proliferation and PDGFR-mediated angiogenesis and tumor progression. While some studies confirm pharmacokinetic interaction (imatinib increases everolimus exposure), clinical efficacy has not shown clear improvement over either agent alone in tested indications[1][3][5].

Brand names
GleevecAfinitor
Other names
everolimus + imatinibeverolimus plus imatinib mesylate
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)Mechanistic target of rapamycin complex 1FKBP1A

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