Canakinumab

Các tên gọi khác (2) :

ACZ-885
ACZ885

anti inflammatory agents, monoclonal antibodies

Thuốc Gốc

Biotech

CAS: 914613-48-2

ATC: L04AC08

CTHH: C₆₄₅₂H₉₉₅₈N₁₇₂₂O₂₀₁₀S₄₂

PTK: 145200.0000

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). Canakinumab binds to human IL-1β and neutralizes its inflammatory activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1alpha or IL-1 receptor antagonist (IL-1ra). Canakinumab is marketed under the brand name Ilaris and indicated for patients 4 years of age and older to treat Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS), which are both part of the Cryopyrin-Associated Periodic Syndromes (CAPS) as well as for patients 2 years of age and older to treat systemic juvenile idiopathic arthritis (SJIA). 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.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₆₄₅₂H₉₉₅₈N₁₇₂₂O₂₀₁₀S₄₂

Phân tử khối

145200.0000

Dược Lực Học : Novartis AG has developed canakinumab as a subcutaneous injection and 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), systemic juvenile idiopathic arthritis (SJIA), and possibly for other complex inflammatory diseases, such as rheumatoid arthritis, COPD disease and ocular diseases.

Cơ Chế Tác Dụng : 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). Canakinumab binds to human IL-1β and neutralizes its inflammatory activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1alpha or IL-1 receptor antagonist (IL-1ra). Canakinumab is marketed under the brand name Ilaris and indicated for patients 4 years of age and older to treat Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS), which are both part of the Cryopyrin-Associated Periodic Syndromes (CAPS) as well as for patients 2 years of age and older to treat systemic juvenile idiopathic arthritis (SJIA). 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. In inflammatory diseases involving Cryopyrin-Associated Periodic Syndromes (CAPS), interleukin-1 beta (IL-1β) is excessively activated and drives inflammation. The protein cryopyrin controls the activation of IL-1β, and mutations in cryopyrin's gene, NLRP-3, up-regulate IL-1β activation. Canakinumab is a human monoclonal anti-human IL-1β antibody of the IgG1/κ isotype. Canakinumab binds to human IL-1β and neutralizes its inflammatory activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1α or IL-1 receptor antagonist (IL-1ra).

Dược Động Học :

▧ 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 :
Canakinumab binds to plasma IL-1β, but plasma protein binding was not quantified.
▧ Metabolism :
The metabolism of canakinumab is not yet determined.
▧ Route of Elimination :
The route of elimination for canakinumab has not yet been determined.
▧ Half Life :
26 days
▧ Clearance :
* 0.174 L/day [typical CAPS patient weighing 70 kg]

Độc Tính : The most common adverse reactions involved the central nervous system (headache and vertigo), gastrointestinal system (diarrhea and nausea), neuromuscular and skeletal system (musculoskeletal pain), and respiratory system (rhinitis, nasopharyngitis and bronchitis). Influenza was also reported.

Chỉ Định : Used in patients 4 years of age and older to treat Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS), which are both part of the Cryopyrin-Associated Periodic Syndromes (CAPS) as well as for patients 2 years of age and older to treat systemic juvenile idiopathic arthritis (SJIA).

Tương Tác Thuốc :

Adalimumab Increases immunosuppressive effects and risk of infection.
Alefacept Increases immunosuppressive effects and risk of infection.
Anakinra results in increased immunosuppressive effects; increases the risk of infection.
Antithymocyte globulin results in increased immunosuppressive effects; increases the risk of infection.
Azathioprine results in increased immunosuppressive effects; increases the risk of infection.
Basiliximab results in increased immunosuppressive effects; increases the risk of infection.
Etanercept Combination should be avoided because Etanercept increase the toxic effects of canakinumab including neutropenia.
golimumab Avoid combination with canakinumab due to the increased chance of neutropenia and/or serious infection.
Infliximab Avoid combination due to increased risk of infection as anti-TNF agents enhance adverse effects of Canakinumab.
Natalizumab Avoid combination due to the increased risk of infection.
Pimecrolimus Avoid combination due the potential increase in immunosuppressant adverse effects.
Rilonacept results in increased immunosuppressive effects; increases the risk of infection.
Tofacitinib Avoid combination with tofacitinib and other potent immunosuppressants due to potential enhancement of immunosuppressant effects.

Liều Lượng & Cách Dùng : Injection, powder, for solution - Subcutaneous - 150mg/mL

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : Novartis

Sản phẩm biệt dược : Ilaris

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB06168

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D09315

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0078-0582-61

Wikipedia

http://en.wikipedia.org/wiki/Canakinumab

RxList

http://www.rxlist.com/ilaris-drug.htm

Drugs.com

http://www.drugs.com/mtm/canakinumab.html

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