Drug intelligence / Profile preview

CP-547,632 + Carboplatin + Paclitaxel

Development stage
Phase 2
Lead developer
Pfizer
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

CP-547,632 combined with carboplatin and paclitaxel is a chemotherapy regimen investigated primarily for non-small cell lung cancer (NSCLC) treatment. CP-547,632 is a novel tyrosine kinase inhibitor that specifically targets vascular endothelial growth factor receptor 2 (VEGFR-2) and fibroblast growth factor receptor (FGFR). The combination was studied in Phase I/II clinical trials, with CP-547,632 administered orally daily alongside standard doses of paclitaxel (225 mg/m²) and carboplatin (AUC = 6) given in 21-day cycles. The maximum tolerable dose for CP-547,632 was determined to be 200 mg/day, with dose-limiting toxicities of rash and diarrhea occurring at 250 mg/day. The theoretical benefit was to enhance anti-tumor activity by simultaneously targeting cancer cells (via chemotherapy) and tumor vasculature (via angiogenesis inhibition). In the Phase I portion of the study, a 20% objective response rate was observed among evaluable patients.

02

Targets

DNAFGFR (Fibroblast growth factor receptor)TUBB (Tubulin (alpha and beta subunits))VEGFR2 (Vascular endothelial growth factor receptor 2)

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