Investigation of the Absorption, Metabolism, and Excretion and the Absolute Bioavailability of YH12852

A Phase I Study to Investigate the Absorption, Metabolism, and Excretion and the Absolute Bioavailability of YH12852 in Healthy Male Subjects

This study investigates the absorption, metabolism, and excretion and the absolute bioavailability of YH12852 in healthy male subjects

Study Overview

• Status: Completed
• Conditions: Constipation
• Intervention / Treatment: Drug: YH12852; Drug: 14C-labeled YH12852

Detailed Description

Part 1 : Investigate the absorption metabolism, and excretion of YH12852 after single oral administration of YH12852 and 14C-labeled YH12852.

Part 2

: Investigate the absolute bioavailability of YH12852 after single oral administration of YH12852 followed by a single i.v. administration of 14C-labeled YH12852.

• Study Type: Interventional
• Enrollment (Actual): 10
• Phase: Phase 1

Contacts and Locations

Study Locations

• Korea, Republic of
  • Seoul, Korea, Republic of
    • Seoul National University Hospital Clinical Trial Center

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 19 years to 55 years (ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Subjects who agreed to voluntarily participate in this study and comply with all the study requirements by signing informed consent form after being informed of the nature of this study and understanding all aspects of this study
• Healthy adult, 19 - 55 of age (inclusive)
• Subjects weighing over 55 kg (inclusive) with BMI between 18 and 25 (inclusive) at screening visit
• Subjects with no clinically significant abnormal findings as determined by physical examination, ECG, medical history, or clinical laboratory test results

Exclusion Criteria:

• History of clinically significant gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorder
• Surgery of the gastrointestinal tract that could interfere with kinetics of the study drug
• History of (or suspected at screening visit) disease listed below Myocardial infarction Cerebral infarction/Stroke Arrythmia that need medical treatment Unstable angina Pulmonary hypertension
• Subjects who are positive for Hepatitis B, Hepatitis C, and HIV
• History of relevant allergy/hypersensitivity
• Subjects who took prescribed medications within 14 days or over-the-counter (OTC) medications within 7 days prior to the first dose of the study drug
• Subjects who have been consuming over 21 unit(1 unit = 10 g of alcohol) per week of alcohol prior to the study initiation or who is not able to stop consuming alcohol throughout the hospitalization period
• Subjects who consumed products listed below within 2 days prior to the first dose of the study drug or who is not able to stop consuming products listed below until the last site visit Foods and/or beverages containing grapefruit Products containing caffeine (Coffee, tea, chocolate, caffeine-containing soft drinks)
• Subject who is not willing to use contraception throughout the study
• Subjects who have smoked over 10 cigarettes until 3 months prior to the study initiation or who is not able to stop smoking throughout the hospitalization period
• Subjects who have donated whole blood within 2 months or blood component within 1 month or received blood transfusion within 1 month of participating in this study
• Administration of any investigational products within 3 months from the first dose of the study drug
• Subject who's serum prolactin is over 3-fold higher than the upper limit of normal range
• Subject who judged not eligible for study participation by investigator

Study Plan

How is the study designed?

Design Details

• Primary Purpose: BASIC_SCIENCE
• Allocation: NON_RANDOMIZED
• Interventional Model: PARALLEL
• Masking: NONE

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: Part 1; Investigate the absorption, metabolism, and excretion of YH12852	Drug: YH12852; YH12852 administration; Drug: 14C-labeled YH12852; 14C-labeled YH12852 administration
EXPERIMENTAL: Part 2; Investigate the absolute bioavailability of YH12852	Drug: YH12852; YH12852 administration; Drug: 14C-labeled YH12852; 14C-labeled YH12852 administration

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Total radioactivity	Total radioactivity recovered	0 - 288 hours (post-dose)
Cmax of YH12852	Peak concentration of YH12852	0(pre-dose), 1, 2, 3, 4, 5, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288 hours (post-dose)
AUClast of YH12852	Area under the concentration-time curve from time 0 to the last measurable time of YH12852	0(pre-dose), 1, 2, 3, 4, 5, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288 hours (post-dose)
Fpo of YH12852	Oral bioavailability of YH12852	0(pre-dose), 1, 2, 3, 4, 5, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288 hours (post-dose)

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Aef of YH12852	Amount excreted in feces of YH12852	0 - 288 hours (post-dose)
Aeu of YH12852	Amount excreted in urine of YH12852	0 - 288 hours (post-dose)

Collaborators and Investigators

• Sponsor: Seoul National University Hospital
• Investigators: Principal Investigator: Howard Lee, MD., PhD, Seoul National University Hospital

Study record dates

Study Major Dates

• Study Start (ACTUAL): March 16, 2017
• Primary Completion (ACTUAL): March 29, 2017
• Study Completion (ACTUAL): March 29, 2017

Study Registration Dates

• First Submitted: October 29, 2017
• First Submitted That Met QC Criteria: December 18, 2017
• First Posted (ACTUAL): December 22, 2017

Study Record Updates

• Last Update Posted (ACTUAL): December 22, 2017
• Last Update Submitted That Met QC Criteria: December 18, 2017
• Last Verified: May 1, 2016

More Information

Terms related to this study

• Keywords: Microtracer; Microdose; Absolute bioavailability; Accelerated Mass Spectrometry; hAME
• Additional Relevant MeSH Terms: Signs and Symptoms, Digestive; Constipation; Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Serotonin Agents; Serotonin Receptor Agonists; Serotonin 5-HT4 Receptor Agonists; YH12852
• Other Study ID Numbers: YH12852-103(I)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: UNDECIDED

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No