Ulipristal acetate
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| Trade names | Ellaone, Ella, Esmya |
| AHFS/Drugs.com | Multum Consumer Information |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | Nearly 100% |
| Protein binding | 96.7–99.5% |
| Metabolism | Likely CYP3A4 |
| Biological half-life | 32 hours |
| Excretion | ca. 90% with faeces |
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| Synonyms | CDB-2914 |
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| Formula | C30H37NO4 |
| Molar mass | 475.62 g/mol |
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Ulipristal acetate (trade name EllaOne in the European Union, Ella in the U.S. for contraception, and Esmya for uterine fibroid) is a selective progesterone receptor modulator (SPRM).
For emergency contraception a 30 mg tablet is used within 120 hours (5 days) after an 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. 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. This phenomenon 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.
Common side effects include nausea, abdominal pain, emesis, dysmenorrhea, pelvic pain, breast tenderness, headache, dizziness, mood swings, myalgia, and fatigue.
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