Androxal enclomiphene: Additional Phase III data

Additional data from the 6-month, open-label, dose-escalation, U.S. Phase III ZA-300 trial in 499 patients showed that oral Androxal significantly reduced mean testosterone levels at week 26 by 286.6 ng/dL at the 12.5 mg dose and 215.5 ng/dL at the 25 mg dose compared to baseline (p<0.05). Repros said change from baseline in total testosterone was significant compared to baseline at 4- and 8-week follow-up after the end of 26-week treatment at the 12.5 mg dose, but only significant at week 4 follow-up for the 25 mg dose (p<0.05 for all). Androxal led to mean testosterone levels within the normal range (300-1,040 ng/dL) at week 26 in 94.6% of patients at the 12.5 mg dose and 81% of patients at the 25 mg dose. Patients initially receive Androxal at the 12.5 mg dose, which was up-titrated to 25 mg if patient's morning testosterone level was <450 ng/dL at any visit.

Additionally, Androxal reduced the proportion of patients with cholesterol levels >200mg/dL to 13.7% at week 26 from 35.1% at baseline. Androxal reduced total cholesterol by 18.3 mg/dL at the 12.5 mg dose and by 18.4 mg/dL at the 25 mg dose at week 26 compared to baseline (p<0.0001 for both). Furthermore, both doses of Androxal reduced fasting plasma glucose (FPG) by 5.2 mg/dL from baseline at week 26 (p<0.0001) and reduced the proportion of patients with high HbA1c to 32% at week 26 from 37% at baseline. No new safety issues were identified. The most common adverse events reported were upper respiratory tract infection-related reactions, headaches, muscle spasms and fatigue. In September 2013, Repros reported that Androxal was well tolerated in the trial. ...