The Safety, Tolerability and Pharmacokinetic Study of Litapiprant Tablets in Healthy Male and Female Subjects

A Randomized, Double-blind, Placebo-controlled, Single Ascending Dose, Single-center Study to Assess the Safety, Tolerability and Pharmacokinetic of Litapiprant Tablets in Healthy Subjects

The Safety, Tolerability and Pharmacokinetic Study of Asthma Treatment Drug Litapiprant Tablets in Healthy Male and Female subjects.

Study Overview

• Status: Completed
• Conditions: Asthma
• Intervention / Treatment: Drug: Litapiprant Tablet

Detailed Description

This was a Randomized，Double-blind, Placebo-controlled, Single Ascending Dose, Single-center Study to Assess the Safety, Tolerability and Pharmacokinetic of Litapiprant Tablets in Healthy Male and Female subjects. A total of 60 healthy subjects were divided into 7 groups. Group 1 consist of 4 subjects, 3 subjects will receive Litapiprant Tablets and 1 subject will receive placebo.Group 2,3,5,6 consist of 8 subjects respectively, in each group, 6 subjects will receive Litapiprant Tablets and 2 subjects will receive placebo.Group 4,7 consist of 12 subjects respectively, in each group, 10 subjects will receive Litapiprant Tablets and 2 subjects will receive placebo.

• Study Type: Interventional
• Enrollment (Actual): 60
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Beijing
    • Beijing, Beijing, China, 100038
      • Beijing Shijitan Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Male or female, overall healthy subjects，female VS male 1:1 ratio;
• Between 18 and 45 years of age, inclusive, similar ages;
• Body weight should be≥50 kg; Body Mass Index (BMI) is between 19.0 and 28.0 kg/m2, inclusive;
• Able to comprehend and sign the ICF voluntarily prior to initiate the study;
• Able to communicate well with the investigator and complete the study according to the protocol.

Exclusion Criteria:

• Pregnant or nursing female, or plan for pregnancy within 6 months;
• A clinically significant abnormal finding on the physical exam, medical history, electrocardiogram (ECG), or clinical laboratory results at screening;
• Has a positive test for hepatitis B surface antigen, hepatitis C antibody, syphilis antibody， or HIV antibody . A clinically significant abnormal finding on HBV-DNA test ;
• Sitting systolic blood pressure (SBP) <90mmHg or >140mmHg, and/or sitting diastolic blood pressure (DBP) <60mmHg or >90mmHg at screening;
• With the history of using any drug which will inhibit or induce liver metabolize drug and/or will infect gastric acid within 1 month before randomization;
• Receipt of any medication including over the counter preparations and vitamins within 14 days of the first study day;
• History of cardiovascular, immune system, Severe digestive system, Circulatory system, respiratory system, urinary system , nervous system,tumor diseases;
• Suffering from blood diseases such as coagulopathy;
• Patients with a history of mental illness or active mental illness;
• Have undergone major surgery within 6 months before enrollment;
• A history of gastrointestinal, liver ,kidney diseases likely to influence drug absorption within 6 months before enrollment;
• Drug or alcohol abuse;
• History of drug abuse and drug use within 1 year prior to the study;
• Habitual consumption of grapefruit juice, tea, coffee and/or caffeinated beverages, which cannot be withdrawn during the trial;
• The average daily smoking volume is >5 within 3 months prior to the study;
• A history of hypersensitivity and/or idiosyncrasy to any of the test compounds or related drugs or excipients employed in this study;
• Participation in a clinical study within 3 months of the first dose of study drug;
• Donation of blood within 3 months of the first dose of study drug or have a plan to donate blood;
• Cannot be tolerant to oral drugs;
• Poor peripheral venous access conditions;
• The investigator believes that it should not be included;
• Additional exclusion criteria apply.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Sequential Assignment
• Masking: Quadruple

Number of Arms

7

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Placebo Comparator: 25mg single doses; Intervention Drug: 25mg Litapiprant Tablet administered orally once daily Intervention Drug: Matching Placebo Tablet administered orally once daily	Drug: Litapiprant Tablet; Small molecules inhibitors of the chemoattractant receptor homologous molecule expressed on Th2 cells
Placebo Comparator: 50mg single doses; Intervention Drug: 50mg Litapiprant Tablet administered orally once daily Intervention Drug: Matching Placebo Tablet administered orally once daily	Drug: Litapiprant Tablet; Small molecules inhibitors of the chemoattractant receptor homologous molecule expressed on Th2 cells
Placebo Comparator: 100mg single doses; Intervention Drug: 100mg Litapiprant Tablet administered orally once daily Intervention Drug: Matching Placebo Tablet administered orally once daily	Drug: Litapiprant Tablet; Small molecules inhibitors of the chemoattractant receptor homologous molecule expressed on Th2 cells
Placebo Comparator: 200mg single doses; Intervention Drug: 200mg Litapiprant Tablet administered orally once daily Intervention Drug: Matching Placebo Tablet administered orally once daily	Drug: Litapiprant Tablet; Small molecules inhibitors of the chemoattractant receptor homologous molecule expressed on Th2 cells
Placebo Comparator: 400mg single doses; Intervention Drug: 400mg Litapiprant Tablet administered orally once daily Intervention Drug: Matching Placebo Tablet administered orally once daily	Drug: Litapiprant Tablet; Small molecules inhibitors of the chemoattractant receptor homologous molecule expressed on Th2 cells
Placebo Comparator: 600mg single doses; Intervention Drug: 600mg Litapiprant Tablet administered orally once daily Intervention Drug: Matching Placebo Tablet administered orally once daily	Drug: Litapiprant Tablet; Small molecules inhibitors of the chemoattractant receptor homologous molecule expressed on Th2 cells
Placebo Comparator: 800mg single doses; Intervention Drug: 800mg Litapiprant Tablet administered orally once daily Intervention Drug: Matching Placebo Tablet administered orally once daily	Drug: Litapiprant Tablet; Small molecules inhibitors of the chemoattractant receptor homologous molecule expressed on Th2 cells

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Adverse events	To assess the safety and tolerability after a single dose of Litapiprant Tablets	Baseline to day 8~10

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
AUC0-∞	area under the concentration versus time curve (AUC) from time zero to infinity	Prior to dosing（0 hour）and 0.25 hour、0.5 hour、1 hour、1.5 hours、2 hours、3 hours、4 hours、6 hours、8 hours、10 hours、12 hours、24 hours、36 hours、48 hours、72 hours、96 hours after dosing
AUC0-t	AUC from time zero to the time of the last quantifiable concentration time zero to the time of the last quantifiable concentration	Prior to dosing（0 hour）and 0.25 hour、0.5 hour、1 hour、1.5 hours、2 hours、3 hours、4 hours、6 hours、8 hours、10 hours、12 hours、24 hours、36 hours、48 hours、72 hours、96 hours after dosing
Cmax	maximum observed plasma concentration	Prior to dosing（0 hour）and 0.25 hour、0.5 hour、1 hour、1.5 hours、2 hours、3 hours、4 hours、6 hours、8 hours、10 hours、12 hours、24 hours、36 hours、48 hours、72 hours、96 hours after dosing
tmax	time of the maximum observed plasma concentration	Prior to dosing（0 hour）and 0.25 hour、0.5 hour、1 hour、1.5 hours、2 hours、3 hours、4 hours、6 hours、8 hours、10 hours、12 hours、24 hours、36 hours、48 hours、72 hours、96 hours after dosing
t½	apparent terminal elimination half-life	Prior to dosing（0 hour）and 0.25 hour、0.5 hour、1 hour、1.5 hours、2 hours、3 hours、4 hours、6 hours、8 hours、10 hours、12 hours、24 hours、36 hours、48 hours、72 hours、96 hours after dosing
Vz/F	apparent volume of distribution	Prior to dosing（0 hour）and 0.25 hour、0.5 hour、1 hour、1.5 hours、2 hours、3 hours、4 hours、6 hours、8 hours、10 hours、12 hours、24 hours、36 hours、48 hours、72 hours、96 hours after dosing

Collaborators and Investigators

• Sponsor: Sunshine Lake Pharma Co., Ltd.
• Investigators: Principal Investigator: Xinghe Wang, MD, Beijing Shijitan Hospital, Capital Medical University

Study record dates

Study Major Dates

• Study Start (Actual): October 25, 2018
• Primary Completion (Actual): January 30, 2019
• Study Completion (Actual): January 30, 2019

Study Registration Dates

• First Submitted: September 2, 2018
• First Submitted That Met QC Criteria: September 6, 2018
• First Posted (Actual): September 10, 2018

Study Record Updates

• Last Update Posted (Actual): July 27, 2020
• Last Update Submitted That Met QC Criteria: July 23, 2020
• Last Verified: November 1, 2018

More Information

Terms related to this study

• Other Study ID Numbers: HEC46877-P-01

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

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