Overview

This study designed as a multicenter, open label, two-step study to determine the optimum dose, pharmacokinetics, and the safety of RS-0139 in patients with a recurrent, locally advanced or metastatic non-small cell lung cancer (NSCLC). The research is planned as a two-step study (Phase Ia and phase Ib) and accelerated titration design (ATD) is used.

Eligibility

Inclusion Criteria:

• Patients who have consented for the participation to the trial.
• Patients of both sexes aged between 18-75 years.
• Patients who have biopsy material prior to the participation in order to confirm the expression of integrin αvβ6 (for Phase Ib only).
• Patients with stage IIIB or IV NSCLC and measurable disease by Response Evaluation Criteria in Solid Tumors and availability of at least one measurable tumor focus under RECIST v.1.1 criteria.
• Patients with NSCLC who progressed after standard therapy options consisting of chemotherapy and/or immunotherapy.
• Patients who completed the previous treatments 21 days before the first dose of the study drug.
• Patients who have at least three months of life expectancy.
• Patients with ECOG performance score 0-1
• Patients with the following laboratory results:
  • Hemoglobin ≥10 mg/dl
  • Neutrophil ≥1,500/µL
  • Platelet ≥100,000/µL
  • Creatinine ≤1.5xULN or creatinine clearance ≥60mL/sec/1.73m2
  • Total bilirubin ≤ 1.5xULN
  • AST/ALT ≤2.5xULN; for patients who have confirmed liver metastasis: AST/ALT ≤5xULN.
  • Prothrombin time ≤1.5xULN (in case of no anticoagulant treatment).
  • Normal levels of serum magnesium and potassium concentrations

Exclusion Criteria:

• Patients who have active and/or uncontrolled central nervous system (CNS) metastasis.
• Patients who have pulmonary carcinosarcoma.
• Patients who have presence of small cell lung cancer components.
• Patients who have interstitial lung disease or interstitial pneumonia.
• Patients who have cavitary lung lesions.
• Patients who have serious cardiac dysfunction.
• Patients who have insufficient target organ function.
• Patients who experienced Grade 3 or higher toxicity related to the previous docetaxel treatment.
• Patients who are pregnant or breastfeeding.
• Patients who are enrolled in a clinical trial.
• Patients who have serious medical conditions such as uncontrolled infection or untreated wound.
• Patients who have bone marrow transplantation history.
• Patients who have hypersensitivity to docetaxel and/or similar medicines.
• Patients who, in the judgment of the Investigator, are likely to be non-compliant or unable to cooperate.
• Patients who cannot be contacted in case of emergency.
• Patients who are the investigator or sub-investigator, research assistant, pharmacist, study coordinator or other staff directly involved in conducting the study.