sparfosic acid

Sparfosic acid (PALA) is a small molecule DNA antimetabolite and a potent inhibitor of aspartate transcarbamoyl transferase, the enzyme that catalyzes the second step in de novo pyrimidine biosynthesis. By inhibiting this enzyme, sparfosic acid blocks pyrimidine synthesis, leading to cytotoxic effects in vitro and potentiation of other cytotoxic drugs such as 5-fluorouracil. It acts as a stable transition state analogue for the reaction catalyzed by aspartate transcarbamoyl transferase. While it has demonstrated anti-tumor activity in preclinical studies, clinical development for cancer and hepatitis B was discontinued due to lack of selective antitumor activity when used alone[1][3][4][5][7].

Other names

sparfosic acidácido esparfósicoAcidum sparfosicumN-(phosphonacetyl)-L-aspartic acidN-(phosphonoacetyl)-L-aspartic acidphosphonoacetyl-L-aspartic acid