Open-Label, Proof-of-Concept and Dose Finding Phase 1b/2 Study of VERU-100 in Men With Advanced Prostate Cancer

• Be over 18 years of age

• Be able to communicate effectively with the study personnel

• Have histologically confirmed prostate cancer

• Have prostate cancer staged T3-4NxMx or TxN1Mx or TxNxM1 according to the TNM classification or the patient should have rising PSA after failed local therapy and be candidate for androgen deprivation therapy

• Have a QTc interval \<440 ms

• Subjects are judged by the attending physician and/or Principal Investigator to be a candidate for androgen deprivation therapy (continuous therapy)

• ECOG performance status of 0 to 2

• Baseline morning serum testosterone levels \>150 ng/dL at Screening Visit

• Have a life expectancy of ≥18 months

• Subjects must agree to use acceptable methods of contraception

∙ If their female partners are pregnant or lactating, acceptable methods of contraception from the time of the first administration of study medication until 6months following administration of the last dose of study medication must be used. Acceptable methods are: Condom used with spermicidal foam/gel/film/cream/suppository. If the subject has undergone surgical sterilization (vasectomy with documentation of azoospermia),a condom with spermicidal foam/gel/film/cream/suppository should be used.

‣ If the male subject's partner could become pregnant, use acceptable methods of contraception from the time of the first administration of study medication until 6 months following administration of the last dose of study medication. Acceptable methods of contraception are as follows: Condom with spermicidal foam/gel/cream/suppository \[i.e.,barrier method of contraception\], surgical sterilization (vasectomy with documentation of azoospermia) and a barrier method {condom used with spermicidal foam/gel/film/cream/suppository}, the female partner uses oral contraceptives (combination estrogen/progesterone pills), injectable progesterone or subdermal implants and a barrier method (condom used with spermicidal foam/gel/film/cream/suppository).

‣ If the female partner has undergone documented tubal ligation (female sterilization), a barrier method (condom used with spermicidal foam/gel/film/cream/suppository) should also be used.

‣ If the female partner has undergone documented placement of an intrauterine device (IUD) or intrauterine system (IUS),a barrier method (condom with spermicidal foam/gel/film/cream/suppository) should also be used.

• Laboratory values within the following ranges: hemoglobin ≥10 gm/dL, total bilirubin

‣ 1.5x upper limit of normal (ULN), AST ≤2.5x ULN, ALT ≤2.5x ULN,

⁃ 1.5 mg/dL, absolute neutrophil count ≥1500 cell/uL and platelets ≥100,000 cells/uL.

• Creatinine clearance ≥60 mL/min based on Cockcroft-Gault equation.

• Subject is willing to comply with the requirements of the protocol through the end of the study