a study evaluating the safety, tolerability, pharmacokinetics, and efficacy of tt125-802 in subjects with advanced solid tumors

Conditions: Advanced Solid Tumor; Adult Solid Tumor; Adult Disease; Cancer; NSCLC

Summary: the purpose of this study is to test the safety and therapeutic effect of tt125-802 (single agent) in subjects with advanced solid tumors.

the purpose of this phase 1, first-in-human, open-label study is to assess the safety, tolerability, pharmacokinetics, pharmacodynamics, and efficacy of tt125-802 as single agent in subjects with advanced solid tumors.

Eligibility criteria:
inclusion criteria: * males and nonpregnant and non-breastfeeding females, aged ≥ 18 years of age at the time of signing the informed consent. * subjects with advanced solid tumors resistant or refractory to standard treatment. * eastern cooperative oncology group (ecog) performance status 0 or 1. * measurable disease per recist 1.1 criteria. * adequate hematological function defined by absolute neutrophil count, ≥ 1.5 × 10\^9/l, platelet count ≥ 100 × 10\^9/l, and hemoglobin ≥ 9 g/dl, and without growth factor treatment or blood transfusion within 2 weeks before the study intervention start. * adequate hepatic function defined by total bilirubin level ≤ 1.5 × upper limit of normal (uln), aspartate aminotransferase (ast) level ≤ 3 × uln, and an alanine aminotransferase (alt) level ≤ 3 × uln. * adequate renal function defined by creatinine clearance \> 60 ml/min according to the cockcroft-gault equation or creatinine levels \<1.5 mg/dl. * adequate coagulation laboratory assessments, as follows: prothrombin time (pt) or partial thromboplastin time (ptt) \< 1.5 x upper limit of normal (uln), or international normalized ratio (inr) \< 1.5 or within target range if on prophylactic anticoagulation therapy. * life expectancy of \> 3 months, in the opinion of the investigator. * willing to adhere to contraception, egg and sperm donation, the fasting requirement, and other criteria as described in lifestyle restrictions * capable of giving signed informed consent. exclusion criteria: * clinically significant (i.e., active) uncontrolled intercurrent illness. * presence of brain metastases unless clinically stable. * history or presence of malignancies unless curatively treated with no evidence of disease ≥ 2 years. * subjects with known human immunodeficiency virus and/or active viral hepatitis (b and/or c), and subjects on viral hepatitis b therapy are excluded. however, subjects with hepatitis c treated with curative therapy are not considered actively infected. * subject received a live vaccine within 30 days prior to the first dose of the study treatment administration. * serious gastrointestinal bleeding within 3 months, refractory nausea and vomiting, uncontrolled diarrhea, known malabsorption, significant small bowel resection or gastric bypass surgery, use of feeding tubes, other chronic gastrointestinal disease, and/or other situation that may preclude adequate absorption of oral medications. * subjects that have received a strong cyp3a4 inhibitor within 7 days prior to the first dose of tt125-802 or a strong cyp3a4 inducer within 14 days prior to the first dose of tt125-802. * hypersensitivity to the active substance or to any of the excipients of tt125-802.

Keywords: tolremo drug resistance tt125-802 small molecule bromodomain inhibitor