ANV221

ANV221 is a first-in-class small molecule inhibitor targeting dolichyl-phosphate N-acetylglucosaminephosphotransferase 1 (DPAGT1), an enzyme that catalyzes the initial step in the N-linked protein glycosylation pathway. By inhibiting DPAGT1, ANV221 disrupts aberrant glycoprotein expression on cancer cell surfaces—a mechanism implicated in tumor growth and drug resistance, particularly in HER2-positive and triple-negative breast cancers as well as pancreatic cancer. Preclinical studies have demonstrated that DPAGT1 inhibition can re-sensitize tumors to anti-HER2 therapies and suppress metastasis. The compound has received orphan drug designation from the FDA for pancreatic cancer and is being developed by Anviron based on technology licensed from the University of Tennessee Research Foundation. As of early 2025, its highest development phase is preclinical[1][4][5].