1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
  3. Frovocimab

Frovocimab  (Synonyms: LY 3015014)

目录号: HY-P99626

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。

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Frovocimab Chemical Structure

Frovocimab Chemical Structure

CAS No. : 1643672-70-1

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生物活性

Frovocimab (LY 3015014) is a humanized IgG4 monoclonal antibody (mAb) that neutralizes PCSK9. Frovocimab inhibits PCSK9 binding to LDL receptor (LDLR) while permitting the normal proteolytic cleavage of the bound intact PCSK9[1].

体外研究
(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6NTac mice injected with vector containing the NC R215A/R218A variant[1]
Dosage: 10 mg/kg
Administration: i.v; once
Result: Caused significant PCSK9 accumulation.
Animal Model: Cynomolgus monkeys[1]
Dosage: 5 mg/kg
Administration: i.v; once
Result: Decreased LDL cholesterol in monkeys.
Clinical Trial
CAS 号
中文名称

弗洛西单抗

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