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Absorption, Metabolism, Excretion and Absolute Bioavailability

2017년 12월 19일 업데이트: Pfizer

A Phase 1, Open-label, Non-randomized, 2-period, Fixed Sequence Study To Investigate The Absorption, Metabolism And Excretion Of [14c-pf-04965842] And To Assess The Absolute Bioavailability And Fraction Absorbed Of Pf-04965842 In Healthy Male Subjects Using A 14c-microtracer Approach

This study will investigate the absorption, metabolism and excretion of 14C-PF 04965842 and characterize plasma, fecal and urinary radioactivity and identify any metabolites, if possible, of 14C PF-04965842 in humans. In addition, this study will provide a better understanding of the pharmacokinetic disposition of PF-04965842 by obtaining intravenous (IV) clearance and delineating the extent of oral absorption (absolute bioavailability (F) and fraction absorbed (Fa)).

연구 개요

상태

완전한

정황

개입 / 치료

연구 유형

중재적

등록 (실제)

6

단계

  • 1단계

연락처 및 위치

이 섹션에서는 연구를 수행하는 사람들의 연락처 정보와 이 연구가 수행되는 장소에 대한 정보를 제공합니다.

연구 장소

      • Groningen, 네덜란드, 9713 GZ
        • PRA Health Sciences
      • Groningen, 네덜란드, 9728 NZ
        • PRA Health Sciences

참여기준

연구원은 적격성 기준이라는 특정 설명에 맞는 사람을 찾습니다. 이러한 기준의 몇 가지 예는 개인의 일반적인 건강 상태 또는 이전 치료입니다.

자격 기준

공부할 수 있는 나이

18년 (성인)

건강한 자원 봉사자를 받아들입니다

아니

연구 대상 성별

남성

설명

Inclusion Criteria:

  1. Healthy male subjects who, at the time of screening, are between the ages of 18 and 55 years, inclusive. Healthy is defined as no clinically relevant abnormalities identified by a detailed medical history, full physical examination, including blood pressure and pulse rate measurement, 12 lead electrocardiogram (ECG), or clinical laboratory tests.
  2. Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lbs).
  3. Evidence of a personally signed and dated informed consent document indicating that the subject has been informed of all pertinent aspects of the study.
  4. Subjects who are willing and able to comply with study confinement period, scheduled visits, treatment plan, laboratory tests, contraceptive requirements and other study procedures.

Exclusion Criteria

Subjects with any of the following characteristics/conditions will not be included in the study:

  1. Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies).
  2. Any clinically significant malabsorption condition (eg, gastrectomy, bowel resection).
  3. A positive urine drug screen for drugs of abuse or recreational drugs.
  4. History of human immunodeficiency virus (HIV), hepatitis B, or hepatitis C; positive testing for HIV, hepatitis B surface antigen (HepBsAg), hepatitis B core antibody (HepBcAb), or hepatitis C antibody (HCVAb).
  5. History of abuse of alcohol or binge drinking and/or any other illicit drug use or dependence within 6 months of Screening. Binge drinking is defined as a pattern of 5 or more alcoholic drinks (male) in about 2 hours. As a general rule, alcohol intake should not exceed 21 units per week (1 unit = ½ pint beer, 25 mL of 40% spirit or a 125 mL glass of wine).
  6. Use of tobacco/nicotine containing products in excess of 5 cigarettes/day.
  7. Treatment with an investigational drug within 60 days.
  8. Total 14C radioactivity measured in plasma exceeding 11 mBq/mL.
  9. Screening supine blood pressure >=140 mm Hg (systolic) or >=90 mm Hg (diastolic), following at least 5 minutes of supine rest. If blood pressure is >=140 mm Hg (systolic) or >=90 mm Hg (diastolic), the blood pressure measurement should be repeated two more times and the average of the three measurements should be used to assess the subject's eligibility.
  10. Supine 12 lead ECG demonstrating QTcF >450 msec or a QRS interval >120 msec at screening. If QTcF exceeds 450 msec, or QRS exceeds 120 msec, the ECG should be repeated two more times and the average of the three QTcF or QRS values should be used to determine the subject's eligibility.
  11. Use of prescription or nonprescription drugs (including vitamins and dietary supplements) within 7 days or 5 half lives (whichever is longer) prior to the first dose of study medication. As an exception, acetaminophen may be used at doses of =<1 g/day. Limited use of non prescription medications that are not believed to affect subject safety or the overall results of the study may be permitted on a case by case basis following approval by Pfizer.
  12. Use of herbal supplements within 28 days prior to the first dose of study medication.
  13. Blood donation (excluding plasma donations) of no more than 100 mL or more within 56 days prior to dosing.
  14. An estimated glomerular filtration rate of <90 mL/min/1.73 m2 based on the four variable Modification of Diet in Renal Disease (MDRD) equation.
  15. History of tuberculosis or active or latent or inadequately treated infection, positive QuantiFERON TB Gold test.
  16. Any medical history of disease (ie, Gilbert's disease) that has the potential to cause a rise in total bilirubin over the upper limit of normal (ULN).
  17. Subjects with ANY of the following abnormalities in clinical laboratory tests at Screening, as assessed by the study specific laboratory and confirmed by a single repeat, if deemed necessary:

    • Serum aspartate aminotransferase (AST) or alanine aminotransferase (ALT) >=1.5 × ULN, total serum bilirubin >= 25.6 micromol/L;
    • Hemoglobin =<2.17 mmol/L (males).
  18. Known participation in a clinical trial for PF 04965842 within 60 days prior to the first dose of study medication.
  19. Serious adverse reaction or serious hypersensitivity to any drug or the formulation excipients.
  20. Unwilling or unable to comply with the Lifestyle Requirements described in this protocol.
  21. Subjects who are investigational site staff members directly involved in the conduct of the study and their family members, site staff members otherwise supervised by the Investigator, or subjects who are Pfizer employees, including their family members, directly involved in the conduct of the study.
  22. Systemic therapy with any of the following medications that are CYP3A4 inhibitors within 7 days or 5 half lives (whichever is longer) or CYP3A inducers within 28 days prior to the first dose of the trial medication, or during the trial (Section 5.7).
  23. History of sensitivity to heparin or heparin induced thrombocytopenia.
  24. Other acute or chronic medical or psychiatric condition including recent (within the past year) or active suicidal ideation or behavior or laboratory abnormality that may increase the risk associated with study participation or investigational product administration or may interfere with the interpretation of study results and, in the judgment of the investigator, would make the subject inappropriate for entry into this study.
  25. Subjects with conditions that affect their ability to taste ie, dysgeusia, respiratory infection, cold, etc.
  26. Male subjects who are unwilling or unable to use a highly effective method of contraception as outlined in this protocol for the duration of the study and for at least 90 days after the last dose of investigational product.

공부 계획

이 섹션에서는 연구 설계 방법과 연구가 측정하는 내용을 포함하여 연구 계획에 대한 세부 정보를 제공합니다.

연구는 어떻게 설계됩니까?

디자인 세부사항

  • 주 목적: 다른
  • 할당: 무작위화되지 않음
  • 중재 모델: 크로스오버 할당
  • 마스킹: 없음(오픈 라벨)

무기와 개입

참가자 그룹 / 팔
개입 / 치료
실험적: Mass Balance
Cumulative recovery of radioactivity in urine and feces
14C labeled PF-04965842
실험적: Absolute Bioavailability
Oral absolute bioavailability
Oral dose of unlabeled PF-04965842 and an IV dose of 14C labeled PF- 04965842

연구는 무엇을 측정합니까?

주요 결과 측정

결과 측정
측정값 설명
기간
Cumulative recovery of radioactivity
기간: From predose to Day 14 day
Total radioactivity in urine and feces based on total administered dose.
From predose to Day 14 day

2차 결과 측정

결과 측정
측정값 설명
기간
Cmax
기간: From predose to Day 5
Maximum plasma concentration
From predose to Day 5
Tmax
기간: From predose to Day 5
Time to maximum concentration
From predose to Day 5
AUClast
기간: From predose to Day 5
Area under the plasma concentration-time curve from time 0 to last quantifiable concentration
From predose to Day 5
AUCinf
기간: From predose to Day 5
Area under the plasma concentration-time curve from time zero to infinity
From predose to Day 5
t1/2
기간: From predose to Day 5
Apparent terminal elimination half-life
From predose to Day 5
CL/F
기간: From predose to Day 5
Apparent total body clearance
From predose to Day 5
Vz/F
기간: From predose to Day 5
Apparent volume of distribution
From predose to Day 5
Vss (IV)
기간: From predose to Day 5
Steady State Volume of distribution
From predose to Day 5
CL (IV)
기간: From predose to Day 5
Total Body Clearance
From predose to Day 5
F
기간: From predose to Day 5
Absolute bioavailability= ratio of the adjusted geometric means of dose normalized AUCinf for unlabeled PF-04965842 and IV labeled 14C-PF-04965842
From predose to Day 5
Fa
기간: Predose to Day Day 5
Fraction of PF 04965842 dose absorbed = Total 14C urine data following both IV and oral administration of 14C PF 04965842 (quantification by AMS).
Predose to Day Day 5

공동 작업자 및 조사자

여기에서 이 연구와 관련된 사람과 조직을 찾을 수 있습니다.

스폰서

간행물 및 유용한 링크

연구에 대한 정보 입력을 담당하는 사람이 자발적으로 이러한 간행물을 제공합니다. 이것은 연구와 관련된 모든 것에 관한 것일 수 있습니다.

연구 기록 날짜

이 날짜는 ClinicalTrials.gov에 대한 연구 기록 및 요약 결과 제출의 진행 상황을 추적합니다. 연구 기록 및 보고된 결과는 공개 웹사이트에 게시되기 전에 특정 품질 관리 기준을 충족하는지 확인하기 위해 국립 의학 도서관(NLM)에서 검토합니다.

연구 주요 날짜

연구 시작 (실제)

2017년 7월 10일

기본 완료 (실제)

2017년 9월 15일

연구 완료 (실제)

2017년 9월 15일

연구 등록 날짜

최초 제출

2017년 7월 11일

QC 기준을 충족하는 최초 제출

2017년 8월 10일

처음 게시됨 (실제)

2017년 8월 15일

연구 기록 업데이트

마지막 업데이트 게시됨 (실제)

2017년 12월 21일

QC 기준을 충족하는 마지막 업데이트 제출

2017년 12월 19일

마지막으로 확인됨

2017년 12월 1일

추가 정보

이 연구와 관련된 용어

기타 연구 ID 번호

  • B7451008
  • 2017-000461-73 (EudraCT 번호)

개별 참가자 데이터(IPD) 계획

개별 참가자 데이터(IPD)를 공유할 계획입니까?

아니

IPD 계획 설명

Information relating to our policy on data sharing and the process for requesting data can be found at the following link: http://www.pfizer.com/research/clinical_trials/trial_data_and_results/data_requests

약물 및 장치 정보, 연구 문서

미국 FDA 규제 의약품 연구

아니

미국 FDA 규제 기기 제품 연구

아니

미국에서 제조되어 미국에서 수출되는 제품

아니

이 정보는 변경 없이 clinicaltrials.gov 웹사이트에서 직접 가져온 것입니다. 귀하의 연구 세부 정보를 변경, 제거 또는 업데이트하도록 요청하는 경우 register@clinicaltrials.gov. 문의하십시오. 변경 사항이 clinicaltrials.gov에 구현되는 즉시 저희 웹사이트에도 자동으로 업데이트됩니다. .

PF-04965842에 대한 임상 시험

유사한 임상시험 검색