A Study to Determine the Absorption, Metabolism, and Routes of Excretion of (14C) Radiolabeled Ibrutinib in Healthy Male Participants

NCT01674322 | Completed Phase 1

• 3 other identifiers: CR100885PCI-32765CLL10042012-002087-27
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to investigate the absorption, the metabolic pathways and the excretion of ibrutinib in healthy male adult participants after administration of a single oral dose of 50 mg to 140 mg (5 mg/mL solution) of unlabeled ibrutinib admixed with 14C ibrutinib.

Conditions

Healthy Participants

Keywords

Healthy participants; Ibrutinib; PCI-32765; B-cell malignancies; CYP3A4

Outcome Measures

Primary Outcomes (4)

• Maximum concentration (Cmax) of ibrutinib

  Pharmacokinetic parameter Cmax of ibrutinib will be determined.

  Day 1 (Predose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 hours), Day 2 (24 hours), Day 3 (48 hours), Day 4 (72 hours)

• Time to reach the maximum concentration (tmax) of ibrutinib

  Pharmacokinetic parameter tmax of ibrutinib will be determined.

  Predose, Day 1 (0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 hours), Day 2 (24 hours), Day 3 (48 hours), Day 4 (72 hours)

• Area under the concentration-time curve (AUC) of ibrutinib

  Pharmacokinetic parameter AUC of ibrutinib will be determined.

  Predose, Day 1 (0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 hours), Day 2 (24 hours), Day 3 (48 hours), Day 4 (72 hours)

• Amount excreted into the urine (Ae) of ibrutinib

  Pharmacokinetic parameter Ae of ibrutinib will be determined by multiplying the urinary volume with the urinary concentration.

  Day -1, Day 1 over intervals 0-2, 2-4, 4-8, 8-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168 hours, Days 9-15

Secondary Outcomes (1)

• Number of patients with adverse events

  Up to 73 days

Study Arms (1)

Ibrutinib

EXPERIMENTAL

All participants will receive a single oral solution dose of 50 mg to 140 mg -ibrutinib containing 1480 kBq (40 µCi) of 14C-labeled ibrutinib, with a total radiation burden of approximately 0.916 mSv.

Drug: Ibrutinib

Interventions

Ibrutinib DRUG

Type=exact number, unit=mg, number=50-140, form=solution, route=oral. Participants will receive a single oral solution dose of 50 mg to 140 mg -ibrutinib containing 1480 kBq (40 µCi) of 14C-labeled ibrutinib, with a total radiation burden of approximately 0.916 mSv.

Also known as: PCI-32765

Ibrutinib

Eligibility Criteria

• Age: 30 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Participant must sign an informed consent document indicating they understand the purpose of and procedures required for the study, including DNA analysis, and are willing to participate in the study
• Must agree to use an adequate contraception method as deemed appropriate by the investigator (eg, vasectomy, double-barrier, partner using effective contraception) during the study and for 3 months after receiving the study drug
• Must agree to not donate sperm during the study and for 3 months after receiving the study drug
• Blood pressure (after the participant is supine for 5 minutes) between 90 and 140 mmHg systolic, inclusive, and no higher than 90 mmHg diastolic
• Non-smoker (not smoked for 6 months prior to screening)

You may not qualify if:

• History of or current clinically significant medical illness including cardiac arrhythmias or other cardiac disease, hematologic disease, coagulation disorders, lipid abnormalities, significant pulmonary disease, including bronchospastic respiratory disease, diabetes mellitus, renal or hepatic insufficiency, thyroid disease, neurologic or psychiatric disease
• Clinically significant abnormal values for hematology, coagulation and platelet function, clinical chemistry or urinalysis at screening as deemed appropriate by the investigator
• Clinically significant abnormal physical examination, vital signs or 12 lead electrocardiogram (ECG) at screening as deemed appropriate by the investigator
• History of clinically significant allergies, especially known hypersensitivity or intolerance to β-lactam antibiotics or sulfonamides
• Known allergy to heparin or history of heparin induced thrombocytopenia

Sponsors & Collaborators

• Janssen Research & Development, LLC: lead

Study Sites (1)

Unknown Facility

Merksem, Belgium

Location

Related Publications (1)

• Scheers E, Leclercq L, de Jong J, Bode N, Bockx M, Laenen A, Cuyckens F, Skee D, Murphy J, Sukbuntherng J, Mannens G. Absorption, metabolism, and excretion of oral (1)(4)C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos. 2015 Feb;43(2):289-97. doi: 10.1124/dmd.114.060061. Epub 2014 Dec 8.

  PMID: 25488930 DERIVED

MeSH Terms

Interventions

ibrutinib

Study Officials

• Janssen Research & Development, LLC Clinical Trial

  Janssen Research & Development, LLC

  STUDY DIRECTOR

Study Design

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

Study Record Dates

• First Submitted: August 9, 2012
• First Posted: August 28, 2012
• Study Start: August 1, 2012
• Primary Completion: September 1, 2012
• Study Completion: September 1, 2012
• Last Updated: November 5, 2014

Record last verified: 2014-11

Locations

BE (1)