PPI-2458

PPI-2458 is a synthetic derivative of fumagillin and a small molecule inhibitor with antineoplastic and cytotoxic properties. It irreversibly inhibits methionine aminopeptidase type 2 (MetAP2), an enzyme involved in cell proliferation and angiogenesis. By targeting MetAP2, PPI-2458 prevents abnormal cell growth and the formation of new blood vessels (angiogenesis), processes that are central to diseases such as cancer and rheumatoid arthritis. Compared to earlier fumagillin derivatives like TNP-470, PPI-2458 demonstrates improved pharmacokinetics and a better toxicity profile, particularly with reduced central nervous system toxicity. Preclinical studies have shown potent anti-proliferative effects on human fibroblast-like synoviocytes from rheumatoid arthritis patients as well as endothelial cells, along with disease-modifying activity in experimental models of arthritis. Clinical trials have included phase 1 studies in non-Hodgkin lymphoma[1][2][3][4][5][6].

Brand names

Metapro

Other names

431077-35-9