Peringatan Keamanan

Data regarding overdose is not readily available.L34929 In a phase 1 clinical trial, patients given a single dose of 20.0 mg/kg experienced upper respiratory tract infections, headache, diarrhea, and nausea.A237044 2 patients in the 3.0 mg/kg single dose group experienced osteomyelitis and skin ulcer.A237044 A single patient in the 1.0 mg/kg/week group developed chronic myelogenous leukemia.A237044 The frequency and severity of adverse effects does not appear to be closely related to dose.A237044 In the event of an overdose, treat patients with symptomatic and supportive measures.

Anifrolumab

DB11976

biotech approved investigational

Deskripsi

Anifrolumab, or MEDI-546, is a type 1 interferon receptor (IFNAR) inhibiting IgG1? monoclonal antibody indicated in the treatment of adults with moderate to severe systemic lupus erythematosus.A237074,L34929 The standard therapy for systemic lupus erythematosus consists of antimalarials like hydroxychloroquine, glucocorticoids like dexamethasone, and disease modifying antirheumatic drugs like methotrexate.A237079,L34929

Three monoclonal antibodies (anifrolumab, rontalizumab, and sifalimumab) that target the type 1 interferon pathway entered clinical trials as potential treatments for systemic lupus erythematosus, but so far only anifrolumab has been approved.A237054

The design of early clinical trials of anti-interferon treatments such as anifrolumab, rontalizumab, and sifalimumab have come under criticism.A237054 The design of the clinical trials use different definitions of autoantibody positivity, making comparison between trials difficult; all trials involve large portions of patients also using corticosteroids, which may alter patient responses in the experimental and placebo groups; and patient populations were largely homogenous, which may have increased the odds of success of the trial.A237054

Anifrolumab has also been investigated for the treatment of Scleroderma.A237044

Anifrolumab was granted FDA approval on 30 July 2021.L34929

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) The serum elimination half life anifrolumab in a phase 1 trial in patients with scleroderma was 0.84 days for a 0.1 mg/kg single dose, 1.24 days for a 0.3 mg/kg single dose, 2.96 days for a 1.0 mg/kg single dose, 4.07 days for a 3.0 mg/kg single dose, and 7.70 days for a 10.0 mg/kg single dose.[A237044]
Volume Distribusi Based on population PK analysis, the estimated volume of distribution at steady state for a typical patient with SLE (69.1 kg) is 6.23 L.[L49286]
Klirens (Clearance) Following the administration of anifrolumab at a dose of 300 mg via intravenous infusion every 4 weeks, the estimated systemic clearance (CL) for anifrolumab was 0.193 L/day.[L49286]

Absorpsi

The PK of anifrolumab was studied in adult patients with SLE following intravenous doses ranging from 100 to 1000 mg once every 4 weeks, and healthy volunteers following a single intravenous dose at 300 mg. Anifrolumab exhibits non-linear PK in the dose range of 100 mg to 1000 mg with more than dose-proportional increases in the exposure as measured by AUC. Following the 300 mg every 4 weeks intravenous administrations of anifrolumab, a steady state was reached by Day 85. The accumulation ratio was approximately 1.36 for Cmax and 2.49 for Ctrough.L49286 A 300 mg intravenous dose reaches a mean Cmax of 82.4 µg/mL, with a Tmax of 0.03 days, and an AUC of 907 day\*µg/mL.A237064 A 300 mg subcutaneous dose reaches a mean Cmax of 36.2 µg/mL, with a Tmax of 4.1 days, and an AUC of 785 day\*µg/mL.A237064 A 600 mg subcutaneous dose reaches a mean Cmax of 63.9 µg/mL, with a Tmax of 7.0 days, and an AUC of 1828 day\*µg/mL.A237064

Metabolisme

Monoclonal antibodies are mainly catabolized to smaller oligopeptides and individual amino acids.A40006,L34929

Rute Eliminasi

Monoclonal IgG is predominantly eliminated by catabolism to individual amino acids that are either recycled in the body or metabolized for energy.A40006

Interaksi Obat

670 Data
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Anifrolumab.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Anifrolumab.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Anifrolumab.
Estrone Estrone may increase the thrombogenic activities of Anifrolumab.
Estradiol Estradiol may increase the thrombogenic activities of Anifrolumab.
Dienestrol Dienestrol may increase the thrombogenic activities of Anifrolumab.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Anifrolumab.
Mestranol Mestranol may increase the thrombogenic activities of Anifrolumab.
Estriol Estriol may increase the thrombogenic activities of Anifrolumab.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Anifrolumab.
Quinestrol Quinestrol may increase the thrombogenic activities of Anifrolumab.
Hexestrol Hexestrol may increase the thrombogenic activities of Anifrolumab.
Tibolone Tibolone may increase the thrombogenic activities of Anifrolumab.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Anifrolumab.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Anifrolumab.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Anifrolumab.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Anifrolumab.
Zeranol Zeranol may increase the thrombogenic activities of Anifrolumab.
Equol Equol may increase the thrombogenic activities of Anifrolumab.
Promestriene Promestriene may increase the thrombogenic activities of Anifrolumab.
Methallenestril Methallenestril may increase the thrombogenic activities of Anifrolumab.
Epimestrol Epimestrol may increase the thrombogenic activities of Anifrolumab.
Moxestrol Moxestrol may increase the thrombogenic activities of Anifrolumab.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Anifrolumab.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Anifrolumab.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Anifrolumab.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Anifrolumab.
Biochanin A Biochanin A may increase the thrombogenic activities of Anifrolumab.
Formononetin Formononetin may increase the thrombogenic activities of Anifrolumab.
Estetrol Estetrol may increase the thrombogenic activities of Anifrolumab.
Cetuximab The risk or severity of adverse effects can be increased when Cetuximab is combined with Anifrolumab.
Human immunoglobulin G The risk or severity of adverse effects can be increased when Human immunoglobulin G is combined with Anifrolumab.
Omalizumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Anifrolumab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Anifrolumab.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Anifrolumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Anifrolumab.
Indium In-111 satumomab pendetide The risk or severity of adverse effects can be increased when Indium In-111 satumomab pendetide is combined with Anifrolumab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Anifrolumab.
Trastuzumab The risk or severity of neutropenia can be increased when Trastuzumab is combined with Anifrolumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Anifrolumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Anifrolumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Anifrolumab.
Digoxin Immune Fab (Ovine) The risk or severity of adverse effects can be increased when Digoxin Immune Fab (Ovine) is combined with Anifrolumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Anifrolumab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Anifrolumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Anifrolumab.
Capromab pendetide The risk or severity of adverse effects can be increased when Capromab pendetide is combined with Anifrolumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Anifrolumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Anifrolumab.
Natalizumab The risk or severity of immunosuppression can be increased when Anifrolumab is combined with Natalizumab.
Palivizumab The risk or severity of adverse effects can be increased when Palivizumab is combined with Anifrolumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Anifrolumab.
Bevacizumab The risk or severity of adverse effects can be increased when Bevacizumab is combined with Anifrolumab.
Technetium Tc-99m arcitumomab The risk or severity of adverse effects can be increased when Technetium Tc-99m arcitumomab is combined with Anifrolumab.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Anifrolumab.
Panitumumab The risk or severity of adverse effects can be increased when Panitumumab is combined with Anifrolumab.
Ranibizumab The risk or severity of adverse effects can be increased when Ranibizumab is combined with Anifrolumab.
Galiximab The risk or severity of adverse effects can be increased when Galiximab is combined with Anifrolumab.
Pexelizumab The risk or severity of adverse effects can be increased when Pexelizumab is combined with Anifrolumab.
Afelimomab The risk or severity of adverse effects can be increased when Afelimomab is combined with Anifrolumab.
Epratuzumab The risk or severity of adverse effects can be increased when Epratuzumab is combined with Anifrolumab.
Bectumomab The risk or severity of adverse effects can be increased when Bectumomab is combined with Anifrolumab.
Oregovomab The risk or severity of adverse effects can be increased when Oregovomab is combined with Anifrolumab.
IGN311 The risk or severity of adverse effects can be increased when IGN311 is combined with Anifrolumab.
Adecatumumab The risk or severity of adverse effects can be increased when Adecatumumab is combined with Anifrolumab.
Labetuzumab The risk or severity of adverse effects can be increased when Labetuzumab is combined with Anifrolumab.
Matuzumab The risk or severity of adverse effects can be increased when Matuzumab is combined with Anifrolumab.
Fontolizumab The risk or severity of adverse effects can be increased when Fontolizumab is combined with Anifrolumab.
Bavituximab The risk or severity of adverse effects can be increased when Bavituximab is combined with Anifrolumab.
CR002 The risk or severity of adverse effects can be increased when CR002 is combined with Anifrolumab.
Rozrolimupab The risk or severity of adverse effects can be increased when Rozrolimupab is combined with Anifrolumab.
Girentuximab The risk or severity of adverse effects can be increased when Girentuximab is combined with Anifrolumab.
Obiltoxaximab The risk or severity of adverse effects can be increased when Obiltoxaximab is combined with Anifrolumab.
XTL-001 The risk or severity of adverse effects can be increased when XTL-001 is combined with Anifrolumab.
NAV 1800 The risk or severity of adverse effects can be increased when NAV 1800 is combined with Anifrolumab.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Anifrolumab.
Otelixizumab The risk or severity of adverse effects can be increased when Otelixizumab is combined with Anifrolumab.
AMG 108 The risk or severity of adverse effects can be increased when AMG 108 is combined with Anifrolumab.
Iratumumab The risk or severity of adverse effects can be increased when Iratumumab is combined with Anifrolumab.
Enokizumab The risk or severity of adverse effects can be increased when Enokizumab is combined with Anifrolumab.
Ramucirumab The risk or severity of adverse effects can be increased when Ramucirumab is combined with Anifrolumab.
Farletuzumab The risk or severity of adverse effects can be increased when Farletuzumab is combined with Anifrolumab.
Veltuzumab The risk or severity of adverse effects can be increased when Veltuzumab is combined with Anifrolumab.
Ustekinumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Anifrolumab.
Trastuzumab emtansine The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Anifrolumab.
PRO-542 The risk or severity of adverse effects can be increased when PRO-542 is combined with Anifrolumab.
TNX-901 The risk or severity of adverse effects can be increased when TNX-901 is combined with Anifrolumab.
Inotuzumab ozogamicin The risk or severity of adverse effects can be increased when Inotuzumab ozogamicin is combined with Anifrolumab.
RI 624 The risk or severity of adverse effects can be increased when RI 624 is combined with Anifrolumab.
Stamulumab The risk or severity of adverse effects can be increased when MYO-029 is combined with Anifrolumab.
CT-011 The risk or severity of adverse effects can be increased when CT-011 is combined with Anifrolumab.
Leronlimab The risk or severity of adverse effects can be increased when Leronlimab is combined with Anifrolumab.
Glembatumumab vedotin The risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Anifrolumab.
Olaratumab The risk or severity of adverse effects can be increased when Olaratumab is combined with Anifrolumab.
IPH 2101 The risk or severity of adverse effects can be increased when IPH 2101 is combined with Anifrolumab.
TB-402 The risk or severity of adverse effects can be increased when TB-402 is combined with Anifrolumab.
Caplacizumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Anifrolumab.
IMC-1C11 The risk or severity of adverse effects can be increased when IMC-1C11 is combined with Anifrolumab.
Eldelumab The risk or severity of adverse effects can be increased when Eldelumab is combined with Anifrolumab.
Lumiliximab The risk or severity of adverse effects can be increased when Lumiliximab is combined with Anifrolumab.

Target Protein

Interferon alpha/beta receptor 1 IFNAR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 24559157
    Goldberg A, Geppert T, Schiopu E, Frech T, Hsu V, Simms RW, Peng SL, Yao Y, Elgeioushi N, Chang L, Wang B, Yoo S: Dose-escalation of human anti-interferon-alpha receptor monoclonal antibody MEDI-546 in subjects with systemic sclerosis: a phase 1, multicenter, open label study. Arthritis Res Ther. 2014 Feb 24;16(1):R57. doi: 10.1186/ar4492.
  • PMID: 25606664
    Peng L, Oganesyan V, Wu H, Dall'Acqua WF, Damschroder MM: Molecular basis for antagonistic activity of anifrolumab, an anti-interferon-alpha receptor 1 antibody. MAbs. 2015;7(2):428-39. doi: 10.1080/19420862.2015.1007810.
  • PMID: 27860434
    Massarotti EM, Allore HG, Costenbader K: Editorial: Interferon-Targeted Therapy for Systemic Lupus Erythematosus: Are the Trials on Target? Arthritis Rheumatol. 2017 Feb;69(2):245-248. doi: 10.1002/art.39985.
  • PMID: 28130918
    Furie R, Khamashta M, Merrill JT, Werth VP, Kalunian K, Brohawn P, Illei GG, Drappa J, Wang L, Yoo S: Anifrolumab, an Anti-Interferon-alpha Receptor Monoclonal Antibody, in Moderate-to-Severe Systemic Lupus Erythematosus. Arthritis Rheumatol. 2017 Feb;69(2):376-386. doi: 10.1002/art.39962.
  • PMID: 29644080
    Tummala R, Rouse T, Berglind A, Santiago L: Safety, tolerability and pharmacokinetics of subcutaneous and intravenous anifrolumab in healthy volunteers. Lupus Sci Med. 2018 Mar 23;5(1):e000252. doi: 10.1136/lupus-2017-000252. eCollection 2018.
  • PMID: 29644082
    Riggs JM, Hanna RN, Rajan B, Zerrouki K, Karnell JL, Sagar D, Vainshtein I, Farmer E, Rosenthal K, Morehouse C, de Los Reyes M, Schifferli K, Liang M, Sanjuan MA, Sims GP, Kolbeck R: Characterisation of anifrolumab, a fully human anti-interferon receptor antagonist antibody for the treatment of systemic lupus erythematosus. Lupus Sci Med. 2018 Apr 5;5(1):e000261. doi: 10.1136/lupus-2018-000261. eCollection 2018.
  • PMID: 32310439
    Bui A, Sanghavi D: Anifrolumab .
  • PMID: 34244988
    Trindade VC, Carneiro-Sampaio M, Bonfa E, Silva CA: An Update on the Management of Childhood-Onset Systemic Lupus Erythematosus. Paediatr Drugs. 2021 Jul;23(4):331-347. doi: 10.1007/s40272-021-00457-z. Epub 2021 Jul 10.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • Saphnelo
    Solution • 150 mg / mL • Intravenous • Canada • Approved
  • Saphnelo
    Injection, solution • 300 mg/2.0mL • Intravenous • US • Approved
  • Saphnelo
    Injection, solution, concentrate • 300 mg • Intravenous • EU • Approved
International Brands
  • Saphnelo — AstraZeneca

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul