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A Study to Evaluate the Pharmacokinetics (PK), Safety and Tolerability of TAK-788 Followed by Evaluation of the Effects of a Low-Fat Meal on TAK-788 PK and Evaluation of Relative Bioavailability of TAK-788 Capsules in Healthy Participants

Phase 1
Completed
Conditions
Healthy Volunteers
Interventions
Drug: Placebo
Registration Number
NCT03482453
Lead Sponsor
Millennium Pharmaceuticals, Inc.
Brief Summary

The purpose of this study is to assess the safety, tolerability of TAK-788 and to identify a tolerable single oral dose of TAK-788 administered as a drug-in-capsule (DiC) formulation, to characterize the effects of a low-fat meal on the PK of the TAK-788 administered as DiC formulation and to evaluate the bioavailability of a test (Process B) DiC of TAK-788 relative to a reference (Process A) DiC of TAK-788 in healthy participants.

Detailed Description

The drug being tested in this study is called TAK-788. The study will assess the safety and tolerability of single oral dose of TAK-788, evaluate the effect of a low-fat meal on PK of TAK-788 and will assess the relative bioavailability of two DiCs of TAK-788.

The study will enroll approximately 69 participants. The study is designed to consist of 3 parts: Part 1- dose escalation phase, Part 2- low fat meal effect and Part 3 - relative bioavailability. The study population of Part 1 will consist of 40 participants enrolled into 5 cohorts. Each cohort will have 8 randomized participants with 6 receiving a single dose of TAK-788, and 2 receiving matching placebo under fasted conditions. In Cohorts 1 to 5, safety of single-dose TAK-788 will be evaluated. For Part 2, the effect of a low-fat meal on a single tolerable dose of TAK-788 will be determined following review of safety and tolerability data from the previous cohorts in Part 1. The study population of Part 2 will consist of 16 participants enrolled into 2 cohorts of different doses, where participants will be randomized to a cross-over sequence of:

* TAK-788 Fed + TAK-788 Fasted

* TAK-788 Fasted + TAK-788 Fed

The study population of Part 3 will consist of 13 participants enrolled into 1 cohort, where participants will be randomized to a cross-over sequence of:

* TAK-788 DiC (reference) + TAK-788 DiC (test)

* TAK-788 DiC (test) + TAK-788 DiC (reference) This single-center trial will be conducted in the United States. The overall time to participate in this study is approximately 7 months. Participants will be contacted by telephone 30 days after the last dose of study drug for a follow-up assessment.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
69
Inclusion Criteria
  1. Body weight of greater than or equal to (>=) 45 kilogram (kg) (women) or >=55 kg (men) and a body mass index of 18.0 to 30.0 kilogram per square meter (kg/m^2) at screening.
  2. Nonsmoker (never smoked or greater than [>] 20 years from last occurrence of smoking).
  3. Normal organ function including hepatic, renal, and bone marrow function.
Exclusion Criteria
  1. Manifestations of malabsorption due to prior gastro-intestinal (GI) surgery, GI disease, or for an unknown other reason that may alter the PK of TAK-788.
  2. Pulmonary infection ongoing or within 30 days of informed consent.
  3. Inability to undergo venipuncture and/or tolerate venous access.
  4. Inability to tolerate multiple blood sampling.
  5. Ongoing or active infection, including but not limited to, the requirement for intravenous (IV) antibiotics.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Part 1 Cohort 1: TAK-788PlaceboTAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1.
Part 1 Cohort 2: TAK-788PlaceboTAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 1.
Part 1 Cohort 3: TAK-788TAK-788TAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 2.
Part 1 Cohort 3: TAK-788PlaceboTAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 2.
Part 1 Cohort 4: TAK-788PlaceboTAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 3.
Part 1 Cohort 5: TAK-788PlaceboTAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 4.
Part 2: TAK-788 Fed + TAK-788 FastedTAK-788TAK-788, capsule, orally, once on Day 1 of Intervention Period 1 under fed conditions with low-fat meal (Treatment A), followed by at least 7 days washout period, further followed by TAK-788, capsule, orally, once on Day 1 of Intervention Period 2 under fasted conditions (Treatment B). TAK-788 dose will be determined based on review of safety and tolerability data from cohorts of Part 1.
Part 2: TAK-788 Fasted + TAK-788 FedTAK-788TAK-788, capsule, orally, once on Day 1 of Intervention Period 1 under fasted conditions (Treatment B), followed by at least 7 days washout period, further followed by TAK-788, capsule, orally, once on Day 1 of Intervention Period 2 under fed conditions with low-fat meal (Treatment A). TAK-788 dose will be determined based on review of safety and tolerability data from cohorts of Part 1.
Part 1 Cohort 2: TAK-788TAK-788TAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 1.
Part 1 Cohort 5: TAK-788TAK-788TAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 4.
Part 1 Cohort 1: TAK-788TAK-788TAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1.
Part 1 Cohort 4: TAK-788TAK-788TAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 3.
Part 3: TAK-788 DiC (reference) + TAK-788 DiC (test)TAK-788TAK-788 160 mg, DiC A (reference), orally, under fasted condition, once on Day 1 of Intervention Period 1, followed by at least 7 days washout period, further followed by TAK-788 160 mg, DiC B (test), orally, under fasted condition, once on Day 1 of Intervention Period 2.
Part 3: TAK-788 DiC (test) + TAK-788 DiC (reference)TAK-788TAK-788 160 mg, DiC B (test), orally, under fasted condition, once, on Day 1 of Intervention Period 1, followed by at least 7 days washout period, further followed by TAK-788 160 mg, DiC A (reference), orally, under fasted condition, once on Day 1 of Intervention Period 2.
Primary Outcome Measures
NameTimeMethod
Part 1: Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)Baseline up to 30 days after the last dose of study drug (Day 31)
Part 1: Number of Participants With One or More Serious Adverse Events (SAEs)Baseline up to 30 days after the last dose of study drug (Day 31)
Part 1: Number of Participants With Clinically Significant Abnormal Laboratory ValuesBaseline up to 30 days after the last dose of study drug (Day 31)
Part 2, Cmax: Maximum Observed Plasma Concentration for TAK-788Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 3, Cmax: Maximum Observed Plasma Concentration for TAK-788Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
Part 2, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-788Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 3, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-788Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
Part 1: Number of Participants With Clinically Significant Abnormal Vital SignsBaseline up to 30 days after the last dose of study drug (Day 31)
Part 2, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for TAK-788Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 3, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for TAK-788Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
Part 2, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-788Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 3, t1/2z: Terminal Disposition Phase Half-life (t1/2z) for TAK-788Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
Part 3, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-788Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
Part 2, t1/2z: Terminal Disposition Phase Half-life (t1/2z) for TAK-788Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Secondary Outcome Measures
NameTimeMethod
Part 1, Cmax: Maximum Observed Plasma Concentration for TAK-788 and Its Active Metabolites AP32960 and AP32914Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Parts 2 and 3: Number of Participants With Clinically Significant Abnormal Laboratory ValuesBaseline up to 30 days after the last dose of study drug (Day 38) (end of Intervention Period 2)
Parts 2 and 3: Number of Participants With One or More SAEsBaseline up to 30 days after the last dose of study drug (Day 38) (end of Intervention Period 2)
Parts 2 and 3: Number of Participants Reporting One or More TEAEsBaseline up to 30 days after the last dose of study drug (Day 38) (end of Intervention Period 2)
Part 1, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-788 and Its Active Metabolites AP32960 and AP32914Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 1, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for TAK-788 and Its Active Metabolites, AP32960 and AP32914Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-788 and Its Active Metabolites AP32960 and AP32914Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 1, t1/2z: Terminal Disposition Phase Half-life (t1/2z) for TAK-788 and Its Active Metabolites AP32960 and AP32914Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Parts 2 and 3: Number of Participants With Clinically Significant Abnormal Vital SignsBaseline up to 30 days after the last dose of study drug (Day 38) (end of Intervention Period 2)

Trial Locations

Locations (1)

PRA Health Sciences

🇺🇸

Salt Lake City, Utah, United States

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