Drug intelligence / Profile preview

cyclophosphamide + fluorouracil + goserelin + methotrexate + tamoxifen

Development stage
Preclinical
Lead developer
Takeda
Modality
Small Molecules
Administration
Intravenous, Oral, Subcutaneous, Intramuscular, Intrathecal
01

Overview

This is a multi-agent combination chemotherapy and hormonal therapy regimen composed of five drugs: - **Cyclophosphamide** is an alkylating agent that crosslinks DNA, leading to cell death. - **Fluorouracil (5-FU)** is an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis. - **Methotrexate** is a folate analog antimetabolite that inhibits dihydrofolate reductase, blocking DNA synthesis and cell replication[7][10]. - **Goserelin** is a gonadotropin-releasing hormone (GnRH) agonist that suppresses ovarian function and reduces estrogen production. - **Tamoxifen** is a selective estrogen receptor modulator (SERM) acting as an antagonist on breast tissue. This combination targets cancer cells through multiple mechanisms—direct cytotoxicity via DNA damage or inhibition of nucleotide synthesis, suppression of hormone-driven tumor growth by reducing estrogen levels, and blockade of the estrogen receptor. Such regimens are primarily used in the treatment of hormone-sensitive cancers like breast cancer. While combinations such as CMF (cyclophosphamide, methotrexate, fluorouracil) are well-established for breast cancer[5], the addition of goserelin and tamoxifen further enhances endocrine suppression.

Brand names
Zoladex
Other names
CMF
02

Targets

ER (Estrogen receptor)TS (Thymidylate synthase)GnRHR (Gonadotropin-releasing hormone receptor)DNADHFR (Dihydrofolate reductase)

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