Efficacy, Safety, and Pharmacokinetics of FP-014, 22.5 mg in Patients With Advanced Prostate Cancer

1. Males aged ≥ 18 years old at Screening.
2. Histologically confirmed carcinoma of the prostate at the time of Screening.
3. Metastatic or biochemically recurrent prostate cancer disease at Screening.
4. Patient agrees to use male contraceptive methods during the study.
5. In the Investigator's opinion, the patient understands the nature of the study and any hazards of participation, communicates satisfactorily with the Investigator, and is able to participate in and comply with the requirements of the entire protocol.
6. Patients judged by the attending physician and/or Principal Investigator to be a candidate for androgen ablation therapy.
7. Patients who are able to tolerate ablation therapy but are considered unable to tolerate androgen receptor pathway inhibitors.
8. ECOG Performance Status score ≤ 2 and life expectancy of at least 18 months at Screening.
9. Baseline morning serum testosterone level > 150 ng/dL at Screening.

10. Laboratory values at Screening:

    • Absolute neutrophil count ≥ 1,500 cells/μL;
    • Platelets ≥ 100,000 cells/μL;
    • Hemoglobin ≥ 10 gm/dL;
    • Total bilirubin ≤ 1.5 × upper limit of normal (ULN);
    • AST ≤ 2.5 × ULN;
    • ALT ≤ 2.5 × ULN;
    • Creatinine Clearance ≥ 30 mL/min or estimated Glomerular Filtration Rate (eGFR) > 30 mL/min/1.73°m2 or evidence of acute kidney injury;
    • Lipid profile within the acceptable range according to the Investigator's opinion;
    • Serum glucose within the acceptable range according to the Investigator's opinion;
    • HbA1c within the acceptable range according to the Investigator's opinion;
    • Clinical chemistries (K, Na, Mg, Ca, and P) within the acceptable range according to the Investigator's opinion;

    • Normal urinalysis results:

      • red blood cells (RBCs) ≤ 3 RBCs/hpf;
      • white blood cells (WBCs) ≤ 5 WBCs/hpf;
      • nitrate: negative;
      • glucose: \<0.1 g/dL in patients without diabetes mellitus Type II and \< 1.0 g/dL in patients with diabetes mellitus Type II.

Exclusion Criteria:

1. Receipt of chemotherapy, immunotherapy, cryotherapy, radiotherapy, or anti- androgen therapy within 8 weeks prior to Screening, for treatment of carcinoma of the prostate.
2. Receipt of any luteinizing hormone-releasing hormone (LH-RH) suppressive therapy within 6 months of the Screening Visit.
3. Receipt of any vaccination (including influenza) within 2 weeks of the Screening Visit.
4. History of blood donation within 2 months of the Screening Visit.
5. History of anaphylaxis to any LH-RH analogues.
6. Contraindication to triptorelin or an LH-RH agonist as indicated on the package labeling.
7. Previous exposure to triptorelin mesylate.
8. Major surgery, including any prostatic surgery (excluding prostatic biopsy), within 4 weeks of the Screening Visit.
9. History of bilateral orchiectomy, adrenalectomy, or hypophysectomy.
10. History of clinical and radiographic evidence of central nervous system dysfunction.
11. Spinal cord metastases and patients at risk for spinal cord compression.
12. Clinical evidence of uncontrolled active urinary tract obstruction and patients at risk for urinary obstruction.
13. Clinically significant abnormal ECG at Screening and/or history of clinically significant ECG.
14. Cardiovascular disease that is clinically significant as judged by the Investigator.
15. History of Uncontrolled diabetes, HbA1C >9.5%, urine glycosuria >1.0 g/dl, or presence of diabetic ketoacidosis.
16. History of liver dysfunction, including patients with moderate (Child-Pugh B) or severe (Child-Pugh C) impairment or disordered coagulation.
17. End-stage renal diseases on peritoneal dialysis or hemodialysis.
18. History or presence of hypogonadism; or receipt of exogenous testosterone supplementation within 6 months of Screening Visit.
19. Use of systemic corticosteroids at a dose > 10 mg/day at Screening.
20. Use of 5-alpha reductase inhibitor within the last 6 months of Screening Visit.
21. Use of any over-the-counter (OTC) medication within 4 weeks of the Screening Visit, except for those listed as permitted concomitant treatment.
22. History of drug and/or alcohol abuse within 6 months of Screening Visit.
23. Use of any investigational agent within 4 weeks of the Screening Visit.
24. Use of any therapeutics with strong inhibitors and strong inducers of CYP3A4 or CYP2C8 [e.g., rifampicin, ketoconazole, phenytoin, ritonavir, macrolide antibiotics (e.g. telithromycin)] at the time of Screening.