A Phase I Study to Test Alternate Oral Formulations vs the Current Tablet Formulation of Lapatinib

Relative Bioavailability of Four Alternative Oral Formulations Versus the Current Tablet Formulation of Lapatinib

This study is designed to estimate the relative bioavailability of alternative lapatinib oral formulations compared to the current tablet formulation.

Study Overview

• Status: Withdrawn
• Conditions: Healthy Subjects
• Intervention / Treatment: Drug: lapatinib

• Study Type: Interventional
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • New York
    • Buffalo, New York, United States, 14202
      • GSK Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 60 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• The subject is healthy as defined per protocol.

• The subject is male or female.

  • A female is eligible to enter and participate in this study if she is of:
• Non-childbearing potential (i.e., physiologically incapable of becoming pregnant), including any female who:
• Has had a documented (medical report verification) hysterectomy or double oophorectomy or
• Is 6 weeks postsurgical bilateral oophorectomy with or without hysterectomy or

• Is post-menopausal (defined as females older than 45 years of age with 12 months of spontaneous amenorrhea or 6 months of spontaneous amenorrhea with serum FSH levels higher than 40 mIU/ml)

  • Childbearing potential, has a negative serum pregnancy test at Screening, and agrees to one of the following :
• Complete abstinence from sexual intercourse from two weeks prior to administration of the study drug and throughout the study, and through the follow-up visit which will occur within 10 to 14 days after completion of the last treatment.
• Vasectomized partner
• Intrauterine device (IUD) with a documented failure rate of less than 1% per year.
• Double-barrier contraception (condom with spermicidal jelly, foam suppository, or film; diaphragm with spermicide; or male condom and diaphragm).
• Hormonal contraceptive plus male condom.
• Age: 18 to 60 years inclusive.
• BMI within the range 19 to 31.0 kg/m2.
• Able to swallow and retain oral medication.
• The subject is willing to refrain from the use of illicit drugs and adhere to other protocol-stated restrictions while participating in the study.
• The subject is able to understand and comply with protocol requirements and instructions and is likely to complete the study as planned.
• A signed and dated written informed consent is obtained from the subject or the subject's legally acceptable representative prior to screening.

Exclusion Criteria:

• As a result of the medical interview, physical examination or screening investigations, the Principal Investigator considers the subject unfit for the study.
• The subject meets ECG-related exclusion criteria listed in the protocol or has serum magnesium or potassium below the normal range at screening.
• The subject has a history of drug or other allergy, which, in the opinion of the Principal Investigator, contraindicates participation.
• The subject has a known immediate or delayed hypersensitivity reaction or idiosyncrasy to drugs chemically related to the study drug, including but not limited to Tarceva (erlotinib) or Iressa (gefitinib).
• The subject has a history of sensitivity to heparin or heparin-induced thrombocytopenia (applicable if heparin is used during pharmacokinetic sampling).
• The subject participated in a study with a new molecular entity or any other trial during the previous 30 days.
• The subject donated blood in excess of 500 mL within 56 days prior to dosing or intends to donate in the month after completing the study.
• Use of prescription or non-prescription drugs (including vitamins and herbal supplements) within two weeks prior to dosing or during the study, however, acetaminophen up to two grams per day is acceptable.
• History of alcohol/drug abuse or dependence within 12 months of the study as per protocol.
• The subject is a smoker or has smoked in the last four months.
• The subject tested positive for hepatitis C antibody, hepatitis B surface antigen, or HIV antibody.
• The subject has a positive urine test for drugs of abuse or is positive for alcohol use at pre-study screening.
• Consumption of red wine, Seville oranges, grapefruit or grapefruit juice from 7 days prior to the first dose of study medication until collection of the final PK blood sample.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Plasma levels for lapatinib will be done at:	Day 1, Day 2, Day 3 for each Treatment Period

Secondary Outcome Measures

Outcome Measure	Time Frame
Medical History	at screening
Physical Exam	at screening & follow-up (f/u)
Continuous Adverse Event monitoring	throughout the study
Vital Signs, ECGs, & Lab tests	at screening, Day 1, and f/u
Response to questionnaire regarding taste and aesthetics of suspension formulations under evaluation

Collaborators and Investigators

• Sponsor: GlaxoSmithKline

Study record dates

Study Major Dates

• Study Start: April 1, 2008
• Primary Completion (Anticipated): May 1, 2008
• Study Completion (Anticipated): May 1, 2008

Study Registration Dates

• First Submitted: August 6, 2007
• First Submitted That Met QC Criteria: August 6, 2007
• First Posted (Estimate): August 8, 2007

Study Record Updates

• Last Update Posted (Estimate): February 16, 2015
• Last Update Submitted That Met QC Criteria: February 12, 2015
• Last Verified: February 1, 2015

More Information

Terms related to this study

• Keywords: lapatinib; Healthy Adult Volunteer
• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Antineoplastic Agents; Protein Kinase Inhibitors; Lapatinib
• Other Study ID Numbers: EGF101950