Drug intelligence / Profile preview

dasatinib + bortezomib + dexamethasone

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

This is a triple drug combination consisting of **dasatinib**, **bortezomib**, and **dexamethasone**, investigated primarily for treatment in patients with multiple myeloma, including those with comorbid conditions such as chronic myeloid leukemia. - **Dasatinib** is a small molecule tyrosine kinase inhibitor that targets multiple kinases involved in cancer cell growth and survival, including BCR-ABL and Src family kinases. - **Bortezomib** is a small molecule proteasome inhibitor, which disrupts protein degradation, leading to cell cycle arrest and apoptosis in malignant plasma cells. - **Dexamethasone** is a synthetic glucocorticoid corticosteroid, which exhibits anti-inflammatory, immunosuppressant, and pro-apoptotic effects. Preclinical and early clinical reports indicate this combination exhibits synergistic antitumor effects, especially in multiple myeloma, deregulating key gene pathways in neoplastic cells and overcoming tumor microenvironment-mediated resistance. This regimen is not an approved, branded combination but has been described in case reports and translational studies as having clinical activity and acceptable tolerability in specific multiple myeloma settings, often where standard regimens have failed[1][3][6].

Brand names
SprycelVelcadeDecadron
Other names
Dasatinib/Bortezomib/DexamethasoneDasatinib with Bortezomib and Dexamethasone
02

Targets

EPHA2 (Ephrin type-A receptor 2)SFK (SRC family kinases)PDGFRB (Platelet-derived growth factor receptor beta)PSMB5 (Proteasome subunit beta Type-5)GR (Glucocorticoid receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)BTK (Bruton tyrosine kinase)

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