Drug intelligence / Profile preview

arsenic trioxide + fluorouracil + leucovorin

Development stage
Unknown
Lead developer
University of Miami Miller School of Medicine
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of arsenic trioxide (ATO), fluorouracil (5-FU), and leucovorin (LV). Arsenic trioxide is known for its ability to downregulate thymidylate synthase (TS), thereby resensitizing tumor cells that have become resistant to 5-fluorouracil. Fluorouracil is an antimetabolite that inhibits DNA synthesis by targeting TS, while leucovorin enhances the binding of 5-FU to TS, increasing its cytotoxicity. This combination has been investigated primarily in patients with relapsed or refractory metastatic colorectal cancer who have failed prior therapies. The regimen aims to improve the efficacy of standard fluoropyrimidine-based chemotherapy by overcoming resistance mechanisms through TS modulation[1][2][6].

Other names
arsenic trioxide5-fluorouracilleucovorinATO + 5-FU + LV
02

Targets

TS (Thymidylate synthase)

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