GLPG0634 is selective inhibitor of
Janus kinase 1 (JAK-1) and I have been quite thrilled by this new drug since
the ACR 2012 in Washington. The big news is, GLPG0634 has a name now:
filgotinib.
F. Namour and colleagues presented [THU0123]:
"DOSE SELECTION OF GLPG0634, A SELECTIVE JAK1 INHIBITOR, FOR RHEUMATOID
ARTHRITIS PHASE 2B STUDIES: PK/PD AND EXPOSURE-DAS28 MODELING APPROACH".
Conclusions: "Current modelling and simulation on the basis of
early clinical data suggests that the pharmacokinetics of GLPG0634 is dose
proportional at doses up to 200 mg QD, in agreement with observed data, and
shows that both GLPG0634 and its main metabolite contribute to biomarker
response. Simulations of the pSTAT1 and DAS28 dose-response relation suggest
that the efficacy is favorable up to a daily dose of 200 mg GLPG0634, with
clinical response in the range of that observed with registered compounds. A
daily dose range from 50 to 200 mg is currently being tested in the DARWIN
Phase 2B program."
C. Belleville-Da-Costa and
colleagues presented [THU0138]: "GLPG0634M1, A MAJOR METABOLITE OF THE
JAK1-SELECTIVE INHIBITOR GLPG0634, IS ALSO JAK1-SELECTIVE AND EFFICIENT IN THE
RAT CIA MODEL". I skip this one.
F. Namour and colleagues presented [AB0460]: "GLPG0634, A
SELECTIVE JAK1 INHIBITOR, CONFIRMS ITS LOW LIABILITY FOR DRUG-DRUG
INTERACTIONS". Let's skip this one, too.
Darwin returned from his voyage with the beagle in
1836 and published his abstract "On the Origin
of Species by Means of Natural Selection, or The Preservation of Favoured Races
in the Struggle for Life" in 1859. Let's hope that the DARWIN study will
publish results more quickly.
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