golimumab

antipsoriatic agents, monoclonal antibodies, tnf inhibitor

Thuốc Gốc

Biotech

CAS: 476181-74-5

ATC: L04AB06

CTHH: C₆₅₃₀H₁₀₀₆₈N₁₇₅₂O₂₀₂₆S₄₄

PTK: 146943.1937 daltons

Golimumab is a human IgG1қ monoclonal antibody derived from immunizing genetically engineered mice with human TNFα. Golimumab binds and inhibits soluble and transmembrane human TNFα. Increased TNFα is associated with chronic inflammation. Thus golimumab is indicated for use in adults (i) as an adjunct to methotrexate treatment in patients with moderate to severe active rheumatoid arthritis (RA), (ii) alone or as an adjunct to methotrexate treatment in patients with active psoriatic arthritis (PsA), (iii) as a single agent in patients with active ankylosing spondylitis (AS), and (iv) as a single agent in patients with moderate to severe ulcerative colitis (UC) who require chronic steroids or have experienced intolerance or only a partial response to previous medications. In the U.S. and Canada, golimumab is marketed under the brand name Simponi®. The FDA label includes a black box warning of serious infections and malignancy. Additionally in children and adolescents taking golimumab, there have been lymphoma and other malignancies observed.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₆₅₃₀H₁₀₀₆₈N₁₇₅₂O₂₀₂₆S₄₄

Phân tử khối

146943.1937 daltons

Dược Lực Học : Golimumab inhibits the activity of the cytokine, tumor necrosis factor alpha (TNFα). In areas such as the joints and blood, increased TNFα is associated with chronic inflammation seen in patients with rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis. Thus golimumab decreases the inflammation in these conditions. Concerning ulcerative colitis, the physiological effects of golimumab has yet to be determined.

Cơ Chế Tác Dụng : Golimumab is a human IgG1қ monoclonal antibody derived from immunizing genetically engineered mice with human TNFα. Golimumab binds and inhibits soluble and transmembrane human TNFα. Increased TNFα is associated with chronic inflammation. Thus golimumab is indicated for use in adults (i) as an adjunct to methotrexate treatment in patients with moderate to severe active rheumatoid arthritis (RA), (ii) alone or as an adjunct to methotrexate treatment in patients with active psoriatic arthritis (PsA), (iii) as a single agent in patients with active ankylosing spondylitis (AS), and (iv) as a single agent in patients with moderate to severe ulcerative colitis (UC) who require chronic steroids or have experienced intolerance or only a partial response to previous medications. In the U.S. and Canada, golimumab is marketed under the brand name Simponi®. The FDA label includes a black box warning of serious infections and malignancy. Additionally in children and adolescents taking golimumab, there have been lymphoma and other malignancies observed. As a human monoclonal antibody, golimumab binds and inhibits soluble and transmembrane human TNFα. Inhibition of TNFα prevents it binding to its receptors, which prevents both leukocyte infiltration through prevention of cell adhesion proteins such as E-selectin, ICAM-1 and VCAM-1, and pro-inflammatory cytokine secretion such as IL-6, IL-8, G-CSF and GM-CSF in vitro. Consequently, in patients with chronic inflammatory conditions, decreases in ICAM-1 and IL-6 as well as C-reactive protein (CRP), matrix metalloproteinase 3 (MMP-3), and vascular endothelial growth factor (VEGF) were observed.

Dược Động Học :

▧ Absorption :
After subcutaneous administration, golimumab can achieve maximum serum concentrations in 2 to 6 days and has an approximate bioavailability of 53%. In healthy volunteers, the maximum average concentration reached was 3.2 ± 1.4 μg/mL.
▧ Volume of Distribution :
After IV administration, golimumab has a volume of distribution of about 58 to 126 mL/kg. This means that golimumab stays mostly in the circulatory system.
▧ Protein binding :
Plasma protein binding was not quantified.
▧ Metabolism :
The metabolism of golimumab has yet to be determined.
▧ Route of Elimination :
The route of elimination for golimumab has yet to be determined.
▧ Half Life :
Golimumab has a long half-life of about 2 weeks.
▧ Clearance :
After one IV dose of golimumab, the systemic clearance was about 4.9 to 6.7 mL/day/kg.

Độc Tính : The FDA label includes a black box warning of serious infections and malignancy. Specifically there have been hospitalizations or death from infections such as bacterial sepsis, tuberculosis (TB), and invasive fungal (histoplasmosis) and other opportunistic infections. Additionally in children and adolescents taking golimumab, there have been lymphoma and other malignancies observed.

Chỉ Định : Used in adults (i) as an adjunct to methotrexate treatment in patients with moderate to severe active rheumatoid arthritis (RA), (ii) alone or as an adjunct to methotrexate treatment in patients with active psoriatic arthritis (PsA), (iii) as a single agent in patients with active ankylosing spondylitis (AS), and (iv) as a single agent in patients with moderate to severe ulcerative colitis (UC) who require chronic steroids or have experienced intolerance or only a partial response to previous medications.

Tương Tác Thuốc :

Abatacept Avoid combination with abatacept due to the increased chance of serious infection.
Anakinra Avoid combination with anakinra due to the increased chance of serious infection.
Belimumab Avoid combination with belimumab due to the increased chance of belimumab associated side effects.
Canakinumab Avoid combination with canakinumab due to the increased chance of neutropenia and/or serious infection.
Certolizumab pegol Avoid combination due to the potential increased immunosuppression of Certolizumab Pegol.
Infliximab Avoid combination with infliximab due to the potential increased immunosuppression of infliximab.
Natalizumab Avoid combination due to the increased chance of infection.
Pimecrolimus Avoid combination due to enhancement of side effects from immunosuppressants.
Rilonacept results in increased immunosuppressive effects; increases the risk of infection.
Rilonacept Avoid combination due to the enhancement of rilonacept associated side effects.
Tacrolimus Avoid combination due to the enhancement of side effects from immunosuppressants.
Tocilizumab Avoid combination due to the enhanced immunosuppression by TNF blockers.
Tofacitinib Golimumab, and other anti-TNF immunosuppressants, when used in combination with tofacitinib, may increase the serum concentration of tofacitinib, and increase tofacitinib associated side effects and immunosuppresion. It is recommended to avoid concurrent therapy.

Liều Lượng & Cách Dùng : Injection, solution - Subcutaneous - 100 mg/1 mL
Injection, solution - Subcutaneous - 50 mg/0.5 mL

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : Centocor Ortho Biotec

Sản phẩm biệt dược : Simponi

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB06674

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D04358

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/57894-071-01

Wikipedia

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

RxList

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

Drugs.com

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

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