Drug intelligence / Profile preview

cyclophosphamide + docetaxel + epirubicin + lapatinib

Development stage
Unknown
Lead developer
Sanofi
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This drug is a combination chemotherapy regimen consisting of four agents used primarily in the treatment of breast cancer, including metastatic and HER2-positive subtypes. - **Cyclophosphamide** is an alkylating agent that interferes with DNA replication by cross-linking DNA strands, leading to cell death. It is commonly used in various cancers including breast cancer. - **Docetaxel** is a taxane class chemotherapeutic that promotes microtubule stabilization, inhibiting mitosis and inducing apoptosis. It has demonstrated synergy with cyclophosphamide and doxorubicin in breast cancer treatment. - **Epirubicin** is an anthracycline antibiotic that intercalates into DNA, inhibits topoisomerase II, and generates free radicals causing cytotoxicity. It enhances the efficacy of taxanes and alkylating agents. - **Lapatinib** is a small molecule tyrosine kinase inhibitor targeting epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor-2 (HER-2). It competitively binds to the ATP-binding site intracellularly, blocking downstream signaling pathways critical for tumor cell proliferation especially in HER-2 positive breast cancer. The combination leverages multiple mechanisms—DNA damage from cyclophosphamide and epirubicin; mitotic inhibition from docetaxel; targeted inhibition of HER family receptors by lapatinib—to achieve enhanced antitumor activity. Lapatinib adds targeted therapy benefits particularly for HER-2 overexpressing tumors resistant or refractory to trastuzumab.

02

Targets

DNAERBB2 (Erb-b2 receptor tyrosine kinase 2)TOP2A (DNA topoisomerase II)EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))

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