A Study Comparing BGB-3111 With Bendamustine Plus Rituximab in Patients With Previously Untreated CLL or SLL

This is a global phase 3, open label, randomized study of BGB-3111 versus bendamustine plus
rituximab (B+R) in subjects with previously untreated chronic lymphocytic leukemia or small
lymphocytic lymphoma (CLL/SLL), including subjects without del(17p) [Cohort 1] and subjects
with del(17p) [Cohort 2]. Subjects in Cohort 1 are randomized 1:1 to BGB-3111 (Arm A) or
bendamustine plus rituximab (Arm B). Randomization will be stratified by age, Binet stage,
immunoglobulin variable region heavy chain (IGHV) mutational status, and geographic region.
Subjects in Cohort 2 receive treatment with BGB-3111.

Inclusion Criteria: All subjects

1. Unsuitable for chemoimmunotherapy with FCR in the opinion of the investigator.

2. Confirmed diagnosis of CD20-positive CLL or SLL.

3. Binet Stage C disease, or Binet Stage B or A disease requiring treatment.

4. ECOG performance status of 0, 1 or 2.

5. Life expectancy ≥ 6 months.

6. Adequate bone marrow function.

7. Adequate renal and hepatic function.

8. Females of childbearing potential and non-sterile males must agree to use highly
effective methods of birth control throughout the course of study

9. Male patients are eligible if vasectomized or if they agree to use of barrier
contraception with other methods described above throughout the course of study.

10. Written informed consent.

Exclusion Criteria: All subjects

1. Previous systemic treatment for CLL/SLL.

2. Known prolymphocytic leukemia or history of or suspected Richter's transformation.

3. Clinically significant cardiovascular disease.

4. Prior malignancy within the past 3 years, except for curatively treated basal or
squamous cell skin cancer, superficial bladder cancer, or carcinoma in situ of the
cervix of breast.

5. Major surgery or significant injury ≤ 4 weeks prior to start of study treatment.

6. History of severe bleeding disorder.

7. History of stroke or intracranial hemorrhage within 6 months before the first dose of
study drug.

8. Severe or debilitating pulmonary disease.

9. Inability to swallow capsules or disease affecting gastrointestinal function.

10. Known central nervous system involvement by leukemia or lymphoma.

11. Active infection requiring systemic treatment.

12. Known infection with human immunodeficiency virus (HIV) or active hepatitis B or C
infection.

13. Vaccination with live vaccine within 35 days prior to the first dose of study drug.

14. Known hypersensitivity to BGB-3111, bendamustine, or rituximab or any other
ingredients of the study drugs.

15. Requires ongoing treatment with strong CYP3A inhibitor or inducer.

16. Pregnant or nursing females.

17. Concurrent participation in another therapeutic clinical trial.