A combined, bioidentical, oral, 17β-estradiol and progesterone capsule for the treatment of moderate to severe vasomotor symptoms due to menopause

Expert Rev Clin Pharmacol. 2019 Aug;12(8):729-739. doi: 10.1080/17512433.2019.1637731. Epub 2019 Jul 22.

Abstract

Introduction: Many women seek treatment to alleviate menopausal vasomotor symptoms (VMS). Numerous women use combination compounded hormone therapy (CHT) to achieve the benefits of estrogen/progesterone for endometrial protection. TX-001HR is a combination of bioidentical 17β-estradiol (E2) and progesterone (P4) in a single capsule designed for continuous daily use to treat moderate to severe VMS. Areas covered: This drug profile describes the efficacy and safety of 4 doses of this E2/P4 (mg/mg: 1/100, 0.5/100, 0.5/50, 0.25/50) for treating moderate to severe VMS in menopausal woman with a uterus. Expert opinion: In REPLENISH (NCT01942668), the two highest doses of TX-001HR significantly reduced VMS frequency and severity at 4 and 12 weeks versus placebo (co-primary endpoints); all doses met the primary endpoint of endometrial safety. Rates of amenorrhea were high and improved over time; the Menopause Quality of Life and Medical Outcomes Study-Sleep instruments improved with E2/P4. TX-001HR was well tolerated and had no clinically significant impact on vital signs, metabolic or coagulation parameters, or breast safety. The combination bioidentical E2/P4 capsule (1 mg/100 mg dose was FDA-approved as Bijuva in October 2018) may provide a safe, effective, rigorously studied alternative for women with a uterus who prefer CHT for relief of VMS.

Keywords: Amenorrhea; endometrial safety; estradiol; menopause; progesterone; vasomotor symptoms.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Capsules
  • Dose-Response Relationship, Drug
  • Estradiol / administration & dosage*
  • Estradiol / adverse effects
  • Estradiol / pharmacology
  • Female
  • Hot Flashes / drug therapy
  • Humans
  • Menopause*
  • Progesterone / administration & dosage*
  • Progesterone / adverse effects
  • Progesterone / pharmacology
  • Quality of Life*
  • Severity of Illness Index
  • Sweating / drug effects

Substances

  • Capsules
  • TX-001HR
  • Progesterone
  • Estradiol