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Open-label PK Study to Evaluate Lansoprazole and Neratinib in Healthy Subjects

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT02334501
Lead Sponsor
Puma Biotechnology, Inc.
Brief Summary

This is an open label, 2-period, fixed-sequence study in 15 healthy adult subjects under fed conditions. To evaluate the effect of multiple doses of lansoprazole on the absorption and pharmacokinetics (PK) of a single dose of neratinib in healthy subjects.

Detailed Description

This is an open label, 2-period, fixed-sequence study in 15 healthy adult subjects under fed conditions. On Day 1 of Period 1 (Treatment A), a single oral dose of neratinib will be administered followed by PK sampling for 72 hours. In Period 2 (Treatment B), multiple oral doses of lansoprazole will be administered once daily for 7 consecutive days with a single oral dose of neratinib administered on Day 5. PK sampling for neratinib will be taken for 72 hours following neratinib dosing on Day 5. The washout period will be at least 14 days between each neratinib dose.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
15
Inclusion Criteria

Healthy, adult, men or women, 18 to 55 years of age, inclusive, at screening. Body Mass Index ≥ 18.5 and ≤ 32.0 kg/m2 at screening. Non to moderate smokers (up to 10 cigarettes a day for at least 3 months prior to screening).

Medically healthy with no clinically significant medical history, physical examination, laboratory profiles, vital signs or 12-lead electrocardiograms (ECGs), as deemed by the principal investigator (PI).

Women of childbearing potential: either be sexually inactive (abstinent) for 14 days prior to the first dose and for at least 28 days following the last dose or be using one of the protocol-specific birth control methods.

Exclusion Criteria

Acute disease state (eg, nausea, vomiting, fever, or diarrhea) within 7 days prior to the first dose of study drug.

History or presence of alcoholism or drug abuse within the past 2 years prior to screening.

History or presence of hypersensitivity or idiosyncratic reaction to the study drugs or related compounds (eg, proton-pump inhibitors [PPIs]).

Women who are pregnant or lactating. Positive results at screening for human immunodeficiency virus, hepatitis B surface antigen, or hepatitis C virus.

Unable to refrain from or anticipates the use of:

  • Any drug, including prescription and nonprescription medications, herbal remedies, or vitamin supplements (including proton-pump inhibitors) beginning 14 days prior to the first dose of study drug and throughout the study. Acetaminophen (up to 2 g per 24 hour period) and/or loperamide (up to 6 mg per 24 hours) may be permitted during the study at the direction of the PI.
  • Any drugs known to be significant inducers of cytochrome p450 enzymes and/or P glycoprotein, including St. John's Wort, for 28 days prior to the first dose of study drug and throughout the study. Appropriate sources will be consulted by the PI or designee to confirm lack of PK/pharmacodynamics interaction with study drug.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Treatment A (Period 1) and Treatment B (Period 2)LansoprazoleTreatment A (240mg Neratinib x1) Treatment B (30mg Lansoprazole X 7 days + 240mg Neratinib x1)
Treatment A (Period 1) and Treatment B (Period 2)NeratinibTreatment A (240mg Neratinib x1) Treatment B (30mg Lansoprazole X 7 days + 240mg Neratinib x1)
Primary Outcome Measures
NameTimeMethod
AUC(0-t) of neratinib with and without lansoprazole0, 0.5, 1, 2, 2.75, 3.5, 4.25, 5, 5.75, 6.5, 7.25, 8, 10, 12, 24, 32, 48, 60, and 72 hours post-dose

The area under the plasma concentration-time curve, from time 0 to the last measurable nonzero concentration, as calculated by the linear trapezoidal method.

AUC(0-inf) of neratinib with and without lansoprazole0, 0.5, 1, 2, 2.75, 3.5, 4.25, 5, 5.75, 6.5, 7.25, 8, 10, 12, 24, 32, 48, 60, and 72 hours post-dose

The area under the plasma concentration-time curve from time 0 extrapolated to infinity. AUC(0-inf) is calculated as the sum of AUC(0-t) plus the ratio of the last measurable plasma concentration to the elimination rate constant.

Cmax of neratinib with and without lansoprazole0, 0.5, 1, 2, 2.75, 3.5, 4.25, 5, 5.75, 6.5, 7.25, 8, 10, 12, 24, 32, 48, 60, and 72 hours post-dose

Maximum observed concentration.

Secondary Outcome Measures
NameTimeMethod
Number of participants with adverse eventsover 4 week study period

Safety endpoints will include all AEs, physical examinations, vital signs, 12-lead electrocardiograms (ECGs), and clinical laboratory tests (hematology, serum chemistry, and urinalysis).

Trial Locations

Locations (1)

Celerion

🇺🇸

Tempe, Arizona, United States

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