Glatiramer acetate

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Glatiramer acetate
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Glatiramer acetate is an immunomodulator drug currently used to treat multiple sclerosis. It is a random polymer of four amino acids found in myelin basic protein, namely L-glutamic acid, L-lysine, L-alanine, and L-tyrosine.

Category
L-Amino Acids
Catalog number
BAT-014243
CAS number
147245-92-9
Molecular Formula
C25H45N5O13
Molecular Weight
623.657
Glatiramer acetate
Size Price Stock Quantity
50 mg $298 In stock
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IUPAC Name
acetic acid;(2S)-2-amino-3-(4-hydroxyphenyl)propanoic acid;(2S)-2-aminopentanedioic acid;(2S)-2-aminopropanoic acid;(2S)-2,6-diaminohexanoic acid
Synonyms
Copaxone; Copolymer 1; Copolymer-1
Appearance
White to Off-white Soild
Melting Point
>239°C
InChI
InChI=1S/C9H11NO3.C6H14N2O2.C5H9NO4.C3H7NO2.C2H4O2/c10-8(9(12)13)5-6-1-3-7(11)4-2-6;7-4-2-1-3-5(8)6(9)10;6-3(5(9)10)1-2-4(7)8;1-2(4)3(5)6;1-2(3)4/h1-4,8,11H,5,10H2,(H,12,13);5H,1-4,7-8H2,(H,9,10);3H,1-2,6H2,(H,7,8)(H,9,10);2H,4H2,1H3,(H,5,6);1H3,(H,3,4)/t8-;5-;3-;2-;/m0000./s1
InChI Key
FHEAIOHRHQGZPC-KIWGSFCNSA-N
Canonical SMILES
CC(C(=O)O)N.CC(=O)O.C1=CC(=CC=C1CC(C(=O)O)N)O.C(CCN)CC(C(=O)O)N.C(CC(=O)O)C(C(=O)O)N
1. Glatiramer acetate in multiple sclerosis
Massimo Filippi,Domenico M Mezzapesa,Marco Rovaris Expert Rev Neurother . 2005 Jul;5(4):451-8. doi: 10.1586/14737175.5.4.451.
Glatiramer acetate (Copaxone) is a disease-modifying agent approved by several health authorities worldwide for the treatment of relapsing-remitting multiple sclerosis. Although its primary target is the inflammatory component of the disease, there are emerging pieces of evidence suggesting that glatiramer acetate might also have a neuroprotective effect. In this review, the results of glatiramer acetate clinical trials and other relevant studies as well as the place of glatiramer acetate among other approved disease-modifying treatments for relapsing-remitting multiple sclerosis are discussed critically.
2. Comparison of Copaxone ® and Synthon's therapeutically equivalent glatiramer acetate
N P Koper,D Wang,M Scheren,R J Arends,C Wolf,M Buurman,J Luten Pharmazie . 2019 Aug 1;74(8):449-461. doi: 10.1691/ph.2019.9515.
Glatiramer acetate is indicated for the treatment of patients with relapsing forms of multiple sclerosis (RMS). In 2016, an alternative to the originator product was approved in the EU through the hybrid procedure regulatory pathway. This paper reviews the scientifically rigorous and multifaceted program undertaken to demonstrate the equivalence of this glatiramer acetate follow-on product (GTR) and the reference product Copaxone®,which resulted in the EU approval of GTR 20 mg/mL and 40 mg/mL. Establishing therapeutic equivalence for non-biological complex drugs is not trivial and requires a complex and multidisciplinary effort. Ultimately, there is not a single test or study that establishes therapeutic equivalence of two heterogeneous products. Instead, it requires a good understanding of the synthesis process together with a full set of data that includes comparative physicochemical testing, nonclinicalin vitroandin vivostudies, and a comparative clinical study to allow for a valid conclusion that two products are therapeutically equivalent. The detailed understanding of glatiramer's synthesis process and its impact on the characteristics of glatiramer, combined with the results of a scientifically rigorous and multifaceted physicochemical and biological characterization program, and the clinical data from the 794-patient Phase III GATE study, demonstrate that GTR and Copaxone are therapeutically equivalent. The data further demonstrate that Synthon's manufacturing process consistently yields drug substance of the same quality as Copaxone and that switching from Copaxone to GTR is safe and well-tolerated.
3. Glatiramer acetate enhances tumor retention and innate activation of immunostimulants
Sebastian G Huayamares,Melissa M Pressnall,M Laird Forrest,Chad E Groer,Cory J Berkland,Aric Huang Int J Pharm . 2021 Aug 10;605:120812. doi: 10.1016/j.ijpharm.2021.120812.
Cancer immunotherapy aims to stimulate immune cells to recognize and attack tumor tissue. The immunostimulatory polyanions polyI:C and CpG induce potent pro-inflammatory immune responses as TLR3 and TLR9 agonists, respectively. Clinical trials of TLR agonists, however, have been fraught with immune-related adverse events, even when injecting intratumorally in an effort to minimize systemic exposure. We identified Glatiramer Acetate (GA), a positively-charged polypeptide approved for multiple sclerosis, as a delivery agent capable of complexing with polyI:C or CpG and reducing the mobility of these actives. Small nanoparticles termed polyplexes form when mixing positively-charged GA and negatively-charged immunostimulant (polyI:C or CpG). The ratio of GA to immunostimulant directly affected the potency of TLR activation and the mobility of these actives in simulated tumor tissue. Polyplexes of GA and CpG were injected intratumorally in a tumor model of head and neck cancer (HNC) and significantly mitigated tumor growth as compared to the vehicle controls. Intratumoral injections of CpG showed the slowest tumor growth but exhibited dramatically higher systemic proinflammatory cytokine levels compared to polyplexes of GA with CpG. Sequencing of RNA from resected tumors revealed a similar pattern of upregulated proinflammatory cytokines for CpG and polyplexes, a finding supported by histological tumor staining showing similar infiltration of immune cells induced by these treatments. Intratumoral administration of polyplexes of GA with immunostimulant represents a translational approach to enhance local immune responses while mitigating systemic immune-related adverse events.
4. Glatiramer acetate for multiple sclerosis
Luca M Munari,Loredana La Mantia,Roberta Lovati Cochrane Database Syst Rev . 2010 May 12;(5):CD004678. doi: 10.1002/14651858.CD004678.pub2.
Background:This is an updated Cochrane review of the previous version published (Cochrane Database of Systematic Reviews 2004 , Issue 1 . Art. No.: CD004678. DOI: 10.1002/14651858.CD004678)Previous studies have shown that glatiramer acetate (Copaxone (R)), a synthetic amino acid polymer is effective in experimental allergic encephalomyelitis (EAE), and improve the outcome of patients with multiple sclerosis (MS).Objectives:To verify the clinical efficacy of glatiramer acetate in the treatment of MS patients with relapsing remitting (RR) and progressive (P) course.Search strategy:We searched the Cochrane MS Group Trials Register (26 March 2009), the Cochrane Central Register of Controlled Trials (The Cochrane Library, Issue 1, 2009), MEDLINE (PubMed) (January 1966 to 26 March 2009), EMBASE (January 1988 to 26 March 2009) and hand searching of symposia reports (1990-2009).Selection criteria:All randomised controlled trials (RCTs) comparing glatiramer acetate and placebo in patients with definite MS, whatever the administration schedule and disease course, were eligible for this review.Data collection and analysis:Both patients with RR and P MS were analysed. Study protocols were comparable across trials. No major flaws were found in methodological quality. However, efficacy of blinding should be balanced against side effects, including injection-site reactions.Main results:Among 409 retrieved references, we identified 16 RCTs; six of them, published between 1987 and 2007, met the selection criteria and were included in this review. Five hundred and forty RR patients and 1049 PMS contributed to the analysis. In RR MS, a decrease in the mean EDSS score (-0.33 and -0.45), was found respectively at 2 years and 35 months without any significant effect on sustained disease progression. The reduction of mean number of relapse was evident at 1 year (-0.35 ) 2 years (-0.51 ) and 35 months (-0.64), but significant studies ' heterogeneity was found. The number of hospitalisations and steroid courses were significantly reduced. No benefit was shown in P MS patients. No major toxicity was found. The most common systemic adverse event was a transient and self-limiting patterned reaction of flushing, chest tightness, sweating, palpitations, anxiety. Local injection-site reactions were observed in up to a half of patients treated with glatiramer acetate, thus making a blind assessment of outcomes questionable.Authors' conclusions:Glatiramer acetate did show a partial efficacy in RR MS in term of relapse -related clinical outcomes, without any significant effect on clinical progression of disease measured as sustained disability. The drug is not effective in progressive MS patients.
5. Glatiramer Acetate 40 mg/mL in Relapsing-Remitting Multiple Sclerosis: A Review
Kate McKeage CNS Drugs . 2015 May;29(5):425-32. doi: 10.1007/s40263-015-0245-z.
Glatiramer acetate (Copaxone(®)) is a synthetic analogue of myelin basic protein, which is thought to be involved in the pathogenesis of multiple sclerosis (MS). The therapeutic effects of the drug in the treatment of MS are thought to be via immunomodulation and neuroprotection. Subcutaneous glatiramer acetate 20 mg/mL once daily is approved in several countries for the treatment of relapsing forms of MS. Recently, a high-concentration formulation of glatiramer acetate 40 mg/mL administered three times weekly was approved in the USA and several European countries in the same indication. This article reviews the efficacy and tolerability of the high-concentration regimen. In the randomized, phase III GALA study in patients with relapsing-remitting MS (RRMS), glatiramer acetate 40 mg/mL three times weekly reduced annualized relapse rates significantly more than placebo, and indirect comparisons indicate that the efficacy of the three-times-weekly regimen is similar to that of the 20 mg/mL once-daily regimen. Results of the randomized, phase IIIb GLACIER study in patients with RRMS demonstrated that the three-times-weekly regimen reduced the risk of injection-site reactions by 50 % and was associated with numerically greater patient convenience scores than the once-daily regimen. Thus, in the treatment of RRMS, glatiramer acetate 40 mg/mL three times weekly is effective and provides a better tolerated and possibly more convenient option than the once-daily regimen.
6. Glatiramer Acetate: from Bench to Bed and Back
Ruth Arnon,Rina Aharoni Isr Med Assoc J . 2019 Mar;21(3):151-157.
Glatiramer acetate (GA, Copaxone®, Copolymer1, Cop 1) is an approved drug for the treatment of relapsing-remitting multiple sclerosis (RRMS). Its efficacy in reducing the frequency of exacerbations and its safety profile establish it as a first-line therapy for MS. Evidence from the animal model experimental autoimmune encephalomyelitis (EAE) and from MS patients indicate that GA affects various levels of the innate and the adaptive immune response, inducing deviation from the pro-inflammatory to the anti-inflammatory pathways. This includes mainly the induction of Th2/3 and T-regulatory cells, and down-regulation of both Th1 and Th17 cells. The immune cells induced by GA reach the CNS and secrete in situ anti-inflammatory cytokines, alleviating the pathological processes. In addition to its immunomodulatory activities, GA promotes neuroprotective repair processes such as secretion of neurotrophic factors, remyelination and neurogenesis, indicating that repair process in the CNS can be up-regulated by therapy.
7. The Evolving Mechanisms of Action of Glatiramer Acetate
Scott S Zamvil,Thomas Prod'homme Cold Spring Harb Perspect Med . 2019 Feb 1;9(2):a029249. doi: 10.1101/cshperspect.a029249.
Glatiramer acetate (GA) is a synthetic amino acid copolymer that is approved for treatment of relapsing remitting multiple sclerosis (RRMS) and clinically isolated syndrome (CIS). GA reduces multiple sclerosis (MS) disease activity and has shown comparable efficacy with high-dose interferon-β. The mechanism of action (MOA) of GA has long been an enigma. Originally, it was recognized that GA treatment promoted expansion of GA-reactive T-helper 2 and regulatory T cells, and induced the release of neurotrophic factors. However, GA treatment influences both innate and adaptive immune compartments, and it is now recognized that antigen-presenting cells (APCs) are the initial cellular targets for GA. The anti-inflammatory (M2) APCs induced following treatment with GA are responsible for the induction of anti-inflammatory T cells that contribute to its therapeutic benefit. Here, we review studies that have shaped our current understanding of the MOA of GA.
8. Glatiramer acetate: A complex drug beyond biologics
Paola Minghetti,Umberto M Musazzi,Paolo Rocco,Ivano Eberini,Silvia Franzè Eur J Pharm Sci . 2019 May 15;133:8-14. doi: 10.1016/j.ejps.2019.03.011.
Complex drugs may be either biological, if the active ingredients are derived from a biological source, or non-biological, if obtained by chemical synthesis. In both cases, their quality depends considerably on the manufacturing process. In the case of Non Biological Complex Drugs (NBCDs), complexity may arise either from the active substance, as in the case of glatiramer acetate, or from other sources, such as the formulation, as in the case of liposomes. In this paper, the case of glatiramer acetate (GA) - a NBCD relevant for clinical and economic reasons - is considered and the differences between US and EU regulatory approaches to GA marketing authorization are highlighted. Indeed, though US and EU regulatory agencies have chosen a generic approach integrated with additional data the implementation is different in the two jurisdictions. In the US, the additional data required are listed in a product specific guideline and copies of Copaxone® have been approved as generics. In the EU, instead regulatory agencies followed a hybrid approach requiring an additional comparative study, and interchangeability policies and substitution schemes have been left to national agencies.

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