Estradiol/progesterone

Estradiol/progesterone (E2/P4), sold under the brand names Bijuva and Juvenum, is a combined estrogen and progestogen medication which is used in the treatment of menopausal symptoms in postmenopausal women.[2] It contains estradiol, an estrogen, and progesterone, a progestogen, and is available in both oral and intramuscular formulations.[2] 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
Routes of
administration		By mouth, intramuscular injection
ATC code
Legal status
Legal status
Identifiers
KEGG
CompTox Dashboard (EPA)

Bijuva (formerly TX-001HR/TX-12-001HR) 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.[3][4] It is also under development for the treatment of endometrial hyperplasia in women.[3] The medication contains 2 mg solubilized E2 and 200 mg P4 in each gelatin capsule.[4][2] It is the first combination of E2 and P4 in oral capsule form that has been developed for clinical use.[4] Bijuva is currently in phase III clinical trials for endometrial hyperplasia.[3] The medication was approved by the Food and Drug Administration for the treatment of menopausal symptoms in October 2018.[3][5][2]

E2/P4 is available as an aqueous suspension of E2 and P4 encapsulated in microspheres for use by intramuscular injection once a month under the brand name Juvenum in Mexico.[6][7][8] It was introduced for the treatment and prevention of menopausal symptoms like hot flashes, vulvovaginal symptoms, and osteoporosis in December 2014.[6][7] 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.[6][7] Studies of this formulation have been published.[9][10]

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.[11][12][13][14][15] 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.[16][17]

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.[18]

References
  1. "Bijuva Product information". Health Canada. 25 April 2012. Retrieved 5 June 2022.
  2. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210132s000lbl.pdf
  3. "Estradiol/Progesterone - TherapeuticsMD - AdisInsight".
  4. 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.
  5. "Bijuva (Estradiol and progesterone) FDA Approval History".
  6. "Juvenum (estradiol/progesterone) - Medicamentos PLM". Medicamentos PLM. Archived from the original on 2018-09-18. Retrieved 2018-09-17.
  7. "Estradiol/Progesterone injection - Laboratorios Carnot - AdisInsight".
  8. "Juvenum - Drugs.com". Archived from the original on 2017-12-23. Retrieved 2017-12-23.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. "Estradiol/Progesterone intravaginal ring - Dare Bioscience - AdisInsight".
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