The purpose of this study is to determine whether OPB-51602 is safe and tolerable when given daily by mouth to subjects with advanced solid tumors.
This study is based on data that support a role for the signal transducer and activator of transcription (STAT) family of proteins in oncogenesis. One of the mechanisms of action of OPB-51602 includes inhibition of STAT3 phosphorylation. Therefore OPB-51602 is expected to be active as an anti-cancer drug. This first-in-human study will characterize the safety profile of OPB-51602, evaluate the pharmacokinetics of OPB-51602, identify a recommended phase II dose, and obtain preliminary efficacy data, in subjects with advanced cancers for whom there is no standard treatment available.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
45
A cycle will consist of 28 days of OPB-51602 be taken by study subjects daily by mouth for every day of each 28 day cycle.
Unnamed facility
Sarasota, Florida, United States
Unnamed facility
Boston, Massachusetts, United States
Unnamed facility
Nashville, Tennessee, United States
To determine the safety and tolerability of OPB-51602
AEs, vital signs, body weight, ECGs, clinical laboratory tests, and performance status will be assessed.
Time frame: Weekly for first cycle, then every 2 weeks (on average up to 8 weeks).
To determine the pharmacokinetics of OPB-51602 and to determine the MTD of OPB-51602
The following PK parameters (Cmax, tmax, AUC₀-t, AUCtau, CLss/F and t½,z) will be determined using a non-compartmental approach for OPB-51602 and selected metabolites after single (Cycle 1, Day 1) and multiple daily doses (Cycle 2, Day 1).
Time frame: 28 days
Pharmacodynamic profile:
Study drug effects on STAT-3 phosphorylation will be assessed in PBMCs of study subjects in the dose escalation and expansion stages.
Time frame: 28 days
Antitumor effects:
Treatment response and/or disease progression in subjects with measurable disease will be evaluated after every 2 cycles using Response Evaluation Criteria in Solid Tumors (RECIST₉).
Time frame: Every 2 cycles (on average 8 weeks).
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.