Peringatan Keamanan

Toxicity information regarding ocrelizumab is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as immune-mediated colitis.L42895 Symptomatic and supportive measures are recommended. The carcinogenic and mutagenic potentials of ocrelizumab have not been evaluated. In monkeys given three loading doses of 15 or 75 mg/kg intravenously, followed by weekly doses of 20 or 100 mg/kg for 8 weeks (2-10 times the recommended human dose), ocrelizumab did not have effects on reproductive organs. No reproductive effects were detected on the estrus cycle of female monkeys given the same ocrelizumab regimen.L42895

Ocrelizumab

DB11988

biotech approved investigational

Deskripsi

Ocrelizumab is a CD20-directed cytolytic antibody indicated for the treatment of patients with primary progressive or relapsing forms of multiple sclerosis (MS).L42895 It is a second-generation recombinant humanized monoclonal IgG1 antibody that selectively targets B-cells that express the CD20 antigen.A31739 Compared to non-humanized CD20 antibodies such as rituximab, ocrelizumab is expected to be less immunogenic with repeated infusions, improving the benefit-to-risk profile for patients with MS.A18875,A251745

MS is a chronic, inflammatory, autoimmune disease of the central nervous system that leads to neurological disabilities and a significantly reduced quality of life.L1199 Most patients with MS experience episodes of relapses with worsening function, followed by recovery periods or remissions. Primary progressive multiple sclerosis (PPMS) accounts for 10-15% of the overall population of patients with MS, and leads to the gradual worsening of neurologic disability from symptom onset, often without early relapses or remissions A31741.

Developed by Genentech/Roche, ocrelizumab was approved by the FDA in March 2017 under the market name Ocrevus for intravenous injection. It was later approved by Health Canada in August 2017, making the drug the first available treatment for PPMS in both the US and Canada. In clinical trials of patients with relapsing forms of MS, treatment with ocrelizumab resulted in reduced relapse rates and reduced worsening of disability compared to interferon beta-1a.L1199 In phase 3 clinical trials of patients with PPMS, treatment with ocrelizumab led to lower clinical and MRI progression rates compared to placebo.A31741

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 terminal elimination half-life of ocrelizumab was 26 days.[L42895]
Volume Distribusi In a population pharmacokinetic estimate, the central volume of distribution of ocrelizumab was 2.78 L.[L42895]
Klirens (Clearance) The constant clearance of ocrelizumab was 0.17 L/day, while the initial time-dependent clearance was 0.05 L/day. Peripheral volume and inter-compartment clearance were 2.68 L and 0.29 L/day, respectively.[L42895]

Absorpsi

Ocrelizumab displays a two-compartment pharmacokinetic model with time-dependent clearance. The overall exposure at the steady-state (AUC over the 24 week dosing intervals) of ocrelizumab was 3,510 mcg/mL per day. Following the intravenous infusion of maintenance doses of 600 mg every 6 months in relapsing MS patients, the mean peak plasma concentration of ocrelizumab (Cmax) was 212 mcg/mL. Following intravenous infusion of two 300 mg doses separated by 14 days every 6 months in patients with PPMS, Cmax was 141 mcg/mL. Ocrelizumab follows linear and dose proportional pharmacokinetics between 400 mg and 2000 mg.L42895

Metabolisme

As with other antibodies, ocrelizumab is expected to undergo nonspecific catabolism and broken into smaller peptides and amino acids.

Rute Eliminasi

Monoclonal antibodies (mAb) such as ocrelizumab are too large to be filtered by the kidneys, and therefore, not eliminated in urine under normal conditions. If antibody fragments of low molecular weight are filtered, they are usually reabsorbed and metabolized in the proximal tubule.A40006 The peptides and amino acids produced by catabolism are recycled or used as an energy source.

Interaksi Obat

671 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Ocrelizumab.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Ocrelizumab.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Ocrelizumab.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Ocrelizumab.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Ocrelizumab.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Ocrelizumab.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Ocrelizumab.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Ocrelizumab.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Ocrelizumab.
Adalimumab Ocrelizumab may increase the immunosuppressive activities of Adalimumab.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Ocrelizumab.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Ocrelizumab.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Ocrelizumab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Ocrelizumab.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Ocrelizumab.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Ocrelizumab.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Ocrelizumab.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Ocrelizumab.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Ocrelizumab.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Ocrelizumab.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Ocrelizumab.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Ocrelizumab.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Ocrelizumab.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Ocrelizumab.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Ocrelizumab.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Ocrelizumab.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Ocrelizumab.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Ocrelizumab.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Ocrelizumab.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Ocrelizumab.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Ocrelizumab.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Ocrelizumab.
Sirolimus Ocrelizumab may increase the immunosuppressive activities of Sirolimus.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Ocrelizumab.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Ocrelizumab.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Ocrelizumab.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Ocrelizumab.
Flucytosine Ocrelizumab may increase the immunosuppressive activities of Flucytosine.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Ocrelizumab.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Ocrelizumab.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Ocrelizumab.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Ocrelizumab.
Budesonide The risk or severity of adverse effects can be increased when Budesonide is combined with Ocrelizumab.
Dasatinib The risk or severity of adverse effects can be increased when Dasatinib is combined with Ocrelizumab.
Sunitinib The risk or severity of adverse effects can be increased when Sunitinib is combined with Ocrelizumab.
Cortisone acetate The risk or severity of adverse effects can be increased when Cortisone acetate is combined with Ocrelizumab.
Ciclesonide The risk or severity of adverse effects can be increased when Ciclesonide is combined with Ocrelizumab.
Everolimus The risk or severity of adverse effects can be increased when Everolimus is combined with Ocrelizumab.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Hydroxychloroquine is combined with Ocrelizumab.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Ocrelizumab.
Nilotinib The risk or severity of adverse effects can be increased when Nilotinib is combined with Ocrelizumab.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Ocrelizumab.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Ocrelizumab.
Apremilast The risk or severity of adverse effects can be increased when Apremilast is combined with Ocrelizumab.
Canakinumab The risk or severity of adverse effects can be increased when Canakinumab is combined with Ocrelizumab.
Rilonacept The risk or severity of adverse effects can be increased when Rilonacept is combined with Ocrelizumab.
Pazopanib The risk or severity of adverse effects can be increased when Pazopanib is combined with Ocrelizumab.
Panobinostat The risk or severity of adverse effects can be increased when Panobinostat is combined with Ocrelizumab.
Mepolizumab The risk or severity of adverse effects can be increased when Mepolizumab is combined with Ocrelizumab.
Bosutinib The risk or severity of adverse effects can be increased when Bosutinib is combined with Ocrelizumab.
Ruxolitinib The risk or severity of adverse effects can be increased when Ruxolitinib is combined with Ocrelizumab.
Teriflunomide The risk or severity of adverse effects can be increased when Teriflunomide is combined with Ocrelizumab.
Ponatinib The risk or severity of adverse effects can be increased when Ponatinib is combined with Ocrelizumab.
Certolizumab pegol The risk or severity of adverse effects can be increased when Certolizumab pegol is combined with Ocrelizumab.
Fluticasone furoate The risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Ocrelizumab.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Dimethyl fumarate is combined with Ocrelizumab.
Pomalidomide The risk or severity of adverse effects can be increased when Pomalidomide is combined with Ocrelizumab.
Secukinumab Ocrelizumab may increase the immunosuppressive activities of Secukinumab.
Ibrutinib The risk or severity of adverse effects can be increased when Ibrutinib is combined with Ocrelizumab.
Idelalisib The risk or severity of adverse effects can be increased when Idelalisib is combined with Ocrelizumab.
Palbociclib The risk or severity of adverse effects can be increased when Palbociclib is combined with Ocrelizumab.
Olaparib The risk or severity of adverse effects can be increased when Olaparib is combined with Ocrelizumab.
Vilanterol The risk or severity of adverse effects can be increased when Vilanterol is combined with Ocrelizumab.
Tixocortol The risk or severity of adverse effects can be increased when Tixocortol is combined with Ocrelizumab.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Peginterferon beta-1a is combined with Ocrelizumab.
Ixekizumab The risk or severity of adverse effects can be increased when Ixekizumab is combined with Ocrelizumab.
Sarilumab The risk or severity of adverse effects can be increased when Sarilumab is combined with Ocrelizumab.
Brodalumab The risk or severity of adverse effects can be increased when Brodalumab is combined with Ocrelizumab.
Baricitinib The risk or severity of adverse effects can be increased when Baricitinib is combined with Ocrelizumab.
Guselkumab Ocrelizumab may increase the immunosuppressive activities of Guselkumab.
Deflazacort The risk or severity of adverse effects can be increased when Deflazacort is combined with Ocrelizumab.
Siponimod The risk or severity of adverse effects can be increased when Ocrelizumab is combined with Siponimod.
Mometasone furoate The risk or severity of adverse effects can be increased when Ocrelizumab is combined with Mometasone furoate.
Hydrocortisone acetate The risk or severity of adverse effects can be increased when Ocrelizumab is combined with Hydrocortisone acetate.
Risankizumab Ocrelizumab may increase the immunosuppressive activities of Risankizumab.
Ozanimod The risk or severity of adverse effects can be increased when Ocrelizumab is combined with Ozanimod.
Fluocinonide The risk or severity of adverse effects can be increased when Fluocinonide is combined with Ocrelizumab.
Hydrocortisone butyrate The risk or severity of adverse effects can be increased when Ocrelizumab is combined with Hydrocortisone butyrate.
Desoximetasone The risk or severity of adverse effects can be increased when Desoximetasone is combined with Ocrelizumab.
Fluticasone The risk or severity of adverse effects can be increased when Ocrelizumab is combined with Fluticasone.
Monomethyl fumarate The risk or severity of adverse effects can be increased when Ocrelizumab is combined with Monomethyl fumarate.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Ocrelizumab.
Fluocortolone The risk or severity of adverse effects can be increased when Fluocortolone is combined with Ocrelizumab.
Fluorometholone The risk or severity of adverse effects can be increased when Fluorometholone is combined with Ocrelizumab.
Difluocortolone The risk or severity of adverse effects can be increased when Difluocortolone is combined with Ocrelizumab.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Ocrelizumab.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Ocrelizumab.
Mometasone The risk or severity of adverse effects can be increased when Mometasone is combined with Ocrelizumab.
Upadacitinib The risk or severity of adverse effects can be increased when Ocrelizumab is combined with Upadacitinib.
Voclosporin The risk or severity of adverse effects can be increased when Voclosporin is combined with Ocrelizumab.

Target Protein

B-lymphocyte antigen CD20 MS4A1

Referensi & Sumber

Synthesis reference: Manfrini, M. (2022). Methods for treating multiple sclerosis with ocrelizumab (U.S. Patent No. US 2022/0064320 A1). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/a3/24/be/d30651ed8b7f68/US20220064320A1.pdf
Artikel (PubMed)
  • PMID: 27756172
    McGinley MP, Moss BP, Cohen JA: Safety of monoclonal antibodies for the treatment of multiple sclerosis. Expert Opin Drug Saf. 2017 Jan;16(1):89-100. Epub 2016 Oct 31.
  • PMID: 26788130
    Sorensen PS, Blinkenberg M: The potential role for ocrelizumab in the treatment of multiple sclerosis: current evidence and future prospects. Ther Adv Neurol Disord. 2016 Jan;9(1):44-52. doi: 10.1177/1756285615601933.
  • PMID: 28002688
    Montalban X, Hauser SL, Kappos L, Arnold DL, Bar-Or A, Comi G, de Seze J, Giovannoni G, Hartung HP, Hemmer B, Lublin F, Rammohan KW, Selmaj K, Traboulsee A, Sauter A, Masterman D, Fontoura P, Belachew S, Garren H, Mairon N, Chin P, Wolinsky JS: Ocrelizumab versus Placebo in Primary Progressive Multiple Sclerosis. N Engl J Med. 2017 Jan 19;376(3):209-220. doi: 10.1056/NEJMoa1606468. Epub 2016 Dec 21.
  • PMID: 33092190
    Florou D, Katsara M, Feehan J, Dardiotis E, Apostolopoulos V: Anti-CD20 Agents for Multiple Sclerosis: Spotlight on Ocrelizumab and Ofatumumab. Brain Sci. 2020 Oct 20;10(10). pii: brainsci10100758. doi: 10.3390/brainsci10100758.
  • PMID: 34354358
    Mancinelli CR, Rossi N, Capra R: Ocrelizumab for the Treatment of Multiple Sclerosis: Safety, Efficacy, and Pharmacology. Ther Clin Risk Manag. 2021 Jul 30;17:765-776. doi: 10.2147/TCRM.S282390. eCollection 2021.
  • PMID: 28653357
    Ryman JT, Meibohm B: Pharmacokinetics of Monoclonal Antibodies. CPT Pharmacometrics Syst Pharmacol. 2017 Sep;6(9):576-588. doi: 10.1002/psp4.12224. Epub 2017 Jul 29.
  • PMID: 35107597
    Alcala C, Quintanilla-Bordas C, Gascon F, Sempere AP, Navarro L, Carcelen-Gadea M, Landete L, Mallada J, Canizares E, Belenguer A, Carratala S, Dominguez JA, Perez-Miralles FC, Gil-Perotin S, Gasque R, Cubas L, Castillo J, Casanova B: Effectiveness of rituximab vs. ocrelizumab for the treatment of primary progressive multiple sclerosis: a real-world observational study. J Neurol. 2022 Jul;269(7):3676-3681. doi: 10.1007/s00415-022-10989-0. Epub 2022 Feb 2.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Ocrevus
    Injection • 300 mg/10mL • Intravenous • US • Approved
  • Ocrevus
    Injection, solution • 920 mg • Subcutaneous • EU • Approved
  • Ocrevus
    Injection, solution, concentrate • 300 mg • Intravenous • EU • Approved
  • Ocrevus
    Injection, solution, concentrate • 300 mg • Intravenous • EU • Approved
  • Ocrevus
    Solution • 30 mg / mL • Intravenous • Canada • Approved
  • Ocrevus Zunovo
    Injection, solution • - • Subcutaneous • US • Approved

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