Drug intelligence / Profile preview

leucovorin + 5-fluorouracil + cisplatin

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

Overview

The combination of leucovorin, 5-fluorouracil (5-FU), and cisplatin is a chemotherapy regimen used primarily for treating various types of cancer, particularly head and neck cancer and gastric cancer. This three-drug combination has shown significant activity in both newly diagnosed and recurrent cases. ## Mechanism of Action This regimen combines three drugs with complementary mechanisms: - **Leucovorin** (folinic acid) is not directly cytotoxic but enhances the efficacy of 5-fluorouracil by stabilizing the binding of 5-FU to its target enzyme, thereby increasing its cytotoxic effects. - **5-Fluorouracil (5-FU)** is a pyrimidine analog that inhibits nucleic acid synthesis in rapidly dividing cells, particularly cancer cells. - **Cisplatin** is a platinum-based compound that forms DNA crosslinks, preventing DNA replication and transcription, ultimately leading to cell death. ## Clinical Applications This combination has demonstrated efficacy in: - **Head and Neck Cancer**: Particularly effective in recurrent disease, including in patients who previously received cisplatin and 5-FU as induction chemotherapy. - **Gastric Cancer**: Used in advanced gastric cancer with promising response rates. ## Dosing Regimen The typical dosing regimen involves: - Cisplatin: 80-100 mg/m² on day 1 - 5-FU: 600-1000 mg/m²/day as continuous infusion for 5 days - Leucovorin: 20-50 mg/m² administered at various intervals throughout treatment The maximally tolerated dose of 5-FU in combination with leucovorin and cisplatin has been established at 800 mg/m²/day in some studies. ## Toxicity Profile Common adverse effects include: - Mucositis (particularly in previously irradiated fields) - Myelosuppression - Neutropenia - Gastrointestinal toxicities The dose-limiting toxicity is typically mucositis in previously irradiated sites.

Other names
5-fluorouracil + leucovorin + cisplatincisplatin + 5-fluorouracil + leucovorin
02

Targets

TS (Thymidylate synthase)DNA

Beyond the preview

Go deeper on leucovorin + 5-fluorouracil + cisplatin.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Full profile access

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Full profile access

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Full profile access

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Full profile access

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Full profile access

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Full profile access

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on leucovorin + 5-fluorouracil + cisplatin.

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call