Acivicin

Acivicin is an inhibitor of gamma-glutamyl transferase. It is fermented product of Streptomyces sviceus and has promise as an antineoplastic agent.^[1] It interferes with glutamate metabolism and inhibits glutamate dependent synthesis of enzymes, and is thereby potentially helpful in treatment of solid tumors.

Research[edit]

In vivo studies have showed that Acivicin at a concentration of 5 µM Acivicin inhibited by 78% the growth of human pancreaticcarcinoma cells (MIA PaCa-2) after 72 hours in continuous culture. It was also found that acivicin at a concentration of 450 µM irreversibly inactivated MIA PaCa-2 γ-glutamyl transpeptidase (10 nmol/min/10⁶ cells) with an inactivation half-life of 80 minutes.^[1]

Phase I studies[edit]

Phase I dose escalating studies conducted in 23 cancer patients administered acivicin with a concomitant 96-h i.v. infusion of a mixture of 16 amino acids showed reversible, dose-limiting CNS toxicity, characterized by lethargy, confusion and decreased mental status.