recombinant human angiostatin

Recombinant human angiostatin is a recombinant protein corresponding to the internal kringle domains (typically kringles 1–3 or 1–4) of human plasminogen that functions as a potent endogenous inhibitor of angiogenesis and tumor growth.[2][4][8][14] Produced in expression systems such as Pichia pastoris, it selectively targets proliferating microvascular endothelial cells, inhibiting their proliferation, migration, tube formation, and neovascularization, thereby suppressing primary and metastatic tumor growth in preclinical models.[2][4][8][14] Mechanistically, angiostatin binds to endothelial cell surface receptors including the catalytic subunit of ATP synthase and signaling hubs near focal adhesion kinase, disrupting extracellular ATP generation, integrin/FAK signaling, and downstream pathways that support angiogenesis within the tumor microenvironment.[4] In early-phase clinical trials, systemically administered recombinant human angiostatin as a continuous or twice-daily subcutaneous infusion showed acceptable safety, rapid clearance, and pharmacokinetics consistent with its short plasma half-life, and was explored alone or in combination with paclitaxel/carboplatin in advanced solid tumors such as non–small cell lung cancer.[4][11][12][13]

Other names

rhAngiostatinrecombinant human Angiostatin proteinrecombinant human angiostatin K1-3angiostatin K1-3human angiostatin