Типирацил

Tipiracil (TPI) is a potent and competitive inhibitor of thymidine phosphorylase (TPase) with an IC₅₀ value of 35 nM for human placental TPase. It is selective for TPase over other pyrimidine-metabolizing enzymes (IC₅₀s = >1 mM for UPase, OPRTase, TK, and DPDase). TPI inhibits the phosphorolysis and degradation of trifluorothymidine , a cytotoxic nucleoside, in human breast and colon carcinoma tumor samples. Oral administration of TPI (12.5-50 mg/kg) enhances the anti-tumor activity of trifluorothymidine in a mouse AZ-521 stomach cancer xenograft model. Formulations containing TPI have been used for the treatment of metastatic colorectal cancer.

Tipiracil Hydrochloride serves as a treatment for metastatic colorectal cancer (mCRC). A thymidine phosphorylase inhibitor.

ChEBI: A hydrochloride obtained by combining tipiracil with one equivalent of hydrochloric acid. Used in combination with trifluridine, a nucleoside metabolic inhibitor, for treatment of advanced/relapsed unresectable colorectal cancer.