Glatiramer

Summary

Glatiramer acetate (Copaxone) is an approved disease-modifying therapy for relapsing forms of multiple sclerosis. It is a random synthetic copolymer that mimics myelin basic protein and modulates immune responses, reducing relapse rates and MRI lesion activity. It is administered by subcutaneous injection.

Mechanism of Action

Glatiramer acetate is a mixture of synthetic polypeptides composed of L-glutamic acid, L-alanine, L-tyrosine, and L-lysine in defined molar ratios. It acts as an antigen decoy by binding to MHC class II molecules and inducing T-cell anergy or shift toward anti-inflammatory Th2 regulatory cells, thereby reducing autoimmune attack on myelin in multiple sclerosis.

Routes of Administration

Goals & Uses

• Reduction of relapse rate in relapsing-remitting multiple sclerosisDisease ModificationHigh
• Treatment of clinically isolated syndrome (CIS)Disease ModificationModerate
• Reduction of MRI T2 lesion burdenRadiological OutcomesHigh
• Delay of disability progressionNeurological PreservationModerate

Contraindications

• Hypersensitivity to glatiramer acetate or mannitolAllergy/immunologyHigh

Adverse Effects

• LipoatrophyDermatologicalUncommon
• Injection site reactionsLocalCommon
• Skin necrosisDermatologicalRare
• Anxiety and depressionNeuropsychiatricUncommon
• Immediate post-injection reaction (IPIR)Systemic/cardiovascularUncommon
• LymphadenopathyLymphoreticularUncommon

Drug Interactions

• Live vaccinesModerate
• Immunosuppressants (e.g., azathioprine, methotrexate)Moderate

Population Constraints

• PregnancyReproductive SafetyRelative
• Renal impairmentOrgan ImpairmentRelative
• Pediatric patients (<18 years)AgeRelative
• LactationReproductiveRelative

Regulatory Status

• European UnionApprovedApproved: Relapsing-remitting multiple sclerosisApproved by EMA; available under Copaxone brand and generic equivalents.
• United StatesApprovedApproved: Relapsing forms of multiple sclerosis, including clinically isolated syndrome, relapsing-remitting MS, and active secondary progressive MSOriginal approval 1996 (20 mg/mL daily); 40 mg/mL three-times-weekly approved 2014. Generic Glatopa approved 2015.
• United KingdomApprovedApproved: Relapsing-remitting multiple sclerosisApproved by MHRA; available on NHS with NICE guidance for eligible MS patients.

Approved by the FDA in 1996 for relapsing-remitting MS. Generic versions (e.g., Glatopa) approved by FDA in 2015. Also approved in the EU and many other jurisdictions. Available in 20 mg/mL daily and 40 mg/mL three-times-weekly formulations.

Evidence & Sources

No sources recorded yet.