Phase 1, Dose-escalation Trial of OPB-51602 in Patients With Advanced Solid Tumors

Inclusion Criteria:

* Patients with pathologically confirmed, locally advanced or metastatic solid tumors who are unresponsive to standard therapy or for whom standard therapy is intolerable or unsuitable
* Age: ≥21 years (at time of informed consent)
* ECOG performance status: ≤2 (Appendix 1)
* Life expectancy of longer than 3 months
* Adequate vital organ function as follows:

  1. Bone marrow function Neutrophils: ≥1,500/μL, platelets: ≥75,000/μL, hemoglobin: ≥9.0 g/dL
  2. Hepatic function Aspartate transaminase (AST) and alanine transaminase(ALT): ≤2.5 ×institutional upper limit of normal(ULN) or ≤5.0 × institutional ULN if there is liver metastasis, serum total bilirubin: \<2.5 × institutional ULN
  3. Renal function Serum creatinine: \<1.5 × institutional ULN
* Capable of swallowing OPB-51602 tablets
* Ability to understand and willingness to sign written informed consent form (ICF) for participation in the trial
* No chemotherapy, radiotherapy, surgery, immunotherapy, or other therapy within 4 weeks prior to start of investigational medicinal product (IMP) administration and recovered from any prior toxicity
* If a subject has received more than 5 regimens of previous chemotherapy, the investigator must discuss with the sponsor regarding subject suitability prior to enrollment.

Exclusion Criteria:

* Uncontrolled central nervous system (CNS) metastasis
* Uncontrolled concurrent illness, including active infection, angina pectoris, cardiac arrhythmia, or heart failure (NYHA class III or IV, Appendix 2 New York Heart Association (NYHA) functional classification)
* Concurrent malignancy of a different type
* Immunocompromised subjects, including those who are known to be infected with human immunodeficiency virus (HIV)
* Psychiatric illness that would limit compliance with trial requirements
* Pregnant or breast-feeding women
* Women of childbearing potential (WOCBP) or male subjects whose partners are WOCBP who cannot or will not use effective contraceptive measures
* Administration of another investigational agent within 6 weeks prior to start of IMP administration
* Use of any of the prohibited medications and other substances listed in Appendix 3 CYP3A4 Inhibitors and Inducers within either 1 week prior to start of IMP administration or a period of at least 5 times the respective elimination halflife, whichever is longer
* Known severe gastrointestinal disorder, including malabsorption (at screening)
* Patients with CTCAE Grade 1 or higher pneumonitis (interstitial pneumonia) or pulmonary fibrosis\* \* If interstitial lung abnormalities, (e.g. ground-glass or linear opacity) are suspected on chest CT scan (high-resolution CT), regardless of whether or not there are any accompanying symptoms it must be confirmed, such as through consultation with a respiratory or radiology expert if necessary, that the patient dose not fall under this exclusion criterion before the patient can be enrolled in the trial.