Know Cancer

forgot password

An Open-label Positron Emission Tomography Study to Investigate and Quantify Brain and Tumour Penetration of [11C]Lapatinib in Subjects With HER2-overexpressing Breast Cancer.

Phase 1
18 Years
Open (Enrolling)

Thank you

Trial Information

An Open-label Positron Emission Tomography Study to Investigate and Quantify Brain and Tumour Penetration of [11C]Lapatinib in Subjects With HER2-overexpressing Breast Cancer.

Lapatinib is an anti-cancer drug taken by mouth which inhibits the HER2 protein,
overexpressed in some breast tumours. It is not known whether lapatinib passes through the
blood-brain barrier, and, therefore, whether it can target secondary tumours in the brain.
This study will investigate whether lapatinib does indeed enter the brain.

Subjects with HER2-overexpressing breast cancer, with and without brain metastases, will
receive lapatinib tablets daily for 8 days. The subjects will also receive lapatinib with a
small amount of radioactivity attached on the first and last days of dosing to investigate
whether it is taken up by the brain, using positron emission tomography (PET) scans.

Inclusion Criteria:

- Female, aged >/= 18 years old

- Advanced or metastatic breast cancer with overexpression of HER2

- Be able to provide written informed consent and comply with protocol requirements

- If of child-bearing potential, using adequate and medically acceptable contraception

- Have an ECOG performance status of 0-2 and be in stable condition

- Able to lie still on the PET scanner for approx. 1.5-2 h

- Adequate hepatic and renal function

- Patent ulnar artery or collateral arterial blood vessels

- If have CNS metastases, disease must be stable

- Subjects with CNS metastases should have at least a single 1 cm diameter lesion as
shown on contrast MRI

Exclusion Criteria:

- Subjects with brain metastases who have undergone prior CNS surgery

- Significant brain abnormalities, neurological disorder, psychiatric disorder or
previous brain damage

- Diabetes type I

- History of HIV, hepatitis B or hepatitis C infection

- Current alcohol and/or drug abuse

- Positive pregnancy test or lactation

- Malabsorption syndrome or disease affecting gastrointestinal function that may affect
intestinal absorption

- Requirement for additional concurrent anti-cancer therapy

- History of uncontrolled or symptomatic angina

- Concurrent treatment with an investigational agent or anti-cytotoxic therapy or use
within 30 days or 5 half-lives

- Known hypersensitivity reaction of idiosyncrasy to drugs chemically related to
lapatinib or its excipients

- Concurrent treatment with CYP3A4 inducers and inhibitors

- Unwillingness to refrain from consuming red wine, Seville oranges, grapefruit,
pomelo, grapefruit hybrids and their juices from 7 days before Day 1 until collection
of the final pharmacokinetic sample

- Known history of claustrophobia

- Known contraindications or likely risk of toxicity to gadlinium-based MRI contrast

- Presence of cardiac pacemaker, other electronic device or ferromagnetic metal foreign

- Any abnormality found on the MRI scan which, in the opinion of the investigator, may
influence the outcome of the PET scans or affect the safety of the volunteer

- Acute or active hepatic or biliary disease

- Any medical condition or circumstance making the volunteer unsuitable for
participation in the study.

Type of Study:


Study Design:

Endpoint Classification: Pharmacodynamics Study, Intervention Model: Single Group Assignment, Masking: Open Label

Outcome Measure:

Brain penetration of [11C]lapatinib

Outcome Time Frame:

8 days

Safety Issue:


Principal Investigator

GSK Clinical Trials

Investigator Role:

Study Director

Investigator Affiliation:



United Kingdom: Medicines and Healthcare Products Regulatory Agency

Study ID:




Start Date:

September 2011

Completion Date:

May 2013

Related Keywords:

  • Cancer
  • Brain penetration
  • positron emission tomography
  • Lapatinib
  • Breast Neoplasms