Peringatan Keamanan

In clinical trials done in patients with rheumatoid arthritis (RA) and neonatal-onset multisystem inflammatory disease (NOMID) treated with anakinra, no cases of overdose were reported.L35415 Sepsis trials were performed using mean calculated doses up to 35 times the ones given to patients with RA over 72 hours. Anakinra did not produce any serious toxicities at this dose range.L35415

In preclinical studies done in rats, where up to 100 mg/kg/day were administered either intravenously or subcutaneously over 14 days, and given at doses of 2, 20 or 200 mg/kg/day subcutaneously for 6 months, anakinra was well tolerated. Toxicity ranged from mild to moderate, and dose-related inflammation, hemorrhage and fibrosis at the injection site were detected in both rats and monkeys.L41634 The no observable adverse effect level (NOAEL) in rats receiving a daily subcutaneous dose of anakinra for 6 months was 2 mg/kg/day. In rats receiving a daily intravenous injection of anakinra for 14 or 28 days, the NOAEL was 30 mg/kg/day. The NOAEL in Rhesus monkeys was 150 mg/kg/day when anakinra was administered via intravenous infusion for 7 days, 10-30 mg/kg/day when administered via intravenous bolus injection for 14 days and 5 mg/kg/day when administered subcutaneously for 14 days.L41634 Anakinra had no effects on fertility and reproductive capacity in both male and female rats given the maximum recommended human dose.L35415

Anakinra

DB00026

biotech approved investigational

Deskripsi

Anakinra is a recombinant human interleukin-1 (IL-1) receptor antagonist (IL-1Ra) composed of 153 amino acid residues. Unlike native human IL-1Ra, anakinra has an additional methionine residue at the amino terminus. This drug binds to the IL-1 receptor, competing with and inhibiting the activity of IL-1 alpha and beta.L35415 Anakinra is indicated for the management of rheumatoid arthritis (RA) in patients 18 years of age or older who have failed one or more disease-modifying antirheumatic drugs (DMARDs), as well as the treatment of neonatal-onset multisystem inflammatory disease (NOMID) and deficiency of interleukin-1 receptor antagonist (DIRA).L35415 Since IL-1 has an important role in inflammation and immunological responses, anakinra is also used for the off-label treatment of inflammatory diseases.A247000

Anakinra is produced using the E. Coli bacterial expression system. On November 14, 2001, it was approved by the FDA for the treatment of rheumatoid arthritis. It was later approved for the treatment of NOMID and DIRA on December 21, 2012, and December 18, 2020, respectively. A few studies have evaluated the use of anakinra for the treatment of coronavirus disease 2019 (COVID-19).A247265 On November 8, 2022, the FDA issued an emergency use authorization (EUA) of anakinra for the treatment of COVID-19 in hospitalized patients who are at risk of progressing to severe respiratory failure.L43932

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) In patients with rheumatoid arthritis (RA), the terminal half-life of anakinra ranged from 4 to 6 hours. In patients with neonatal-onset multisystem inflammatory disease (NOMID), the median half-life of anakinra was 5.7 h (range=3.1-28.2, n=12).[L35415]
Volume Distribusi In adult subjects with rheumatoid arthritis (RA) treated with anakinra (n=35), the volume of distribution averaged 18.5 L.[L41628]
Klirens (Clearance) In patients with rheumatoid arthritis (RA), the clearance of anakinra was relatively consistent for different dose levels.[L41628] Clearance is variable and increases with increasing creatinine clearance and body weight. However, gender and age were not significant factors.[L35415] In patients with mild (creatinine clearance 50-80 mL/min) and moderate (creatinine clearance 30-49 mL/min) renal impairment, the mean plasma clearance of anakinra was 16% and 50% lower, respectively. In patients with severe renal insufficiency and end-stage renal disease (creatinine clearance < 30 mL/min), the mean plasma clearance of anakinra was 70% and 75% lower, respectively.[L35415]

Absorpsi

The bioavailability of anakinra is 95% in healthy subjects administered a 70 mg subcutaneous bolus injection. In patients with rheumatoid arthritis (RA) administered a subcutaneous dose of anakinra, the maximum plasma concentration was detected 3 to 7 hours later. No unexpected accumulation was observed in RA patients receiving this drug for up to 24 weeks.L35415 In a phase 1, single-center, randomized, sequential single-dose escalation PK study done in patients with stable RA, AUC increased in a relatively dose-proportional manner. While the tmax and Cmax fluctuated across the different doses provided to these patients (range from 0.5 to 6 mg/kg), clearance appeared to be consistent.L41628 In patients with neonatal-onset multisystem inflammatory disease (NOMID) treated with a subcutaneous dose of 3 mg/kg of anakinra for an average of 3.5 years (n=16), Cmax was 3628 ng/mL and C24h was 203 ng/mL.L35415

Metabolisme

As a protein-based therapy, anakinra is expected to be metabolized by proteases throughout the body.

Rute Eliminasi

Anakinra is mostly excreted by the kidney; therefore, the risk of toxic reactions may increase in patients with impaired renal function.L35415

Interaksi Obat

1028 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Anakinra.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Anakinra.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Anakinra.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Anakinra.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Anakinra.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Anakinra is combined with Interferon gamma-1b.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Anakinra is combined with Interferon alfa-2a.
Aldesleukin The risk or severity of adverse effects can be increased when Anakinra is combined with Aldesleukin.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Anakinra is combined with Gemtuzumab ozogamicin.
Pegaspargase The risk or severity of adverse effects can be increased when Anakinra is combined with Pegaspargase.
Interferon beta-1b The risk or severity of adverse effects can be increased when Anakinra is combined with Interferon beta-1b.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Anakinra is combined with Interferon alfacon-1.
Rituximab The risk or severity of adverse effects can be increased when Anakinra is combined with Rituximab.
Basiliximab The risk or severity of adverse effects can be increased when Anakinra is combined with Basiliximab.
Muromonab The risk or severity of adverse effects can be increased when Anakinra is combined with Muromonab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Anakinra is combined with Ibritumomab tiuxetan.
Tositumomab The risk or severity of adverse effects can be increased when Anakinra is combined with Tositumomab.
Alemtuzumab The risk or severity of adverse effects can be increased when Anakinra is combined with Alemtuzumab.
Alefacept The risk or severity of adverse effects can be increased when Anakinra is combined with Alefacept.
Efalizumab The risk or severity of adverse effects can be increased when Anakinra is combined with Efalizumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Anakinra is combined with Antithymocyte immunoglobulin (rabbit).
Interferon alfa-2b The risk or severity of adverse effects can be increased when Anakinra is combined with Interferon alfa-2b.
Daclizumab The risk or severity of adverse effects can be increased when Anakinra is combined with Daclizumab.
Phenylalanine The risk or severity of adverse effects can be increased when Anakinra is combined with Phenylalanine.
Cladribine Anakinra may increase the immunosuppressive activities of Cladribine.
Amsacrine The risk or severity of adverse effects can be increased when Anakinra is combined with Amsacrine.
Bleomycin The risk or severity of adverse effects can be increased when Anakinra is combined with Bleomycin.
Chlorambucil The risk or severity of adverse effects can be increased when Anakinra is combined with Chlorambucil.
Raltitrexed The risk or severity of adverse effects can be increased when Anakinra is combined with Raltitrexed.
Mitomycin The risk or severity of adverse effects can be increased when Anakinra is combined with Mitomycin.
Floxuridine The risk or severity of adverse effects can be increased when Anakinra is combined with Floxuridine.
Tioguanine The risk or severity of adverse effects can be increased when Anakinra is combined with Tioguanine.
Dexrazoxane The risk or severity of adverse effects can be increased when Anakinra is combined with Dexrazoxane.
Streptozocin The risk or severity of adverse effects can be increased when Anakinra is combined with Streptozocin.
Trifluridine The risk or severity of adverse effects can be increased when Anakinra is combined with Trifluridine.
Gemcitabine The risk or severity of adverse effects can be increased when Anakinra is combined with Gemcitabine.
Epirubicin The risk or severity of adverse effects can be increased when Anakinra is combined with Epirubicin.
Chloramphenicol The risk or severity of adverse effects can be increased when Anakinra is combined with Chloramphenicol.
Lenalidomide The risk or severity of adverse effects can be increased when Anakinra is combined with Lenalidomide.
Altretamine The risk or severity of adverse effects can be increased when Anakinra is combined with Altretamine.
Cisplatin The risk or severity of adverse effects can be increased when Anakinra is combined with Cisplatin.
Oxaliplatin The risk or severity of adverse effects can be increased when Anakinra is combined with Oxaliplatin.
Propylthiouracil The risk or severity of adverse effects can be increased when Anakinra is combined with Propylthiouracil.
Pentostatin The risk or severity of adverse effects can be increased when Anakinra is combined with Pentostatin.
Linezolid The risk or severity of adverse effects can be increased when Anakinra is combined with Linezolid.
Clofarabine The risk or severity of adverse effects can be increased when Anakinra is combined with Clofarabine.
Methimazole The risk or severity of adverse effects can be increased when Anakinra is combined with Methimazole.
Sulfasalazine The risk or severity of adverse effects can be increased when Anakinra is combined with Sulfasalazine.
Temozolomide The risk or severity of adverse effects can be increased when Anakinra is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Anakinra is combined with Penicillamine.
Mechlorethamine The risk or severity of adverse effects can be increased when Anakinra is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Anakinra is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Anakinra is combined with Carboplatin.
Dactinomycin The risk or severity of adverse effects can be increased when Anakinra is combined with Dactinomycin.
Hydroxyurea The risk or severity of adverse effects can be increased when Anakinra is combined with Hydroxyurea.
Mycophenolic acid The risk or severity of adverse effects can be increased when Anakinra is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Anakinra is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Anakinra is combined with Mercaptopurine.
Melphalan The risk or severity of adverse effects can be increased when Anakinra is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Anakinra is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Anakinra is combined with Flucytosine.
Procarbazine The risk or severity of adverse effects can be increased when Anakinra is combined with Procarbazine.
Arsenic trioxide The risk or severity of adverse effects can be increased when Anakinra is combined with Arsenic trioxide.
Mitoxantrone The risk or severity of adverse effects can be increased when Anakinra is combined with Mitoxantrone.
Lomustine The risk or severity of adverse effects can be increased when Anakinra is combined with Lomustine.
Eculizumab The risk or severity of adverse effects can be increased when Anakinra is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Anakinra is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Anakinra is combined with Nelarabine.
Stepronin The risk or severity of adverse effects can be increased when Anakinra is combined with Stepronin.
Castanospermine The risk or severity of adverse effects can be increased when Anakinra is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Anakinra is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Anakinra is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Anakinra is combined with Brequinar.
Interferon alfa The risk or severity of adverse effects can be increased when Anakinra is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Anakinra is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Anakinra is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Anakinra is combined with Human interferon omega-1.
Tocilizumab The risk or severity of adverse effects can be increased when Anakinra is combined with Tocilizumab.
Rilonacept The risk or severity of adverse effects can be increased when Anakinra is combined with Rilonacept.
Mepolizumab The risk or severity of adverse effects can be increased when Anakinra is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Anakinra is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Anakinra is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Anakinra is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Anakinra is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Anakinra is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Anakinra is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Anakinra is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Anakinra is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Anakinra is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Anakinra is combined with Obinutuzumab.
Secukinumab The risk or severity of adverse effects can be increased when Anakinra is combined with Secukinumab.
Vedolizumab The risk or severity of adverse effects can be increased when Anakinra is combined with Vedolizumab.
Siltuximab The risk or severity of adverse effects can be increased when Anakinra is combined with Siltuximab.
Blinatumomab The risk or severity of adverse effects can be increased when Anakinra is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Anakinra is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Anakinra is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Anakinra is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Anakinra is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Anakinra is combined with Tepoxalin.
Ixekizumab The risk or severity of adverse effects can be increased when Anakinra is combined with Ixekizumab.

Target Protein

Interleukin-1 receptor type 1 IL1R1

Referensi & Sumber

Synthesis reference: Thompson, RC., et al. (2005). Nucleic acids encoding interleukin-1 inhibitors and processes for preparing interleukin-1 inhibitors (U.S. Patent No. US 6,858,409 B1). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/cf/f9/7c/87bba89b312e38/US6858409.pdf
Artikel (PubMed)
  • PMID: 11752352
    Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
  • PMID: 17947302
    Lequerre T, Quartier P, Rosellini D, Alaoui F, De Bandt M, Mejjad O, Kone-Paut I, Michel M, Dernis E, Khellaf M, Limal N, Job-Deslandre C, Fautrel B, Le Loet X, Sibilia J: Interleukin-1 receptor antagonist (anakinra) treatment in patients with systemic-onset juvenile idiopathic arthritis or adult onset Still disease: preliminary experience in France. Ann Rheum Dis. 2008 Mar;67(3):302-8. Epub 2007 Oct 18.
  • PMID: 12687534
    Fleischmann RM, Schechtman J, Bennett R, Handel ML, Burmester GR, Tesser J, Modafferi D, Poulakos J, Sun G: Anakinra, a recombinant human interleukin-1 receptor antagonist (r-metHuIL-1ra), in patients with rheumatoid arthritis: A large, international, multicenter, placebo-controlled trial. Arthritis Rheum. 2003 Apr;48(4):927-34. doi: 10.1002/art.10870.
  • PMID: 27790031
    Bachove I, Chang C: Anakinra and related drugs targeting interleukin-1 in the treatment of cryopyrin-associated periodic syndromes. Open Access Rheumatol. 2014 Mar 3;6:15-25. doi: 10.2147/OARRR.S46017. eCollection 2014.
  • PMID: 30459597
    Cavalli G, Dinarello CA: Anakinra Therapy for Non-cancer Inflammatory Diseases. Front Pharmacol. 2018 Nov 6;9:1157. doi: 10.3389/fphar.2018.01157. eCollection 2018.
  • PMID: 33391477
    Kim JS, Lee JY, Yang JW, Lee KH, Effenberger M, Szpirt W, Kronbichler A, Shin JI: Immunopathogenesis and treatment of cytokine storm in COVID-19. Theranostics. 2021 Jan 1;11(1):316-329. doi: 10.7150/thno.49713. eCollection 2021.

Contoh Produk & Brand

Produk: 8 • International brands: 0
Produk
  • Kineret
    Injection, solution • 100 mg/0.67mL • Subcutaneous • US • Approved
  • Kineret
    Solution • 150 mg / mL • Subcutaneous • Canada • Approved
  • Kineret
    Injection, solution • 100 mg • Subcutaneous • EU • Approved
  • Kineret
    Injection, solution • 100 mg • Subcutaneous • EU • Approved
  • Kineret
    Injection, solution • 100 mg • Subcutaneous • EU • Approved
  • Kineret
    Injection, solution • 100 mg/0.67ml • Subcutaneous • EU • Approved
  • Kineret
    Injection, solution • 100 mg/0.67ml • Subcutaneous • EU • Approved
  • Kineret
    Injection, solution • 100 mg/0.67ml • Subcutaneous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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