Drug intelligence / Profile preview

dasatinib + fulvestrant

Development stage
Phase 2
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Dasatinib + fulvestrant is an investigational **combination therapy** comprising dasatinib, a small-molecule tyrosine kinase inhibitor that targets SRC family kinases, BCR-ABL, c-KIT, PDGFR, c-FMS, and EPHA2, and fulvestrant, a selective estrogen receptor degrader (SERD) that binds, blocks, and accelerates degradation of the estrogen receptor. Dasatinib is primarily used in hematologic malignancies, and fulvestrant in hormone receptor-positive metastatic breast cancer. The rationale for their combination is to target both estrogen receptor signaling and compensatory oncogenic pathways (SRC/SFKs) that drive tumor growth and resistance in breast cancer, particularly in models resistant to endocrine therapy. Clinical trials have evaluated dasatinib and fulvestrant together in metastatic breast cancer but have not demonstrated significant improvement in progression-free survival compared to fulvestrant alone. Their combination may alter fulvestrant serum levels and increase the risk or severity of adverse events[1][3].

02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)CSF1R (Macrophage colony-stimulating factor receptor)EPHA2 (Ephrin type-A receptor 2)ER (Estrogen receptor)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)SRC (Proto-oncogene tyrosine-protein kinase Src)

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