Drug intelligence / Profile preview

doxorubicin + fluorouracil + melphalan + tamoxifen

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

Overview

This is a combination regimen consisting of four drugs—doxorubicin, fluorouracil, melphalan, and tamoxifen—used primarily in the treatment of breast cancer. - **Doxorubicin** is an anthracycline antibiotic that intercalates DNA and inhibits topoisomerase II, leading to DNA strand breaks and apoptosis in rapidly dividing cells. - **Fluorouracil (5-FU)** is an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and repair. - **Melphalan** is an alkylating agent that crosslinks DNA strands, preventing cell replication. - **Tamoxifen** is a selective estrogen receptor modulator (SERM) that acts as an antagonist on estrogen receptors in breast tissue but can have agonist effects elsewhere. This combination has been studied for adjuvant therapy in node-positive breast cancer patients. Some studies have shown potential antagonistic interactions between tamoxifen and both melphalan and fluorouracil when used together[1]. However, clinical trials have also demonstrated improved disease-free survival with regimens combining these agents compared to tamoxifen alone[2][5]. The use of this specific four-drug combination (sometimes called PFT or PAFT when cyclophosphamide or doxorubicin are added) has become less common due to the development of newer regimens.

Other names
PFTPAFT
02

Targets

ESR1 (ERα)TOP2A (DNA topoisomerase II)DNATS (Thymidylate synthase)

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