A Study of CBP-1018 in Patients With Advanced Solid Tumors

Inclusion Criteria:

• Provision of informed consent (ICF) prior to any study-specific procedures.

• Men or women ≥ 18 years old when signed ICF.

• Eastern Cooperative Oncology Group (ECOG) performance status 0-1.

• Life expectancy of ≥ 3 months, in the opinion of the Investigator.

• Pathologically documented, advanced solid tumor including metastatic castrationresistant prostate cancer (mCRPC), advanced renal cell cancer (RCC), advanced lungsquamous cell cancer (LSCC), etc.

• Subjects must have received prior standard therapy appropriate for their tumor typeand stage of disease, or in the opinion of the Investigator, would be unlikely totolerate or derive clinically meaningful benefit from appropriate standard of caretherapy.

• At least one non-irradiated measurable lesion per RECIST 1.1 or bone lesion perPCWG3 (only for mCRPC), optional for low dose level (≤ 0.08 mg/kg) of Part A.

• Available archived or fresh tumor tissue samples, optional for low dose level (≤ 0.08 mg/kg) of Part A.

• Adequate bone marrow and organ function, defined as:

• Absolute neutrophil count (ANC) ≥ 1.5 × 109/L, not requiring growth factor supportfor at least 28 days prior to the first dose of CBP-1018.

• Hemoglobin (Hb) ≥ 100 g/L, not requiring transfusion support for at least 14 days orgrowth factor support for at least 28 days prior to the first dose of CBP-1018.

• Platelet count ≥ 100 × 109/L, not requiring transfusion support for at least 7 daysprior to the first dose of CBP-1018.

• Total bilirubin (TBIL) ≤ 1.5 × ULN, alkaline phosphatase (ALP) ≤ 1.5 × ULN, alanineaminotransferase (ALT) and aspartate aminotransferase (AST) ≤ 3.0× ULN if nodemonstrable liver metastases.

• TBIL≤ 1.5 × ULN, ALT and AST ≤ 5.0 × ULN in the presence of liver metastases.

• TBIL < 2.0 × ULN for subjects with documented Gilbert's syndrome or < 3.0 × ULN forsubjects for whom the indirect bilirubin level suggests an extrahepatic source ofelevation.

• Creatinine ≤ 1.0 × ULN, or creatinine clearance ≥ 50 mL/min as calculated usingCockcroft-Gault formula.

• International Normalized Ratio (INR) ≤ 1.5 × ULN (within the therapeutic range forsubjects receiving anticoagulation therapeutic) and activated partial thromboplastintime (APTT) ≤ 1.5 × ULN.

• LVEF ≥ 50% by either echocardiography (ECHO) or multiple-gated acquisition (MUGA).

• Female subjects of childbearing/reproductive potential must have a negative urine orserum pregnancy test within 72 hours prior to receiving the first dose of CBP-1018.If the urine test is positive or cannot be confirmed as negative, a serum pregnancytest will be required.

• Male subjects of fathering potential and subjects of childbearing/reproductivepotential must agree to use highly effective methods of contraception (see Appendix

4. throughout the study and for at least 30 days after the last dose of CBP-1018.

Exclusion Criteria:

• Known prior or suspected hypersensitivity to study drugs or any component in theirformulations.

• Concurrent malignancy within 5 years prior to the first dose of CBP-1018, other thanadequately treated cervical carcinoma-in-situ, localized squamous cell cancer of theskin, basal cell carcinoma, prostate cancer not requiring treatment, ductalcarcinoma in situ of the breast, or < T1 urothelial carcinoma.

• Active central nervous system (CNS) metastases. Previously diagnosed CNS metastasesare eligible if have been treated and recovered from the acute effects of radiationtherapy or surgery prior to the first dose of CBP-1018, have discontinuedcorticosteroid treatment for CNS metastases for at least 4 weeks and areneurologically stable.

• Major surgery, systemic anticancer therapy (chemotherapy, targeted therapy,immunotherapy, endocrine therapy, biotherapy) or participation in other therapeuticstudies within 4 weeks prior to the first dose of CBP-1018.

• Radiotherapy administrated within 21 days prior to the first dose of CBP-1018, orlocalized palliative radiotherapy administered within 7 days prior to the first doseof CBP-1018.

• Any toxicities attributed to prior anti-cancer therapy, other than alopecia andfatigue, that have not resolved to Grade 1 (NCI CTCAE 5.0) or baseline prior to thefirst dose of CBP-1018.

• Poorly controlled concurrent diseases as diabetes, hypertension (systolic bloodpressure >160 mmHg or diastolic blood pressure > 100 mmHg), etc.

• History of any of the following cardiovascular conditions within 12 months ofenrollment: cardiac angioplasty or stenting, myocardial infarction, unstable angina,coronary artery by-pass graft surgery, symptomatic peripheral vascular disease,class III or IV congestive heart failure, as defined by the New York HeartAssociation.

• History of clinically significant lung diseases as interstitial pneumonia,pneumonitis, pulmonary fibrosis, and severe radiation pneumonitis, or suspected tohave these diseases by imaging at screening period.

• Active bleeding disorder or other history of grade ≥ 3 hemorrhage within 4 weeksprior to the first dose of CBP-1018.

• Requirement of anticoagulant therapy with oral vitamin K antagonists. Low-doseanticoagulants for maintenance of patency of central venous access device orprevention of deep venous thrombosis is allowed. Therapeutic use of low molecularweight heparin is allowed.

• History of deep vein thrombosis or pulmonary embolism within 6 months prior to thefirst dose of CBP-1018.

• Active infection requiring intravenous (IV) antibiotics within 1 weeks prior to thefirst dose of CBP-1018.

• Known history of testing positive for human immunodeficiency virus (HIV) or knownacquired immunodeficiency syndrome (AIDS).

• Positive Hepatitis B Surface Antigen (HepBsAg) (indicative of chronic Hepatitis B),positive Hepatitis total core antibody with negative HepBsAg (suggestive of occulthepatitis B) or detectable Hepatitis C virus Ribonucleic acid (RNA) by PCR (Hepatitis C Antibody test for screening, followed by PCR for Hepatitis C virus RNAif HepCAb is positive).

• Live-virus vaccination within 30 days prior to the first dose of CBP-1018. Seasonalinfluenza vaccines that do not contain live virus are allowed.

• Current or anticipated need for treatment with strong cytochrome P450 3A4 (CYP3A4)inhibitors or inducers.

• History or current evidence of any other condition, therapy, or laboratoryabnormality that might confound the results of the trial, interfere with thesubject's participation for the full duration of the trial, or is not in the bestinterest of the subject to participate, in the opinion of the Investigator.