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A Phase 1 Open-Label Study to Evaluate the Effect of CYP450 and P-gp Inhibition and Induction on the Pharmacokinetics of Pomalidomide (CC-4047) in Healthy Male Subjects

Phase 1
Completed
Conditions
Healthy
Pharmacology, Clinical
Interventions
Registration Number
NCT01707407
Lead Sponsor
Celgene
Brief Summary

1. To evaluate the pharmacokinetics (PK) of pomalidomide administered with the CYP3A4/P-gp inhibitor ketoconazole compared with pomalidomide alone in healthy male subjects.

2. To evaluate the PK of pomalidomide administered with the CYP3A4/P-gp inhibitor ketoconazole plus the CYP1A2 inhibitor fluvoxamine compared with pomalidomide alone in healthy male subjects.

3. To assess the PK of pomalidomide administered with the CYP1A2 inhibitor fluvoxamine and the CYP3A4/P-gp inhibitor ketoconazole compared with pomalidomide plus the CYP3A4/P-gp inhibitor ketoconazole in healthy male subjects.

Part 2

1) To evaluate the pharmacokinetics of pomalidomide administered with the CYP3A4 inducer carbamazepine compared with pomalidomide alone in healthy male volunteers.

Secondary Objectives

1) To evaluate the safety of pomalidomide in Part 1 and Part 2 when administered with ketoconazole, fluvoxamine and/or carbamazepine.

In addition: To evaluate the safety of pomalidomide in Part 1 and Part 2 when administered with ketoconazole, fluvoxamine and/or carbamazepine.

Detailed Description

This will be a single-center, open label non randomized, 2-part study with 3 periods in Part 1, and 2 periods in Part 2. Parts 1 and 2 will be conducted in parallel. The entire study will consist of a screening phase, two dosing parts, and a follow-up telephone call for safety. All Periods will be separated by a washout period of at least 3 days (no more than 5 days) from the last pomalidomide dose to the next drug dose.

Safety will be monitored throughout the study. Safety evaluations will include adverse event (AE) reporting, concomitant medications, PEs, vital sign measurements, 12-lead ECGs, and clinical laboratory safety tests.

Thirty-two healthy (16 per each Part), male adult subjects 18 to 55 years of age who meet all inclusion criteria and do not meet any of the exclusion criteria will be enrolled in the study. Subjects enrolled in Part 1 cannot participate in Part 2 and vice versa.

Study treatments (pomalidomide, ketoconazole, fluvoxamine and carbamazepine) should be administered with meals and subjects should be a served a standard meal (ie, breakfast or dinner) approximately 30 minutes prior to dosing. The meal should be consumed within 30 minutes from serving and dosing must occur 30 minutes (±5 minutes) after serving the meal. Subjects should be encouraged to consume the whole meal served prior to dosing. After each dosing, food and beverages (except water) will be withheld from all subjects until at least 4 hours post dose; thereafter, subjects will be served standard meals and snacks.

For determination of plasma concentrations of pomalidomide, ketoconazole, fluvoxamine and carbamazepine (and its active metabolite carbamazepine 10,11-epoxide) in each dosing regimen (Period), serial blood samples will be collected.

A safety follow-up will be conducted by telephone within 4 to 7 days from the last dose. In the event a subject discontinues from the study prematurely, an early termination visit will be performed within 4 days following the day of discontinuation.

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
32
Inclusion Criteria

Not provided

Exclusion Criteria
  • History of any clinically significant and relevant neurological, gastrointestinal, renal, hepatic, cardiovascular, psychological, pulmonary, metabolic, endocrine, hematological, allergic disease, drug allergies, known hypersensitivity to a member of the class of-IMIDs (immune-mediated inflammatory diseases), or other major disorders
  • Any significant medical condition, laboratory abnormality, or psychiatric illness that would prevent the subject from participating in the study.
  • Any condition including the presence of laboratory abnormalities, which places the subject at unacceptable risk if he were to participate in the study.
  • Any condition that confounds the ability to interpret data from the study.
  • Used any prescribed systemic or topical medication within 30 days of the first dose administration, unless Sponsor agreement is obtained.
  • Used any non-prescribed systemic or topical medication (including vitamin/mineral supplements, and herbal medicines) within 14 days of the first dose administration, unless Sponsor agreement is obtained.
  • Has any surgical or medical conditions possibly affecting drug absorption, distribution, metabolism and excretion (ADME), eg, bariatric procedure.
  • Donated blood or plasma within 8 weeks before the first dose administration to a blood bank or blood donation center.
  • History of drug abuse (as defined by the current version of the Diagnostic and Statistical Manual within 2 years before dosing, or positive drug screening test reflecting consumption of illicit drugs.
  • History of alcohol abuse (as defined by the current version of the DSM) within 2 years before dosing, or positive alcohol screen.
  • Known to have, or tests positive for, active or chronic hepatitis B, hepatitis C, or HIV antibodies.
  • Exposed to an investigational drug (new chemical entity) within 60 days preceding the first dose administration, or 5 half-lives of that investigational drug, if known (whichever is longer).
  • Received vaccination (excluding seasonal flu vaccination) within 90 days of the study drug administration.
  • Smokes more than 10 cigarettes, or consumes the equivalent in tobacco, per day.
  • Subjects who are part of the staff personnel or family members of the investigational study staff.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
PomalidomidePomalidomide-
Pomalidomide plus Ketoconazole plus FluvoxaminePomalidomide-
Pomalidomide plus KetoconazolePomalidomide-
Pomalidomide plus KetoconazoleKetoconazole-
Pomalidomide plus Ketoconazole plus FluvoxamineKetoconazole-
Pomalidomide plus Ketoconazole plus FluvoxamineFluvoxamine-
Pomalidomide plus CarbamazepineCarbamazepine-
Pomalidomide plus CarbamazepinePomalidomide-
Primary Outcome Measures
NameTimeMethod
PK-CmaxUp to 13 days

Cmax-Maximum observed concentration in plasma

PK-TmaxUp to 13 days

Tmax: Time to maximum concentration

PK-AUCUp to 13 days

AUC-Area under the plasma concentration-time curve

PK-Vz/FUp to 13 days

Vz/F: Apparent total volume of distribution

PK-(T1/2)Up to 13 days

T1/2-Terminal half-life

PK-CL/FUp to 13 days

CL/F-Apparent total plasma clearance

Secondary Outcome Measures
NameTimeMethod
Adverse EventsUp to 15 days

Number of participants with adverse events

Trial Locations

Locations (1)

Covance Research Unit, Inc

🇺🇸

Madison, Wisconsin, United States

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