A Multicenter, Phase 1/2, Open-Label, Dose-Escalation Study of JI-101, an Oral Angiogenesis Inhibitor, in Patients With Advanced Solid Tumors

Inclusion Criteria:

- Be 18 years of age or greater at the time of consent.

- Have solid tumors for which no approved therapy or standard of care is available or
have solid tumors and have failed standard-of-care therapy.

- Have life expectancy of greater than 3 months.

- Have Eastern Cooperative Oncology Group (ECOG) performance status 0 to 2.

- Have organ and marrow function as defined below:

- absolute neutrophil count ≥ 1.5 x 10^9 cells/L

- hemoglobin ≥ 9.0 g/dL

- platelets ≥ 75 x 10^9 cells/L

- total bilirubin ≤ 1.5 x upper limit of normal (ULN)

- AST(SGOT)/ALT(SGPT) ≤ 2.5 x ULN (≤ 5 x ULN for liver metastases)

- serum creatinine < 1.5 x ULN

- < 500 mg urinary protein/24 hours or dipstick < 2+

- No evidence of preexisting uncontrolled hypertension as documented by two baseline
blood pressure readings taken at least 1 hour apart (the baseline systolic blood
pressure readings must be <140 mm Hg, and the baseline diastolic blood pressure
readings must be <90 mm Hg. Patients whose hypertension is controlled by
antihypertensive therapies are eligible)

- Have no clinically significant disease that poses a risk to the patient and/or would
interfere with study evaluations or procedures.

- Have within normal range cardiac function as measured by twelve-lead
electrocardiogram at Screening.

- Be clinically euthyroid.

- If female, must be postmenopausal (at least 1 year from last menses), or surgically
sterile, or if a female patient of childbearing potential they must agree to use
acceptable methods of birth control, which include local double-barrier contraceptive
methods, such as cervical diaphragm plus spermicide, female condom plus spermicide,
or a non-hormonal intrauterine device (IUD) plus spermicide, or systemic
contraceptive methods, such as oral, injectable, transdermal or implantable hormonal
contraceptives (including hormone-containing IUDs) during the study period, and for
30 days after the last dose of study drug. Female patients of childbearing potential
must have a negative serum pregnancy test within the 3 days before the first study
drug administration. Male patients must be surgically sterile or also agree to use
acceptable methods of birth control with their female partners, and this may include
use of a male condom plus spermicide. If the subject is practicing abstinence at the
time of Screening, he/she must agree to use a double-barrier contraceptive method if
he/she becomes sexually active.

- Be able to understand and the willingness to sign a written informed consent
document.

Exclusion Criteria:

- Be pregnant or breastfeeding.

- Have a known history of human immunodeficiency virus (HIV) infection because the
effect of JI-101 on immunosuppression and drug interactions with anti-retroviral
medications is unknown.

- Have participated in an investigational drug/device/biologic study within 30 days (or
within 5 half-lives of the treatment, whichever is longer) before Visit 1 or who are
currently participating in another investigational drug/device/biologic study.
Participation in non-interventional or observational studies is allowed.

- Have a history of cardiac abnormalities including: abnormal and clinically relevant
ECGs; frequent palpitations or syncopal episodes; heart failure; hypokalemia; stroke;
family history of Long QT Syndrome; acute myocardial infarction or ventricular
tachyarrhythmia within the previous 12 months.

- Have used concomitant medications that prolong the QT/QTc interval within 14 days
prior to Day 1.

- Have a history of significant retinopathy or any progressive eye disease that could
lead to severe loss of visual acuity or visual field loss during the study period.

- Have had therapeutic reanticoagulation with heparin or heparin analogs (low molecular
weight heparins) or warfarin within the past 4 weeks. Low dose warfarin (1 to 2
mg/day) is allowed for prophylaxis treatment.

- Have had major surgery, radiotherapy, chemotherapy, or cytokine therapy within 4
weeks of treatment initiation. Patients must have recovered to baseline or grade 1
from any clinically significant adverse event experienced during those prior
therapies.

- Have gastrointestinal abnormalities including inability to take oral medications,
malabsorption syndromes or other clinically significant GI abnormalities that may
impair the absorption of JI-101 in the opinion of the Investigator.

- Have uncontrolled intercurrent illness including, but not limited to, ongoing or
active infection, unstable angina pectoris, or psychiatric illness/social situations
that would pose a risk to patient safety or that would limit compliance with study
requirements.

- Have any condition that, in the opinion of the Investigator, would interfere with a
patient's ability to perform the required activities of the study or would subject
the patient to undue risk.

- Patients with proteinuria (patients with >2+ protein on urine dipstick) at baseline
should undergo a 24-hour urine collection. Results must demonstrate <500 mg of
protein in 24 hours to allow participation in the study)

- Patients with any of the following contraindications to FDG-PET can participate in
the study if all of the inclusion criteria and none of the exclusion criteria are
met, but these patients are excluded from FDG PET assessments:

o Inability to remain lying down in PET scanner (for PET portion of the study).

- Absence of at least one metastatic lesion greater than or equal to 2 cm on pre-dose
CT (computed tomography) scan or other radiographic imaging as defined by response
evaluation criteria in solid tumors (RECIST) criteria.