Oral administration of GLPG0259, an inhibitor of MAPKAPK5, a new target for the treatment of rheumatoid arthritis: A phase II, randomised, double-blind, placebo-controlled, multicentre trial

Annals of the Rheumatic Diseases

Volumn 72, Issue 5, 2013, Pages 741-744

  Westhovens, René ^a   De Keyser, Filip ^b   Rekalov, Dmytro ^c   Nasonov, Evgeny L ^d   Beetens, Johan ^e   Van Der Aa, Annegret ^e   Wigerinck, Piet ^e   Namour, Florence ^f   Vanhoutte, Frédéric ^e   Durez, Patrick ^g  

^a UNIVERSITY HOSPITALS LEUVEN   (Belgium)

^b GHENT UNIVERSITY HOSPITAL   (Belgium)

^c Zaporizhzhia Regional Hospital   (Ukraine)

^d V A NASONOVA RESEARCH INSTITUTE OF RHEUMATOLOGY   (Russian Federation)

^e US Human Health   (Belgium)

^f Galápagos SASU   (France)

^g UNIVERSITÉ CATHOLIQUE DE LOUVAIN   (Belgium)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIRHEUMATIC AGENT; GLPG 0259; METHOTREXATE; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE KINASE 5; PLACEBO; UNCLASSIFIED DRUG;

ADULT; AGED; ARTICLE; CLINICAL ARTICLE; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG MEGADOSE; DRUG SAFETY; ENZYME INHIBITION; FEMALE; HUMAN; LOW DRUG DOSE; MALE; MULTICENTER STUDY; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL; PROTEIN TARGETING; RANDOMIZATION; RANDOMIZED CONTROLLED TRIAL; RHEUMATOID ARTHRITIS; TREATMENT DURATION; TREATMENT RESPONSE; UNSPECIFIED SIDE EFFECT;

ADMINISTRATION, ORAL; ADULT; AGED; ANTIRHEUMATIC AGENTS; ARTHRITIS, RHEUMATOID; DOUBLE-BLIND METHOD; DRUG THERAPY, COMBINATION; FEMALE; HUMANS; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; MALE; METHOTREXATE; MIDDLE AGED; PLACEBOS; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; TREATMENT FAILURE;

EID: 84875934524     PISSN: 00034967     EISSN: 14682060     Source Type: Journal    
DOI: 10.1136/annrheumdis-2012-202221     Document Type: Article

References (9)

1. Firestein GS. Evolving concepts of rheumatoid arthritis. Nature 2003;423:356-61. (Pubitemid 40852711)
2. Smolen JS, Steiner G. Therapeutic strategies for rheumatoid arthritis. Nat Rev Drug Discov 2003;2:473-88. (Pubitemid 37361728)
3. Smolen JS, Aletaha D, Koeller M, et al. New therapies for treatment of rheumatoid arthritis. Lancet 2007;370:1861-74. (Pubitemid 350180008)
4. Andrews M, Brys R, Vandeghinste N, et al. Small molecules against the novel target MAPKAPK5 show bone protection and anti-inflammatory activity in in vivo models of rheumatoid arthritis. Ann Rheum Dis 2009; 68(Suppl 3):590.
5. Pujuguet P, Vandeghinste N, Dupont S, et al. GLPG0259, an inhibitor of novel target MAPKAPK5, dose-dependently reduces pro-inflammatory cytokines and MMPs and blocks disease progression in vivo. Ann Rheum Dis 2011;70(Suppl 3):275.
6. Namour F, Vanhoutte FP, Beetens J, et al. Pharmacokinetics, safety and tolerability of GLPG0259, a MAPKAPK5 inhibitor, given as single and multiple doses to healthy male subjects. Drugs R D 2012;12:141-63.
7. McInnes IB, Schett G. The pathogenesis of rheumatoid arthritis. N Engl J Med 2011;365:2205-19.
8. Yazici Y, Regens AL. Promising new treatments for rheumatoid arthritis - the kinase inhibitors. Bull NYU Hosp Jt Dis 2011;69:233-7.
9. Landewé RB, Houbiers JG, Van den Bosch F, et al. Intranasal administration of recombinant human cartilage glycoprotein-39 as a treatment for rheumatoid arthritis: a phase II, multicentre, double-blind, randomised, placebo-controlled, parallel-group, dose-finding trial. Ann Rheum Dis 2010;69:1655-9.