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Completed

NCT Number: NCT01866033

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

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.

Completed

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Key information

Conditions

Healthy Volunteer

Age range

18 year–55 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Merksem, Belgium

About this study

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.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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

Treatment and study plan

PCI-32765 (Treatment A)

Drug

560 mg capsules administered by mouth on Day 1, Period 1

PCI-32765 (Treatment B)

Drug

560 mg capsules administered by mouth (without grapefruit juice) on Day 1 during Period 2 or 3 according to randomization schedule

PCI-32765 (Treatment C)

Drug

140 mg capsule administered by mouth (with grapefruit juice) on Day 1 during Period 2 or 3 according to randomization schedule

13C6 PCI-32765 (reference)

Drug

100 mcg administered intravenously 2 h after study drug

Primary outcomes

  1. 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

  2. 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

  3. 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

  4. 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 outcomes

  1. 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

  2. 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

  3. 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

  4. Number of participants affected by an adverse event

    Time frame: Up to 30 days after the last dose of study medication

Sponsors and collaborators

Lead sponsor

Janssen Research & Development, LLC

Industry

Collaborators

  • Pharmacyclics LLC.

Registry information

Official study 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

Important dates

Study start
2013
Primary completion
2013
Study completion
2013
First posted
May 31, 2013
Registry last updated
Mar 18, 2014

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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