A Drug-drug Interaction Trial of Loperamide Pharmacokinetics Effect on Pyrotinib Maleate

October 27, 2022 updated by: Jiangsu HengRui Medicine Co., Ltd.

A Single Center, Single Arm, Open and Fixed Sequence Study to Investigate the Pharmacokinetic Effects of Loperamide on Pyrotinib Maleate in Healthy Subjects

The primary objective of the study was to assess the effect of repeated oral doses of Loperamide on the pharmacokinetic profile of a single dose of Pyrotinib Maleate.

The secondary objective of the study was to assess the safety of Pyrotinib Maleate given alone versus Fluzoparib coadministered with Loperamide.

Study Overview

Status

Completed

Study Type

Interventional

Enrollment (Actual)

18

Phase

  • Phase 1

Contacts and Locations

This section provides the contact details for those conducting the study, and information on where this study is being conducted.

Study Locations

    • Hunan
      • Changsha, Hunan, China, 410008
        • Xiangya Hospital Central South University

Participation Criteria

Researchers look for people who fit a certain description, called eligibility criteria. Some examples of these criteria are a person's general health condition or prior treatments.

Eligibility Criteria

Ages Eligible for Study

18 years to 45 years (ADULT)

Accepts Healthy Volunteers

Yes

Genders Eligible for Study

All

Description

Inclusion Criteria:

  • 1) Sign the informed consent form before the trial and fully understand the trial content, process and possible adverse reactions; 2) Ability to complete the study as required by the protocol; 3) Age on the date of signing the informed consent form is 18 to 45 years old (including both ends); 4) The fasting weight is not less than 50kg (male) and 45kg (female), and the body mass index (BMI) is in the range of 19 kg/m2 to 26 kg/m2 (including both ends);

Exclusion Criteria:

  • 1) Participate in blood donation within 3 months before screening and donate blood volume ≥400mL or blood loss ≥400mL, or receive blood transfusion; 2) Allergic constitution, including a history of severe drug allergy or drug allergy; a history of allergies to Pyrotinib/ Loperamide capsule or its excipients; 3) with drug and/or alcohol abuse history, or alcohol and drug screening positives, or drug abuse in the past five years or used drugs 3 months before the trial; 4) Patients with bad habits (such as drinking 14 units of alcohol per week: 1 unit = 285mL of beer, 25mL of spirits, or 100mL of wine), smoking addiction (≥5 cigarettes per day);and could not prohibit smoking and alcohol during the trial period ; 5) QTc interval ≥ 450 ms in males and ≥ 470 ms in females; 6) left ventricular ejection fraction (LVEF) < 50% by echocardiography; 7) Other important organ diseases such as the nervous system, cardiovascular system, urinary system, digestive system, respiratory system, metabolic and musculoskeletal system with clear medical history (such as uncontrolled diabetes, high blood pressure, etc.), enabling investigators considered unsuitable for participation in the study; 8) Anyone who has undergone any surgery within the first 6 months of screening; 9) Take any hepatotoxic drugs (eg dapsone, erythromycin, fluconazole, ketoconazole, rifampicin, etc.) within the first 6 months of screening; 10) Those who have taken any clinical trial drugs within 3 months; 11) Take any drug that affects liver metabolism within 4 weeks before taking the investigational drug; 12) Take any prescription or over-the-counter medication, vitamin products or herbs within 2 weeks before taking the investigational drug; 13) Clinical laboratory tests are abnormal and clinically significant, or other clinical findings indicate the following diseases, including but not limited to gastrointestinal, kidney, liver, nerve, blood, endocrine, tumor, lung, immune, mental or cardiovascular disease; 14) Female subjects during pregnancy, lactation, and subjects who were unable to abstain or take effective non-drug contraceptives during the study period and for at least 3 months after the last study drug administration (for female subjects Require abstinence or effective non-drug contraceptives two weeks before study entry); 15) combined with other viral infections (anti-HCV, anti-HIV positive, HBsAg positive) or combined with syphilis infection; 16) Anyone who has ingested grapefruit or grapefruit-containing products, foods or drinks containing caffeine, xanthine or alcohol; strenuous exercise, or other factors affecting drug absorption, distribution, metabolism, excretion Within 48 hours; 17) Anyone who has pseudoulcerative colitis caused by acute ulcerative colitis or broad-spectrum antibiotics, or those who need to avoid inhibition of bowel movements, especially patients with intestinal obstruction, flatulence or constipation, or have diarrhea, dry mouth, Gastrointestinal symptoms such as bloating, loss of appetite, gastrointestinal cramps, nausea, vomiting, constipation, and dizziness, headache, and fatigue; 18) Anyone who has special requirements for diet and cannot comply with the diet and corresponding regulations provided by the test; 19) Anyone who has a history of dizzy needles and blood halo, who have difficulty collecting blood or cannot tolerate venipuncture; 20) The investigator believes that the subjects are not eligible to participate in this trial.

Study Plan

This section provides details of the study plan, including how the study is designed and what the study is measuring.

How is the study designed?

Design Details

  • Primary Purpose: BASIC_SCIENCE
  • Allocation: NA
  • Interventional Model: SINGLE_GROUP
  • Masking: NONE

Arms and Interventions

Participant Group / Arm
Intervention / Treatment
EXPERIMENTAL: Treament
Subjects receiving a single oral dose of pyrotinib maleate and wash-out for 6 days, then receiving Loperamide 4 mg bid from day 7 to day 13, with a single oral dose of pyrotinib maleate coadministered on day 10 .
a single oral dose of pyrotinib maleate on day 1 & day10 .
Loperamide 4 mg bid from day 7 to day 13

What is the study measuring?

Primary Outcome Measures

Outcome Measure
Measure Description
Time Frame
Pharmacokinetics parameter: Cmax of pyrotinib
Time Frame: through study completion, an average of 20 days
Peak Plasma Concentration (Cmax) of pyrotinib
through study completion, an average of 20 days
Pharmacokinetics parameter: AUC of pyrotinib
Time Frame: through study completion, an average of 20 days
Area under the plasma concentration versus time curve (AUC) of pyrotinib
through study completion, an average of 20 days

Secondary Outcome Measures

Outcome Measure
Measure Description
Time Frame
Pharmacokinetics parameter: Tmax of pyrotinib
Time Frame: through study completion, an average of 20 days
Time of maximum observed concentration (Tmax) of pyrotinib
through study completion, an average of 20 days
Pharmacokinetics parameter: T1/2 of pyrotinib
Time Frame: through study completion, an average of 20 days
Time of maximum observed concentration (Tmax) of pyrotinib
through study completion, an average of 20 days
Pharmacokinetics parameter: CL/F of pyrotinib
Time Frame: through study completion, an average of 20 days
Total body clearance for extravascular administration (CL/F) of pyrotinib
through study completion, an average of 20 days
Pharmacokinetics parameter: Vz/F of pyrotinib
Time Frame: through study completion, an average of 20 days
Volume of distribution (Vz/F) of pyrotinib
through study completion, an average of 20 days
Number of participants with treatment-related adverse events as assessed by CTCAE v5.0
Time Frame: through study completion, an average of 20 days
An adverse event is any untoward medical occurrence in a patient or clinical study participant
through study completion, an average of 20 days

Collaborators and Investigators

This is where you will find people and organizations involved with this study.

Study record dates

These dates track the progress of study record and summary results submissions to ClinicalTrials.gov. Study records and reported results are reviewed by the National Library of Medicine (NLM) to make sure they meet specific quality control standards before being posted on the public website.

Study Major Dates

Study Start (ACTUAL)

April 13, 2020

Primary Completion (ACTUAL)

April 30, 2020

Study Completion (ACTUAL)

September 1, 2020

Study Registration Dates

First Submitted

March 18, 2020

First Submitted That Met QC Criteria

March 18, 2020

First Posted (ACTUAL)

March 19, 2020

Study Record Updates

Last Update Posted (ACTUAL)

October 28, 2022

Last Update Submitted That Met QC Criteria

October 27, 2022

Last Verified

March 1, 2020

More Information

Terms related to this study

Additional Relevant MeSH Terms

Other Study ID Numbers

  • HR-BLTN-DDI-04

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

This information was retrieved directly from the website clinicaltrials.gov without any changes. If you have any requests to change, remove or update your study details, please contact register@clinicaltrials.gov. As soon as a change is implemented on clinicaltrials.gov, this will be updated automatically on our website as well.

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