Drug intelligence / Profile preview

erlotinib + dasatinib

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Erlotinib + dasatinib is a combination of two small molecule tyrosine kinase inhibitors investigated primarily for the treatment of advanced non-small cell lung cancer (NSCLC). Erlotinib is an epidermal growth factor receptor (EGFR) inhibitor, while dasatinib inhibits Src family kinases and multiple other tyrosine kinases. The rationale for combining these agents stems from the frequent activation and cooperation between EGFR and Src signaling pathways in cancer, which can promote tumor growth, survival, invasion, and angiogenesis. Clinical studies have shown that this combination is tolerable with adverse effects consistent with each agent individually. Disease control rates around 59–63% were observed in NSCLC trials; however, significant clinical benefit was mainly seen in patients with activating EGFR mutations. The combination has not demonstrated sufficient efficacy to support its use in unselected NSCLC populations[1][2][3].

Other names
erlotinib hydrochloride
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)SFK (SRC family kinases)PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)EGFR T790M (Epidermal growth factor receptor T790M mutant)EPHA2 (Ephrin type-A receptor 2)

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