A Mass Balance Study to Investigate the Absorption, Metabolism, and Excretion Of [14C] Fruquintinib

NCT02689752 | Completed Phase 1

• 1 other identifier: 2015-013-00CH2
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

This will be an open-label, single-center study to evaluate pharmacokinetics and safety of HMPL-013 in approximately 6 healthy male subjects receiving a single oral 5mg dose of HMPL-013 containing approximately 100 microcuries of \[14C\] HMPL-013. This study will investigate the absorption, drug biotransformation and mass balance of HMPL-013, seek to identify the compound's major metabolites and supply information for clinical application.

Conditions

Healthy

Keywords

mass balance; 14C

Outcome Measures

Primary Outcomes (1)

• Total radioactivity on blood, urine and faeces (radiocarbon) following oral suspension [14C]HMPL-013 dosing

  Total radioactivity in blood to determine Cmax, Tmax, Half-life, AUC0-t, AUC0-∞ Total radioactivity in urine and faeces at each time interval and cumulative radioactivity (mass balance)

  Up to 14 days

Secondary Outcomes (4)

• Blood concentrations of HMPL-013 and its metabolites

  Up to 14 days

• Mass balance after a single oral dose of [14C] HMPL-013 as generated from recovery of total radioactivity excreted in urine and faeces.

  Up to 14 days

• Metabolite profililing and identification of metabolites in blood, urine and faeces

  up to 14 days

• Safety and tolerability parameters, including adverse events (AEs), vital signs, ECGs, and clinical laboratory assessments.

  Up to 14 days

Study Arms (1)

fruquintinib

EXPERIMENTAL

fruquintinib suspension, 5 mg （100 mCi）oral taken once

Drug: fruquintinib

Interventions

fruquintinib DRUG

fruquintinib suspension, 5mg ( 100mCi), oral, taken once, fast

Also known as: HMPL-013

fruquintinib

Eligibility Criteria

• Age: 18 Years - 40 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• A Healthy Male Volunteer between 18 and 40 years of age inclusive;
• A Body Mass Index (BMI) within the range of 19 to 25 kg/m2 and a total body weight \>50kg;
• Medically normal subjects with no significant abnormal findings at the screening vital signs, physical examination, electrocardiogram (ECG), and laboratory parameters as evaluated by the investigator;
• Fertile male subjects and their partners are willing to undergo contraception as follows: condom, contraceptive sponge, contraceptive gel, contraceptive diaphragm, intrauterine devices, hormonal contraceptives (oral or injectable), subepidermal contraceptive implant and other contraception methods during the study and until 1 year after taking the dose of investigational product,
• Subject must voluntarily consent to participate in this study, provide their written informed consent prior to start of any study- specific procedures and be willing to comply with all study procedures.

You may not qualify if:

• Subjects who have a family history of coronary heart disease;
• Subjects who have a known history of bleeding such as gingival hemorrhage, epistaxis and hemorrhoid bleeding etc.;
• Subjects have hypertension (Systolic Pressure ≥140 mmHg or Diastolic Pressure ≥90 mmHg);
• Subjects who are taking, or have taken any drugs that affect metabolism or prescription medication during the screening or within 30 days prior to the screening; Subjects who are taking, or have taken any OTC, herbal remedies or Vitamin during the screening or within 14 days prior to the screening; Subjects who are taking, or have taken any plant extracts like Hypericum Perforatum L. which are not therapeutic but have health function and can affect the absorption and metabolism during the screening or within 3 days prior to the screening; Subjects who have participated in another clinical trial within 2 months prior to the screening;
• Subjects who are taking, or have taken any drugs which have toxicity to major organs during the screening or within 3 months prior to the screening;
• Subjects who test positive for nicotine screening or can't quit smoking completely in the study;
• Subjects who have history or presence of any clinically significant diseases within 3 months prior to the screening;
• Subjects who have history or presence of gastrointestinal, hepatic, renal diseases or any other known condition that can affect the absorption, distribution, metabolism or excretion of the investigational product;
• Subjects who have chronic constipation, diarrhea, irritable bowel syndrome or inflammatory bowel disease;
• Subjects who have hemorrhoids or perianal complications with regular hematochezia;
• Subjects who have a known history of severe allergic reaction such as drug allergy or had an acute allergic rhinitis or food allergy within 14 days prior to the study medication;
• Subjects who have donated blood or plasma more than 500ml within 2 months prior to the study medication or more than 50ml within 14 days prior to the study medication;
• Subjects who have had a positive test for hepatitis B (HBsAg) or hepatitis C (excluded immunization);
• Subjects who have had a positive test for human immunodeficiency virus (HIV);
• Subjects who have taken vaccination during the screening or within 6 months prior to the screening;

Sponsors & Collaborators

• Hutchison Medipharma Limited: lead

Study Sites (1)

Jiangsu Province Hospital

Nanjing, Jiangsu, 210029, China

Location

MeSH Terms

Interventions

HMPL-013

Study Officials

• Weiguo Su, PHD

  Hutchison Medipharma Limited

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: OTHER
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 3, 2016
• First Posted: February 24, 2016
• Study Start: July 1, 2016
• Primary Completion: September 1, 2016
• Study Completion: September 1, 2016
• Last Updated: February 13, 2020

Record last verified: 2020-02

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)