Ulipristal acetate, sold under the brand name Ella among others, is a medication used for emergency birth control and uterine fibroids. As emergency birth control it should be used within 120 hours of sex. For fibroids it may be taken for up to six months. It is taken by mouth.
Ulipristal acetate was approved for medical use in the United States in 2010. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. In the United Kingdom it costs the NHS about 17 pounds per course of emergency birth control of 2015. To improve access, some recommend all who can get pregnant be given a prescription for use if needed.
For emergency contraception a 30 mg tablet is used within 120 hours (5 days) after unprotected intercourse or contraceptive failure. It has been shown to prevent about 62–85% of expected pregnancies, and prevents more pregnancies than emergency contraception with levonorgestrel. Ulipristal acetate is available by prescription for emergency contraception in over 50 countries, with access through pharmacists without a prescription being tested in the United Kingdom. In November 2014 European Medicines Agency recommended availability of ellaOne emergency contraceptive without prescription in the European Union. In January 2015 the European Commission issued an implementing decision amending accordingly the marketing authorization of EllaOne in the EU. Since July 2016, it is available without prescription in Israel.
Ulipristal acetate is used for pre-operative treatment of moderate to severe symptoms of uterine fibroids in adult women of reproductive age in a daily dose of a 5 mg tablet.
Treatment of uterine fibroids with ulipristal acetate for 13 weeks effectively controlled excessive bleeding due to uterine fibroids and reduced the size of the fibroids.
Two intermittent 3-months treatment courses of ulipristal acetate 10 mg resulted in amenorrhea at the end of the first treatment course in 79.5%, at the end of the second course in 88.5% of subjects. Mean myoma volume reduction observed during the first treatment course (−41.9%) was maintained during the second one (−43.7%). After two to four 3-months courses of treatment, UPA-treated fibroids shown about -70% in volume reduction.
Volume reduction of uterine fibroid induced by ulipristal acetate was tentatively explained by the combination of multifactorial events involving control of proliferation of the tumor cells, induction of apoptosis and remodeling of the extracellular matrix under the action of matrix metalloproteinases.
In May 2018, the European Medicines Agency recommended measures to minimise the risk of rare but serious liver injury with ulipristal, including contraindication in women with known liver problems; liver tests before, during and after stopping treatment; a card for people to inform them about the need for liver monitoring and to contact their doctor should they develop symptoms of liver injury. In addition, use of the medicine for more than one treatment course has been restricted to women who are not eligible for surgery.
Ulipristal acetate should not be taken by women with severe liver diseases because of its CYP mediated metabolism. It has not been studied in women under the age of 18.
It is also not recommended for women with severe asthma receiving glucocorticoid treatment because it has shown antiglucocorticoid effects in animal studies.
Unlike levonorgestrel, and like mifepristone, ulipristal acetate is embryotoxic in animal studies. Before taking the drug, a pregnancy must be excluded. The EMA proposed to avoid any allusion to a possible use as an abortifacient in the package insert to avert off-label use. It is unlikely that ulipristal acetate could effectively be used as an abortifacient, since it is used in much lower doses (30 mg) than the roughly equipotent mifepristone (600 mg), and since mifepristone has to be combined with a prostaglandin for the induction of abortion. However, data on embryotoxicity in humans are very limited, and it is not clear what the risk for an abortion or for teratogenicity (birth defects) is. Of the 29 women studied who became pregnant despite taking ulipristal acetate, 16 had induced abortions, six had spontaneous abortions, six continued the pregnancies, and one was lost to follow-up.
It is not recommended to breast feed within 36 hours of taking the drug since it is not known whether ulipristal acetate or its metabolites are excreted into the breast milk.
Ulipristal acetate is marketed in the United States under the brand name Ella and in Canada under the brand name Fibristal. It is also marketed under the brand names EllaOne and Esmya both in over 20 countries, of which include the United Kingdom and Ireland. A few less-widely used brand names also exist.
^Glasier, Anna F; Cameron, Sharon T; Fine, Paul M; Logan, Susan JS; Casale, William; Van Horn, Jennifer; Sogor, Laszlo; Blithe, Diana L; Scherrer, Bruno; Mathe, Henri; Jaspart, Amelie; Ulmann, Andre; Gainer, Erin (2010). "Ulipristal acetate versus levonorgestrel for emergency contraception: a randomised non-inferiority trial and meta-analysis". The Lancet. 375 (9714): 555–62. doi:10.1016/S0140-6736(10)60101-8. PMID20116841.
^Trussell, James; Cleland, Kelly (13 February 2013). "Dedicated emergency contraceptive pills worldwide"(PDF). Princeton: Office of Population Research at Princeton University, Association of Reproductive Health Professionals. Archived(PDF) from the original on 4 March 2016. Retrieved 25 March 2014.
^ECEC (2014). "Emergency contraception availability in Europe". New York: European Consortium for Emergency Contraception (ECEC). Archived from the original on 25 March 2014. Retrieved 25 March 2014. Ulipristal acetate Emergency Contraception Pills (UPA ECPs), while available in most European countries since 2010, are not yet available in Albania, Estonia, Macedonia, Malta, Switzerland and Turkey. For now UPA ECPs are sold with a prescription in all countries, although provision without a prescription is currently being tested in the United Kingdom.
^Šauer, Pavel; Stará, Alžběta; Golovko, Oksana; Valentová, Olga; Bořík, Adam; Grabic, Roman; Kocour Kroupová, Hana (2018). "Two synthetic progestins and natural progesterone are responsible for most of the progestagenic activities in municipal wastewater treatment plant effluents in the Czech and Slovak republics". Water Research. 137: 64–71. doi:10.1016/j.watres.2018.02.065.
^Attardi, Barbara J.; Burgenson, Janet; Hild, Sheri A.; Reel, Jerry R. (2004). "In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone". The Journal of Steroid Biochemistry and Molecular Biology. 88 (3): 277–88. doi:10.1016/j.jsbmb.2003.12.004. PMID15120421.