Brolucizumab (DLX1008) is a single-chain anti-VEGF-A antibody fragment with low picomolar affinity (KD=1.05 pM). Brolucizumab can be used for the research of cancer.
Brolucizumab (2683 nM) inhibits VEGF-A112-induced phosphorylation of VEGFR1 in U87MG human glioma cells and of VEGFR2 in ZHE-483-2 GMEC[1].
Brolucizumab (15 mg/kg; i.p. 5 days per week for 21 or 41 days) slows the growth of mSLK-KSHV xenograft tumors[2].Brolucizumab (5-50 mg/kg; i.p. once or twice daily for 28 days) delays in vivo tumor growth in U87MG glioma models[1].Brolucizumab (10 mg/kg; i.v.) shows a half-life of 5.4-7.8 minutes for the rapid decline phase and 1.4-1.9 hours for the slow decline phase in mice[2].
References:
[1]. Szabó E, et, al. Antitumor Activity of DLX1008, an Anti-VEGFA Antibody Fragment with Low Picomolar Affinity, in Human Glioma Models. J Pharmacol Exp Ther. 2018 May;365(2):422-429.
[2]. Eason AB, et, al. DLX1008 (brolucizumab), a single-chain anti-VEGF-A antibody fragment with low picomolar affinity, leads to tumor involution in an in vivo model of Kaposi Sarcoma. PLoS One. 2020 May 14;15(5):e0233116.