A Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Efficacy of TT125-802 in Subjects With Advanced Solid Tumors

A Phase 1, First-in-Human, Open-label Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Efficacy of TT125-802 in Subjects With Advanced Solid Tumors

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.

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.