A Study to Evaluate Safety, Tolerability and Pharmacokinetics of Ascending Oral Single Dose of TAK-418 in Healthy Participants

NCT03228433 | Completed Phase 1 Results FDA Drug

• 2 other identifiers: TAK-418-1001U1111-1195-7777
• Study Type: interventional
• Target: 40
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to evaluate the safety and tolerability of TAK-418 following single oral doses in healthy participants.

Conditions

Healthy Participants

Keywords

Drug Therapy

Outcome Measures

Primary Outcomes (6)

• Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)

  Baseline Up to Day 184

• Number of Participants Who Discontinued Due to an Adverse Event (AE)

  Baseline Up to Day 184

• Number of Participants Who Meet the Markedly Abnormal Criteria for Neurological Assessment Measurements at Least Once Post Dose

  Baseline Up to Day 184

• Number of Participants Who Meet the Markedly Abnormal Criteria for Safety Laboratory Tests at Least Once Post Dose

  Baseline Up to Day 184

• Number of Participants Who Meet the Markedly Abnormal Criteria for Vital Sign Measurements at Least Once Post Dose

  Baseline Up to day 184

• Number of Participants Who Meet the Markedly Abnormal Criteria for Safety 12-lead Electrocardiogram (ECG) Parameters at Least Once Post Dose

  Baseline Up to Day 14

Secondary Outcomes (4)

• AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration of TAK-418F (TAK-418 Free Base)

  Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose

• AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-418F

  Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose

• Cmax: Maximum Observed Plasma Concentration for TAK-418F

  Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose

• Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-418F

  Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose

Study Arms (6)

Cohort 1: TAK-418 5 mg

EXPERIMENTAL

TAK-418 5 milligram (mg), capsule, orally, once on Day 1.

Drug: TAK-418

Cohort 2: TAK-418 15 mg

EXPERIMENTAL

TAK-418 15 mg, capsule, orally, once on Day 1. Actual dose of TAK-418 may vary based on safety, tolerability and PK data from previous Cohorts.

Drug: TAK-418

Cohort 3: TAK-418 30 mg Fasted + TAK-418 30 mg Fed

EXPERIMENTAL

TAK-418 30 mg, capsule, in fasted state, orally, once on Day 1, followed by a 28-day washout period, further followed by TAK-418 30 mg, capsule, in fed state, orally, once on Day 1. Actual dose of TAK-418 may vary based on safety, tolerability and PK data from previous Cohorts.

Drug: TAK-418

Cohort 4: TAK-418 40 mg

EXPERIMENTAL

TAK-418 40 mg, capsule, orally, once on Day 1. Actual dose of TAK-418 may vary based on safety, tolerability and PK data from previous Cohorts.

Drug: TAK-418

Cohort 5: TAK-418 60 mg

EXPERIMENTAL

TAK-418 60 mg, capsule, orally, once on Day 1. Actual dose of TAK-418 may vary based on safety, tolerability and PK data from previous Cohorts.

Drug: TAK-418

Cohorts 1-5: Placebo

PLACEBO COMPARATOR

TAK-418 placebo-matching, capsule, orally, once on Day 1.

Drug: TAK-418 Placebo

Interventions

TAK-418 DRUG

TAK-418 Capsule.

Cohort 1: TAK-418 5 mg; Cohort 2: TAK-418 15 mg; Cohort 3: TAK-418 30 mg Fasted + TAK-418 30 mg Fed; Cohort 4: TAK-418 40 mg; Cohort 5: TAK-418 60 mg

TAK-418 Placebo DRUG

TAK-418 placebo-matching capsules.

Cohorts 1-5: Placebo

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Is a male or female participants with a body mass index (BMI) within the range of 18.5 -30.0 kilogram per square meter (kg/m\^2) at the Screening Visit.
• Is a nonsmoker who has not used tobacco or nicotine-containing products (example, nicotine patch) for at least 6 months before trial drug administration of the initial dose of trial drug or invasive procedure.
• Must be judged to be in good health by the investigator, based on clinical evaluations including laboratory safety tests, medical history, physical examination, 12-lead ECG, and vital sign measurements performed at the Screening Visit and before administration of the initial dose of trial drug or invasive procedure as per principal investigator's judgment.
• Female subjects with no childbearing potential, defined by at least 1 of the following criteria:
• Postmenopausal (defined as 12 months of spontaneous amenorrhea in women aged greater than \[\>\]45 years, 6 months of spontaneous amenorrhea in women aged \>45 years with serum follicle-stimulating hormone \[FSH\] levels \>40 milli-international units per milliliter \[mIU/mL\]). Appropriate documentation of FSH levels is required.
• Surgically sterile by hysterectomy and/or bilateral oophorectomy with appropriate documentation of surgical procedure.
• Had a tubal ligation with appropriate documentation of surgical procedure.
• Has a congenital condition resulting in no uterus.

You may not qualify if:

• Has had major surgery, donated or lost 1 unit of blood (approximately 500 milliliter \[mL\]) within 4 weeks before the Screening Visit.
• Has a risk of suicide according to the investigator's clinical judgment per the Columbia-Suicide Severity Rating Scale at Screening or has made a suicide attempt in the 6 months before Screening.

Sponsors & Collaborators

• Takeda: lead

Study Sites (1)

PAREXEL International

Glendale, California, 91206, United States

Location

Related Publications (1)

• Yin W, Arkilo D, Khudyakov P, Hazel J, Gupta S, Quinton MS, Lin J, Hartman DS, Bednar MM, Rosen L, Wendland JR. Safety, pharmacokinetics and pharmacodynamics of TAK-418, a novel inhibitor of the epigenetic modulator lysine-specific demethylase 1A. Br J Clin Pharmacol. 2021 Dec;87(12):4756-4768. doi: 10.1111/bcp.14912. Epub 2021 Jun 10.

  PMID: 33990969 DERIVED

MeSH Terms

Interventions

TAK-418

Results Point of Contact

• Title: Medical Director
• Organization: Takeda

trialdisclosures@takeda.com

+1-877-825-3327

Study Officials

• Medical Director

  Takeda

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: QUADRUPLE
• Who Masked: PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
• Purpose: OTHER
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 21, 2017
• First Posted: July 24, 2017
• Study Start: July 21, 2017
• Primary Completion: May 12, 2018
• Study Completion: May 12, 2018
• Last Updated: September 9, 2019
• Results First Posted: September 9, 2019

Record last verified: 2019-08

Data Sharing

• IPD Sharing: Will share

Locations

US (1)