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crenolanib + axitinib + docetaxel
- Development stage
- Phase 2
- Lead developer
- AROG Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This is a **combination regimen** of three drugs: crenolanib (a selective inhibitor of class III receptor tyrosine kinases FLT3, PDGFRα, and PDGFRβ), axitinib (a highly selective inhibitor of vascular endothelial growth factor receptors VEGFR-1, -2, and -3), and docetaxel (a microtubule-stabilizing chemotherapeutic agent). Crenolanib is an investigational oral benzimidazole developed for the treatment of malignancies driven by PDGFR or FLT3 mutations; axitinib is an approved small molecule VEGFR inhibitor used for various carcinomas; docetaxel is an approved cytotoxic agent widely used in solid tumors. This triple combination has been evaluated in phase Ib studies for safety and pharmacokinetics in advanced solid tumors, aiming to achieve additive or synergistic effects through simultaneous inhibition of tumor cell proliferation (via PDGFR/FLT3), anti-angiogenesis (via VEGFR), and direct cytotoxicity (via microtubule stabilization), but also results in increased mucositis and neutropenia compared to dual combinations[1][3][4][5][6][7].
- Other names
- crenolanib besylate + axitinib + docetaxel
02
Targets
FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)TUBB (Tubulin (alpha and beta subunits))VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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