Dose-ranging Study of the Luteinizing Hormone-releasing Hormone Receptor Antagonist Cetrorelix Pamoate in the Treatment of Patients With Symptomatic Benign Prostatic Hyperplasia

Abstract

To compare the efficacy of 4 dosage regimens of cetrorelix pamoate, a sustained release formulation that allows for more convenient dosing, in patients with symptomatic benign prostatic hyperplasia (BPH). Repeated dosing with cetrorelix acetate was shown to be active in the treatment of BPH symptoms. Double-blind, randomized, multicenter study was undertaken among patients with International Prostate Symptom Score (IPSS) ≥ 13. After a single-blind placebo run-in phase of 4 weeks, treatment was administered at 2-week intervals as follows: 30 + 30 mg, 30 + 30 + 30 mg, 60 + 30, 60 + 60 mg cetrorelix pamoate, or matching placebo. Patients were followed-up for 28 weeks after randomization. A statistically significant overall difference was found with respect to the primary variable, the IPSS (P ≤ .001). Optimal results, a 4-point improvement in IPSS in excess of the changes observed in the placebo group, were achieved with a starting dose of 60 mg cetrorelix pamoate followed by a dose of 30 mg 2 weeks later. In all dosage groups, the symptomatic improvement was paralleled by an increase in uroflow. There was a marked dissociation between only moderate and transient testosterone suppression and the persisting effects on BPH signs and symptoms. Tolerability was good at all cetrorelix dosages. Intramuscular injections of 60 and 30 mg of cetrorelix pamoate within 2 weeks provide rapid symptomatic improvements of BPH that are sustained for the following 6 months.