Drug intelligence / Profile preview

dasatinib + paclitaxel + trastuzumab

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination therapy consisting of three agents: dasatinib, paclitaxel, and trastuzumab. Dasatinib is an orally available small molecule tyrosine kinase inhibitor that targets BCR-ABL and SRC-family kinases. Paclitaxel is a microtubule-stabilizing chemotherapeutic agent that inhibits cell division. Trastuzumab is a humanized monoclonal antibody targeting the extracellular domain of HER2/neu receptor. This triple regimen has been investigated in clinical trials for first-line treatment of HER2-positive metastatic breast cancer, particularly in patients with resistance to standard anti-HER2 therapies. The rationale for this combination stems from preclinical evidence showing synergistic effects between SRC inhibition (by dasatinib) and HER2 blockade (by trastuzumab), with added cytotoxicity from paclitaxel[1][5][6]. Clinical studies have demonstrated that this regimen can be safely administered with manageable toxicity and shows promising efficacy, including high objective response rates[1][4].

Brand names
Sprycel (dasatinib)Herceptin (trastuzumab)Paclitaxel (no unique brand for the combination)
Other names
dasatinib, paclitaxel, and trastuzumab combination
02

Targets

TUBB (Tubulin (alpha and beta subunits))ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)SFK (SRC family kinases)

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