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药品详细

Canakinumab (Canakinumab )

化学结构式图
没有图片
中文名
Canakinumab
英文名
Canakinumab
分子式
Not Available
化学名
分子量
CAS号
914613-48-2
ATC分类
L04A 未知
药物类型
biotech
阶段
商品名
Ilaris (Novartis);
同义名
ACZ-885;ACZ885;
基本介绍

Canakinumab is a recombinant, human anti-human-IL-1β monoclonal antibody that belongs to the IgG1/κ isotype subclass. It is expressed in a murine Sp2/0-Ag14 cell line and comprised of two 447- (or 448-) residue heavy chains and two 214-residue light chains, with a molecular mass of 145157 Daltons when deglycosylated. Both heavy chains of canakinumab contain oligosaccharide chains linked to the protein backbone at asparagine 298 (Asn 298). The biological activity of canakinumab is measured by comparing its inhibition of IL-1β-dependent expression of the reporter gene luciferase to that of a canakinumab internal reference standard, using a stably transfected cell line.

生产厂家
  • Novartis pharmaceuticals corp
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Church LD, McDermott MF: Canakinumab, a fully-human mAb against IL-1beta for the potential treatment of inflammatory disorders. Curr Opin Mol Ther. 2009 Feb;11(1):81-9. Pubmed
  2. IMGT Link
  3. Lachmann HJ, Kone-Paut I, Kuemmerle-Deschner JB, Leslie KS, Hachulla E, Quartier P, Gitton X, Widmer A, Patel N, Hawkins PN: Use of canakinumab in the cryopyrin-associated periodic syndrome. N Engl J Med. 2009 Jun 4;360(23):2416-25. Pubmed
剂型
Form Route Strength
Injection, powder, for solution Subcutaneous 150mg/mL
规格
化合物类型
Type biotech
Classes Not Available
Substructures Not Available
适应症
Diabetes 糖尿病;
药理
Indication Investigated for use/treatment in rheumatoid arthritis, juvenile rheumatoid arthritis, inflammatory disorders (unspecified), and autoimmune diseases.
Pharmacodynamics Novartis AG is developing canakinumab, an intravenously or subcutaneously infused, fully human mAb that neutralizes the bioactivity of human IL-1beta, which is involved in several inflammatory disorders. Canakinumab has promising clinical safety and pharmacokinetic properties, and demonstrated potential for the treatment of cryopyrin-associated periodic syndromes (CAPS) and possibly for other complex inflammatory diseases, such as rheumatoid arthritis, systemic-onset juvenile idiopathic arthritis (SoJIA), COPD disease and ocular diseases. Early clinical trials have established the administration of canakinumab every 2 weeks to be safe and effective, offering a considerable advantage over the existing treatment with the human IL-1 receptor antagonist anakinra, which must be injected daily and which is often poorly tolerated by patients.
Mechanism of action Canakinumab is a human monoclonal anti-human IL-1β antibody of the IgG1/κ isotype. Canakinumab binds to human IL-1β and neutralizes its activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1α or IL-1 receptor antagonist (IL-1ra).
Absorption The absolute bioavailability of subcutaneous canakinumab is estimated to be 70%.
Volume of distribution
  • 6.01 L [typical CAPS patient weighing 70 kg]
Protein binding Not Available
Metabolism
Route of elimination Not Available
Half life 26 days
Clearance
  • 0.174 L/day [typical CAPS patient weighing 70 kg]
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State liquid
Melting point Not Available
Experimental Properties Not Available
药物相互作用
食物相互作用
Not Available

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