INTRAROSA (prasterone) vaginal inserts

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 INDICATION: Steroid indicated for the treatment of moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause. 


Mechanism of Action Prasterone is an inactive endogenous steroid and is converted into active androgens and/or estrogens. The mechanism of action of INTRAROSA in postmenopausal women with vulvar and vaginal atrophy is not fully established.
Pharmacodynamics (PD) Not reported.
Pharmacokinetics (PK) In a study conducted in postmenopausal women, administration of the INTRAROSA vaginal insert once daily for 7 days resulted in a mean prasterone Cmax and area under the curve from 0 to 24 hours (AUC0- 24) at Day 7 of 4.4 ng/mL and 56.2 ngh/mL, respectively, which were significantly higher than those in the group treated with placebo.

 The Cmax and AUC0- 24 on Day 7 of the testosterone metabolite (metabolite of prasterone) were 0.15 ng/mL and 2.79 ngh/mL, respectively which were slightly higher in women treated with the INTRAROSA vaginal insert compared to those receiving placebo, 0.12 ng/mL and 2.58 ngh/mL, respectively.

 The Cmax and AUC0- 24 on Day 7 of the estradiol metabolite (metabolite of prasterone) were 5.04 pg/mL and 96.93 pgh/mL, respectively which were also slightly higher in women treated with the INTRAROSA vaginal insert compared to those receiving placebo, 3.33 pg/mL and 66.49 pgh/mL, respectively.

 Exogenous prasterone is metabolized in the same manner as endogenous prasterone. Human steroidogenic enzymes such as hydroxysteroid dehydrogenases, 5α-reductases and aromatases transform prasterone into androgens and estrogens.

 In two primary efficacy trials, daily administration of INTRAROSA vaginal insert for 12 weeks increased mean serum Ctrough of prasterone and its metabolites testosterone and estradiol by 47%, 21% and 19% from baseline, respectively. This comparison based on Ctrough may underestimate the magnitude of increase in prasterone and metabolites’ exposure because it does not take into account the overall concentration-time profile following administration of INTRAROSA.

PK-PD Analysis                          Not reported.
Population PK Not reported.
 Special Populations  Not reported.
Drug Interactions Not reported.

Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208470s000lbl.pdf

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