Peringatan Keamanan

In mice given 60 mg/kg/day of glatiramer acetate subcutaneously (15 times the human therapeutic dose of 20 mg/day on a mg/m2 basis), glatiramer acetate did not increase systemic neoplasms. Similar results were obtained in rats given 30 mg/kg/day of glatiramer acetate subcutaneously (15 times the human therapeutic dose of 20 mg/day on a mg/m2 basis).L41940 In vitro studies suggest that glatiramer acetate is non-mutagenic. No adverse effects were observed on reproductive or developmental parameters during in vivo studies.L41940 Overdose information regarding glatiramer acetate is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as hepatic injury, lipoatrophy and skin necrosis at the injection site.L41940 Symptomatic and supportive measures are recommended.

Glatiramer

DB05259

biotech approved investigational

Deskripsi

Glatiramer acetate is a mix of synthetic polypeptides that includes L-glutamic acid, L-alanine, L-tyrosine, and L-lysine at an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively.L41940 Since glatiramer acetate is a heterogeneous drug, there is limited information about its physicochemical properties.A248870 Originally, glatiramer acetate was designed as a stimulant of myelin basic protein (MBP), a myelin antigen involved in the development of multiple sclerosis (MS), to induce experimental autoimmune encephalitis (MS animal model).A248870 However, the opposite was observed. Glatiramer acetate exhibits several immunomodulatory effects and reduces the relapse rate of relapsing-remitting multiple sclerosis (RRMS) by 30%.A248870 Along with human interferon beta, teriflunomide, and dimethyl fumarate, glatiramer acetate is a first-line drug for patients with MS.A248880 It was approved by the FDA in 1996, and a generic version became available in 2017.

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) Not available.
Volume Distribusi Not available.
Klirens (Clearance) Not available.

Absorpsi

After subcutaneous administration, most glatiramer acetate is rapidly absorbed and hydrolyzed locally.L41940 In 7 out of 9 healthy volunteers that received 60 mg of glatiramer acetate subcutaneously, the Cmax ranged from 69 to 126 ng/mL, while the other two subjects showed significantly higher values (605 and 301 ng/mL).L41945 AUC values showed great variability, ranging from 1,644 to 67,532 min?ng/mL.L41945 The Tmax of glatiramer acetate went from 15 to 30 min, and in all subjects, glatiramer acetate levels returned to baseline after 30-60 min.A248870,L41945 In healthy volunteers given 60 mg of glatiramer acetate subcutaneously, immunorecognizable fragments were no longer detected after 24 hours.A248875,L41945 The systemic bioavailability of glatiramer acetate is considered to be minimal.A248870 The pharmacokinetic parameters of glatiramer acetate in multiple sclerosis (MS) patients have not been determined.A248870

Metabolisme

Glatiramer acetate ??is a mixture of synthetic polypeptides hydrolyzed by proteases.A248875,L41940

Rute Eliminasi

In vivo studies have shown that glatiramer acetate is mainly excreted through urine.A248875

Interaksi Obat

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

Target Protein

MHC class II protein complex

Referensi & Sumber

Synthesis reference: Dolitzky, BZ. (2006). Process for producing polypeptide mixtures using hydrogenolysis (U.S. Patent No. US 2006/0172942 A1). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/b6/b3/7d/a80568fe5c6998/US20060172942A1.pdf
Artikel (PubMed)
  • PMID: 15371592
    Arnon R, Aharoni R: Mechanism of action of glatiramer acetate in multiple sclerosis and its potential for the development of new applications. Proc Natl Acad Sci U S A. 2004 Oct 5;101 Suppl 2:14593-8. Epub 2004 Sep 15.
  • PMID: 30414463
    Song JY, Larson NR, Thati S, Torres-Vazquez I, Martinez-Rivera N, Subelzu NJ, Leon MA, Rosa-Molinar E, Schoneich C, Forrest ML, Middaugh CR, Berkland CJ: Glatiramer acetate persists at the injection site and draining lymph nodes via electrostatically-induced aggregation. J Control Release. 2019 Jan 10;293:36-47. doi: 10.1016/j.jconrel.2018.11.007. Epub 2018 Nov 7.
  • PMID: 23795716
    Messina S, Patti F: The pharmacokinetics of glatiramer acetate for multiple sclerosis treatment. Expert Opin Drug Metab Toxicol. 2013 Oct;9(10):1349-59. doi: 10.1517/17425255.2013.811489. Epub 2013 Jun 25.
  • PMID: 25906331
    McKeage K: Glatiramer Acetate 40 mg/mL in Relapsing-Remitting Multiple Sclerosis: A Review. CNS Drugs. 2015 May;29(5):425-32. doi: 10.1007/s40263-015-0245-z.
  • PMID: 26244148
    Gajofatto A, Benedetti MD: Treatment strategies for multiple sclerosis: When to start, when to change, when to stop? World J Clin Cases. 2015 Jul 16;3(7):545-55. doi: 10.12998/wjcc.v3.i7.545.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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