The pharmacokinetics of glatiramer acetate for multiple sclerosis treatment

Abstract

Introduction: Multiple sclerosis (MS) is a T-cell-mediated disease affecting the central nervous system (CNS), characterized by demyelination and axonal degeneration. INF-β1b was the first drug approved for MS patients in 1993. In 1996, glatiramer acetate (GA), a synthetic copolymer, was approved in the USA for the treatment of relapsing-remitting MS (RRMS) and clinically isolated syndrome (CIS). Although the immunological action of GA has been fully investigated, the exact mechanisms of action of GA are still not completely elucidated. Several in vitro studies on mice and human antigen-presenting cells (APCs) have shown that GA is able to bind to the major histocompatibility complex (MHC), on the surface of APCs, recognizing myelin basic protein (MBP).

Areas covered: This review explores the pharmacological characteristics of GA, its mechanism of action and its pharmacokinetics properties. The article also provides information on the efficacy, tolerability and an overview of the most important clinical data on GA.

Expert opinion: Despite the development of novel compounds, it is not surprising that GA is, to date, one of the most prescribed drugs for RRMS patients and CIS patients. The proven efficacy and the mild adverse events, makes GA a good therapeutic option in the early stage of the disease. This is particularly useful for patients who suffer flu-like symptoms from other RRMS therapies as an alternative.

Keywords::

• clinically isolated syndrome
• glatiramer acetate
• immunomodulator
• multiple sclerosis
• pharmacodynamics
• pharmacokinetics
• relapsing-remitting.