Drug intelligence / Profile preview

dasatinib + exemestane

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

Dasatinib + exemestane is a combination therapy under investigation for the treatment of advanced estrogen receptor-positive (ER+) breast cancer, particularly after progression on non-steroidal aromatase inhibitor (NSAI) therapy. Dasatinib is a small molecule inhibitor targeting multiple tyrosine kinases, including Src family kinases (SFK) and BCR-ABL, and is approved for certain leukemias. Exemestane is an aromatase inhibitor that blocks estrogen biosynthesis, suppressing growth of hormone receptor-positive breast cancer cells. The rationale for combining dasatinib with exemestane is to enhance anti-tumor activity and delay disease progression, especially in cases of endocrine resistance, through dual inhibition of tumor signaling and estrogen synthesis[1][4].

Brand names
AromasinSprycelPhyrago
02

Targets

SIK2 (Salt inducible kinase 2)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)BTK (Bruton tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)CYP19A1 (Aromatase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)AR (Adrenergic receptors)DDR1 (Discoidin domain receptor 1)EPHA2 (Ephrin type-A receptor 2)SFK (SRC family kinases)

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