Drug intelligence / Profile preview

Picoplatin + 5-fluorouracil + leucovorin

Development stage
Unknown
Lead developer
Poniard Pharmaceuticals
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Picoplatin + 5-fluorouracil + leucovorin is an investigational chemotherapy combination regimen studied primarily for the treatment of metastatic colorectal cancer. Picoplatin is a platinum-based chemotherapeutic agent designed to overcome resistance associated with other platinum drugs and has demonstrated reduced neurotoxicity compared to oxaliplatin. It acts by forming DNA adducts that inhibit DNA replication and transcription, leading to cell death. 5-Fluorouracil (5-FU) is a pyrimidine analog that inhibits thymidylate synthase, disrupting DNA synthesis in rapidly dividing cells. Leucovorin (folinic acid) is not itself cytotoxic but enhances the efficacy of fluorouracil by stabilizing the binding of its active metabolite to thymidylate synthase, thereby increasing cytotoxicity against tumor cells[2][4][6][7]. This combination aims to maximize antitumor activity while minimizing certain toxicities seen with other regimens.

Other names
FOLPIfolinic acid5-FU
02

Targets

SLC46A1 (Proton-coupled folate transporter)DHFR (Dihydrofolate reductase)DNATS (Thymidylate synthase)

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