Drug intelligence / Profile preview

chiauranib + paclitaxel

Development stage
Phase 3
Lead developer
Akeso
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Chiauranib + paclitaxel is a combination regimen of a novel multi-targeted kinase inhibitor (chiauranib) and paclitaxel, developed and investigated primarily for the treatment of platinum-resistant or refractory ovarian cancer. **Chiauranib** is an orally available small-molecule inhibitor that targets multiple kinases involved in tumor biological processes, including Aurora B (cell mitosis), CSF-1R (tumor-associated macrophage function), and angiogenesis-related kinases such as VEGFR1, VEGFR2, VEGFR3, PDGFRα, and c-Kit. Its mechanism targets cell cycle regulation, tumor microenvironment, and tumor vasculature. **Paclitaxel** is a well-established microtubule-stabilizing chemotherapeutic agent that inhibits cell mitosis. The combination aims to exploit synergistic anti-tumor effects by simultaneously interfering with tumor cell division, angiogenesis, and immune modulation pathways. In clinical studies (phase Ib and phase II), the combination was administered to patients with recurrent, platinum-resistant ovarian cancer (chiauranib 50 mg orally daily, paclitaxel 60 mg/m² intravenously weekly on days 1, 8, and 15 for up to 6 cycles). The combination showed enhanced efficacy over monotherapy, with manageable adverse events; most toxicities were hematological (neutropenia, leucopenia, lymphopenia) and hypertension[1][3].

Other names
chiauranib plus paclitaxelchiauranib combined with paclitaxel
02

Targets

AURKB (Aurora kinase B)CSF1R (Macrophage colony-stimulating factor receptor)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)TUBB (Tubulin (alpha and beta subunits))

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