Drug intelligence / Profile preview

paclitaxel + vatalanib

Development stage
Phase 1
Lead developer
Indiana University School of Medicine
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This combination therapy consists of the taxane chemotherapy agent paclitaxel and the oral small molecule tyrosine kinase inhibitor vatalanib (PTK787/ZK 222584). Paclitaxel is a well-established antineoplastic agent that works by stabilizing microtubules, thereby disrupting microtubule function and inhibiting cell division. Vatalanib is a multi-targeted tyrosine kinase inhibitor that primarily targets all three vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3), as well as platelet-derived growth factor receptor beta (PDGFR-beta) and c-kit, thereby exerting potent anti-angiogenic and anti-tumor effects. This specific combination was investigated in a Phase I trial led by the Indiana University School of Medicine for patients with advanced solid tumors. The study aimed to determine the maximum tolerated dose and evaluate pharmacokinetic interactions. Results indicated that the combination was generally well tolerated and showed evidence of anti-cancer activity, although pharmacokinetic analysis revealed a significant drug-drug interaction where vatalanib increased the clearance of paclitaxel.

Other names
paclitaxel + PTK787paclitaxel + ZK 222584
02

Targets

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)CSF1R (Macrophage colony-stimulating factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)TUBB (Tubulin (alpha and beta subunits))

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