Positive Safety and Tolerability for Novel Potentiator GLPG1837
Galapagos NV presents topline Phase 1 results with novel potentiator GLPG1837 at the North American Cystic Fibrosis Conference (NACFC) in Phoenix this week. GLPG1837 was shown to be safe and well-tolerated and demonstrated favorable drug-like properties in the study.
GLPG1837 is a candidate drug for the treatment of the Class III mutation in cystic fibrosis. It is expected that GLPG1837 will be combined with other Galapagos candidate drugs to create a potential triple combination therapy for Class II patients, the largest CF-patient group.
Galapagos conducted a randomized, double-blind, placebo-controlled study over a range of single and multiple doses of GLPG1837 in healthy human volunteers in Belgium. In the single ascending dose (SAD) part of the study subjects were exposed to single oral doses of 30 to 2000 mg. In the multiple ascending dose (MAD) part of the study, GLPG1837 was given orally at doses of 125 to 800 mg twice daily for a period of 14 days.
On safety, GLPG1837 up to a single dose of 2000 mg and up to 800 mg twice daily for 14 days was generally safe and well tolerated in this study. There were no adverse effects observed on ECG, vital signs, or on laboratory parameters. Treatment-emergent adverse events were rare, with the most common adverse events reported being headache and tiredness.
The pharmacokinetics of GLPG1837 also proved favorable in this study. Rapid absorption occurred, with a mean apparent elimination half-life of 6-15 hours. The bioavailability of GLPG1837 was improved with food. Steady state was attained within the second dosing, with no accumulation.
The company believes the results from this Phase 1 study support rapid progression into a Phase 2 study in Class III mutation patients, which is expected to commence before year end 2015.