title: Laquinimod in the treatment of relapsing remitting multiple sclerosis.
abstract: BACKGROUND
  Laquinimod is a new once-daily oral administrable agent, which is under investigation in a phase 3 clinical trial for relapsing remitting multiple sclerosis (RRMS) and in a phase 2 clinical trial for primary progressive MS (PPMS).
  
  
  METHODS
  The pharmacokinetic, pharmacodynamic and the safety profiles of laquinimod are covered in this review. In preclinical studies, the ability to prevent both experimental autoimmune encephalomyelitis and experimental autoimmune neuritis has been demonstrated. Reduced cell infiltration, demyelination, axonal damage and a shift of T-helper cell responses have been shown. Accordingly, in human studies, a decrease of pro-inflammatory and an increase of anti-inflammatory cytokines have been measured and a significant reduction of disease progression and a decrease in brain volume loss has been demonstrated. During all clinical studies a favorable safety profile was observed for 0.6mg laquinimod. New information about cardiovascular events is prompting the discontinuation of higher dosing regimens in both ongoing trials.
  
  
  CONCLUSIONS
  Laquinimod is a first in class oral agent with high potential to reduce disease progression in RRMS and PPMS. Owing to its favorable safety profile, a combination with 0.6mg laquinimod and other disease modifying therapies could be an option in future MS therapy.
authors.affiliation: a Department of Neurology, Multiple Sclerosis Center, Center of Clinical Neuroscience, University Hospital Carl Gustav Carus , Dresden University of Technology , Dresden , Germany.
authors.forename: Undine
authors.initials: U
authors.lastname: Hainke
authors.affiliation: a Department of Neurology, Multiple Sclerosis Center, Center of Clinical Neuroscience, University Hospital Carl Gustav Carus , Dresden University of Technology , Dresden , Germany.
authors.forename: Katja
authors.initials: K
authors.lastname: Thomas
authors.affiliation: a Department of Neurology, Multiple Sclerosis Center, Center of Clinical Neuroscience, University Hospital Carl Gustav Carus , Dresden University of Technology , Dresden , Germany.
authors.forename: Tjalf
authors.initials: T
authors.lastname: Ziemssen
mesh_terms: D000284:Administration, Oral; D000818:Animals; D004195:Disease Models, Animal; D018450:Disease Progression; D004681:Encephalomyelitis, Autoimmune, Experimental / Q000517:prevention & control; D006801:Humans; D007155:Immunologic Factors / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics; D020528:Multiple Sclerosis, Chronic Progressive / Q000188:drug therapy* / Q000503:physiopathology; D020529:Multiple Sclerosis, Relapsing-Remitting / Q000188:drug therapy* / Q000503:physiopathology; D009444:Neuritis, Autoimmune, Experimental / Q000517:prevention & control; D015363:Quinolones / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics
chemical_list: D007155:Immunologic Factors; D015363:Quinolones; C476223:laquinimod
keywords: Cytokines; MRI; demyelination; immunomodulation; laquinimod; neuroprotection