Drug intelligence / Profile preview

dasatinib + docetaxel

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

Overview

Dasatinib + docetaxel is a combination regimen of the oral multi-kinase inhibitor **dasatinib** and the intravenous antineoplastic agent **docetaxel**. Dasatinib targets multiple tyrosine kinases, most notably **SRC family kinases**, BCR-ABL, c-KIT, EPHA2, EGFR, and PDGF receptors, thereby inhibiting tumor cell proliferation and affecting the tumor microenvironment, including bone turnover. Docetaxel is a microtubule stabilizing agent that inhibits cell division by binding to and stabilizing tubulin, inducing apoptosis in rapidly dividing cells. This combination has been explored especially in metastatic castration-resistant prostate cancer (mCRPC) and various solid tumor preclinical models, aiming to achieve synergistic antitumor effects by targeting tumor cells and the tumor microenvironment. While early-phase studies showed some synergistic activity and acceptable safety, phase 3 clinical trial data failed to demonstrate improved overall survival relative to docetaxel alone in mCRPC. The combination has also been explored preclinically in uterine leiomyosarcoma and other cancers[1][2][3][4].

02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)EGFR (Epidermal growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)ERBB2 (Erb-b2 receptor tyrosine kinase 2)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MAPK14 (p38 mitogen-activated protein kinase alpha)EPHA2 (Ephrin type-A receptor 2)PDGFRA (Platelet-derived growth factor receptor alpha)SRC (Proto-oncogene tyrosine-protein kinase Src)TUBB (Tubulin (alpha and beta subunits))

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