A Phase 1, Bio-equivalence Study of TAK-536 Pediatric Formulation
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ClinicalTrials.gov Identifier: NCT03042299 |
Recruitment Status :
Completed
First Posted : February 3, 2017
Results First Posted : October 9, 2018
Last Update Posted : November 14, 2018
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Condition or disease | Intervention/treatment | Phase |
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Japanese Healthy Adult Male Participants | Drug: TAK-536 | Phase 1 |
Study Type : | Interventional (Clinical Trial) |
Actual Enrollment : | 14 participants |
Allocation: | Randomized |
Intervention Model: | Crossover Assignment |
Masking: | None (Open Label) |
Primary Purpose: | Treatment |
Official Title: | A Randomized, Open Label, 2-Period, 2-Treatment, Cross-over Phase 1 Study to Evaluate the Bio-equivalence of Single Oral Dose of TAK-536 Pediatric Formulation and TAK-536 Commercial Formulation in Healthy Adult Male Subjects |
Actual Study Start Date : | February 10, 2017 |
Actual Primary Completion Date : | March 11, 2017 |
Actual Study Completion Date : | March 11, 2017 |

Arm | Intervention/treatment |
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Experimental: TAK-536 Granules + TAK-536 Tablet
TAK-536 10 milligram (mg), granules (pediatric formulation), under fasted condition, orally, once on Day 1 of Intervention Period 1, followed by a Washout Period of at least 6 days, further followed by TAK-536 10 mg, tablet (commercial formulation), under fasted condition, orally, once on Day 1 of Intervention Period 2.
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Drug: TAK-536
TAK-536 granules. Drug: TAK-536 TAK-536 tablet. |
Experimental: TAK-536 Tablet + TAK-536 Granules
TAK-536 10 mg, tablet (commercial formulation), under fasted condition, orally, once on Day 1 of Intervention Period 1, followed by a Washout Period of at least 6 days, further followed by TAK-536 10 mg, granules (pediatric formulation), under fasted condition, orally, once on Day 1 of Intervention Period 2.
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Drug: TAK-536
TAK-536 granules. Drug: TAK-536 TAK-536 tablet. |
- AUC(0-48): Area Under the Plasma Concentration-time Curve From Time 0 to 48 Hours Postdose for TAK-536 [ Time Frame: Day 1 pre-dose and at multiple time points post-dose (0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, and 48 hours post-dose; up to 48 hours) ]
- Cmax: Maximum Observed Plasma Concentration for TAK-536 [ Time Frame: Day 1 pre-dose and at multiple time points post-dose (0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, and 48 hours post-dose; up to 48 hours) ]
- AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-536 [ Time Frame: Day 1 pre-dose and at multiple time points post-dose (0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, and 48 hours post-dose; up to 48 hours) ]
- Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-536 [ Time Frame: Day 1 pre-dose and at multiple time points post-dose (0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, and 48 hours post-dose; up to 48 hours) ]
- MRT∞,ev: Mean Residence Time After Extravascular Administration From Time 0 to Infinity for TAK-536 [ Time Frame: Day 1 pre-dose and at multiple time points post-dose (0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, and 48 hours post-dose; up to 48 hours) ]
- Terminal Disposition Phase Rate Constant (λz) for TAK-536 [ Time Frame: Day 1 pre-dose and at multiple time points post-dose (0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, and 48 hours post-dose; up to 48 hours) ]
- Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs) [ Time Frame: Baseline up to Day 6 of Intervention Period 2 (Day 18) ]An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant who has signed informed consent to participate in a study; it does not necessarily have to have a causal relationship with this treatment or study participation. An AE can therefore be any unfavorable and unintended sign (for example, a clinically significant abnormal laboratory finding), symptom, or disease temporally associated with the study participation, whether or not it is considered related to the drug. A TEAE is defined as an adverse event with an onset that occurs after receiving study drug.
- Number of Participants With TEAEs Related to Vital Signs [ Time Frame: Baseline up to Day 6 of Intervention Period 2 (Day 18) ]
- Number of Participants With TEAEs Related to Body Weight [ Time Frame: Baseline up to Day 6 of Intervention Period 2 (Day 18) ]
- Number of Participants With TEAEs Related to Electrocardiograms (ECGs) [ Time Frame: Baseline up to Day 6 of Intervention Period 2 (Day 18) ]
- Number of Participants With TEAEs Related to Clinical Laboratory Tests [ Time Frame: Baseline up to Day 6 of Intervention Period 2 (Day 18) ]

Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies.
Ages Eligible for Study: | 20 Years to 35 Years (Adult) |
Sexes Eligible for Study: | Male |
Gender Based Eligibility: | Yes |
Accepts Healthy Volunteers: | Yes |
Inclusion Criteria:
- In the opinion of the investigator or sub-investigator, the participant is capable of understanding and complying with protocol requirements.
- Signs and dates a written, informed consent form prior to the initiation of any study procedures.
- Is a Japanese healthy adult male.
- Aged 20 to 35 years, inclusive, at the time of informed consent.
- Weighs at least 50.0 kilogram (kg), and has a body mass index (BMI) between 18.5 and 25.0 kilogram per square meter (kg/m^2), inclusive, at Screening.
Exclusion Criteria:
- Has suspected hypotension with associated physical findings, such as dizziness postural, facial pallor, or cold sweats based on evaluation/physical examination at Screening, on the day before the study drug administration (Day -1) in Period 1, or up to the study drug administration on the Period 1.
- Has received any study drug within 16 weeks (112 days) prior to the study drug administration in Period 1.
- Has received TAK-536 or TAK-491 in a previous clinical study or as a therapeutic agent.
- Has uncontrolled, clinically significant neurologic, cardiovascular, pulmonary, hepatic, renal, metabolic, gastrointestinal, or endocrine disease or other abnormality, which may impact the ability of the participant to participate or potentially confound the study results.
- Has a known hypersensitivity to any component of the formulation of TAK-536 or any angiotensin II receptor blocker (ARB).
- Has a positive urine drug result for drugs of abuse (defined as any illicit drug use) at Screening.
- Has a history of drug abuse (defined as any illicit drug use) or a history of alcohol abuse within 2 years prior to the Screening visit or is unwilling to agree to abstain from alcohol and drugs throughout the study.
- Has taken any excluded medication, supplements, dietary products, or food products during the time periods specified in the protocol.
- Has any current or recent (within 6 months) gastrointestinal diseases that would be expected to influence the absorption of drugs (that is, a history of malabsorption, esophageal reflux, peptic ulcer disease, erosive esophagitis, frequent [more than once per week] occurrence of heartburn, or any surgical intervention).
- Has a history of cancer, except basal cell carcinoma which has been in remission for at least 5 years prior to Day 1 of Period 1.
- Has a positive test result for hepatitis B surface antigen (HBsAg), hepatitis C virus (HCV) antibody, human immunodeficiency virus (HIV) antibody/antigen, or serological reactions for syphilis at Screening.
- Has poor peripheral venous access.
- Has undergone whole blood collection of at least 200 milliliter (mL) within 4 weeks (28 days) or at least 400 mL within 12 weeks (84 days) prior to the start of the study drug administration in Period 1.
- Has undergone whole blood collection of at least 800 mL in total within 52 weeks (364 days) prior to the start of the study drug administration in Period 1.
- Has undergone blood component collection within 2 weeks (14 days) prior to the start of the study drug administration in Period 1.
- Has an abnormal (clinically significant) ECG at Screening or prior to the study drug administration in Period 1.
- Has abnormal laboratory values that suggest a clinically significant underlying disease, or participant with the following laboratory abnormalities at Screening or prior to the study drug administration in Period 1: alanine aminotransferase (ALT) and/or aspartate aminotransferase (AST) greater than (>) 1.5 * the upper limits of normal (ULN).
- Who, in the opinion of the investigator or sub-investigator, is unlikely to comply with the protocol or is unsuitable for any other reason.

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.
Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT03042299
Japan | |
Nishi Kumamoto Hospital | |
Kumamoto, Japan |
Study Director: | Study Director | Takeda |
Documents provided by Takeda:
Responsible Party: | Takeda |
ClinicalTrials.gov Identifier: | NCT03042299 |
Other Study ID Numbers: |
Azilsartan-1004 U1111-1190-0845 ( Registry Identifier: WHO ) JapicCTI-173503 ( Registry Identifier: JapicCTI ) |
First Posted: | February 3, 2017 Key Record Dates |
Results First Posted: | October 9, 2018 |
Last Update Posted: | November 14, 2018 |
Last Verified: | October 2018 |
Individual Participant Data (IPD) Sharing Statement: | |
Plan to Share IPD: | Yes |
Plan Description: | Takeda makes patient-level, de-identified data sets and associated documents available after applicable marketing approvals and commercial availability have been received, an opportunity for the primary publication of the research has been allowed, and other criteria have been met as set forth in Takeda's Data Sharing Policy (see www.TakedaClinicalTrials.com/Approach for details). To obtain access, researchers must submit a legitimate academic research proposal for adjudication by an independent review panel, who will review the scientific merit of the research and the requestor's qualifications and conflict of interest that can result in potential bias. Once approved, qualified researchers who sign a data sharing agreement are provided access to these data in a secure research environment. |
Studies a U.S. FDA-regulated Drug Product: | No |
Studies a U.S. FDA-regulated Device Product: | No |
Drug therapy |
Azilsartan medoxomil Angiotensin II Type 1 Receptor Blockers Angiotensin Receptor Antagonists Molecular Mechanisms of Pharmacological Action |