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GLPG1837

Phase 2

Cystic Fibrosis | Small molecule | Respiratory |Lakefront Biotherapeutics|Last Updated: Dec 7, 2016

Target and mechanism

ModalitySmall molecule

Also known as GLPG1837 as, GLPG1837 single ascending doses, GLPG1837 dose 1

Success Probability

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Market & Valuation

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Trial Design

UNCONTROLLEDDMC
Total Trials2
Total Enrollment33

FDA Designations

No designations recorded

Clinical trial landscape

GLPG1837 · 5 trials · 2 indications

Phase 2 2Phase 1 3
NCT02707562Study of GLPG1837 in Subjects With Cystic Fibrosis (G551D Mutation)Cystic Fibrosis
COMPLETED26 Analytics
NCT02690519Study of GLPG1837 in Subjects With Cystic Fibrosis (S1251N Mutation)Cystic Fibrosis
COMPLETED7 Analytics
PHASE2COMPLETED
Study of GLPG1837 in Subjects With Cystic Fibrosis (G551D Mutation)
Cystic FibrosisUnlock trial analytics
PHASE2COMPLETED
Study of GLPG1837 in Subjects With Cystic Fibrosis (S1251N Mutation)
Cystic FibrosisUnlock trial analytics

Study Endpoints

Primary Endpoints

Changes in adverse events
Up to 9 weeks

To evaluate the safety and tolerability of GLPG1837 in terms of adverse events at every visit

Changes in laboratory parameters
Up to 7 weeks

To evaluate the safety and tolerability of GLPG1837 in terms of abnormal laboratory parameters at every visit

Changes in vital signs - composite outcome measure
Up to 9 weeks

To evaluate the safety and tolerability of GLPG1837 in terms of abnormal vital signs as measured by temperature, blood pressure, heart rate and respiratory rate, at every visit

Changes in physical examination - composite outcome measure
Up to 9 weeks

To evaluate the safety and tolerability of GLPG1837 in terms of abnormalities during physical examination at every visit

Changes in electrocardiogram
Up to 7 weeks

To evaluate the safety and tolerability of GLPG1837 in terms of abnormal electrocardiogram at every visit

Changes in vital signs
Up to 9 weeks

To evaluate the safety and tolerability of GLPG1837 in terms of abnormal vital signs at every visit

Changes in physical examination
Up to 9 weeks

To evaluate the safety and tolerability of GLPG1837 in terms of abnormal physical examination at every visit

The maximum observed concentration (Cmax) of GLPG1837 (metabolite) in plasma
Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837)

To characterize and compare the maximum observed concentration (Cmax) of GLPG1837 (metabolite) in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition

The concentration observed at 24 hours post dose (C24h) of GLPG1837 (metabolite) in plasma
Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 2 (24h post dose) in period 3 (last dose of GLPG1837)

To characterize and compare the concentration observed at 24 hours post dose (C24h) of GLPG1837 (metabolite) in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition

The time of occurrence of Cmax (tmax) of GLPG1837 (metabolite) in plasma
Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837)

To characterize and compare the time of occurrence of Cmax (tmax) of GLPG1837 (metabolite) in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition

The area under the plasma concentration versus time curve (AUC) of GLPG1837 (metabolite) in plasma
Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837)

To characterize and compare the area under the plasma concentration versus time curve of GLPG1837 (metabolite) in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition

The apparent terminal half-life (t1/2) of GLPG1837 (metabolite) in plasma
Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837)

To characterize and compare the apparent terminal half-life of GLPG1837 (metabolite) in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition

The metabolite over GLPG1837 ratios in plasma
Between Day 1 (predose) in period 1 (first dose of GLPG1837) and Day 4 (72h post dose) in period 3 (last dose of GLPG1837)

To characterize and compare the metabolite over GLPG1837 ratios in plasma in male healthy subjects after a single administration of an oral suspension versus an oral tablet formulation in fasted condition, and an oral tablet formulation in fasted versus fed condition

The maximum observed concentration (Cmax) of (1'-OH) Midazolam in plasma before and after multiple oral doses of GLPG1837
Between Day 1 (predose) and Day 13 (24h post last dose on Day 12)

To characterize the maximum observed concentration (Cmax) of (1'-OH) Midazolam in plasma over time before and after multiple doses of GLPG1837 in healthy male subjects

The time of occurrence of Cmax (tmax) of (1'-OH) Midazolam in plasma before and after multiple oral doses of GLPG1837
Between Day 1 (predose) and Day 13 (24h post last dose on Day 12)

To characterize the time of occurrence of Cmax (tmax) of (1'-OH) Midazolam in plasma before and after multiple doses of GLPG1837 in healthy male subjects

The area under the plasma concentration versus time curve (AUC) of (1'-OH) Midazolam before and after multiple oral doses of GLPG1837
Between Day 1 (predose) and Day 13 (24h post last dose on Day 12)

To characterize the area under the plasma concentration versus time curve (AUC) of (1'-OH) Midazolam before and after multiple doses of GLPG1837 in healthy male subjects

The apparent terminal half-life (t1/2) of (1'-OH) Midazolam in plasma before and after multiple oral doses of GLPG1837
Between Day 1 (predose) and Day 13 (24h post last dose on Day 12)

To characterize the apparent terminal half-life (t1/2) of (1'-OH) Midazolam in plasma before and after multiple doses of GLPG1837 in healthy male subjects

Number of subjects with adverse events
Between screening and 7-10 days after the last dose

To evaluate the safety and tolerability of GLPG1837 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of adverse events

Number of subjects with abnormal laboratory parameters
Between screening and 7-10 days after the last dose

To evaluate the safety and tolerability of GLPG1837 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal laboratory parameters

Number of subjects with abnormal vital signs
Between screening and 7-10 days after the last dose

To evaluate the safety and tolerability of GLPG1837 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal vital signs

Number of subjects with abnormal electrocardiogram
Between screening and 7-10 days after the last dose

To evaluate the safety and tolerability of GLPG1837 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal electrocardiograms

Number of subjects with abnormal physical examination
Between screening and 7-10 days after the last dose

To evaluate the safety and tolerability of GLPG1837 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal physical examination

Secondary Endpoints

Changes in sweat chloride concentration
Up to 9 weeks
Changes in pulmonary function (forced expiratory volume in 1 second, FEV1) assessed by spirometry
Up to 9 weeks
Plasma levels of GLPG1837: Cmax, the maximum observed plasma concentration
Up to 3 weeks
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
GLPG1837 dose 1, GLPG1837 dose 2, GLPG1837 dose 3EXPERIMENTALGLPG1837 twice daily oral dosing - morning and evening, for 4 weeks
GLPG1837 dose 1 and GLPG1837 dose 2EXPERIMENTALGLPG1837 twice daily oral dosing - morning and evening, for 4 weeks
GLPG1837 as oral suspension fastedEXPERIMENTALSingle dose of 500 mg GLPG1837 as oral suspension after an overnight fast
GLPG1837 as oral tablet fastedEXPERIMENTALSingle dose of 500 mg GLPG1837 as oral tablet after an overnight fast
GLPG1837 as oral tablet fedEXPERIMENTALSingle dose of 500 mg GLPG1837 as oral tablet after a high-fat high-calorie breakfast
Midazolam and 500 mg GLPG1837EXPERIMENTALEach subject will receive a single oral dose of midazolam (2 mg) on 2 occasions (Days 1 and 12) and multiple oral doses of GLPG1837 (250 mg b.i.d daily for 10 days) from Days 2 to 11.
Midazolam and 1000 mg GLPG1837EXPERIMENTALEach subject will receive a single oral dose of midazolam (2 mg) on 2 occasions (Days 1 and 12) and multiple oral doses of GLPG1837 (500 mg b.i.d daily for 11 days) from Days 2 to 12.
GLPG1837 single doseEXPERIMENTALSingle oral dose of GLPG1837 suspension - ascending doses
Placebo single dosePLACEBO_COMPARATORSingle oral dose of placebo suspension
GLPG1837 muliple dosesEXPERIMENTALMultiple oral doses of GLPG1837 suspension - ascending doses
Placebo multiple dosesPLACEBO_COMPARATORMultiple oral doses of placebo suspension

Interventions

NameTypeDescription
GLPG1837 dose 1DRUGtwo GLPG1837 tablets in the morning and two GLPG1837 tablets in the evening, for one week
GLPG1837 dose 2DRUGtwo GLPG1837 tablets in the morning and two GLPG1837 tablets in the evening, for one week
GLPG1837 dose 3DRUGtwo GLPG1837 tablets in the morning and two GLPG1837 tablets in the evening, for two weeks
500 mg GLPG1837 as oral suspensionDRUGA single dose of 500 mg GLPG1837 administered as oral suspension
500 mg GLPG1837 as oral tabletDRUGA single dose of 500 mg GLPG1837 administered as oral tablet
GLPG1837 500 mgDRUGEach subject will receive multiple oral daily doses of GLPG1837 (250 mg b.i.d. for 11 days) from Days 2 to 12.
MidazolamDRUGEach subject will receive a single oral dose of midazolam (2 mg) on 2 occasions (Days 1 and 12).
GLPG1837 1000 mgDRUGEach subject will receive multiple oral doses of GLPG1837 (500 mg b.i.d. for 11 days) from Days 2 to 12.
GLPG1837 single ascending dosesDRUGSingle dose, oral suspension
Placebo single doseDRUGSingle dose, oral suspension matching placebo
GLPG1837 multiple ascending dosesDRUGMultiple doses, daily for 14 days, oral suspension
Placebo multiple dosesDRUGMultiple doses, daily for 14 days, oral suspension, matching placebo
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites16

Inclusion Criteria: * Male or female subjects ≥ 18 years of age, with a confirmed diagnosis of cystic fibrosis * Subjects with gating G551D CFTR mutation on at least one allele in the CFTR gene * Subjects currently receiving treatment with ivacaftor on a stable regimen or not on a treatment regimen...

Countries:AustraliaCzechiaGermanyIrelandUnited KingdomBelgiumNetherlands
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Competitive Landscape -Cystic Fibrosis 15 trials