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

Inclusion Criteria:

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 andany hazards of participation, communicates satisfactorily with the Investigator, andis 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 acandidate for androgen ablation therapy.

7. Patients who are able to tolerate ablation therapy but are considered unable totolerate androgen receptor pathway inhibitors.

8. ECOG Performance Status score ≤ 2 and life expectancy of at least 18 months atScreening.

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'sopinion;

• Serum glucose within the acceptable range according to the Investigator'sopinion;

• HbA1c within the acceptable range according to the Investigator's opinion;

• Clinical chemistries (K, Na, Mg, Ca, and P) within the acceptable rangeaccording 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 < 1.0g/dL in patients with diabetes mellitus Type II.

Exclusion Criteria:

1. Receipt of chemotherapy, immunotherapy, cryotherapy, radiotherapy, or anti- androgentherapy within 8 weeks prior to Screening, for treatment of carcinoma of theprostate.

2. Receipt of any luteinizing hormone-releasing hormone (LH-RH) suppressive therapywithin 6 months of the Screening Visit.

3. Receipt of any vaccination (including influenza) within 2 weeks of the ScreeningVisit.

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 packagelabeling.

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 atrisk for urinary obstruction.

13. Clinically significant abnormal ECG at Screening and/or history of clinicallysignificant 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, orpresence of diabetic ketoacidosis.

16. History of liver dysfunction, including patients with moderate (Child-Pugh B) orsevere (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 testosteronesupplementation 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 orCYP2C8 [e.g., rifampicin, ketoconazole, phenytoin, ritonavir, macrolide antibiotics (e.g. telithromycin)] at the time of Screening.