Segesterone acetate
Progestin; Progestogen ester | |
| ATC code |
|
|---|---|
| Legal status | |
| Legal status |
|
| Identifiers | |
| |
JSmol) | |
| |
| |
Segesterone acetate (SGA), sold under the brand names Nestorone, Elcometrine, and Annovera, is a
birth control and in the treatment of endometriosis in the United States, Brazil, and other South American countries.[1][4][7] It is available both alone and in combination with an estrogen.[1][4][7] It is not effective by mouth and must be given by other routes, most typically as a vaginal ring or implant that is placed into fat.[1][4][8]
SGA was developed by the
ethinyl estradiol was approved in the United States.[4][16] It is marketed under the brand name Annovera and is reusable for up to one year as a method of birth control in women. Annovera does not require refrigeration which is very useful for low resource areas.[4][17]
Medical uses
SGA is used as a
Available forms
Side effects
Side effects of SGA are similar to those of other progestins.[citation needed]
Pharmacology
Pharmacodynamics
SGA acts primarily as a high-
transdermal gel (delivering 200–300 μg/day SGA) for 2 weeks suppressed testosterone levels from ~581 ng/dL to ~276 ng/dL (–52%).[18]
Pharmacokinetics
SGA is only weakly active
parenteral SGA has been reported to be 24 to 72 hours.[5][6] One study specifically reported a biological half-life of 26.8 hours.[6] It has been reported that the biological half-life of SGA with oral administration is only 1 to 2 hours.[1] In contrast to all of the preceding however, the Food and Drug Administration (FDA) label for Annovera, a one-year vaginal ring containing ethinylestradiol and SGA, lists a circulating half-life of SGA of 4.5 hours.[4]
Chemistry
SGA, also known as 16-methylene-17α-acetoxy-19-norprogesterone or as 16-methylene-17α-acetoxy-19-norpregn-4-ene-3,20-dione, is a
History
SGA was developed by the Population Council.[11] It has been marketed since at least 2000.[7]
Society and culture
Generic names
Segesterone acetate is the
generic name of the drug and its USAN.[24][25] It is also known by its brand names nestorone and elcometrine,[26] as well as by its former developmental code names ST-1435, AC-6844, and CS-0411.[citation needed
]
Brand names
SGA is marketed alone under the brand names Nestorone and Elcometrine and in combination with ethinylestradiol under the brand name Annovera.[4][7]
Availability
SGA is available alone in several
South American countries, including Brazil.[1] It is available in the United States as a contraceptive vaginal ring in combination with ethinylestradiol.[4]
Research
A
contraceptive in women by the Population Council in conjunction with Antares Pharma in the United States and Europe.[12][14] As of December 2017, it is in phase III clinical trials for this indication.[12] The medication has the tentative brand name NestraGel.[12] A combination of SGA and the estrogen ethinylestradiol in a vaginal ring formulation for use as a one-year contraceptive was developed by the Population Council in multiple regions including Latin America, Europe, and Australia.[17] It completed phase III clinical trials and [17] was approved in the United States in August 2018.[4][16]
A combination of SGA and the androgen testosterone is under development as a transdermal gel formulation for use as a hormonal contraceptive in men by the Population Council.[13][15] As of December 2017, it is in phase II clinical studies for this purpose.[15][27] In a trial, 100 couples used segesterone/testosterone dermal gel as the sole contraception method, which resulted in no pregnancy. Side effects were described as mild, comprising acne, weight gain and nocturnal sweating.[28]
See also
- Ethinylestradiol/segesterone acetate
References
- ^ ISBN 978-1-60913-345-0. Retrieved 13 September 2012.
- ^ ISBN 978-1-84214-038-3.
- ^ S2CID 24616324.
- ^ a b c d e f g h i j k l "ANNOVERATM (segesterone acetate and ethinyl estradiol vaginal system)" (PDF). Population Council. U.S. Food and Drug Administration. 2018.
- ^ a b c d e Rabe T, Goeckenjan M, Ahrendt HJ, Crosignani PG, Dinger JC, Mueck AO, et al. (October 2011). "Oral Contraceptive Pills: Combinations, Dosages and the Rationale behind 50 Years or Oral Hormonal Contraceptive Development" (PDF). Journal für Reproduktionsmedizin und Endokrinologie-Journal of Reproductive Medicine and Endocrinology. 8 (1): 58–129.
- ^ PMID 18061700.
- ^ S2CID 42296395.
- ^ ISBN 978-0-7817-4499-7. Retrieved 13 September 2012.
- ^ PMID 21828184.
- ^ S2CID 13722269.
- ^ a b Prasad, P. V., & Shrivastav, T. G. (2015). Nestorone®: A new hope for Gynecologists, Andrologists and Neurologists. of, 3, 2.
- ^ a b c d "Elcometrine/Estradiol - Population Council/Therapeutics MD - AdisInsight".
- ^ PMID 22791756.
- ^ a b "Nestorone®/Estradiol Transdermal Gel Contraception | Population Council".
- ^ a b c "Nestorone®/Testosterone Transdermal Gel for Male Contraception | Population Council". 14 September 2022.
- ^ a b "FDA approves new vaginal ring for one year of birth control". Food and Drug Administration. 24 March 2020.
- ^ a b c "The Nestorone®/Ethinyl Estradiol One-Year Vaginal Contraceptive System". Population Council.
- ^ S2CID 41502711.
- ^ S2CID 205253216.
- ISBN 978-1-351-74347-1.
- S2CID 37188669.
- S2CID 34984413.
- PMID 27824503.
- ^ "Segesterone acetate" (PDF). Population Council, Inc. American Medical Association.
- ^ "7759-35-5 - CKFBRGLGTWAVLG-GOMYTPFNSA-N - Segesterone acetate [USAN] - Similar structures search, synonyms, formulas, resource links, and other chemical information". ChemIDplus. Archived from the original on 2016-08-11. Retrieved 2016-06-17.
- ISBN 978-3-527-30247-5. Retrieved 13 September 2012.
- ^ Clinical trial number NCT03452111 for "Clinical Evaluation of Daily Application of Nestorone® (NES) and Testosterone (T) Combination Gel for Male Contraception" at ClinicalTrials.gov
- ^ Stöckel M (2022-06-13). "Verhütung für den Mann: Das Hormon-Gel lässt hoffen" [Contraception for men: The hormone gel inspires hope] (in German). Swiss Radio and Television SRF. Retrieved 2022-06-15.