This is the first study of this drug in human beings. Every patient will receive the drug, there is no placebo group. Patients with advanced tumors will be treated. Different groups of patients will receive different dosages to determine the safety and maximum tolerated dose (MTD) of BAY87-2243. The study will also assess how the drug is metabolized by the body, its biologic effects in the body, and changes in tumor size. BAY87-2243 will be given as a tablet which dissolves in the gut. Based on findings from this study it may be later given as a tablet which dissolves in the stomach. BAY87-2243 will be given per mouth, once a day, every day. Treatment will stop if the tumor continues to grow, if side effects occur which the patient can not tolerate or if the patients decides to exit treatment. The study will be conducted in 3 - 4 centers in 3 countries (Norway, United Kingdom and Germany). The study will have a part where doses are escalated in different groups of patients. Each dose level will be evaluated in a new group of 3 - 6 subjects. This will be followed by an extension part where patients are treated at the highest tolerable dose in groups of up to 25 patients. The extension part will be described in an amendment to the study protocol later. The number of subjects estimated for this study will depend on the number of groups enrolled. The starting dose will be 5 mg given orally as a tablet formulation.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
5
Oral administration once daily in a continuous schedule. Starting dose will be 5 mg and dose will be escalated dependent on any dose limiting toxicities.
Unnamed facility
Freiburg im Breisgau, Baden-Wurttemberg, Germany
Unnamed facility
Oslo, Norway
Unnamed facility
Sutton, Surrey, United Kingdom
Frequency of adverse events
Time frame: Up to 3 years or longer if indicated
Maximum tolerated dose, measured by adverse event profile
Time frame: Up to 3 years or longer if indicated
Plasma concentrations of BAY87-2243, measured by Cmax, tmax, AUC(0-tn), AUC and half-life
Time frame: Up to 3 years or longer if indicated
Biomarkers evaluation (analysis of carbonic anhydrase 9 and VEGF in plasma)
Time frame: Up to 3 years or longer if indicated
Tumor response evaluation based on RECIST 1.1 every 2 cycles
Time frame: Up to 3 years or longer if indicated
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