Global, phase 3, open-label, single arm studies to evaluate the efficacy, safety, and pharmacokinetics of FP-014, 11.25 mg (triptorelin mesylate injection, 11.25 mg) and FP-014, 22.5 mg (triptorelin mesylate injection, 22.5 mg) in patients with advan

TPS284 Background: When given continuously, long-acting LH-RH agonist triptorelin is known to inhibit pituitary gonadotropin secretion and suppress testicular and ovarian steroidogenesis. Serum testosterone concentrations in males have been reduced to levels associated with castration (< 50 ng/dL in serum). This effect is generally observed within two to four weeks after the start of treatment and is maintained as long as treatment continues. Induction and maintenance of castrate levels of serum testosterone concentrations in prostate cancer patients is a standard palliative treatment and slows cancer cell growth. FP-014 was formulated in N-methyl-2-pyrrolidone (NMP) and poly (D, L-lactide-co-glycolide) (PLGA) to control and sustain the release of bioactive triptorelin after subcutaneous administration. Two dosages of FP-014 are under investigation: 11.25 mg for three-month release, and 22.5 mg for six-month release. Methods: The FP-014 11.25 mg three-month formulation study and FP-014 22.5 mg six-month formulation study are designed for six months and 12 months, respectively, to evaluate the safety, efficacy, and pharmacokinetics of subcutaneously administered FP-014 (triptorelin mesylate) in subjects with advanced prostate cancer who are candidates for androgen ablation therapy. Subjects will receive up to 2 doses of long-acting FP-014 every three months with the 11.25 mg formulation or every six months with the 22.5 mg formulation. Results: Primary endpoints: 1. The percentage of patients with a serum testosterone concentration suppressed to castrate levels (< 50 ng/dL) by Week 4 following the first SC injection of FP-. 2. The percentage of patients with serum testosterone concentration suppressed to castrate levels (< 50 ng/dL) from Week 4 through Week 24 (11.25 mg formulation) or Week 48 (22.5 mg formulation). Secondary endpoints: 1. Mean acute-on-chronic changes in serum testosterone and LH levels prior to the second injection through 48-72 hours after the second injection of FP-014. 2. Mean change in serum LH levels. 3. Mean change in serum PSA levels. 4. The percentage of patients with: PSA relapse (defined as an increase in serum PSA of > 50% PSA nadir) by End of Study after achieving serum PSA level ≤ 4 ng/mL post administration of FP-014; within normal limit serum PSA level (< 4 ng/mL) by End of Study; the percentage of patients with enhanced serum testosterone concentration suppression to < 20 ng/dL at Week 4 and at End of Study; and urinary signs and symptoms as assessed by International Prostate Symptom Score (I-PSS). Conclusion: Two Phase 3 studies are designed to evaluate the safety, efficacy, and pharmacokinetics of long-acting injectable FP-014 (triptorelin mesylate), aiming to demonstrate an alternative therapeutic option for patients with prostate cancer. Clinical trial information: TBD.