A Food Effect Study of Apatinib Mesylate in Healthy Subjects

A Randomized, Open-label, Single Dose, Three-period, Six-sequences, Crossover Study of High-fat and Low-fat Meal Effect on the Pharmacokinetics of Apatinib Mesylate in Chinese Healthy Adult Subjects

The primary objective of the study was to assess the effect of high-fat and low-fat meal on the pharmacokinetics of apatinib mesylate in Chinese adult healthy subjects.

The secondary objective of the study was to assess the safety of apatinib mesylate administered in adult healthy subjects.

Study Overview

• Status: Completed
• Conditions: Healthy Subjects
• Intervention / Treatment: Drug: Apatinib Mesylate

• Study Type: Interventional
• Enrollment (Actual): 42
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Beijing
    • Beijing, Beijing, China, 101100
      • Beijing Luhe Hospital, Capital Medical University

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:

1. 18-45 years of age, male or female, each gender should be more than 1/4 of the whole sample size.
2. The weight of male subject ≥50kg, weight of female subject ≥45kg, 19≤BMI≤28kg/m2
3. In good health, determined by no clinically significant findings from medical history, physical examination, 12-lead ECG;
4. Agree to take approved method of contraception during the clinical trail and 8 weeks after the last dose of apatinib. Female subject should be negative in the pregnancy test;
5. Able to comprehend and willing to sign an informed consent form (ICF)

Exclusion Criteria:

1. History of drug allergy, or allergic to apatinib or ingredients;
2. Drinking 14 units of alcohol per week within 6 months prior dosing(1 unit = 360 mL of beer, or 150mL of wine) ;
3. Take any prescription or traditional Chinese medicines within four weeks prior dosing; take any over-the-counter medication, vitamin products within two weeks before dosing;
4. Take any clinical trial drugs within 3 months prior dosing;
5. Participate in blood donation within 3 months before screening and donate blood volume ≥400mL or blood loss ≥400mL, or receive blood transfusion; or donate blood volume≥200mL or blood loss ≥200mL within 1 month prior dosing.
6. Combined with other viral infections (anti-HCV, anti-HIV positive, HBsAg positive) or combined with syphilis infection;
7. Anyone who refuse to stop ingest foods or drinks containing caffeine, xanthine or alcohol from 48 hours before dosing to the end of the study;
8. Anyone who refuse to stop ingesting grapefruit or grapefruit-containing products from 7 days before dosing to the end of the study;
9. The investigator believes that the subjects are not eligible to participate in this trial.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: OTHER
• Allocation: RANDOMIZED
• Interventional Model: CROSSOVER
• Masking: NONE

Number of Arms

6

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: Arm 1; Drug:apatinib mesylate tablet , 250 mg, 3 discrete single doses separated by 4-days: the first dose will be after fasted, the second dose will be after low-fat meal, the third dose will be after high-fat meal	Drug: Apatinib Mesylate; Single dose of apatinib mesylate after high-fat meal, low fat meal and fast
EXPERIMENTAL: Arm 2; Drug:apatinib mesylate tablet , 250 mg, 3 discrete single doses separated by 4-days: the first dose will be after high-fat meal, the second dose will be after fasted, the third dose will be after low-fat meal	Drug: Apatinib Mesylate; Single dose of apatinib mesylate after high-fat meal, low fat meal and fast
EXPERIMENTAL: Arm 3; Drug:apatinib mesylate tablet , 250 mg, 3 discrete single doses separated by 4-days: the first dose will be after low-fat meal, the second dose will be after high-fat meal, the third dose will be after fasted	Drug: Apatinib Mesylate; Single dose of apatinib mesylate after high-fat meal, low fat meal and fast
EXPERIMENTAL: Arm 4; Drug:apatinib mesylate tablet , 250 mg, 3 discrete single doses separated by 4-days: the first dose will be after fasted, the second dose will be after high-fat meal, the third dose will be after low-fat meal	Drug: Apatinib Mesylate; Single dose of apatinib mesylate after high-fat meal, low fat meal and fast
EXPERIMENTAL: Arm 5; Drug:apatinib mesylate tablet , 250 mg, 3 discrete single doses separated by 4-days: the first dose will be after low-fat meal, the second dose will be after fasted, the third dose will be after high-fat meal	Drug: Apatinib Mesylate; Single dose of apatinib mesylate after high-fat meal, low fat meal and fast
EXPERIMENTAL: Arm 6; Drug:apatinib mesylate tablet , 250 mg, 3 discrete single doses separated by 4-days: the first dose will be after high-fat meal, the second dose will be after low-fat meal, the third dose will be after fasted	Drug: Apatinib Mesylate; Single dose of apatinib mesylate after high-fat meal, low fat meal and fast

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax	Maximum Observed Plasma Concentration for apatinib [ Time Frame: Day 1: 0-72 hours; Day5: 0-72 hours;Day9:0-72hours ]	Time Frame: Day 1: 0-72 hours; Day5: 0-72 hours;Day9:0-72hours
AUC0-t	Area Under the Concentration-time Curve From Zero (Pre-dose) to Time of Last Quantifiable Concentration for apatinib	Time Frame: Day 1: 0-72 hours; Day5: 0-72 hours;Day9:0-72hours
AUC0-inf	Area Under the Plasma Concentration-time Curve from Time 0 to Infinite Time for apatinib	Time Frame: Day 1: 0-72 hours; Day5: 0-72 hours;Day9:0-72hours

Collaborators and Investigators

• Sponsor: Jiangsu HengRui Medicine Co., Ltd.

Study record dates

Study Major Dates

• Study Start (ACTUAL): May 13, 2020
• Primary Completion (ACTUAL): July 6, 2020
• Study Completion (ACTUAL): July 6, 2020

Study Registration Dates

• First Submitted: April 8, 2020
• First Submitted That Met QC Criteria: April 8, 2020
• First Posted (ACTUAL): April 10, 2020

Study Record Updates

• Last Update Posted (ACTUAL): October 22, 2021
• Last Update Submitted That Met QC Criteria: October 19, 2021
• Last Verified: October 1, 2021

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Antineoplastic Agents; Protein Kinase Inhibitors; Apatinib
• Other Study ID Numbers: HR-APTN-I-009

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