Tipiracil is a thymidine phosphorylase inhibitor used as an adjunct treatment of adult patients with certain types of gastric or colorectal malignancies. It is used in combination with trifluridine, in a ratio of 1:0.5, to form TAS-102.
- Mechanism
- Curator reviewed · 3 references
Tipiracil is a thymidine phosphorylase inhibitor. Its function prevents the breakdownof the active component of trifluridine, thus increasing the bioavailability of trifluridine and boosting its systemic presence. In addition, it is reported that thymidine phosphorylase is an angiogenic factor usually overexpressed in solid tumors. There is a direct association of thymidine phosphorylase with a poor prognosis; where the tumors with an elevated expression of this enzyme tend to present an increased angiogenesis and ergo, be more malignant. Therefore, it has been suggested that tipiracil presents an aditional function by downregulating tumoral angiogenesis.
- Primary indication
- Tipiracil is also available as a combination product with Trifluridine, which is indicated either alone or in combination with bevacizumab for the treatment of adult patients with metastatic colorectal cancer who have been previously treated...Curator reviewed · 3 structured indications
- Formula / weight
- C9H11ClN4O2 · 242.662 g/mol (avg)
- First approval
- Canada, 2018 · United States, 2015 · European Union, 2016
- Brand names
Resolves to
QQHMKNYGKVVGCZ-UHFFFAOYSA-NSMILESClC1=C(CN2CCCC2=N)NC(=O)NC1=OWhat you can answer from here — as of September 13, 2026
Which drugs share a target with Tipiracil, and which of those have an active Phase 3 trial?
Create a free account or log in to explore the full data card.
Create Account