Rilonacept

Các tên gọi khác (2) :

Arcalyst
interleukin-1 (IL-1) trap

Thuốc giảm miễn dịch

Thuốc Gốc

Biotech

CAS: 501081-76-1

CTHH: C₉₀₃₀H₁₃₉₃₂N₂₄₀₀O₂₆₇₀S₇₄

PTK: 251 kDa

Rilonacept is a dimeric fusion protein consisting of portions of IL-1R and the IL-1R accessory protein linked to the Fc portion of immunoglobulin G1. Rilonacept functions as an interleukin 1 inhibitor and is used in the treatment of CAPS, also known as cryopyrin-associated periodic syndromes, including familial cold auto-inflammatory syndrome (FCAS) and Muckle-Wells Syndrome (MWS), in adults and children greater than 12 years old.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₉₀₃₀H₁₃₉₃₂N₂₄₀₀O₂₆₇₀S₇₄

Phân tử khối

251 kDa

Dược Lực Học : Treatment with Rilonacept resulted in decreased levels of mean C-Reactive Protein (CRP) and Serum Amyloid A (SAA). Higher levels of CRP and SAA are associated with inflammatory disease activity found in patients with Cryopyrin-Associated Periodic Syndromes.

Cơ Chế Tác Dụng : Rilonacept is a dimeric fusion protein consisting of portions of IL-1R and the IL-1R accessory protein linked to the Fc portion of immunoglobulin G1. Rilonacept functions as an interleukin 1 inhibitor and is used in the treatment of CAPS, also known as cryopyrin-associated periodic syndromes, including familial cold auto-inflammatory syndrome (FCAS) and Muckle-Wells Syndrome (MWS), in adults and children greater than 12 years old. CAPS refer to rare genetic syndromes generally caused by mutations in the NLRP-3 [Nucleotide-binding domain, leucine rich family (NLR), pyrin domain containing 3] gene (also known as Cold-Induced Auto-inflammatory Syndtrome-1 [CIAS1]). CAPS disorders are inherited in an autosomal dominant pattern with male and female offspring equally affected. Fever, urticaria-like rash, arthralgia, myalgia, fatigue, and conjunctivitis are features common to all disorders. In most cases, inflammation in CAPS is associated with mutations in the NLRP-3 gene which encodes the protein cryopyrin, an important component of the inflammasome. Cryopyrin regulates the protease caspase-1 and controls the activation of interleukin-1 beta (IL-1β). Mutations in NLRP-3 result in an overactive inflammasome resulting in excessive release of activated IL-1β that drives inflammation. Rilonacept blocks IL-1β signaling by acting as a soluble decoy receptor that binds IL-1β and prevents its interaction with cell surface receptors. Rilonacept also binds IL-1α and IL-1 receptor antagonist (IL-1ra) with reduced affinity. By binding IL-1, rilonacept prevents the activation of IL-1 receptors, thus reducing inflammatory responses and other effects related to an excess of IL-1.

Dược Động Học :

▧ Half Life :
8.6 days

Chỉ Định : Rilonacept is currently used in the treatment of cryopyrin-associated periodic syndrome. In May 2012, an advisory panel for the FDA voted 11-0 against the use of Rilonacept for the treatment of gout.

Tương Tác Thuốc :

Adalimumab results in increased immunosuppressive effects; increases the risk of infection.
Alefacept results in increased immunosuppressive effects; increases the 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.
Belatacept Belatacept decreases immunosuppressive effects while rilonacept increases immunosuppressive effects. Potential risk of infection although the effect of interaction is not known; use caution and monitor closely if using both.
Belatacept Belatacept decreases immunosuppressive effects while rilonacept increases immunosuppressive effects. Potential risk of infection although the effect of interaction is not known; use caution and monitor closely if using both.
Belatacept Belatacept decreases immunosuppressive effects while rilonacept increases immunosuppressive effects. Potential risk of infection although the effect of interaction is not known; use caution and monitor closely if using both.
Canakinumab results in increased immunosuppressive effects; increases the risk of infection.
Cyclosporine results in increased immunosuppressive effects; increases the risk of infection.
Daclizumab results in increased immunosuppressive effects; increases the risk of infection.
Denileukin diftitox decreases effects of toxoids by pharmacodynamic antagonism.
Denosumab Use caution with patients on concomitant immunosuppressants or those with compromised immune systems; increased risk of serious infection.
Efalizumab results in increased immunosuppressive effects; increases the risk of infection.
Etanercept results in increased immunosuppressive effects; increases the risk of infection.
Everolimus results in increased immunosuppressive effects; increases the risk of infection.
Glatiramer Acetate results in increased immunosuppressive effects; increases the risk of infection.
golimumab results in increased immunosuppressive effects; increases the risk of infection.
golimumab Avoid combination due to the enhancement of rilonacept associated side effects.
Hydroxychloroquine results in increased immunosuppressive effects; increases the risk of infection.
Infliximab Anti-TNF alfa agents enhance adverse effects of rilonacept thus combination should be avoided.
Leflunomide results in increased immunosuppressive effects; increases the risk of infection.
Methotrexate Rilonacept and methotrexate both increase immunosuppressive effects; combination may increase risk of myelosuppression.
Muromonab results in increased immunosuppressive effects; increases the risk of infection.
Mycophenolate mofetil results in increased immunosuppressive effects; increases the risk of infection.
Sipuleucel-T decreases effectiveness of APC8015 by pharmacodynamic antagonism.
Sirolimus results in increased immunosuppressive effects; increases the risk of infection.
Tacrolimus results in increased immunosuppressive effects; increases the risk of infection.
Temsirolimus results in increased immunosuppressive effects; increases the risk of infection.
Thalidomide Thalidomide may increase the adverse effects of Rilonacept. Increased risk of serious infection. Concomitant therapy should be avoided.
Tocilizumab results in increased immunosuppressive effects; increases the risk of infection.
Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.

Liều Lượng & Cách Dùng : Injection, powder, lyophilized, for solution - Subcutaneous - 220mg

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : Regeneron

Sản phẩm biệt dược : Arcalyst

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB06372

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D06635

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/61755-001-01

Wikipedia

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

RxList

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

Drugs.com

http://www.drugs.com/ppa/rilonacept.html

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