Drug intelligence / Profile preview

dasatinib + zoledronic acid

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

Overview

Dasatinib + zoledronic acid is a combination therapy consisting of dasatinib, a small molecule tyrosine kinase inhibitor, and zoledronic acid, a bisphosphonate. Dasatinib inhibits multiple kinases including SRC family kinases, BCR-ABL, c-KIT, PDGFRβ, and others. It disrupts osteoclast-mediated bone resorption by inhibiting SRC kinase activity. Zoledronic acid acts primarily by inhibiting osteoclast-mediated bone resorption through inhibition of farnesyl pyrophosphate synthase in the mevalonate pathway. The combination has been studied for the treatment of breast cancer with bone metastases to target both tumor growth and skeletal-related events. Clinical studies have shown that this regimen is generally well tolerated and can produce partial responses in bone lesions in patients with hormone receptor-positive breast cancer[1][2][5].

02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)FDPS (Farnesyl pyrophosphate synthase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)SRC (Proto-oncogene tyrosine-protein kinase Src)

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