Drug intelligence / Profile preview

amuvatinib + erlotinib

Development stage
Preclinical
Lead developer
Astex Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Amuvatinib (MP470) is a small molecule receptor tyrosine kinase inhibitor that targets multiple kinases including PDGFR, c-Kit, and c-Met. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor marketed as Tarceva. The combination of amuvatinib and erlotinib has been studied for its additive effects in inhibiting tumor growth in prostate cancer models by targeting the HER family/PI3K/Akt pathway. This dual inhibition results in reduced phosphorylation of HER1, HER2, and HER3 receptors and downstream signaling through PI3K/Akt, leading to increased cytotoxicity and apoptosis in cancer cells[2][4]. Amuvatinib was developed by SuperGen (now Astex Pharmaceuticals), while erlotinib was developed by OSI Pharmaceuticals (acquired by Astellas Pharma). The combination has primarily been investigated preclinically for prostate cancer.

Brand names
Tarceva
Other names
MP-470 + erlotinibamuvatinib + Tarceva
02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)ERBB3 (Erb-b2 receptor tyrosine kinase 3)ERBB2 (Erb-b2 receptor tyrosine kinase 2)PDGFR (PDGFR family)EGFR T790M (Epidermal growth factor receptor T790M mutant)MET (Mesenchymal-epithelial transition factor receptor)

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