Development of the drug program has been discontinued

To evaluate the effect of Osanetant on testosterone levels in men with prostate cancer within 28 days of therapy.

Primary:

To evaluate the effect of Osanetant on testosterone levels in men with prostate cancer within 28 days of therapy.

Secondary:

• To evaluate the effect Osanetant on pituitary hormones (LH/FSH) and estrogen within 28 days of therapy.
• To evaluate the effect of Osanetant on PSA levels after 28 days (approximately 4 weeks) of therapy.

Inclusion Criteria:

• Ability of participant OR Legally Authorized Representative (LAR) to understand this study, and participant or LAR willingness to sign a written informed consent

• Males ≥ 18 years

• Histologic diagnosis of adenocarcinoma of the prostate (PCa)

• Planned radical prostatectomy within the study period

• Testosterone >150ng/ml

• Adequate organ function, defined as follows: Result Date

  • Leukocytes >1.5K/UL
  • Absolute Neutrophil Count >1.5K/UL
  • NOTE: Patients with established diagnosis of benign neutropenia are eligible to participate with ANC between 1000-1500 if in the opinion of treating physician the trial treatment does not pose excessive risk of infection to the patient.

• Platelets >100K/UL

• Hemoglobin ≥ 9 g/dL

• Serum creatinine ≤ 1.5 x upper limit of normal (ULN) or calculated creatinine clearance ≥ 50 mL/min using the Cockcroft-Gault equation

• Total bilirubin ≤ 1.5 x ULN OR direct bilirubin ≤ 1 x ULN

• Aspartate aminotransferase and alanine aminotransferase ≤ 2.5 x ULN unless liver metastases are present, in which case they must be ≤ 5 x ULN

• Men with partners of child-bearing potential must agree to practice sexual abstinence or to use the forms of contraception listed in Child-Bearing Potential/Pregnancy section for the duration of study participation. Men of child-bearing potential must not father a child or donate sperm while receiving investigational treatment. Following treatment (standard of care prostatectomy) there is no further child-bearing potential.

Exclusion Criteria:

• Current or recent (within 6 months) use of testosterone/estrogen modulating agents (leuprolide, degarelix, bicalutamide, enzalutamide, apalutamide, darolutamide, abiraterone, systemic ketoconazole, tamoxifen, etc)

• Current use of CYP3A4 inhibitors

• Subjects using the following medications within 2 weeks prior to first dosing (or within 5 times the half-life of that medication, whichever is longer) will be excluded from the study:

  • Inhibitors of CYP3A4 (including but not limited to macrolide antibiotics, HIV protease inhibitor, azole antifungal drugs, cyclosporine, calcium channel inhibitor, cimetidine)
  • Inducers of CYP3A4 (including but not limited to rifampicin, carbamazepine, efavirenz, bosentan, modafinil, St. John's Wort), Medications with narrow therapeutic index that are metabolized CYP3A4 and/or CYP2D6 are not allowed from screening until up to 5 half-lives after last dose of Osanetant is administered.

• Cognitive impairment (defined as the presence of diagnosed dementia)

• Impaired renal function: Cr >1.8

• Medical history of osteoporosis

• Current systemic corticosteroid, long-term opioid, spironolactone, or eplerenone use

• Has a known allergic reaction to any excipient contained in the study drug formulation

• Active Grade 3 (per the NCI CTCAE, Version 5.0) or higher viral, bacterial, or fungal infection within 2 weeks prior to the first dose of study treatment.

• Active COVID-19 infection

• Any history of underlying liver disorder, including hepatitis (see below)

• Any evidence of acute or chronic hepatitis B or C on screening testing

• Elevation of any or all liver enzymes (ALT, AST, total bilirubin) above the upper limit of normal (ULN) at baseline testing prior to enrollment

• A family history of hepatitis or currently living with a person who has been given a diagnosis of hepatitis

• A history of or currently working as a sex worker

• A history of or currently using intravenous (IV) drugs

• A self-reported history of alcoholic dependency or abuse

• A history of or current diagnosis of cardiovascular disease including heart failure, coronary artery disease, uncontrolled hypertension, uncontrolled diabetes; arrhythmias (or history of), or clinically relevant ECG abnormalities at baseline