Study of an Investigational Drug, ASP3026, in Patients With Advanced Malignancies (Solid Tumors and B-Cell Lymphoma)

This study will be conducted using a traditional 3 + 3 dose escalation study design.
Enrollment of at least 3 subjects is planned for each dosing cohort until the Maximum
Tolerated Dose (MTD) is determined. Up to three additional subjects per cohort may be
enrolled if each additional subject is known to be positive for Anaplastic Lymphoma Kinase
(ALK) or Proto-Oncogene Tyrosine-Protein Kinase ROS (ROS) abnormalities. The decision to
expand a cohort or dose escalate will be based on the occurrence of dose limiting toxicities
(DLTs) in Cycle 1 that are considered by the Investigator to be related (possibly or
probably) to ASP3026. Intra-subject dose escalation will be allowed at the discretion of the
investigators. The Safety Data Review Committee may elect to enroll additional subjects in a
cohort to further evaluate the dose level. Once the MTD is determined, approximately 20
additional subjects with Anaplastic Lymphoma Kinase (ALK) abnormalities will be enrolled at
the Recommended Phase 2 Dose. Each cycle will include 28 days of continuous dosing with
ASP3026. Treatment with ASP3026 may continue until one of the discontinuation criteria is
met.

Inclusion Criteria:

- Eastern Cooperative Oncology Group (ECOG) performance status ≤ 2

- Histologically or cytologically confirmed diagnosis of a relapsed/refractory solid
tumor or B-cell lymphoma and meets at least 1 of the following criteria:

- Disease progression despite standard therapies

- No standard therapies are available or such therapies are not anticipated to
result in a durable response

- Standard therapies are considered unsuitable or have been refused

- Able to take oral medications

- Life expectancy > 12 weeks

- For the expansion cohort of the study, all subjects must be confirmed to be positive
for ALK gene abnormalities

- Subjects with stable brain metastasis will be allowed

Exclusion Criteria:

- Active central nervous system (CNS) metastases or leptomeningeal involvement as
assessed through medical history review and physical examination (dose escalation
subjects only)

- Known history of a positive test for hepatitis B surface antigen (HBsAg) or hepatitis
C antibody (anti-HCV)

- Known hereditary or acquired immunodeficiency syndrome or human immunodeficiency
virus (HIV) infection

- Cardiac arrhythmias > Grade 1 using National Cancer Institute Common Terminology
Criteria for Adverse Events (NCI CTCAE) v. 4.03

- Class 3 or 4 New York Heart Association congestive heart failure, acute coronary
syndrome, myocardial infarction or cerebrovascular accident within 6 months prior to
Cycle 1, Day 1

- Inadequate bone marrow, renal, and/or hepatic function

- Confirmed active peptic ulcer disease or history of gastrointestinal bleeding within
the past 3 months

- Known history of long QT syndrome