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A Phase I, Open-Label, Dose Escalating, Multiple Dose Study to Determine the Safety, Tolerability, Maximum Tolerated Dose and Pharmacokinetics of Oral TAK-165 Administered Once Daily to Subjects With Tumors Known to Express HER2.

Phase 1
18 Years
Not Enrolling
Breast Neoplasm, Pancreatic Neoplasm, Lung Neoplasm, Ovarian Neoplasm, Renal Neoplasm

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Trial Information

A Phase I, Open-Label, Dose Escalating, Multiple Dose Study to Determine the Safety, Tolerability, Maximum Tolerated Dose and Pharmacokinetics of Oral TAK-165 Administered Once Daily to Subjects With Tumors Known to Express HER2.

The human epidermal growth factor receptor 2 (HER2) is a member of the Type 1 family of
growth factor tyrosine kinases. HER2 forms hetero- and homo-dimers with other members of
this family of tyrosine kinases. As a result of dimerization at the cell surface,
intracellular signal transduction is initiated, resulting in cell proliferation.

HER2 expression has been observed in a variety of human tumors including breast cancer,
non-small cell lung cancer, prostate cancer, pancreatic cancer, renal cell cancer, and
ovarian cancer. HER2 overexpression is associated with clinically more aggressive breast
cancer, and is an independent predictor of poor prognosis in patients with breast cancer.

TAK-165 is an active and selective inhibitor of tyrosine kinase activity of HER2 being
developed for patients with lower levels of HER2 expression. This study will seek to
determine the safety, tolerability, maximum tolerated dose and pharmacokinetics of TAK-165
administered to subjects with tumors known to express HER2.

The total duration of the study will be at minimum 8 weeks, or 56 Days. Subjects without
progressive disease after 8 weeks may continue to receive study drug, provided that they do
not meet criteria for withdrawal.

Inclusion Criteria:

- Have advanced or metastatic cancer which is refractory to standard therapy or
subjects for whom there is no known effective therapy.

- Have a histologically or cytologically proven diagnosis of a solid tumor known to
express HER2.

- Have a predicted life expectancy of greater than or equal to 12 weeks.

- Have a Karnofsky Performance Status of greater than or equal to 60%

- Have recovered from toxicities of prior chemotherapy, surgery, or radiotherapy.

Exclusion Criteria:

- Be pregnant or lactating. Women of childbearing potential must have a negative serum
pregnancy test result within 7 days of enrollment into the study. Male and female
subjects of childbearing potential (including women who have been amenorrheic for
less than 1 year) must use appropriate birth control during the entire duration of
the study, or the subject must be surgically sterile.

- Have symptomatic brain metastasis

- Have received any other anti-cancer treatment or investigational drug/treatment
within 28 days prior to study Day 1.

- Have a history of another malignancy within the last 5 years.

- Have inadequate organ function.

- Have heart failure defined by an ejection fraction of less than or equal to 50% as
measured by MUGA.

- Have Class II, III or IV symptoms of heart failure as defined by the New York Heart
Association, or uncontrolled arrhythmias, or recent history of myocardial infarction
or angina pectoris.

- Have a medical condition that may interfere with intake and/or absorption of the
study drug (e.g., gastrectomy or resection of major portion of small intestine).

- Have any other serious disease or condition present at screening or at study Day 1
that might affect life expectancy or make it difficult to successfully manage and
follow the subject according to the protocol.

Type of Study:


Study Design:

Allocation: Non-Randomized, Endpoint Classification: Safety Study, Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Treatment

Outcome Measure:

Dose Limiting Toxicity

Outcome Time Frame:

Days 8, 15, 22, 28 and every 14 days thereafter to Final Visit

Safety Issue:


Principal Investigator

Medical Director

Investigator Role:

Study Director

Investigator Affiliation:



United States: Food and Drug Administration

Study ID:




Start Date:

June 2002

Completion Date:

September 2003

Related Keywords:

  • Breast Neoplasm
  • Pancreatic Neoplasm
  • Lung Neoplasm
  • Ovarian Neoplasm
  • Renal Neoplasm
  • Gene, HER2
  • Clinical Trial, Phase I
  • Breast neoplasm
  • Pancreatic neoplasm
  • Ovarian neoplasm
  • Colorectal neoplasm
  • Renal neoplasm
  • Prostate neoplasm
  • Cancer
  • Breast Neoplasms
  • Neoplasms
  • Kidney Neoplasms
  • Lung Neoplasms
  • Ovarian Neoplasms
  • Pancreatic Neoplasms



Arizona Cancer Center Tucson, Arizona  85724
Brooke Army Medical Center/Drug Development Unit San Antonio, Texas  78234
The Institute for Drug Development San Antonio, Texas  78229
South Texas VA, Audie Murphy Division San Antonio, Texas  78284