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GLPG1972

Phase 2

Osteoarthritis | Small molecule | Musculoskeletal |Lakefront Biotherapeutics|Last Updated: Jul 28, 2021

Target and mechanism

ModalitySmall molecule

Also known as GLPG1972 single ascending doses, GLPG1972 fasted, GLPG1972 fed, GLPG1972 film-coated tablets, GLPG1972 film-coated, [14C]-GLPG1972 solution for infusion, GLPG1972 for infusion, [14C]-GLPG1972 oral solution

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindCONTROLLEDDMC
Total Trials3
Total Enrollment974

FDA Designations

No designations recorded

Clinical trial landscape

GLPG1972 · 7 trials · 2 indications

Phase 2 1Phase 1 6
NCT03595618A Study to Assess Efficacy and Safety of GLPG1972/S201086 in Participants With Knee OsteoarthritisOsteoarthritis
COMPLETED932 Analytics
PHASE2COMPLETED
A Study to Assess Efficacy and Safety of GLPG1972/S201086 in Participants With Knee Osteoarthritis
Osteoarthritis
NCT03595618932
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Study Endpoints

Primary Endpoints

Change From Baseline in Cartilage Thickness of the cMTFC as Assessed by qMRI on the Target Knee to Week 52
Baseline, Week 52

Reduction in cartilage loss was assessed by cartilage thickness as measured in the medial cMTFC of the target knee using qMRI.

Area under the plasma concentration-time curve from time zero until the time corresponding with the last observed quantifiable concentration calculated by the linear up (AUC0-t) ratio between tablet formulations
From Day 1 pre-dose up to Day 4

To assess the bioavailability of two candidate tablet formulations (Tablet B and Tablet C) relative to that of the current tablet formulation (Tablet A) of GLPG1972

Area under the plasma concentration-time curve from time zero to infinity (AUC0-∞) ratio between tablet formulations
From Day 1 pre-dose up to Day 4

To assess the bioavailability of two candidate tablet formulations (Tablet B and Tablet C) relative to that of the current tablet formulation (Tablet A) of GLPG1972

Maximum observed plasma concentration (Cmax) ratio between tablet formulations
From Day 1 pre-dose up to Day 4

To assess the food effect of the selected Phase 3 tablet formulation (in case Tablet B or Tablet C) of GLPG1972

Area under the plasma concentration-time curve from time zero until the time corresponding with the last observed quantifiable concentration calculated by the linear up (AUC0-t) ratio between fed and fasted
From Day 1 pre-dose up to Day 4

To assess the food effect of the selected Phase 3 tablet formulation (in case Tablet B or Tablet C) of GLPG1972

Area under the plasma concentration-time curve from time zero to infinity (AUC0-∞) ratio between fed and fasted
From Day 1 pre-dose up to Day 4

To assess the food effect of the selected Phase 3 tablet formulation (in case Tablet B or Tablet C) of GLPG1972

Maximum observed plasma concentration (Cmax) ratio between fed and fasted
From Day 1 pre-dose up to Day 4

To assess the bioavailability of two candidate tablet formulations (Tablet B and Tablet C) relative to that of the current tablet formulation (Tablet A) of GLPG1972

Change of total radioactivity excreted in urine and feces combined (Period 2)
From Day 1 pre-dose up to Day 10

To assess the mass balance, using \[14C\]-GLPG1972

Maximum observed plasma concentration (Cmax) of total radioactivity (Period 2)
From Day 1 pre-dose up to Day 10

To assess the pharmacokinetics (PK) of GLPG1972 and its main metabolites in plasma

Cmax of GLPG1972 (Period 2)
From Day 1 pre-dose up to Day 10

To assess the PK of GLPG1972 and its main metabolites in plasma

Area under the plasma concentration-time curve (AUC) of total radioactivity (Period 2)
From Day 1 pre-dose up to Day 10

To assess the PK of GLPG1972 and its main metabolites in plasma

AUC of GLPG1972 (Period 2)
From Day 1 pre-dose up to Day 10

To assess the PK of GLPG1972 and its main metabolites in plasma

Change in amount of [14C]-GLPG1972 excreted in urine and feces combined (μg) from baseline at Day 7 (Part 2)
From Day 1 pre-dose up to Day 7

To characterize the elimination pathways and metabolite profile of GLPG1972

Difference between GLPG1972 treated subjects and placebo subjects in the number of Adverse Events
From screening until the final follow up visit (day 50)

To assess safety and tolerability of GLPG1972 in OA patients

Difference in the number of GLPG1972 treated subjects and placebo subjects with abnormal vital signs
From screening until the final follow up visit (day 50)

To assess safety and tolerability of GLPG1972 in OA patients

Difference in the number of GLPG1972 treated subjects and placebo subjects with abnormal clinical laboratory evaluations
Screening, Days -1, 2, 4, 8, 9, 15, 22, 29, 43 and the final follow up visit (day 50)

To assess safety and tolerability of GLPG1972 in OA patients

Difference in the number of GLPG1972 treated subjects and placebo subjects with abnormal physical examination
Screening, days -1, 1, 2, 8, 15, 22, 29, 43 and the final follow up visit (day 50

To assess safety and tolerability of GLPG1972 in OA patients

Difference in the number of GLPG1972 treated subjects and placebo subjects with abnormal ECG
Screening, days 1, 2, 3, 4, 8, 15, 22, 29, 43 and the final follow up visit (day 50)

To assess safety and tolerability of GLPG1972 in OA patients

Difference in the number of GLPG1972 treated subjects and placebo subjects with abnormal Holter assessment
Day -1 to days 1 and Day 10 to day 11

To assess safety and tolerability of GLPG1972 in OA patients

The maximum observed plasma concentration of GLPG1972 (Cmax)
Days 1, 2, 3, 4, 6, 8, 10, 15, 16, 22, 29 and 43

To assess PK of GLPG1972 in OA patients

The time (tmax) to reach Cmax of GLPG1972
Days 1, 2, 3, 4, 6, 8, 10, 15, 16, 22, 29 and 43

To assess PK of GLPG1972 in OA patients

The plasma concentration of GLPG1972 24 after the last dose
Days 1, 2, 3, 4, 6, 8, 10, 15, 16, 22, 29 and 43

To assess PK of GLPG1972 in OA patients

The area under the plasma concentration time curve from time 0 until the last quantifieble dose
Days 1, 2, 3, 4, 6, 8, 10, 15, 16, 22, 29 and 43

To assess PK of GLPG1972 in OA patients

Assessment of the maximum observed plasma concentration of GLPG1972 after single oral doses
on day 1 pre-dose and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post doses

Determine bioavailability of GLPG1972 by assessing PK parameters

Assessment of plasma concentration of GLPG1972 24hrs post-dose after single oral doses
At 24 hours post dose

Determine bioavailability of GLPG1972 by assessing PK parameters

Assessment of time to achieve the maximal plasma concentration of GLPG1972 after single oral doses
on day 1 pre-dose and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post doses

Determine bioavailability of GLPG1972 by assessing PK parameters

Assessment of the last quantifiable plasma concentration of GLPG1972 after single oral doses
on day 1 pre-dose and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post doses

Determine bioavailability of GLPG1972 by assessing PK parameters

Maximum observed plasma concentration (Cmax) of GLPG1972
From pre-dose (period 1) until 6 days after the last dose (period 3)

To study the pharmacokinetics of 600 mg GLPG1972 administered as oral liquid solution or as oral tablet after overnight fasting or administered as oral tablet after a high-fat high calorie breakfast

Plasma concentration of GLPG1972 24 hours after dosing
24 hours after each dose

To study the pharmacokinetics of 600 mg GLPG1972 administered as oral liquid solution or as oral tablet after overnight fasting or administered as oral tablet after a high-fat high calorie breakfast

The time of the occurrence of Cmax of GLPG1972
From pre-dose (period 1) until 6 days after the last dose (period 3)

To study the pharmacokinetics of 600 mg GLPG1972 administered as oral liquid solution or as oral tablet after overnight fasting or administered as oral tablet after a high-fat high calorie breakfast

The area under the plasma concentration versus time curve
From pre-dose until 6 days post-dose for each dosing period

To study the pharmacokinetics of 600 mg GLPG1972 administered as oral liquid solution or as oral tablet after overnight fasting or administered as oral tablet after a high-fat high calorie breakfast

The apparent terminal half-life of GLPG1972
From pre-dose (period 1) until 6 days after the last dose (period 3)

To study the pharmacokinetics of 600 mg GLPG1972 administered as oral liquid solution or as oral tablet after overnight fasting or administered as oral tablet after a high-fat high calorie breakfast

The number of adverse events reported
From pre-dose until the Follow up (FU) visit anticipated to take place 7-10 days after the last dose

To evaluate safety and tolerability of single oral doses of GLPG1972

Changes in clinical laboratory evaluations
From pre-dose until the Follow up (FU) visit anticipated to take place 7-10 days after the last dose

To evaluate safety and tolerability of single oral doses of GLPG1972

Changes in vital signs
From pre-dose until the Follow up (FU) visit anticipated to take place 7-10 days after the last dose

To evaluate safety and tolerability of single oral doses of GLPG1972

Changes in physical examination parameters
From pre-dose until the Follow up (FU) visit anticipated to take place 7-10 days after the last dose

To evaluate safety and tolerability of single oral doses of GLPG1972

Changes in ECG parameters
From pre-dose until the Follow up (FU) visit anticipated to take place 7-10 days after the last dose

To evaluate safety and tolerability of single oral doses of GLPG1972

Change versus placebo in number of subjects with adverse events
Between screening and 7-10 days after the last dose

To evaluate the safety and tolerability of GLPG1972 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of adverse events

Change versus placebo in number of subjects with abnormal laboratory parameters
Between screening and 7-10 days after the last dose

To evaluate the safety and tolerability of GLPG1972 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal laboratory parameters

Change versus placebo in number of subjects with abnormal vital signs
Between screening and 7-10 days after the last dose

To evaluate the safety and tolerability of GLPG1972 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal vital signs

Change versus placebo in number of subjects with abnormal electrocardiogram
Between screening and 7-10 days after the last dose

To evaluate the safety and tolerability of GLPG1972 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal electrocardiograms

Change versus placebo in number of subjects with abnormal physical examination
Between screening and 7-10 days after the last dose

To evaluate the safety and tolerability of GLPG1972 in comparison with placebo after a single oral dose and multiple oral doses in healthy subjects in terms of abnormal physical examination

Secondary Endpoints

Number of Participants Who Were Osteoarthritis (OA) Structural Progressors Based on Cartilage Thickness in the cMTFC Assessed by qMRI on the Target Knee
Week 52
Change From Baseline in Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) Total Score and Subscales Scores for Pain, Function, and Stiffness to Week 52
Baseline, Week 52
Change From Baseline in Pain Assessment in the Target Knee as Measured by Visual Analog Scale (VAS) to Week 52
Baseline, Week 52
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Study Design & Arms

AllocationRANDOMIZED
MaskingQUADRUPLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
GLPG1972 75 mgEXPERIMENTALParticipants received 1 film-coated tablet of GLPG1972 75 mg and 3 GLPG1972 matching placebo tablets, orally once daily for 52 weeks.
GLPG1972 150 mgEXPERIMENTALParticipants received 2 film-coated tablets of GLPG1972 75 mg (total dose 150 mg) and 2 GLPG1972 matching placebo tablets, orally once daily for 52 weeks.
GLPG1972 300 mgEXPERIMENTALParticipants received 4 film-coated tablets of GLPG1972 75 mg (total dose 300 mg), orally once daily for 52 weeks.
PlaceboPLACEBO_COMPARATORParticipants received 4 film-coated tablets of GLPG1972 matching placebo, orally once daily for 52 weeks.
Tablet AEXPERIMENTALA single oral 300-mg dose of GLPG1972 in fasted state
Tablet BEXPERIMENTALA single oral 300-mg dose of GLPG1972 in fasted state
Tablet CEXPERIMENTALA single oral 300-mg dose of GLPG1972 in fasted state
Food effectEXPERIMENTALselected tablet B or C under fed conditions
GLPG1972 oral and [14C]-GLPG1972 IVEXPERIMENTALGLPG1972 film-coated tablet followed by \[14C\]-GLPG1972 solution for infusion
[14C]-GLPG1972 oral solutionEXPERIMENTAL\[14C\]-GLPG1972 oral solution
GLPG1972EXPERIMENTAL -
Treatment AEXPERIMENTALGLPG1972 oral solution after overnight fast
Treatment BEXPERIMENTALGLPG1972 oral DC tablet after breakfast
Treatment CEXPERIMENTALGLPG1972 oral WG tablet after overnight fast
Treatment DEXPERIMENTALGLPG1972 oral WG tablet after breakfast
GLPG1972 600 mg oral solution fastedEXPERIMENTAL600 mg GLPG1972 administered as oral solution after overnight fasting
GLPG1972 600 mg oral tablet fastedEXPERIMENTAL600 mg GLPG1972 administered as oral tablet after overnight fasting
GLPG1972 600 mg oral tablet fedEXPERIMENTAL600 mg GLPG1972 administered as oral tablet after a high-fat high-calorie breakfast
GLPG1972 single doseEXPERIMENTALSingle oral dose of GLPG1972 solution - ascending doses
Placebo single dosePLACEBO_COMPARATORSingle oral dose of placebo solution
GLPG1972 multiple dosesEXPERIMENTALMultiple oral doses of GLPG1972 solution - ascending doses
Placebo multiple dosesPLACEBO_COMPARATORMultiple oral doses of placebo solution

Interventions

NameTypeDescription
GLPG1972DRUGFilm-coated tablets of GLPG1972 for oral use.
PlaceboDRUGFilm-coated tablets of matching placebo for oral use.
GLPG1972 - ADRUGFilm-coated tablet, formulation A
GLPG1972 - BDRUGFilm-coated tablet, formulation B
GLPG1972 - CDRUGFilm-coated tablet, formulation C
GLPG1972 film-coated tabletsDRUGsingle oral dose of GLPG1972
[14C]-GLPG1972 solution for infusionDRUGa 15-minute IV infusion \[14C\]-GLPG1972
[14C]-GLPG1972 oral solutionDRUGsingle oral dose of \[14C\]-GLPG1972
GLPG1972 cohort 1DRUGGLPG1972 dose 1 provided as oral tablets q.d.
GLPG1972 cohort 2DRUGGLPG1972 dose 2 provided as oral tablets q.d.
GLPG1972 cohort 3DRUGGLPG1972 dose 3 provided as oral tablets q.d.
GLPG1972 600 mg oral solution fastedDRUGdosing after overnight fasting
GLPG1972 600 mg oral tablet fastedDRUGdosing after overnight fasting
GLPG1972 600 mg oral tablet fedDRUGdosing after high-fat high-calorie breakfast
GLPG1972 single ascending dosesDRUGsingle dose, oral solution
Placebo single doseDRUGsingle dose, oral solution, matching placebo
GLPG1972 multiple ascending dosesDRUGmultiple doses, daily for 14 days, oral solution
Placebo multiple dosesDRUGmultiple doses, daily for 14 days, oral solution
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Eligibility Criteria

Age Range40 Years to 75 Years
SexALL
Healthy VolunteersNo
Study Sites44

Inclusion Criteria: * Male participants or female participants of non-childbearing potential and not breastfeeding. * Body weight \> 40 kg, body mass index (BMI) \< 40 kg/m\^2. * Diagnosed for knee osteoarthritis based on clinical and radiological criteria of the American College of Rheumatology. *...

Countries:United StatesUnited KingdomBelgiumNetherlands
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Competitive Landscape -Osteoarthritis 114 trials

Top 5 of 13 competitors

CompanyTickerTrialsLead PhaseDrugs
Eli Lilly and CompanyLLY3PHASE3Eloralintide and Tirzepatide, Orforglipron, LY3016859, LY3556050, LY3526318
Pacira Biosciences, Inc.PCRX4PHASE3ZILRETTA, Enekinragene Inzadenovec, FX201
Novo Nordisk A/S Sponsored ADR Class BNVO1PHASE3NNC0487-0111
Bioventus, Inc. Class ABVS1PHASE2PTP-001
Enlivex Ltd.ENLV2PHASE1Allocetra
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