Drug intelligence / Profile preview

erlotinib + capecitabine + oxaliplatin

Development stage
Unknown
Lead developer
The Chinese University of Hong Kong
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

erlotinib + capecitabine + oxaliplatin is a combination chemotherapy and targeted therapy regimen evaluated for the first-line treatment of metastatic colorectal cancer. This regimen combines erlotinib (Tarceva), a small molecule tyrosine kinase inhibitor targeting the epidermal growth factor receptor (EGFR), with the XELOX chemotherapy backbone, which consists of capecitabine (Xeloda) and oxaliplatin (Eloxatin). Erlotinib works by inhibiting the intracellular phosphorylation of tyrosine kinases associated with EGFR, thereby blocking downstream signaling pathways involved in cell proliferation and survival. Capecitabine is an orally administered prodrug that is enzymatically converted to 5-fluorouracil (5-FU) within tumors, where it inhibits thymidylate synthase to disrupt DNA synthesis. Oxaliplatin is a platinum-based agent that forms reactive complexes which cross-link DNA, leading to the inhibition of DNA replication and transcription. This specific combination was investigated by the Chinese University of Hong Kong in a randomized Phase II trial (NCT01243047) to compare intermittent versus continuous erlotinib dosing schedules.

Brand names
TarcevaXelodaEloxatin
Other names
Erlotinib + XELOXErlotinib + mXELOXerlotinib + capecitabine + oxaliplatin
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)DNATS (Thymidylate synthase)

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