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Picoplatin + 5-fluorouracil + leucovorin
- Development stage
- Phase 2
- Lead developer
- Poniard Pharmaceuticals
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed 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
DNADHFR (Dihydrofolate reductase)SLC46A1 (Proton-coupled folate transporter)TS (Thymidylate synthase)
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