Five disease-modifying agents are currently approved for long-term treatment of multiple sclerosis (MS), namely three interferon-beta preparations, glatiramer acetate, and mitoxantrone(1). Pharmacokinetics describes the fate of drugs in the human body by studying their absorption, distribution, metabolism and excretion. Pharmacodynamics is dedicated to the mechanisms of action of drugs. The understanding of the pharmacokinetics and pharmacodynamics of the approved disease-modifying agents against MS is of importance as it might contribute to the development of future derivatives with a potentially higher efficacy and a more favourable safety profile. This article reviews data thus far present both on the pharmacokinetics as well as on the putative mechanisms of action of the interferon-betas, glatiramer acetate, and mitoxantrone in the immunopathogenesis of MS.