Drug intelligence / Profile preview

afatinib + dasatinib

Development stage
Phase 1
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

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

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