Phase 1
Completed N=276
A Study to Evaluate the Bioequivalence (BE) and the Food Effect of TAK-438ASA Tablet
Healthy Volunteers
Source: ClinicalTrials.gov NCT03456960 ↗
Enrolled (actual)
276
Serious AEs
0.0%
Results posted
Nov 2019
Primary outcomePrimary: Study 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Free Base of TAK-438 (TAK-438F) — 92.46; 91.95 hour*nanogram per milliliter (h*ng/mL)
Summary
The purposes of this study are to evaluate BE between a single-dose of TAK-438ASA tablet versus a single-dose combination of TAK-438 tablet 10 milligram (mg) and aspirin enteric-coated tablet 100 mg in Japanese healthy adult men (Study 1), and to evaluate the effects of food on the pharmacokinetics of TAK-438ASA tablet in Japanese healthy adult men (Study 2).
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Study 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Free Base of TAK-438 (TAK-438F) |
92.46; 91.95 | — |
| PRIMARY Study 1, Cmax: Maximum Observed Plasma Concentration for TAK-438F |
13.87; 13.22 | — |
| PRIMARY Study 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Unchanged Aspirin |
873.5; 831.9; 912.3; 832.7 | — |
| PRIMARY Study 1, Cmax: Maximum Observed Plasma Concentration for Unchanged Aspirin |
647.6; 597.5; 701.8; 558.0 | — |
| SECONDARY Study 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-438F |
94.71; 93.78 | — |
| SECONDARY Study 1, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-438F |
1.500; 1.500 | — |
| SECONDARY Study 1, MRT (Infinity,ev): Mean Residence Time From Time 0 to Infinity for TAK-438F |
9.610; 9.751 | — |
| SECONDARY Study 1, Lambda (z): Terminal Disposition Phase Rate Constant for TAK-438F |
0.08565; 0.08788 | — |
| SECONDARY Study 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Unchanged Aspirin |
876.5; 834.6; 915.8; 855.4 | — |
| SECONDARY Study 1, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Unchanged Aspirin |
4.000; 4.500; 4.000; 4.500 | — |
| SECONDARY Study 1, MRT (Infinity,ev): Mean Residence Time From Time 0 to Infinity for Unchanged Aspirin |
4.629; 5.194; 4.398; 5.152 | — |
| SECONDARY Study 1, Lambda (z): Terminal Disposition Phase Rate Constant for Unchanged Aspirin |
1.734; 1.703; 1.754; 1.795 | — |
| SECONDARY Study 2, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-438F and Its Metabolites (M) (M-I, M-II, M-III and M-IV-Sul) |
84.26; 104.3; 290.4; 266.9; 50.77; 58.29 | — |
| SECONDARY Study 2, AUC(0-48): Area Under the Plasma Concentration-time Curve From Time 0 to Time 48 Hours Over the Dosing Interval for TAK-438F and Its Metabolites (M-I, M-II, M-III and M-IV-Sul) |
82.89; 102.9; 272.1; 251.9; 30.80; 24.17 | — |
| SECONDARY Study 2, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-438F and Its Metabolites (M-I, M-II, M-III and M-IV-Sul) |
82.23; 102.4; 258.6; 239.5; 26.86; 20.66 | — |
| SECONDARY Study 2, Cmax: Maximum Observed Plasma Concentration for TAK-438F and Its Metabolites (M-I, M-II, M-III and M-IV-Sul) |
12.73; 18.35; 41.26; 35.22; 2.820; 2.131 | — |
| SECONDARY Study 2, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-438F and Its Metabolites (M-I, M-II, M-III and M-IV-Sul) |
1.500; 1.500; 1.500; 1.500; 4.000; 4.000 | — |
| SECONDARY Study 2, T1/2z: Terminal Disposition Phase Half-life for TAK-438F and Its Metabolites (M-I, M-II, M-III and M-IV-Sul) |
8.293; 7.951; 9.653; 9.153; 12.92; 27.52 | — |
| SECONDARY Study 2, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Unchanged Aspirin and Its Metabolite (Salicylic Acid) |
817.9; 1008; 20010; 20290 | — |
| SECONDARY Study 2, AUC(0-24): Area Under the Plasma Concentration-time Curve From Time 0 to Time 24 Hours Over the Dosing Interval for Unchanged Aspirin and Its Metabolite (Salicylic Acid) |
816.7; 1007; 20070; 20340 | — |
| SECONDARY Study 2, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Unchanged Aspirin and Its Metabolite (Salicylic Acid) |
816.5; 1007; 19370; 19760 | — |
| SECONDARY Study 2, Cmax: Maximum Observed Plasma Concentration for Unchanged Aspirin and Its Metabolite (Salicylic Acid) |
632.5; 949.0; 4414; 5374 | — |
| SECONDARY Study 2, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Unchanged Aspirin and Its Metabolite (Salicylic Acid) |
4.500; 4.000; 5.500; 4.500 | — |
| SECONDARY Study 2, T1/2z: Terminal Disposition Phase Half-life for Unchanged Aspirin and Its Metabolite (Salicylic Acid) |
0.3749; 0.4373; 2.050; 1.901 | — |
| SECONDARY Study 2, Ae(0-48): Amount of Drug Excreted in Urine From Time 0 to 48 Hours for TAK-438F and Its Metabolites (M-I, M-II, M-III, and M-IV-Sul) |
433.3; 583.1; 150.1; 153.4; 0.000; 0.000 | — |
| SECONDARY Study 2, Fe(0-48): Fraction of Administered Dose Excreted Into Urine From Time 0 to Time 48 Hours for TAK-438F and Its Metabolites (M-I, M-II, M-III and M-IV-Sul) |
4.333; 5.831; 1.499; 1.529; 0.000; 0.000 | — |
| SECONDARY Study 2, CLR: Renal Clearance for TAK-438F and Its Metabolites (M-I, M-II, M-III, and M-IV-Sul) |
5.213; 5.604; 0.5577; 0.6018; 0.000; 0.000 | — |
| SECONDARY Study 2, Ae(0-24): Amount of Drug Excreted in Urine From Time 0 to 24 Hours for Unchanged Aspirin and Its Metabolites (Salicylic Acid and Salicyluric Acid) |
481.3; 817.3; 2318; 2076; 80180; 83800 | — |
| SECONDARY Study 2, Fe(0-24): Fraction of Administered Dose Excreted Into Urine From Time 0 to Time 24 Hours for Unchanged Aspirin and Its Metabolites (Salicylic Acid and Salicyluric Acid) |
0.4813; 0.8173; 3.025; 2.708; 74.02; 77.34 | — |
| SECONDARY Study 2, CLR: Renal Clearance for Unchanged Aspirin and Its Metabolites (Salicylic Acid and Salicyluric Acid) |
0.6181; 0.7818; 0.1135; 0.1022 | — |
Eligibility Criteria
Inclusion Criteria
- In the opinion of the investigator or sub-investigator, participants are capable of understanding the procedures required for the study and complying with its requirements.
- Participants sign and date an informed consent form by themselves prior to the initiation of any study procedures.
- Japanese healthy men aged greater than or equal to (>=) 20 and less than or equal to (= =50 kilogram (kg) as well as body mass index (BMI) >=18.5 kilogram per meter square (kg/m^2) and = =5 years prior to Day 1.
- Positive results at screening for hepatitis B surface antigen (HBsAg), hepatitis C virus (HCV) antibody, human immunodeficiency virus (HIV) antibody/antigen, or serological test for syphilis.
- Participants who have difficulties in blood draw from peripheral veins.
- Participants who had >=200 milliliter (mL) of whole blood drawn within 4 weeks (28 days) prior to the start of study treatment in Period 1 or who had >=400 mL of whole blood drawn within 12 weeks (84 days) prior to the start of study treatment in Period 1.
- Participants who had a total of >=800 mL of whole blood drawn within 52 weeks (364 days) prior to the start of study treatment in Period 1.
- Participants who had blood components drawn within 2 weeks (14 days) prior to the start of study treatment in Period 1.
- Clinically significant abnormalities in electrocardiogram at screening or admission (Day -1).
- Participants with abnormal laboratory parameters suggestive of clinically significant underlying diseases or who have abnormal values in the following measures at screening: alanine aminotransferase (ALT) or aspartate aminotransferase (AST) over the upper limit of normal.
- Participants who are unlikely to comply with the protocol or deemed ineligible due to other reasons by the principal investigator or other investigators.
Data sourced from ClinicalTrials.gov (NCT03456960). 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.