tipiracil

Ligand id: 8696

Name: tipiracil

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 3
Rotatable bonds 2
Topological polar surface area 85.29
Molecular weight 242.06
XLogP 0.45
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Tipracil is a component of the anticancer therapeutic Lonsurf® (code-named TAS-102) [3], which is approved in Japan for the treatment of metastatic/unresectable colorectal cancer. The other component of TAS-102 is trifluridine [2]. In addition, TAS-102 is being assessed in Phase III clinical trial for metastatic gastric cancer (NCT02500043).
Mechanism Of Action and Pharmacodynamic Effects
By reducing the breakdown of trifluridine, tipiracil improves its antineoplastic activity by increasing its bioavailability.
Thymidine phosphorylase is also reported to be involved in angiogenesis in human gastric cancer [1], suggesting that tipracil may have dual effects when used in combination antineoplastic therapies such as TAS-102.