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.
Allocation: Non-Randomized, Endpoint Classification: Safety Study, Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Treatment
Dose Limiting Toxicity
Days 8, 15, 22, 28 and every 14 days thereafter to Final Visit
United States: Food and Drug Administration
|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|