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A Study to Assess the Absolute Bioavailability of Oral PCI-32765 and the Effect of Grapefruit Juice on the Bioavailability of PCI-32765 in Healthy Participants

This study has been completed.
Sponsor:
ClinicalTrials.gov Identifier:
NCT01866033
First Posted: May 31, 2013
Last Update Posted: March 18, 2014
The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details.
Collaborator:
Pharmacyclics LLC.
Information provided by (Responsible Party):
Janssen Research & Development, LLC
  Purpose
The purpose of this study is to assess the absolute bioavailability of oral PCI-32765 and the effect of grapefruit juice on the absorption of PCI-32765 in healthy adult participants.

Condition Intervention Phase
Healthy Volunteer Drug: PCI-32765 (Treatment A) Drug: PCI-32765 (Treatment B) Drug: PCI-32765 (Treatment C) Drug: 13C6 PCI-32765 (reference) Phase 1

Study Type: Interventional
Study Design: Intervention Model: Single Group Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: An Open-Label, Sequential and 2-Way Crossover Pharmacokinetic Study to Assess the Absolute Bioavailability of Oral PCI-32765 and the Effect of Grapefruit Juice on the Bioavailability of PCI-32765 in Healthy Subjects

Resource links provided by NLM:


Further study details as provided by Janssen Research & Development, LLC:

Primary Outcome Measures:
  • Area under the plasma concentration-time curve from time 0 to 24 hours of PCI-32765 [ Time Frame: Predose, and postdose at 30 min, 1 h, 1.5 h, 2 h, 2 h 2 min, 2 h 5 min, 2.2 h, 2.25 h, 2.5 h, 3 h, 3.5 h, 4 h, 5 h, 6 h, 8 h, 12 h, 16 h, 24 h, 36 h, 48 h, 72 h ]
  • Area under the plasma concentration-time curve from time 0 to time of the last quantifiable concentration of PCI-32765 [ Time Frame: Predose, and postdose at 30 min, 1 h, 1.5 h, 2 h, 2 h 2 min, 2 h 5 min, 2.2 h, 2.25 h, 2.5 h, 3 h, 3.5 h, 4 h, 5 h, 6 h, 8 h, 12 h, 16 h, 24 h, 36 h, 48 h, 72 h ]
  • Area under the plasma concentration-time curve from time 0 to infinite time of PCI-32765 [ Time Frame: Predose, and postdose at 30 min, 1 h, 1.5 h, 2 h, 2 h 2 min, 2 h 5 min, 2.2 h, 2.25 h, 2.5 h, 3 h, 3.5 h, 4 h, 5 h, 6 h, 8 h, 12 h, 16 h, 24 h, 36 h, 48 h, 72 h ]
  • Absolute bioavailability of PCI-32765 [ Time Frame: Predose, and postdose at 30 min, 1 h, 1.5 h, 2 h, 2 h 2 min, 2 h 5 min, 2.2 h, 2.25 h, 2.5 h, 3 h, 3.5 h, 4 h, 5 h, 6 h, 8 h, 12 h, 16 h, 24 h, 36 h, 48 h, 72 h ]

Secondary Outcome Measures:
  • Maximum observed plasma concentration of PCI-32765 [ Time Frame: Predose, and postdose at 30 min, 1 h, 1.5 h, 2 h, 2 h 2 min, 2 h 5 min, 2.2 h, 2.25 h, 2.5 h, 3 h, 3.5 h, 4 h, 5 h, 6 h, 8 h, 12 h, 16 h, 24 h, 36 h, 48 h, 72 h ]
  • Time to reach the maximum plasma concentration of PCI-32765 [ Time Frame: Predose, and postdose at 30 min, 1 h, 1.5 h, 2 h, 2 h 2 min, 2 h 5 min, 2.2 h, 2.25 h, 2.5 h, 3 h, 3.5 h, 4 h, 5 h, 6 h, 8 h, 12 h, 16 h, 24 h, 36 h, 48 h, 72 h ]
  • Elimination half-life of PCI-32765 [ Time Frame: Predose, and postdose at 30 min, 1 h, 1.5 h, 2 h, 2 h 2 min, 2 h 5 min, 2.2 h, 2.25 h, 2.5 h, 3 h, 3.5 h, 4 h, 5 h, 6 h, 8 h, 12 h, 16 h, 24 h, 36 h, 48 h, 72 h ]
  • Number of participants affected by an adverse event [ Time Frame: Up to 30 days after the last dose of study medication ]

Enrollment: 8
Study Start Date: June 2013
Study Completion Date: August 2013
Primary Completion Date: August 2013 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: PCI-32765
During Period 1, all patients will receive PCI-32765 560 mg administered by mouth (Treatment A). In Periods 2 and 3, patients will receive PCI-32765 560 mg administered by mouth without grapefruit juice (Treatment B) and PCI-32765 140 mg administered by mouth with grapefruit juice (Treatment C) according to a randomization schedule. An intravenous dose of 13C6 PCI-32765 will be administered 2 hours after each oral dose for reference purposes.
Drug: PCI-32765 (Treatment A)
560 mg capsules administered by mouth on Day 1, Period 1
Drug: PCI-32765 (Treatment B)
560 mg capsules administered by mouth (without grapefruit juice) on Day 1 during Period 2 or 3 according to randomization schedule
Drug: PCI-32765 (Treatment C)
140 mg capsule administered by mouth (with grapefruit juice) on Day 1 during Period 2 or 3 according to randomization schedule
Drug: 13C6 PCI-32765 (reference)
100 mcg administered intravenously 2 h after study drug

Detailed Description:
This is an open-label (identity of assigned study drug will be known), sequential and 2-way crossover design, pharmacokinetic (study of what the body does to a drug) study to assess the absolute bioavailability of oral (by mouth) PCI-32765 and the effect of grapefruit juice on the absorption of PCI-32765 in approximately 8 healthy adult participants. The duration of the study is approximately 45 days (screening, treatment, and follow-up). All patients will receive PCI-32765 560 mg (Treatment A) administered by mouth in the first period and Treatment B (560 mg administered by mouth without grapefruit juice) and Treatment C (140 mg administered by mouth with grapefruit juice) according to a randomization schedule in Periods 2 and 3. Participants will fast overnight for at least 10 hours prior to study drug dosing. Participants will stay in the study center for pharmacokinetic sampling. Serial pharmacokinetic samples will be collected before dosing and over 72 hours after dosing and safety will be monitored throughout the study.
  Eligibility

Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 55 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Women must be postmenopausal or surgically sterile
  • Men must agree to use an adequate contraception method during the study and for 3 months after receiving the last dose of study drug, and to not donate sperm during the study and for 3 months after receiving the last dose of study drug
  • Body mass index between 18 and 30 kg/m2 and body weight not less than 50 kg
  • Blood pressure (after lying down for 5 minutes) between 90 and 140 mmHg systolic and no higher than 90 mmHg diastolic

Exclusion Criteria:

  • History of or current clinically significant medical illness including (but not limited to) cardiac arrhythmias or other cardiac disease, hematologic disease, coagulation disorders (including any abnormal bleeding or blood dyscrasias), lipid abnormalities, significant pulmonary disease, including bronchospastic respiratory disease, diabetes mellitus, renal or hepatic insufficiency, thyroid disease, neurologic or psychiatric disease, infection, history of immune disorders (eg, lupus, rheumatoid arthritis, psoriatic arthritis), or any other illness that the investigator considers should exclude the participant or that could interfere with the interpretation of the study results
  • Clinically significant abnormal values for hematology, coagulation, PFA 100, clinical chemistry, or urinalysis at screening
  • Clinically significant abnormal physical examination, vital signs, or 12 lead electrocardiogram at screening
  • Use of aspirin, NSAIDs, thienopyridines, vitamin E supplements, fish oil, or flax seed within 1 week before PFA-100 assay test at screening
  • Use of any prescription or nonprescription medication (including vitamins and herbal supplements), except for paracetamol, hormonal replacement therapy and topical anesthetics (intravenous administration), within 14 days before the first dose of the study drug is scheduled
  • Use of herbal supplements within 30 days of the first dose administration
  • History of drug or alcohol abuse according to the Diagnostic and Statistical Manual of Mental Disorders (4th edition) (DSM-IV) criteria within 2 years before screening or positive test result(s) for alcohol and/or drugs of abuse at screening and Day -1 of each treatment period
  • History of clinically significant allergies, especially known hypersensitivity or intolerance to sulfonamide or beta-lactam antibiotics
  • Known allergy to the study drug or any of the excipients of the formulation
  • Donated blood or blood products or had substantial loss of blood (more than 500 mL) within 3 months before the first administration of study drug or intention to donate blood or blood products during the study
  • Received an experimental drug or used an experimental medical device within 1 month or within a period less than 10 times the drug's half life, whichever is longer, before the first dose of the study drug is scheduled
  • Unable to swallow solid, oral dosage forms whole with the aid of water
  • If a woman, pregnant, breast-feeding or planning to become pregnant during the study
  • Positive test for human immunodeficiency virus 1 and 2 antibodies, hepatitis B surface antigen, or hepatitis C antibodies
  • History of smoking or use of nicotine-containing substances within the previous 2 months or positive cotinine test
  • Preplanned surgery or procedures that would interfere with the conduct of the study
  Contacts and Locations
Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT01866033


Locations
Belgium
Merksem, Belgium
Sponsors and Collaborators
Janssen Research & Development, LLC
Pharmacyclics LLC.
Investigators
Study Director: Janssen Research & Development, LLC Clinical Trial Janssen Research & Development, LLC
  More Information

Publications automatically indexed to this study by ClinicalTrials.gov Identifier (NCT Number):
Responsible Party: Janssen Research & Development, LLC
ClinicalTrials.gov Identifier: NCT01866033     History of Changes
Other Study ID Numbers: CR101359
PCI-32765CLL1011 ( Other Identifier: Janssen Research & Development, LLC )
2013-000963-96 ( EudraCT Number )
First Submitted: May 28, 2013
First Posted: May 31, 2013
Last Update Posted: March 18, 2014
Last Verified: March 2014

Keywords provided by Janssen Research & Development, LLC:
Healthy volunteer
PCI-32765
PCI 45227
13C6 PCI-32765
Pharmacokinetic
Bioavailability