Drospirenone/estetrol

Drospirenone/estetrol, sold under the brand name Nextstellis, among others, is a fixed-dose combination medication containing drospirenone, a progestin, and estetrol, an estrogen, which is used as a combined birth control pill for the prevention of pregnancy in women.^[2][6] It is taken by mouth.^[2][6]

Drospirenone/estetrol

Combination of
Drospirenone	Progestogen
Estetrol (medication)	Estrogen
Clinical data
Trade names	Nextstellis, Drovelis, Lydisilka, others
Other names	E4/DRSP; FSN-013
AHFS/Drugs.com	Monograph
License data	US DailyMed: Drospirenone_and_estetrol
Pregnancy category	AU: B3 [1]
Routes of administration	By mouth
ATC code	G03AA18 (WHO)
Legal status
Legal status	AU: S4 (Prescription only)[1] CA: ℞-only[2][3][4][5] US: ℞-only[6] EU: Rx-only[7][8][9][10]
Identifiers
ChemSpider	None
KEGG	D12047

It was approved for medical use in Canada in March 2021,^[3] and in the United States in April 2021.^[6]

Medical uses

Drospirenone/estetrol is used as a combined birth control pill to prevent pregnancy in women.^[2][6]

Side effects

Estetrol-containing birth control pills, similarly to estradiol-containing birth control pills, may have a lower risk of venous thromboembolism (VTE) than ethinylestradiol-containing birth control pills based on studies of coagulation.^[11][12] However, it is likely that another decade will be required before post-marketing epidemiological studies of VTE incidence with these birth control pills are completed and able to confirm this.^[13]

Pharmacology

Pharmacodynamics

Drospirenone/estetrol has a much lower impact on liver protein synthesis, including of sex hormone-binding globulin, angiotensinogen, and coagulation factors, than does ethinylestradiol/drospirenone.^[14]

Society and culture

Legal status

Drospirenone/estetrol is approved for the use of hormonal contraception in the European Union,^[7][8] the United States,^[15] and Canada.^[3]

Brand names

Drospirenone/estetrol in sold under the brand names Nexstellis,^[3] Drovelis,^[7] and Lydisilka.^[8]

See also

• Birth control pill formulations
• List of combined sex-hormonal preparations § Estrogens and progestogens

References

1. "Nextstellis". Therapeutic Goods Administration (TGA). 6 December 2021. Archived from the original on 28 December 2021. Retrieved 28 December 2021.
2. "PRODUCT MONOGRAPH INCLUDING PATIENT MEDICATION INFORMATION NEXTSTELLIS" (PDF). 5 March 2021. Archived (PDF) from the original on 9 July 2022. Retrieved 4 July 2024.
3. "Nextstellis Product information". Health Canada. 25 April 2012. Archived from the original on 22 September 2021. Retrieved 4 November 2021.
4. "Summary Basis of Decision (SBD) for Nextstellis". Health Canada. 23 October 2014. Archived from the original on 30 May 2022. Retrieved 29 May 2022.
5. "Health product highlights 2021: Annexes of products approved in 2021". Health Canada. 3 August 2022. Archived from the original on 25 March 2024. Retrieved 25 March 2024.
6. "Nextstellis- drospirenone and estetrol kit". DailyMed. Archived from the original on 2 June 2021. Retrieved 1 June 2021.
7. "Drovelis EPAR". European Medicines Agency (EMA). 24 March 2021. Archived from the original on 4 November 2021. Retrieved 4 November 2021.
8. "Lydisilka EPAR". European Medicines Agency (EMA). 24 March 2021. Archived from the original on 4 November 2021. Retrieved 4 November 2021.
9. "Drovelis Product information". Union Register of medicinal products. Archived from the original on 5 March 2023. Retrieved 3 March 2023.
10. "Lydisilka Product information". Union Register of medicinal products. Archived from the original on 5 March 2023. Retrieved 3 March 2023.
11. Morimont L, Haguet H, Dogné JM, Gaspard U, Douxfils J (2021). "Combined Oral Contraceptives and Venous Thromboembolism: Review and Perspective to Mitigate the Risk". Front Endocrinol (Lausanne). 12: 769187. doi:10.3389/fendo.2021.769187. PMC 8697849. PMID 34956081.
12. Douxfils J, Morimont L, Bouvy C (November 2020). "Oral Contraceptives and Venous Thromboembolism: Focus on Testing that May Enable Prediction and Assessment of the Risk". Semin Thromb Hemost. 46 (8): 872–886. doi:10.1055/s-0040-1714140. PMID 33080636. S2CID 224821517.
13. Grandi G, Facchinetti F, Bitzer J (February 2022). "Confirmation of the safety of combined oral contraceptives containing oestradiol on the risk of venous thromboembolism". Eur J Contracept Reprod Health Care. 27 (2): 83–84. doi:10.1080/13625187.2022.2029397. PMID 35133236. S2CID 246651102. Moreover, the introduction of other new natural oestrogenic components, such as estetrol (E4) [12], could have a similar lower VTE impact; however, we will likely need another decade to obtain results from post-marketing studies.
14. Farris M, Bastianelli C, Rosato E, Brosens I, Benagiano G (October 2017). "Pharmacodynamics of combined estrogen-progestin oral contraceptives: 2. effects on hemostasis". Expert Rev Clin Pharmacol. 10 (10): 1129–1144. doi:10.1080/17512433.2017.1356718. PMID 28712325. S2CID 205931204.
15. "Drug Approval Package: Nextstellis". U.S. Food & Drug Administration (FDA). 12 May 2021. Archived from the original on 6 November 2021. Retrieved 30 November 2021.

External links

• Clinical trial number NCT02817828 for "E4 FREEDOM (Female Response Concerning Efficacy and Safety of Estetrol/Drospirenone as Oral Contraceptive in a Multicentric Study) - EU/Russia Study" at ClinicalTrials.gov
• Clinical trial number NCT02817841 for "E4 FREEDOM (Female Response Concerning Efficacy and Safety of Estetrol/Drospirenone as Oral Contraceptive in a Multicentric Study) - United States/Canada Study" at ClinicalTrials.gov