Peringatan Keamanan

Toxicity information regarding mepolizumab is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as newly established or worsening chronic infections, including those caused by helminths, and generalized immune depression. Symptomatic and supportive measures are recommended.L16518

Mepolizumab

DB06612

biotech approved investigational

Deskripsi

Eosinophils are involved in inflammatory immune responses, and prolonged hypereosinophilia (typically defined as absolute eosinophil levels of 1500/mm3 or more) is associated with a spectrum of diseases, including severe asthma, eosinophilic granulomatosis with polyangiitis (EGPA), and hypereosinophilic syndrome (HES). The pathogenesis of eosinophilia is complex, but IL-5 is recognized as a key cytokine involved in the differentiation, recruitment, activation, and prolonged survival of eosinophils in peripheral tissue. Activated eosinophils further stimulate an inflammatory response and also induce tissue lesions and promote fibrosis, all of which contribute to the multifactorial symptomatology of hypereosinophilic diseases.A221048, A221053, A221058, A221063, A221068, L16518

Mepolizumab is a fully-humanized recombinant IgG1 kappa monoclonal antibody directed against IL-5 produced in Chinese hamster ovary cells. Mepolizumab was first approved by the FDA on November 4, 2015, as an add-on therapy for severe asthma and marketed under the brand name Nucala by GlaxoSmithKline. This indication was subsequently expanded to cover EGPA on December 12, 2017, and HES on September 25, 2020.L16518

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) Mepolizumab has a mean terminal half-life of between 16 and 22 days.[L16518]
Volume Distribusi Mepolizumab has a population central volume of distribution of 3.6 L (for a 70 kg individual) in adult asthma patients.[L16518]
Klirens (Clearance) Mepolizumab has an estimated apparent population systemic clearance of 0.28 L/day (for a 70-kg individual) in adult and adolescent subjects.[L16518]

Absorpsi

Mepolizumab is administered subcutaneously and has a bioavailability of approximately 80% based on a 100 mg dose given to both adult and adolescent subjects with asthma. With the recommended four-week dosing schedule, there is an approximately two-fold accumulation of mepolizumab at steady-state.L16518

Metabolisme

As a monoclonal antibody, mepolizumab is subject to proteolytic degradation at sites distributed throughout the body.L16518

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

670 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Mepolizumab.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Mepolizumab.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Mepolizumab.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Mepolizumab.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Mepolizumab.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Mepolizumab.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Mepolizumab.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Mepolizumab.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Mepolizumab.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Mepolizumab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Mepolizumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Mepolizumab.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Mepolizumab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Mepolizumab.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Mepolizumab.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Mepolizumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Mepolizumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Mepolizumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Mepolizumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Mepolizumab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Mepolizumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Mepolizumab.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Mepolizumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Mepolizumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Mepolizumab.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Mepolizumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Mepolizumab.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Mepolizumab.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Mepolizumab.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Mepolizumab.
Cladribine Mepolizumab may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Mepolizumab.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Mepolizumab.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Mepolizumab.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Mepolizumab.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Mepolizumab.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Mepolizumab.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Mepolizumab.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Mepolizumab.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Mepolizumab.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Mepolizumab.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Mepolizumab.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Mepolizumab.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Mepolizumab.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Mepolizumab.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Mepolizumab.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Mepolizumab.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Mepolizumab.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Mepolizumab.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Mepolizumab.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Mepolizumab.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Mepolizumab.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Mepolizumab.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Mepolizumab.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Mepolizumab.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Mepolizumab.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Mepolizumab.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Mepolizumab.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Mepolizumab.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Mepolizumab.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Mepolizumab.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Mepolizumab.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Mepolizumab.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Mepolizumab.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Mepolizumab.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Mepolizumab.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Mepolizumab.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Mepolizumab.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Mepolizumab.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Mepolizumab.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Mepolizumab.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Mepolizumab.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Mepolizumab.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Mepolizumab.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Mepolizumab.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Mepolizumab.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Mepolizumab.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Mepolizumab.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Mepolizumab.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Mepolizumab.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Mepolizumab.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Mepolizumab.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Mepolizumab.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Mepolizumab.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Mepolizumab.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Mepolizumab.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Mepolizumab.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Mepolizumab.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Mepolizumab.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Mepolizumab.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Mepolizumab.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Mepolizumab.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Mepolizumab.
Doxorubicin The risk or severity of adverse effects can be increased when Doxorubicin is combined with Mepolizumab.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Mepolizumab.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Mepolizumab.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Mepolizumab.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Mepolizumab.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Mepolizumab.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Mepolizumab.

Target Protein

Interleukin-5 IL5

Referensi & Sumber

Synthesis reference: Robert S. Ames, Edward Robert Appelbaum, Irwin M. Chaiken, Richard M. Cook, Mitchell Stuart Gross, Stephen Dudley Holmes, Lynette Jane McMillan, Timothy Wayne Theisen, "Recombinant il-5 antagonists useful in treatment of il-5 mediated disorders." Patent WO1996021000A2, issued July 11, 1996.
Artikel (PubMed)
  • PMID: 29751154
    Kuang FL, Fay MP, Ware J, Wetzler L, Holland-Thomas N, Brown T, Ortega H, Steinfeld J, Khoury P, Klion AD: Long-Term Clinical Outcomes of High-Dose Mepolizumab Treatment for Hypereosinophilic Syndrome. J Allergy Clin Immunol Pract. 2018 Sep - Oct;6(5):1518-1527.e5. doi: 10.1016/j.jaip.2018.04.033. Epub 2018 May 8.
  • PMID: 26475367
    Curtis C, Ogbogu P: Hypereosinophilic Syndrome. Clin Rev Allergy Immunol. 2016 Apr;50(2):240-51. doi: 10.1007/s12016-015-8506-7.
  • PMID: 31391853
    Caminati M, Menzella F, Guidolin L, Senna G: Targeting eosinophils: severe asthma and beyond. Drugs Context. 2019 Jul 23;8:212587. doi: 10.7573/dic.212587. eCollection 2019.
  • PMID: 31480806
    Bakakos A, Loukides S, Bakakos P: Severe Eosinophilic Asthma. J Clin Med. 2019 Sep 2;8(9). pii: jcm8091375. doi: 10.3390/jcm8091375.
  • PMID: 18344568
    Rothenberg ME, Klion AD, Roufosse FE, Kahn JE, Weller PF, Simon HU, Schwartz LB, Rosenwasser LJ, Ring J, Griffin EF, Haig AE, Frewer PI, Parkin JM, Gleich GJ: Treatment of patients with the hypereosinophilic syndrome with mepolizumab. N Engl J Med. 2008 Mar 20;358(12):1215-28. doi: 10.1056/NEJMoa070812. Epub 2008 Mar 16.

Contoh Produk & Brand

Produk: 18 • International brands: 1
Produk
  • Nucala
    Injection, powder, for solution • 100 mg/1mL • Subcutaneous • US • Approved
  • Nucala
    Injection, solution • 100 mg • Subcutaneous • EU • Approved
  • Nucala
    Injection, solution • 100 mg • Subcutaneous • EU • Approved
  • Nucala
    Injection, solution • 40 mg • Subcutaneous • EU • Approved
  • Nucala
    Injection, powder, for solution • 100 mg/1mL • Subcutaneous • US • Approved
  • Nucala
    Injection, solution • 40 mg • Subcutaneous • EU • Approved
  • Nucala
    Injection, solution • 100 mg/1mL • Subcutaneous • US • Approved
  • Nucala
    Solution • 100 mg / mL • Subcutaneous • Canada • Approved
Menampilkan 8 dari 18 produk.
International Brands
  • Bosatria — GlaxoSmithKline

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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