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Frovocimab

CAS No. : 1643672⁻⁷0-1

MCE 国际站：Frovocimab

产品活性：Frovocimab (LY 3015014) 是一种人源化 IgG4 单克隆抗体 (mAb)，可中和 PCSK9。Frovocimab 抑制 PCSK9 与 LDL 受体 (LDLR) 的结合，同时使结合的完整 PCSK9 进行正常的蛋白水解切割。

研究领域：Metabolic Enzyme/Protease

作用靶点：Ser/Thr Protease

In Vitro: Frovocimab (LY 3015014) binds to intact but not truncated PCSK9. The selective binding of Frovocimab to intact PCSK9 is related to its binding epitope, the linear sequence of amino acids 160-181 of the catalytic domain of human PCSK9, which is absent in truncated PCSK9. Frovocimab inhibits PCSK9 binding to LDLR while permitting the normal proteolytic cleavage of the bound intact PCSK9. Additionally, upon cleavage, truncated inactive PCSK9 is released from Frovocimab.

In Vivo: Frovocimab (LY 3015014; 10 mg/kg; i.v; once) causes significant PCSK9 accumulation, its duration of LDL lowering is reduced, ａnd its clearance (CL) from serum is accelerated in mice expressing a noncleavable variant of human PCSK9.
Frovocimab (LY 3015014; 5 mg/kg; i.v; once) decreases LDL cholesterol in monkeys and, unlike other PCSK9 mAbs, does not cause an accumulation of intact PCSK9 in serum.

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