tas-103

TAS-103 is a **novel small molecule anticancer agent** that acts as a dual inhibitor of **topoisomerase I and II**[1][2][3][5][7]. It is a quinoline derivative with the chemical name 6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)quinolin-7-one dihydrochloride[1][7]. TAS-103 promotes DNA cleavage by both topoisomerase I and II, but its principal cytotoxic activity results from inhibition of topoisomerase II-mediated DNA religation, leading to accumulation of DNA breaks and cell death[3][5]. It intercalates into DNA and has broad-spectrum, growth-inhibitory activity against various tumor cell lines, including those with multidrug resistance[2]. Preclinical and clinical studies have shown antitumor activity in models of small-cell lung cancer and other solid tumors[1][4][6]. The drug is metabolized to TAS-103-glucuronide predominantly by the enzyme UGT1A1[4]. TAS-103 is administered intravenously in clinical trials[4][6].

Other names

TAS-103 dihydrochlorideTAS103 dihydrochlorideTAS 103 dihydrochloride