Phase Ia/Ib Study of RS-0139 in Patients with a Recurrent, Locally Advanced or Metastatic Solid Tumors

Inclusion Criteria:

• Patients who have consented to participation in the trial.

• Patients of both sexes aged between 18 and 75 years.

• Patients with relapsed or refractory solid tumors who have failed available standardtherapy or are not candidates for standard therapy.

• Patients who are willing to provide fresh or archival biopsy material before theirparticipation to identify the integrin expression levels (for Phase Ib only).

• Patients who completed the previous treatments 21 days before the first dose of thestudy drug.

• Patients who have at least three months of life expectancy.

• Patients with ECOG performance score 0 to 1.

• Patients with adequate organ function defined as:

• 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 with active and/or uncontrolled central nervous system (CNS) metastasis.

• Patients who have interstitial lung disease or interstitial pneumonia.

• Patients who have serious cardiac dysfunction.

• Patients who have insufficient target organ function.

• Patients with positive tests for HAV, HBV, HCV or HIV.

• Patients who experienced grade 3 or higher toxicity related to the previousdocetaxel treatment.

• Female patients who are pregnant or breastfeeding.

• Male patients with pregnant female partners.

• Patients enrolled in another clinical trial at the same time or recently completedan investigational drug study and received the last dose of an investigational drugwithin 30 days or five half-lives (whichever is longer).

• Patients who have serious medical conditions such as uncontrolled infection oruntreated wounds.

• Patients who have bone marrow transplantation history.

• Patients who have hypersensitivity to docetaxel, components of RS-0139 and/or othertaxanes.

• Patients taking inhibitors or inducers of CYP3A4, including grapefruit juice and OTCmedications such as St. John's Wort.

• Patients who, in the judgment of the PI, are likely to be non-compliant or unable tocooperate.

• Patients who cannot be contacted in case of emergency.

• Patients who are the PI or sub-investigator, research assistant, pharmacist, studycoordinator or other staff directly involved in conducting the study.