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Phase 1 Completed N=20 Treatment

Evaluation of Pharmacokinetic Interaction Between GSK3640254 and Caffeine, Metoprolol, Montelukast, Flurbiprofen, Omeprazole, Midazolam, Digoxin, and Pravastatin in Healthy Adults

Source: ClinicalTrials.gov NCT04425902 ↗
Enrolled (actual)
20
Serious AEs
0.0%
Results posted
May 2022
Primary outcomePrimary: Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to Time t (AUC[0-t]) for Caffeine — 37970; 42230 Hour*nanograms per milliliter (h*ng/mL)

Summary

This is an open-label, single sequence study that is being conducted to investigate the potential drug-drug interaction (DDI) when GSK3640254 is co-administered with a cocktail of cytochrome P450 (CYP) enzymes and transporter probe substrates in healthy participants. This study will aid in understanding these interactions and resulting changes in exposure (if any) when drugs that are metabolized via these pathways are given in combination with GSK3640254. The study will consist of a Screening period and 3 sequential treatment regimens. Participants will be administered a single dose of probe substrate drugs (caffeine 200 milligram (mg), metoprolol 100 mg, montelukast 10 mg, flurbiprofen 100 mg, omeprazole 40 mg, midazolam 5 mg, digoxin 0.25 mg and pravastatin 40 mg) on Day 1. Participants will then receive GSK3640254 200 mg once daily on Days 11 to 20 followed by co-administration of probe substrate drugs with GSK3640254 on Day 21.

Outcome Measures

OutcomeResultp-value
PRIMARY
Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to Time t (AUC[0-t]) for Caffeine
37970; 42230
PRIMARY
AUC From Time Zero Extrapolated to Infinity (AUC[0-infinity]) for Caffeine
39720; 44440
PRIMARY
Maximum Observed Plasma Concentration (Cmax) for Caffeine
4340; 4110
PRIMARY
Time to Cmax (Tmax) for Caffeine
2.000; 3.000
PRIMARY
Apparent Terminal Phase Half-life (t1/2) for Caffeine
5.380; 6.085
PRIMARY
AUC(0-t) for Metoprolol
655.0; 807.3
PRIMARY
AUC(0-infinity) for Metoprolol
659.1; 813.1
PRIMARY
Cmax for Metoprolol
127.4; 141.1
PRIMARY
Tmax for Metoprolol
2.000; 3.000
PRIMARY
t1/2 for Metoprolol
4.872; 5.342
PRIMARY
AUC(0-t) for Montelukast
2724; 2940
PRIMARY
AUC(0-infinity) for Montelukast
2859; 3109
PRIMARY
Cmax for Montelukast
379.8; 393.5
PRIMARY
Tmax for Montelukast
5.000; 6.000
PRIMARY
t1/2 for Montelukast
5.035; 5.135
PRIMARY
AUC(0-t) for Flurbiprofen
64930; 66170
PRIMARY
AUC(0-infinity) for Flurbiprofen
66700; 68660
PRIMARY
Cmax for Flurbiprofen
10220; 10710
PRIMARY
Tmax for Flurbiprofen
3.000; 4.000
PRIMARY
t1/2 for Flurbiprofen
6.123; 6.088
PRIMARY
AUC(0-t) for Omeprazole
728.1; 817.9
PRIMARY
AUC(0-infinity) for Omeprazole
1127; 1093
PRIMARY
Cmax for Omeprazole
224.4; 256.6
PRIMARY
Tmax for Omeprazole
6.000; 6.000
PRIMARY
t1/2 for Omeprazole
1.439; 1.219
PRIMARY
AUC(0-t) for Midazolam
67.11; 62.95
PRIMARY
AUC(0-infinity) for Midazolam
70.08; 65.46
PRIMARY
Cmax for Midazolam
15.44; 13.95
PRIMARY
Tmax for Midazolam
1.000; 1.000
PRIMARY
t1/2 for Midazolam
5.756; 5.222
PRIMARY
AUC(0-t) for Digoxin
16690; 17840
PRIMARY
AUC(0-infinity) for Digoxin
19180; 20090
PRIMARY
Cmax for Digoxin
1026; 1282
PRIMARY
Tmax for Digoxin
3.000; 2.000
PRIMARY
t1/2 for Digoxin
40.279; 38.784
PRIMARY
AUC(0-t) for Pravastatin
69.92; 51.03
PRIMARY
AUC(0-infinity) for Pravastatin
72.09; 43.70
PRIMARY
Cmax for Pravastatin
19.45; 15.19
PRIMARY
Tmax for Pravastatin
1.500; 3.000
PRIMARY
t1/2 for Pravastatin
3.189; 3.156
SECONDARY
Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
1; 5; 5; 0; 0; 0
SECONDARY
Treatment A: Absolute Values of Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
258.6; 265.9; 5.64; 6.30; 3.1504; 3.7430
SECONDARY
Treatment B: Absolute Values of Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
265.9; 261.9; 6.30; 5.79; 3.7430; 3.2680
SECONDARY
Treatment C: Absolute Values of Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
262.3; 249.2; 260.7; 5.86; 5.81; 5.98
SECONDARY
Treatment A: Absolute Values of Hematocrit
0.4188; 0.4098
SECONDARY
Treatment B: Absolute Values of Hematocrit
0.4098; 0.4216
SECONDARY
Treatment C: Absolute Values of Hematocrit
0.4239; 0.4022; 0.4168
SECONDARY
Treatment A: Absolute Values of Hemoglobin
141.9; 137.7
SECONDARY
Treatment B: Absolute Values of Hemoglobin
137.7; 140.0
SECONDARY
Treatment C: Absolute Values of Hemoglobin
140.6; 134.7; 138.3
SECONDARY
Treatment A: Absolute Values of Erythrocytes
4.836; 4.664
SECONDARY
Treatment B: Absolute Values of Erythrocytes
4.664; 4.746
SECONDARY
Treatment C: Absolute Values of Erythrocytes
4.769; 4.608; 4.756
SECONDARY
Treatment A: Absolute Values of Erythrocytes Mean Corpuscular Volume
86.71; 88.02
SECONDARY
Treatment B: Absolute Values of Erythrocytes Mean Corpuscular Volume
88.02; 88.96
SECONDARY
Treatment C: Absolute Values of Erythrocytes Mean Corpuscular Volume
89.03; 87.38; 87.74
SECONDARY
Treatment A: Absolute Values of Erythrocytes Mean Corpuscular Hemoglobin
29.37; 29.57
SECONDARY
Treatment B: Absolute Values of Erythrocytes Mean Corpuscular Hemoglobin
29.57; 29.52
SECONDARY
Treatment C: Absolute Values of Erythrocytes Mean Corpuscular Hemoglobin
29.51; 29.28; 29.12
SECONDARY
Treatment A: Absolute Values of Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
5.0348; 4.8211; 104.1; 25.4; 4.4570; 3.8118
SECONDARY
Treatment B: Absolute Values of Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
4.8211; 4.7378; 25.4; 24.9; 3.8118; 3.6915
SECONDARY
Treatment C: Absolute Values of Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
4.7184; 4.8060; 4.8703; 24.9; 25.4; 26.2
SECONDARY
Treatment A: Absolute Values of Urate, Creatinine, Bilirubin, Direct Bilirubin
347.3632; 365.5046; 84.9524; 86.4110; 9.8325; 8.0028
SECONDARY
Treatment B: Absolute Values of Urate, Creatinine, Bilirubin, Direct Bilirubin
365.5046; 337.8464; 86.4110; 90.7868; 8.0028; 8.6184
SECONDARY
Treatment C: Absolute Values of Urate, Creatinine, Bilirubin, Direct Bilirubin
343.1057; 303.0349; 340.6013; 92.1686; 87.3764; 90.5867
SECONDARY
Treatment A: Absolute Values of Albumin, Globulin, Protein
42.9; 42.2; 27.4; 25.9; 70.3; 68.1
SECONDARY
Treatment B: Absolute Values of Albumin, Globulin, Protein
42.2; 41.4; 25.9; 26.8; 68.1; 68.2
SECONDARY
Treatment C: Absolute Values of Albumin, Globulin, Protein
41.6; 40.5; 42.0; 26.9; 25.1; 26.6
SECONDARY
Treatment A: Absolute Values of Creatine Kinase, Lactate Dehydrogenase, Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), Gamma-glutamyl Transferase
103.7; 66.9; 131.3; 114.8; 15.6; 20.1
SECONDARY
Treatment B: Absolute Values of Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase
66.9; 68.9; 114.8; 115.9; 20.1; 20.3
SECONDARY
Treatment C: Absolute Values of Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase
71.3; 65.7; 63.8; 116.6; 120.6; 119.3
SECONDARY
Treatment A: Absolute Values of Amylase, Lipase
29.4; 31.6; 59.5; 56.9
SECONDARY
Treatment B: Absolute Values of Amylase, Lipase
31.6; 32.4; 56.9; 60.1
SECONDARY
Treatment C: Absolute Values of Amylase, Lipase
32.9; 33.5; 33.1; 62.2; 64.7; 60.7
SECONDARY
Treatment A: Change From Baseline in Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
7.3; 0.66; 0.5926; 0.0748; -0.0375; 0.0150
SECONDARY
Treatment B: Change From Baseline in Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
-4.1; -0.51; -0.4750; -0.0610; -0.0080; 0.0310
SECONDARY
Treatment C: Change From Baseline in Platelet Count, Leukocyte Count, Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils
-13.1; -1.6; -0.05; 0.12; -0.1254; 0.1351
SECONDARY
Treatment A: Change From Baseline in Hematocrit
-0.0090
SECONDARY
Treatment B: Change From Baseline in Hematocrit
0.0118
SECONDARY
Treatment C: Change From Baseline in Hematocrit
-0.0217; -0.0071
SECONDARY
Treatment A: Change From Baseline in Hemoglobin
-4.2
SECONDARY
Treatment B: Change From Baseline in Hemoglobin
2.3
SECONDARY
Treatment C: Change From Baseline in Hemoglobin
-5.8; -2.3
SECONDARY
Treatment A: Change From Baseline in Erythrocytes
-0.172
SECONDARY
Treatment B: Change From Baseline in Erythrocytes
0.083
SECONDARY
Treatment C: Change From Baseline in Erythrocytes
-0.161; -0.013
SECONDARY
Treatment A: Change From Baseline in Erythrocytes Mean Corpuscular Volume
1.31
SECONDARY
Treatment B: Change From Baseline in Erythrocytes Mean Corpuscular Volume
0.94
SECONDARY
Treatment C: Change From Baseline in Erythrocytes Mean Corpuscular Volume
-1.64; -1.28
SECONDARY
Treatment A: Change From Baseline in Erythrocytes Mean Corpuscular Hemoglobin
0.20
SECONDARY
Treatment B: Change From Baseline in Erythrocytes Mean Corpuscular Hemoglobin
-0.05
SECONDARY
Treatment C: Change From Baseline in Erythrocytes Mean Corpuscular Hemoglobin
-0.23; -0.39
SECONDARY
Treatment A: Change From Baseline in Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
-0.2137; -78.7; -0.6452; -0.0418; 5.9; -0.0624
SECONDARY
Treatment B: Change From Baseline in Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
-0.0833; -0.6; -0.1203; -0.0989; 0.8; 0.0000
SECONDARY
Treatment C: Change From Baseline in Glucose, Carbon Dioxide, Cholesterol, Triglycerides, Anion Gap, Calcium, Chloride, Phosphate, Potassium, Sodium, Urea
0.0876; 0.1519; 0.5; 1.2; -0.4355; -0.2926
SECONDARY
Treatment A: Change From Baseline in Urate, Creatinine, Bilirubin, Direct Bilirubin
18.1414; 1.4586; -1.8297; -0.3506
SECONDARY
Treatment B: Change From Baseline in Urate, Creatinine, Bilirubin, Direct Bilirubin
-27.6582; 4.3758; 0.6156; 0.1112
SECONDARY
Treatment C: Change From Baseline in Urate, Creatinine, Bilirubin, Direct Bilirubin
-40.0707; -2.5044; -4.7922; -1.5819; 1.1340; 0.2880
SECONDARY
Treatment A: Change From Baseline in Albumin, Globulin, Protein
-0.7; -1.5; -2.2
SECONDARY
Treatment B: Change From Baseline in Albumin, Globulin, Protein
-0.9; 0.9; 0.1
SECONDARY
Treatment C: Change From Baseline in Albumin, Globulin, Protein
-1.1; 0.4; -1.8; -0.3; -2.9; 0.2
SECONDARY
Treatment A: Change From Baseline in Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase
-36.9; -16.5; 4.5; -1.9; 1.0; -0.2
SECONDARY
Treatment B: Change From Baseline in Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase
2.1; 1.1; 0.3; -2.4; 0.6; -0.6
SECONDARY
Treatment C: Change From Baseline in Creatine Kinase, Lactate Dehydrogenase, ALT, ALP, AST, Gamma-glutamyl Transferase
-5.6; -7.5; 4.0; 2.6; -3.1; 0.5
SECONDARY
Treatment A: Change From Baseline in Amylase, Lipase
2.2; -2.6
SECONDARY
Treatment B: Change From Baseline in Amylase, Lipase
0.9; 3.2
SECONDARY
Treatment C: Change From Baseline in Amylase, Lipase
0.6; 0.2; 2.5; -1.5
SECONDARY
Treatment A: Absolute Values for Electrocardiogram (ECG) Parameters: PR Interval, QRS Duration, QT Interval, Corrected QT Interval Using Fridericia's Formula (QTcF)
154.8; 158.2; 92.5; 95.0; 391.2; 398.3
SECONDARY
Treatment B: Absolute Values for ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF Interval
158.6; 161.8; 94.2; 96.4; 403.1; 408.8
SECONDARY
Treatment C: Absolute Values for ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF Interval
160.8; 162.3; 159.6; 95.8; 98.7; 96.8
SECONDARY
Treatment A: Change From Baseline in ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF
3.4; 2.5; 7.1; 4.8
SECONDARY
Treatment B: Change From Baseline in ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF
3.2; 2.3; 5.7; 5.1
SECONDARY
Treatment C: Change From Baseline in ECG Parameters: PR Interval, QRS Duration, QT Interval, QTcF
1.5; -1.2; 2.9; 1.0; 18.0; -3.9
SECONDARY
Treatment A: Absolute Values of Oral Temperature
36.38; 36.26
SECONDARY
Treatment B: Absolute Values of Oral Temperature
36.31; 36.28
SECONDARY
Treatment C: Absolute Values of Oral Temperature
36.31; 36.18; 36.31
SECONDARY
Treatment A: Absolute Values of Pulse Rate
64.5; 65.0
SECONDARY
Treatment B: Absolute Values of Pulse Rate
61.6; 62.8
SECONDARY
Treatment C: Absolute Values of Pulse Rate
63.2; 56.2; 61.7
SECONDARY
Treatment A: Absolute Values of Respiratory Rate
16.1; 15.8
SECONDARY
Treatment B: Absolute Values of Respiratory Rate
15.0; 14.7
SECONDARY
Treatment C: Absolute Values of Respiratory Rate
15.7; 15.7; 16.5
SECONDARY
Treatment A: Absolute Values of Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
111.0; 107.7; 65.1; 59.7
SECONDARY
Treatment B: Absolute Values of SBP and DBP
107.7; 107.2; 61.6; 59.6
SECONDARY
Treatment C: Absolute Values of SBP and DBP
107.5; 105.6; 109.7; 62.7; 58.4; 62.2
SECONDARY
Treatment A: Change From Baseline in Oral Temperature
-0.12
SECONDARY
Treatment B: Change From Baseline in Oral Temperature
-0.03
SECONDARY
Treatment C: Change From Baseline in Oral Temperature
-0.13; 0.01
SECONDARY
Treatment A: Change From Baseline in Pulse Rate
0.5
SECONDARY
Treatment B: Change From Baseline in Pulse Rate
1.3
SECONDARY
Treatment C: Change From Baseline in Pulse Rate
-7.1; -1.5
SECONDARY
Treatment A: Change From Baseline in Respiratory Rate
-0.3
SECONDARY
Treatment B: Change From Baseline in Respiratory Rate
-0.3
SECONDARY
Treatment C: Change From Baseline in Respiratory Rate
-0.1; 0.8
SECONDARY
Treatment A: Change From Baseline in SBP and DBP
-3.3; -5.4
SECONDARY
Treatment B: Change From Baseline in SBP and DBP
-0.5; -2.0
SECONDARY
Treatment C: Change From Baseline in SBP and DBP
-1.9; 2.2; -4.3; -0.5
SECONDARY
Treatment C: AUC(0-t) for GSK3640254
51840
SECONDARY
Treatment C: AUC From Time Zero to the End of the Dosing Interval at Steady State (AUC[0-tau]) for GSK3640254
22920
SECONDARY
Treatment C: Cmax for GSK3640254
1450
SECONDARY
Treatment C: Plasma Concentration at the End of the Dosing Interval (Ctau) for GSK3640254
729.5
SECONDARY
Treatment C: Tmax for GSK3640254
4.500
SECONDARY
Treatment C: t1/2 for GSK3640254
29.556
SECONDARY
AUC(0-t) for Alpha-hydroxymetoprolol
531.3; 487.9
SECONDARY
AUC(0-infinity) for Alpha-hydroxymetoprolol
682.8; 632.8
SECONDARY
Cmax for Alpha-hydroxymetoprolol
45.70; 39.21
SECONDARY
Tmax for Alpha-hydroxymetoprolol
3.033; 4.000
SECONDARY
t1/2 for Alpha-hydroxymetoprolol
8.040; 8.339
SECONDARY
AUC(0-t) for 36-hydroxymontelukast
234.2; 230.9
SECONDARY
AUC(0-infinity) for 36-hydroxymontelukast
252.5; 249.3
SECONDARY
Cmax for 36-hydroxymontelukast
24.62; 23.22
SECONDARY
Tmax for 36-hydroxymontelukast
6.000; 6.000
SECONDARY
t1/2 for 36-hydroxymontelukast
5.310; 5.644
SECONDARY
AUC(0-t) for 5-hydroxyomeprazole
713.5; 785.1
SECONDARY
AUC(0-infinity) for 5-hydroxyomeprazole
767.4; 762.0
SECONDARY
Cmax for 5-hydroxyomeprazole
181.1; 203.3
SECONDARY
Tmax for 5-hydroxyomeprazole
6.000; 6.000
SECONDARY
t1/2 for 5-hydroxyomeprazole
1.580; 1.569
SECONDARY
AUC(0-t) for 1-hydroxymidazolam
31.07; 28.07
SECONDARY
AUC(0-infinity) for 1-hydroxymidazolam
31.86; 28.99
SECONDARY
Cmax for 1-hydroxymidazolam
7.933; 6.722
SECONDARY
Tmax for 1-hydroxymidazolam
1.000; 1.000
SECONDARY
t1/2 for 1-hydroxymidazolam
3.632; 3.717
SECONDARY
Ratio of Cmax of Alpha-hydroxymetoprolol to Metoprolol
0.7869; 0.7066
SECONDARY
Ratio of AUC(0-infinity) of Alpha-hydroxymetoprolol to Metoprolol
1.733; 1.449
SECONDARY
Ratio of Cmax of 36-hydroxymontelukast to Montelukast
0.06766; 0.06308
SECONDARY
Ratio of AUC(0-infinity) of 36-hydroxymontelukast to Montelukast
0.09182; 0.08562
SECONDARY
Ratio of Cmax of 5-hydroxyomeprazole to Omeprazole
0.9461; 0.8810
SECONDARY
Ratio of AUC(0-infinity) of 5-hydroxyomeprazole to Omeprazole
1.151; 1.077
SECONDARY
Ratio of Cmax of 1-hydroxymidazolam to Midazolam
0.5286; 0.4955
SECONDARY
Ratio of AUC(0-infinity) of 1-hydroxymidazolam to Midazolam
0.4677; 0.4618

Eligibility Criteria

Inclusion Criteria

  • Participant must be 18 to 50 years of age inclusive, at the time of signing the informed consent.
  • Participants who are overtly healthy as determined by the investigator or medically qualified designee based on a medical evaluation including medical history, physical examination (including cardiopulmonary examination), laboratory tests, and cardiac monitoring (history and ECG).
  • Body weight more than or equal to (>=) 50.0 kilograms (kg) (110 pounds [lbs]) for men and >=45.0 kg (99 lbs) for women and body mass index within the range 18.5 to 31.0 kilogram per square meter (kg/m^2) (inclusive).
  • Contraceptive use by men or women should be consistent with local regulations regarding the methods of contraception for those participating in clinical studies.
  • Male participants should not engage in intercourse while confined in the clinic. There is no need for an extended period of double barrier use or prolonged abstinence after study discharge.
  • A female participant is eligible to participate if she is not pregnant or breastfeeding and at least one of the following conditions applies:
  • Is not a woman of childbearing potential (WOCBP) or
  • Is a WOCBP and using a non-hormonal contraceptive method that is highly effective, with a failure rate of less than ( 6 months) outpatient treatment.

Participants with other conditions such as adjustment disorder or dysthymia that have required shorter term medical therapy ( =1.5 × upper limit of normal (ULN). A single repeat of ALT is allowed within a single screening period to determine eligibility.

  • Bilirubin >=5 × ULN (isolated bilirubin >=5 × ULN is acceptable if bilirubin is fractionated and direct bilirubin 100 bpm, PR interval- >200 milliseconds and QTcF- >450 milliseconds.
  • History of regular alcohol consumption within 6 months of the study defined as an average weekly intake of >14 units. One unit is equivalent to 8 grams (g) of alcohol: a half-pint (approximately 240 mL) of beer, 1 glass (125 mL) of wine, or 1 (25 mL) measure of spirits.
  • Unable to refrain from tobacco or nicotine-containing products within 3 months prior to Screening.
  • History of sensitivity to any of the study medications, or components thereof or a history of drug or other allergy that, in the opinion of the investigator or medical monitor, contraindicates their participation.
  • History of aspirin allergy.
  • A participant with known or suspected active coronavirus disease of 2019 (COVID-19) infection OR contact with an individual with known COVID-19, within 14 days of study enrollment.
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT04425902). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.

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