Estradiol/progesterone

Estradiol/progesterone (E2/P4), sold under the brand name Bijuva among others, is a combined estrogen and progestogen medication which is used in the treatment of menopausal symptoms in postmenopausal women.[3] It contains estradiol, an estrogen, and progesterone, a progestogen, and is available in both oral and intramuscular formulations.[3] E2/P4 differs from other estrogen–progestogen formulations in that the sex-hormonal agents used are bioidentical.

Estradiol/progesterone
Estradiol (top) and progesterone (bottom)
Combination of
EstradiolEstrogen
ProgesteroneProgestogen
Clinical data
Trade namesBijuva, Juvenum, Lutes
Other namesE2/P4; TX-001HR; TX-12-001HR; CA682-2
License data
Routes of
administration		By mouth, intramuscular injection
ATC code
Legal status
Legal status
Identifiers
KEGG
CompTox Dashboard (EPA)

Estradiol/progesterone is an oral combination of estradiol (E2), an estrogen, and progesterone (P4), a progestogen, which was developed by TherapeuticsMD and is approved in the United States for the treatment of menopausal symptoms in women.[4][5] It is also under development for the treatment of endometrial hyperplasia in women.[4] The medication contains 2 mg solubilized E2 and 200 mg P4 in each gelatin capsule.[5][3] It is the first combination of E2 and P4 in oral capsule form that has been developed for clinical use.[5] Bijuva is currently in phase III clinical trials for endometrial hyperplasia.[4] The medication was approved by the Food and Drug Administration for the treatment of menopausal symptoms in October 2018.[4][6][3] It is available as a generic medication.[7]

E2/P4 is available as an aqueous suspension of E2 and P4 encapsulated in microspheres for use by intramuscular injection under the brand name Juvenum in Mexico.[8][9][10] It was introduced for the treatment and prevention of menopausal symptoms like hot flashes, vulvovaginal symptoms, and osteoporosis in December 2014.[8][9] The combination contains relatively low doses of E2 and P4 (1 mg and 20 mg, respectively) contained within microspheres that results in a slower release of the hormones.[8][9] Studies of this formulation have been published.[11][12]

E2/P4 with 5 mg E2 and 150 to 300 mg P4 encapsulated in microspheres in an aqueous suspension has been studied as a once-a-month combined injectable contraceptive but has not been further developed or introduced for medical use.[13][14][15][16][17] E2/P4 with 5 mg E2 and 100 mg P4 in a macrocrystalline aqueous suspension has also been studied as a once-a-month combined injectable contraceptive, but likewise was not further developed.[18][19]

Research

As of April 2022, a vaginal ring containing E2/P4 (developmental code names DARE-HRT1 and JNP-0201) is under development for use in menopausal hormone therapy.[20]

References
  1. "Bijuva (Theramex Australia Pty Ltd)". Therapeutic Goods Administration (TGA). 22 September 2022. Archived from the original on 12 March 2023. Retrieved 29 April 2023.
  2. "Bijuva Product information". Health Canada. 25 April 2012. Archived from the original on 6 June 2022. Retrieved 5 June 2022.
  3. "Bijuva- estradiol and progesterone capsule". DailyMed. 30 June 2021. Archived from the original on 12 March 2023. Retrieved 12 March 2023.
  4. "Estradiol/Progesterone - TherapeuticsMD - AdisInsight". Archived from the original on 22 October 2016. Retrieved 21 October 2016.
  5. Pickar JH, Bon C, Amadio JM, Mirkin S, Bernick B (2015). "Pharmacokinetics of the first combination 17β-estradiol/progesterone capsule in clinical development for menopausal hormone therapy". Menopause. 22 (12): 1308–16. doi:10.1097/GME.0000000000000467. PMC 4666011. PMID 25944519.
  6. "Bijuva (Estradiol and progesterone) FDA Approval History". Archived from the original on 3 November 2018. Retrieved 3 November 2018.
  7. "First Generic Drug Approvals". U.S. Food and Drug Administration. 17 October 2022. Archived from the original on 26 January 2021. Retrieved 28 November 2022.
  8. "Juvenum (estradiol/progesterone) - Medicamentos PLM". Medicamentos PLM. Archived from the original on 18 September 2018. Retrieved 17 September 2018.
  9. "Estradiol/Progesterone injection - Laboratorios Carnot - AdisInsight". Archived from the original on 29 August 2021. Retrieved 23 December 2017.
  10. "Juvenum - Drugs.com". Archived from the original on 23 December 2017. Retrieved 23 December 2017.
  11. Cortés-Bonilla M, Alonso-Campero R, Bernardo-Escudero R, Francisco-Doce MT, Chavarín-González J, Pérez-Cuevas R, Chedraui P (October 2016). "Improvement of quality of life and menopausal symptoms in climacteric women treated with low-dose monthly parenteral formulations of non-polymeric microspheres of 17β-estradiol/progesterone". Gynecol. Endocrinol. 32 (10): 831–834. doi:10.1080/09513590.2016.1183628. PMID 27187320. S2CID 22688585.
  12. Cortés-Bonilla M, Bernardo-Escudero R, Alonso-Campero R, Francisco-Doce MT, Hernández-Valencia M, Celis-González C, Márquez-Oñate R, Chedraui P, Uribe JA (July 2015). "Treatment of menopausal symptoms with three low-dose continuous sequential 17β-estradiol/progesterone parenteral monthly formulations using novel non-polymeric microsphere technology". Gynecol. Endocrinol. 31 (7): 552–9. doi:10.3109/09513590.2015.1019853. PMC 4776687. PMID 26062108.
  13. Toppozada MK (April 1994). "Existing once-a-month combined injectable contraceptives". Contraception. 49 (4): 293–301. doi:10.1016/0010-7824(94)90029-9. PMID 8013216.
  14. Garza-Flores J (April 1994). "Pharmacokinetics of once-a-month injectable contraceptives". Contraception. 49 (4): 347–59. doi:10.1016/0010-7824(94)90032-9. PMID 8013219.
  15. Bagade O, Pawar V, Patel R, Patel B, Awasarkar V, Diwate S (2014). "Increasing use of long-acting reversible contraception: safe, reliable, and cost-effective birth control" (PDF). World J Pharm Pharm Sci. 3 (10): 364–392. ISSN 2278-4357. Archived (PDF) from the original on 10 August 2017. Retrieved 18 September 2018.
  16. Newton JR, D'arcangues C, Hall PE (1994). "A review of "once-a-month" combined injectable contraceptives". J Obstet Gynaecol (Lahore). 4 (Suppl 1): S1–34. doi:10.3109/01443619409027641. PMID 12290848.
  17. Garza-Flores J, Hall PE, Perez-Palacios G (1991). "Long-acting hormonal contraceptives for women". J. Steroid Biochem. Mol. Biol. 40 (4–6): 697–704. doi:10.1016/0960-0760(91)90293-E. PMID 1958567. S2CID 26021562.
  18. Alvarez-Sanchez, Francisco; Brache, Vivian; Faundes, Anibal (1993). "Recent experience with and future directions of contraceptive implants and injectable contraceptives". Current Opinion in Obstetrics and Gynecology. 5 (6): 805–814. doi:10.1097/00001703-199312000-00016. ISSN 1040-872X. PMID 8286694.
  19. Garza-Flores J, Fatinikun T, Hernandez L, Ramos I, Cardenas M, Menjivar M (July 1991). "A pilot study on the assessment of a progesterone/estradiol sustained release as once-a-month-injectable contraceptive". Contraception. 44 (1): 45–59. doi:10.1016/0010-7824(91)90105-O. PMID 1893701.
  20. "Estradiol/Progesterone intravaginal ring - Dare Bioscience - AdisInsight". Archived from the original on 29 April 2023. Retrieved 29 April 2023.
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