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dasatinib + docetaxel + prednisone

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Combination therapy of **dasatinib + docetaxel + prednisone** consists of three agents with distinct mechanisms of action, used together in the treatment of metastatic castration-resistant prostate cancer (mCRPC)[1][4][7]. - **Dasatinib** is a small molecule, oral tyrosine kinase inhibitor targeting multiple kinases, including SRC family kinases and BCR-ABL, with potential effects on both tumor cells and the bone microenvironment. - **Docetaxel** is a small molecule, cytotoxic taxane chemotherapeutic that stabilizes microtubules, inducing apoptosis and inhibiting cell division. - **Prednisone** is a synthetic glucocorticoid corticosteroid, commonly used as an adjunct to chemotherapy to reduce inflammation and manage side effects. This combination was investigated for synergistic effects in mCRPC patients due to dasatinib’s ability to inhibit SRC kinases in both tumor and bone, docetaxel’s cytotoxic activity, and prednisone’s supportive role. Clinical trials found that while the combination was feasible and safe, it did not show improved overall survival over docetaxel plus prednisone alone[2][3][4][7].

Other names
dasatinibdocetaxelprednisone
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)TUBB (Tubulin (alpha and beta subunits))GR (Glucocorticoid receptor)FAK (Focal adhesion kinase)PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)SFK (SRC family kinases)EPHA2 (Ephrin type-A receptor 2)

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