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5－乙炔尿嘧啶是5－氟尿嘧啶（5－FU）治疗活性的调节剂。它能不可逆地失活尿嘧啶还原酶，从而防止5－FU的降解，保存5－FU。临床上它能增加5－FU的抗肿瘤效果和5－FU的治疗指数，防止由于个体间尿嘧啶还原酶水平不同而引起的5－FU血浆水平的差异，并使5－FU口服代替静脉用药成为可能。
5-Acetylene Uracil is a modulator of 5-fluorouracil (5-FU) therapeutic activity. It irreversibly inactivates uracil reductase, thereby preventing the degradation of 5-FU and preserving 5-FU. Clinically it increases the anti-tumor effect of 5-FU and the therapeutic index of 5-FU, preventing differences in 5-FU plasma levels due to differences in uracil reductase levels between individuals and 5-FU instead of intravenous become possible.