Brolucizumab

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[1][2].

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

Brolucizumab (2683 nM) 抑制 VEGF-A112 诱导的 U87MG 人神经胶质瘤细胞中的 VEGFR1 磷酸化和 ZHE-483-2 GMEC 中的 VEGFR2 磷酸化[1]。

Brolucizumab (15 mg/kg; i.p. 5 days per week for 21 or 41 days) 可减缓 mSLK-KSHV 异种移植肿瘤的生长[2]。 Brolucizumab (5-50 mg/kg; i.p. once or twice daily for 28 days) 在 U87MG 神经胶质瘤模型中延迟体内肿瘤生长[1]。 Brolucizumab (10 mg/kg; i.v.) 在小鼠中显示出快速衰退期的半衰期为 5.4-7.8 分钟，缓慢衰退期的半衰期为 1.4-1.9 小时[2]。 Animal Model: NSG mice were subcutaneously injected with mSLK-KSHV cell suspension[2] Dosage: 15 mg/kg Administration: I.p. 5 days per week for 21 or 41 days Result: Significantly lowed tumor growth there was no difference in survival between experimental and combined control groups.

[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.