Drug intelligence / Profile preview

PTK787 + pemetrexed + cisplatin

Development stage
Phase 2
Lead developer
Eli Lilly
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules, Device-based Delivery → Drug Delivery Systems
Administration
Oral, Intravenous
01

Overview

Combination treatment consisting of PTK787 (also known as PTK787/ZK222584), an oral angiogenesis inhibitor targeting VEGF receptors (VEGFR1, VEGFR2, and VEGFR3), along with the chemotherapy drugs pemetrexed and cisplatin. This combination was investigated in phase I/II clinical trials for various cancers, particularly lung cancer. Studies showed dose-limiting toxicities, which prevented dose escalation of PTK787, and ultimately led to trial closure due to toxicity and lack of efficacy. Pemetrexed and cisplatin are established chemotherapy agents commonly used together for conditions like non-small cell lung cancer and malignant pleural mesothelioma.

02

Targets

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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