Drug intelligence / Profile preview

cyclophosphamide + fluorouracil + methotrexate + tamoxifen

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

Overview

This is a combination regimen consisting of four drugs—cyclophosphamide, fluorouracil (5-FU), methotrexate, and tamoxifen—used in the treatment of breast cancer. Cyclophosphamide is an alkylating agent that interferes with DNA replication and cell division. Methotrexate and fluorouracil are antimetabolite chemotherapeutic agents that inhibit DNA synthesis by targeting folate metabolism (methotrexate) or thymidylate synthase (fluorouracil). Tamoxifen is a selective estrogen receptor modulator (SERM) that acts as an antagonist on estrogen receptors in breast tissue, thereby inhibiting the growth-promoting effects of estrogen on hormone receptor–positive breast cancer cells. This combination has been studied as adjuvant therapy for early-stage and node-positive breast cancer, particularly in postmenopausal women with hormone receptor–positive tumors[2][7]. The addition of chemotherapy to tamoxifen does not significantly improve survival but increases toxicity compared to tamoxifen alone[2][7].

Brand names
Cytoxan (cyclophosphamide)Amethopterin (methotrexate)Folex (methotrexate)Mexate (methotrexate)Rheumatrex (methotrexate)
Other names
5-FU (fluorouracil)
02

Targets

DHFR (Dihydrofolate reductase)ER (Estrogen receptor)DNATS (Thymidylate synthase)

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