A Randomized, Double-Blind, Placebo-Controlled, Multicenter Efficacy and Safety Study of Toremifene Citrate for the Prevention of Prostate Cancer in Men With High Grade Prostatic Intraepithelial Neoplasia (PIN)

Inclusion Criteria:

- Give voluntary signed informed consent in accordance with institutional policies

- Be male, aged ≥ 30 years

- Have a diagnosis of high grade PIN from any previous prostate biopsy. The diagnosis
of high grade PIN must be confirmed by the central pathologist

- Have had a prostate biopsy in the last 6 months with a minimum of 10 cores that shows
no evidence of cancer as confirmed by the central pathologist; OR, have had 2
prostate biopsies (each with a minimum of 6 cores) in the 12 months prior to
screening with at least one of the biopsies occurring within 6 months prior to the
screening visit. Both biopsies should have no evidence of cancer as confirmed by the
central pathologist

- Have a serum PSA of ≤ 10 ng/mL

- Agree to provide tablet containers for tablet counts

- Agree to use an effective method of contraception, if the partner is of child-bearing
age, while on study

- Have adequate bone marrow, liver and renal function:

- White Blood Cell (WBC) Count ≥ 3,000/mm3;

- Platelet Count ≥ 100,000/mm3;

- Bilirubin ≤ 1.5 mg/dL;

- AST and ALT < 2x upper limit of normal;

- Serum Creatinine ≤ 2.0 mg%

Exclusion Criteria:

- Previous exposure to toremifene citrate

- Have evidence of prostate cancer (local, regional and/or distal metastasis)

- Have any history of other malignancies (exceptions include non-melanoma skin cancer
or other cancer that has no evidence of tumor reoccurrence, 5 years after definitive
treatment). Superficial bladder cancer is acceptable as long as it has been greater
than 1 year since any treatment with no evidence of recurrence.

- Have active systemic viral, bacterial, or fungal infections requiring treatment

- Have, in the judgment of the investigator, a clinically significant concurrent
illness or psychological, familial, sociological, geographical or other concomitant
condition that would not permit adequate follow-up and compliance with the study
protocol

- Concurrently being treated with other investigational agents or have participated in
an investigational study within 30 days prior to screening

- Currently taking dutasteride. Subject is eligible if he stops dutasteride for a
total washout of 90 days prior to the Screening Visit and agrees not to use
dutasteride for the duration of the study.

- Have previously taken finasteride for greater than two years

- Currently taking finasteride. Subject is eligible if he stops finasteride for a total
washout of 30 days prior to the Screening Visit and agrees not to use finasteride for
the duration of the study.

- Currently taking testosterone or testosterone-like supplements, such as
dehydroepiandrosterone (DHEA). Subject is eligible if he stops these agents for a
total washout of 30 days prior to the Screening Visit and agrees not to use these
agents for the duration of the study.

- Have a history of taking PC-SPES within the past two years.

- Currently taking herbal medicine or dietary supplements for prostate health, such as
Saw Palmetto (also known as Serenoa repens).

Subject is eligible if he stops these agents for a total washout of 30 days prior to
taking the first dose of study drug and agrees not to use these agents for the duration of
the study.

Lycopene, vitamin E and selenium are not prohibited and no washout is required. However,
vitamin E intake should be limited to less than 400 i.u. per day.

- Have a history of thromboembolic event or disease including deep vein thrombosis,
pulmonary embolus, or thrombotic stroke

- History of chronic hepatitis or cirrhosis