Drug intelligence / Profile preview

afatinib + dasatinib

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

Afatinib + dasatinib is a combination therapy consisting of two targeted anti-cancer agents. Afatinib is an irreversible pan-HER tyrosine kinase inhibitor that targets EGFR, HER2, and HER4. Dasatinib is a multikinase inhibitor that targets BCR-ABL and several SRC-family kinases. The combination has shown synergistic effects in various cancer types, including stomach cancer, triple-negative breast cancer (TNBC), and lung cancer with EGFR mutations[1][2][9][10]. The rationale behind this combination is to simultaneously inhibit multiple signaling pathways that contribute to cancer cell growth and survival. Preclinical studies have demonstrated that the combination can overcome resistance to single-agent therapy in some cancer models[1][6]. Clinical investigation of this combination has been conducted in a phase 1/2 trial (NCT01999985) for patients with lung cancer, particularly those with EGFR mutations who developed resistance to prior EGFR TKI therapy[3][8].

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)KIT (c-KIT proto-oncogene receptor tyrosine kinase)BTK (Bruton tyrosine kinase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)PDGFRB (Platelet-derived growth factor receptor beta)SFK (SRC family kinases)ERBB4 (Erb-b2 receptor tyrosine kinase 4)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)EPHA2 (Ephrin type-A receptor 2)

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