A Phase 1/1b Dose Escalation Study Evaluating BSI-201 as a Single Agent and in Combination With Irinotecan in Subjects With Advanced Solid Tumors

Inclusion Criteria:

- Pathologically documented, advanced solid tumor that is refractory to standard
therapy or for which no standard therapy is available.

- ECOG performance status of 0, 1, or 2

- Adequate hematological status

- Any prior toxicity from prior chemotherapeutic treatment recovered to grade 1 or
grade 0

- 18 years of age or older

- Competent to comprehend, sign, and date an Institutional Review Board (IRB) approved
informed consent form

- For phase 1b portion only: metastatic breast cancer

Exclusion Criteria:

- Hematologic malignancies

- Symptomatic or untreated brain metastases requiring concurrent treatment, inclusive
of but not limited to surgery, radiation, and corticosteroids

- Myocardial infarction within 6 months of study day 1, unstable angina, congestive
heart failure with NYHA > class II, uncontrolled hypertension

- Known positive test for HIV or hepatitis C virus, or chronic active hepatitis

- Major surgery within 1 month of study day 1

- History of second neoplasm, except for curatively treated non-melanoma skin cancer,
carcinoma in situ of the cervix and other primary cancer with no known active disease
present and no curative treatment administered for the last 3 years

- History of seizure disorder or currently on anti-seizure medication

- Systemic chemotherapy or radiation therapy within 28 days of study day 1

- Antibody therapy for treatment of underlying malignancy within 1 month of study day 1

- Evidence of liver disease shown by elevated enzymes

- Evidence of renal disease shown by serum creatinine > 1.5 x upper limit of normal

- Currently receiving platelet of GCF support for any medical condition

- Concurrent use of herbal medications taken with the intent to treat cancer

- Enrolled in or not yet completed at least 30 days since ending other investigational
device or drug study