Safety, Preliminary Efficacy and Pharmacokinetics of ASN001 in Metastatic Castrate Resistant Prostate Cancer

Parts A and B will include a screening period (up to 28 days) and a 12-week treatment period.
A subject with no serious adverse drug reactions and who is expected to benefit from
continued treatment in the opinion of the investigator will have the opportunity to
participate in the long-term extension (Part C). If the subject is not a candidate for or
chooses not to participate in the long-term extension (Part C), a post-treatment period of 4
weeks will commence that concludes with an end-of-study visit.

Subjects participating in only Part A or Part B will have approximately 9 study site visits
over 18 weeks. Part C will include monthly visits to the study site for 9 months. Thereafter,
visits will occur every 3 months. A subject with stable disease or response may continue
ASN001 treatment with the approval of the investigator; treatment can continue until a
subject experiences an intolerable adverse event (AE) or disease progression, withdraws
consent or until termination of the study by the sponsor. At the end of treatment, a
post-treatment period of 4 weeks will commence that concludes with an end-of-study visit.

Part B of the study will not be completed as enrollment was halted after Part A (Phase 1)

Inclusion Criteria

- Histologically confirmed adenocarcinoma of the prostate.

- Ongoing androgen deprivation therapy with a luteinizing hormone-releasing hormone
(LHRH) agonist or antagonist, or bilateral orchiectomy and serum testosterone level <
50 ng/dL (< 0.5 ng/mL, < 1.7 nmol/L) at screening

- Metastatic disease documented by computed tomography (CT)/magnetic resonance imaging
(MRI) or bone scan.

- Progressive disease despite ongoing androgen deprivation therapy.

- Adequate liver, kidney, and bone marrow function

- Life expectancy of at least 3 months

- Eastern Cooperative Oncology Group (ECOG) performance status of 0 to 2 at screening

- Patients with prior cytotoxic chemotherapy are eligible to participate if they have
been progression free for at least 12 months since the initiation of cytotoxic
chemotherapy

Exclusion Criteria:

- Patients with rapidly progressive disease who are candidates for other approved
therapies such as docetaxel, abiraterone, and enzalutamide.

- Prior therapy with abiraterone, orteronel, ketoconazole, or any other Cytochrome P450
(CYP) 17 lyase inhibitor; enzalutamide or other experimental androgen receptor
antagonist; or experimental immunotherapy agent.

- History of impaired adrenal gland function

- Any investigational treatments for any condition within 4 weeks prior to the start of
study treatment.

- Therapy with herbal products known to effect PSA, or estrogen within 30 days prior to
the start of study medication

- Known gastrointestinal disease or condition that affects the absorption of ASN001, or
difficulty swallowing large capsules.

- Use of systemic glucocorticoid (eg, prednisone, dexamethasone) within 14 days prior to
the start of study medication

- Major surgery within 30 days of study medication

- Known brain metastasis

- Previous history of another cancer within 5 years, except completely removed basal or
squamous cell skin cancer.

- Serious concurrent medical conditions including: serious heart disease, heart
conduction abnormalities, persistent infection, uncontrolled psychiatric illness,
liver cirrhosis, chronic liver disease, active or symptomatic viral hepatitis, any
other condition that may place the subject at an increased risk or confound the
results of the study.