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paclitaxel + rebastinib
- Development stage
- Unknown
- Lead developer
- Deciphera Pharmaceuticals
- Modality
- Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Fragment-Derived Small Molecules → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Paclitaxel + rebastinib is an investigational combination therapy consisting of the microtubule-stabilizing chemotherapeutic agent paclitaxel and the oral small molecule kinase inhibitor rebastinib. Paclitaxel disrupts cell division by stabilizing microtubules, leading to apoptosis in rapidly dividing cancer cells. Rebastinib is a potent and selective switch-control inhibitor of tunica interna endothelial cell kinase 2 (TIE2), a receptor tyrosine kinase involved in angiogenesis and tumor microenvironment regulation. The combination aims to enhance anti-tumor efficacy by targeting both tumor cells directly (paclitaxel) and the tumor vasculature/microenvironment (rebastinib). This regimen has been studied primarily in advanced or metastatic solid tumors, including HER2-negative metastatic breast cancer, endometrial cancer, platinum-resistant ovarian cancer, gynecological carcinosarcoma, triple-negative breast cancer (TNBC), and inflammatory breast cancer[1][2][3][4][5].
02
Targets
MicrotubuleTEK (Tie2)
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