Effect of Itraconazole on the Pharmacokinetics of Apatinib

Effect of Itraconazole on the Pharmacokinetics of Apatinib in Chinese Healthy Volunteers

he primary purpose of this study is to investigate potential pharmacokinetic interaction in healthy volunteers when apatinib is administered in combination with itraconazole. Secondary objective is evaluating the safety and tolerability of apatinib alone and when co-administered with itraconazole.

Study Overview

• Status: Completed
• Conditions: Neoplasms
• Intervention / Treatment: Drug: Apatinib Mesylate Tablets; Drug: Itraconazole Capsules

• Study Type: Interventional
• Enrollment (Actual): 20
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Shanghai
    • Shanghai, Shanghai, China, 200030
      • Shanghai Xuhui Central Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• female of non-childbearing potential or male;
• age 18-45 years;
• body mass index 19-24 kg/m2 with total body weight;

Exclusion Criteria:

• clinically signiWcant medical or surgical conditions with the potential to interfere with the absorption, distribution, metabolism or excretion of the study drugs;
• history of alcohol abuse; smoker;
• electrocardiogram(ECG) abnormality;
• blood pressure >140/90 mmHg;
• treatment with an investigational drug or any known CYP450 enzyme inducing/-inhibiting agents or herbal supplements within 14 days prior to first dose of study medication;
• Subjects were to abstain from using prescription and non-prescription drugs (other than acetaminophen as deemed necessary), vitamins and dietary supplements within 14 days prior to the first dose of study medication and throughout the study.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Treatment; subjects receiving a single 250 mg oral dose of apatinib mesylate tablets and wash-out for 3 days,then Itraconazole capsules 100 mg/day orally for 6 days with a single 250 mg oral dose of apatinib mesylate tablets co-administered on day 4 . apatinib mesylate tablets was administered in the morning after an overnight fast of at least 10 h	Drug: Apatinib Mesylate Tablets; apatinib was administered in the morning after an overnight fast of at least 10 h; Other Names: apatinib; Drug: Itraconazole Capsules; rifampicin was administered in the morning 0.5 hours after breakfast; Other Names: itraconazole

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Area under the plasma concentration versus time curve (AUC) of Apatinib	0~72h after apatinib administration

Secondary Outcome Measures

Outcome Measure	Time Frame
Number of participants with treatment-related adverse events as assessed by CTCAE v4.0	From first administration to the seventh day after last administration
Peak Plasma Concentration (Cmax) of Apatinib	0~72h after apatinib administration

Collaborators and Investigators

• Sponsor: Jiangsu HengRui Medicine Co., Ltd.
• Investigators: Principal Investigator: Chen Yu, Shanghai Xuhui Central Hospital

Study record dates

Study Major Dates

• Study Start: July 1, 2016
• Primary Completion (Actual): February 1, 2017
• Study Completion (Actual): February 1, 2017

Study Registration Dates

• First Submitted: July 14, 2016
• First Submitted That Met QC Criteria: July 15, 2016
• First Posted (Estimate): July 18, 2016

Study Record Updates

• Last Update Posted (Actual): February 27, 2017
• Last Update Submitted That Met QC Criteria: February 23, 2017
• Last Verified: July 1, 2016

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Anti-Infective Agents; Enzyme Inhibitors; Antineoplastic Agents; Hormones, Hormone Substitutes, and Hormone Antagonists; Protein Kinase Inhibitors; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inhibitors; Hormone Antagonists; Antifungal Agents; Steroid Synthesis Inhibitors; 14-alpha Demethylase Inhibitors; Itraconazole; Apatinib; Hydroxyitraconazole
• Other Study ID Numbers: HR-APTN-DDI-03

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
• product manufactured in and exported from the U.S.: No