Products
Tipiracil is commercially available in the form of film-coated tablets in fixed combination with trifluridine (Lonsurf). The drug was approved in the United States in 2015, in the EU in 2016, and in many countries in 2017.
Structure and properties
Tipiracil (C9H12Cl2N4O2, Mr = 279.1 g/mol) is present in the drug as tipiracil hydrochloride. It exists as a white crystalline powder and is soluble in water.
Effects
Tipiracil (ATC L01BC59) is combined with the antineoplastic and antiproliferative nucleoside analogue trifluridine because the latter is rapidly degraded by thymidine phosphorylase (TPase) and undergoes high first-pass metabolism. Tipiracil is an inhibitor of TPase and leads to a relevant increase in bioavailability. Trifluridine is incorporated into DNA, interferes with DNA synthesis, and inhibits cell proliferation.
Indications
Metastatic colorectal carcinoma in combination with trifluridine.
