Evaluation of bazedoxifene/conjugated estrogens for the treatment of menopausal symptoms and effects on metabolic parameters and overall safety profile

Fertil Steril. 2009 Sep;92(3):1025-1038. doi: 10.1016/j.fertnstert.2009.03.113. Epub 2009 Jul 26.

Abstract

Objective: To evaluate the effects of a tissue-selective estrogen complex (TSEC) composed of bazedoxifene/conjugated estrogens (BZA/CE) on menopausal symptoms, metabolic parameters, and overall safety.

Design: Multicenter, double-blind, placebo- and active-controlled phase 3 trial (Selective estrogens, Menopause, And Response to Therapy [SMART]-1).

Setting: Outpatient clinical.

Patient(s): Healthy, postmenopausal women (n = 3,397) age 40 to 75 with an intact uterus.

Intervention(s): Single tablets of BZA (10, 20, or 40 mg), each with CE (0.625 or 0.45 mg); raloxifene 60 mg; or placebo taken daily for 2 years.

Main outcome measure(s): Hot flushes, breast pain, vaginal atrophy, metabolic parameters, and adverse events.

Result(s): BZA (20 mg)/CE (0.625 or 0.45 mg) significantly reduced the frequency and severity of hot flushes and improved measures of vaginal atrophy compared with placebo. At week 12, the daily number of hot flushes decreased by 51.7% to 85.7% with all BZA/CE doses vs. 17.1% for placebo. BZA/CE improved lipid parameters and homocysteine levels, did not significantly change carbohydrate metabolism, and had only minor effects on some coagulation parameters. The incidences of breast pain and adverse events were similar between BZA/CE and placebo.

Conclusion: The TSEC composed of BZA (20 mg)/CE (0.625 or 0.45 mg) is an effective and safe treatment for menopausal symptoms.

Trial registration: ClinicalTrials.gov NCT00675688.

Publication types

  • Clinical Trial, Phase III
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Atrophy / drug therapy
  • Atrophy / pathology
  • Carbohydrate Metabolism / drug effects
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Drug Therapy, Combination
  • Estrogens / adverse effects
  • Estrogens / pharmacology
  • Estrogens / therapeutic use*
  • Estrogens, Conjugated (USP) / adverse effects
  • Estrogens, Conjugated (USP) / pharmacology
  • Estrogens, Conjugated (USP) / therapeutic use*
  • Female
  • Homocysteine / metabolism
  • Hot Flashes / drug therapy*
  • Humans
  • Indoles / adverse effects
  • Indoles / pharmacology
  • Indoles / therapeutic use*
  • Lipid Metabolism / drug effects
  • Menopause / drug effects
  • Menopause / metabolism*
  • Middle Aged
  • Outpatients
  • Selective Estrogen Receptor Modulators / adverse effects
  • Selective Estrogen Receptor Modulators / pharmacology
  • Selective Estrogen Receptor Modulators / therapeutic use*
  • Treatment Outcome
  • Vagina / drug effects
  • Vagina / pathology*

Substances

  • Estrogens
  • Estrogens, Conjugated (USP)
  • Indoles
  • Selective Estrogen Receptor Modulators
  • Homocysteine
  • bazedoxifene

Associated data

  • ClinicalTrials.gov/NCT00675688