Figure 4 The maintenance of
castration in men treated with triptorelin pamoate, 3.75 mg (green line, open circles), or leuprolide acetate, 7.5 mg (red line, open squares), for 9 months (Kaplan-Meier mostly survival analysis). Reproduced with permission from Heyns CF … Secondary endpoints (9-month survival rate, mean LH concentrations during treatment, median bone pain values as measured by the visual analog scale, quality of life, median PSA concentrations) were equivalent in both groups except for the 9-month overall survival rate, which was 97% in the triptorelin pamoate group versus 90.5% in the leuprolide acetate Inhibitors,research,lifescience,medical group (P = .033). Mean and cumulative castration maintenance rates between 29 and 253 days were equivalent between the treatment groups. Mean serum T levels were analyzed every 28 days in the leuprolide Inhibitors,research,lifescience,medical acetate and triptorelin pamoate treatment groups. These levels fell below the predefined levels for medical
castration (≤ 50 ng/dL in this trial) at 29 days and 57 days for 91% and 98% of www.selleckchem.com/products/kpt-330.html subjects in the triptorelin pamoate group and 99% and 97% of the subjects in the leuprolide group, respectively. Although Inhibitors,research,lifescience,medical the mean difference was significant between the leuprolide acetate and triptorelin pamoate treatment groups at 29 days, it was not significant at 57 days (Figure 5). Figure 5 Mean serum testosterone levels were analyzed every 28 days in 277 men receiving androgen deprivation with either leuprolide acetate or triptorelin pamoate. These levels fell below the predefined levels for medical castration (50 ng/dL) at 29 days and … The results from Heyns and colleagues71 indicate that triptorelin pamoate may induce castration at a slightly slower rate than leuprolide acetate, but triptorelin Inhibitors,research,lifescience,medical pamoate maintains castration at least as effectively as leuprolide. A possible reason for this outcome may be dosing differences between triptorelin pamoate and leuprolide acetate. The repeated exposure to the higher leuprolide
acetate dose (7.5 mg), as Inhibitors,research,lifescience,medical compared with the lower triptorelin pamoate dose (3.75 mg) may more likely cause an escape resulting from weak desensitization of pituitary GnRH receptors.71 The hypothesis is supported by an insignificant trend throughout the study, evidenced where there was more LH Dacomitinib stimulation with leuprolide than triptorelin pamoate at day 85 (98% vs 94%) and 169 days (98% vs 93%).71 Additional data support this claim with individual patients; there were fewer triptorelin pamoate than leuprolide patients who achieved castration at 29 days but had T escape at least once between months 2 and 9 of the study (4 vs 11, respectively); this result correlated with the pharmacological data. Assessment of T levels over 24 hours in a patient subset showed that 3 of 15 patients treated with leuprolide escaped castrate T levels as compared to none of the 14 patients treated with triptorelin pamoate.