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• Description

  Ulipristal acetate (UPA) is a selective progesterone receptor modulator. Attributing to its higher efficacy and a similar rate of side effects compared to levonorgestrel emergency contraception, it is now recommended as first line treatment for emergency contraception. Emergency contraception is defined as the use of drug or device after unprotected or under-protected intercourse to prevent an unwanted pregnancy. Ulipristal acetate can be used up to 5 days (120 h) after unprotected sexual intercourse.
  As progesterone promotes the growth of uterine fibroids, the blocking characteristic of ulipristal acetate can thereby be used to reduce the size of uterine fibroids. Ulipristal acetate has also shown efficacy with a significant reduction in uterine bleeding caused by uterine fibroids. The treatment of fibroids by ulipristal acetate should begin in the first week of a menstrual period.
  Drugs or herbal products that induce enzymes, including CYP3A4, such as carbamazepine, phenytoin, rifampin, St. John's Wort, etc., may decrease the plasma concentrations of ulipristal acetate, and may decrease its effectiveness while CYP3A4 inhibitors such as itraconazole, ketoconazole, etc., may increase plasma concentrations of ulipristal acetate.
  The half-life after oral intake is 32 h; it binds to plasma proteins for 97–99%, and it is metabolized by the citochrome P450. ;

• Oral emergency contraception

  Ulinastal acetate is a new oral contraceptive pill, and it is the active chemical composition of Ella, a new generation of emergency contraceptive wildly on the market in United States currently. It can protect women within 120 hours after intercourse without medication, and the emergency contraceptive efficacy will not decline with the delay of treatment time. At the same time, it is safe and durable. Compared with the most commonly used emergency contraceptive levonorgestrel, Ulinastal acetate is more suitable for clinical use, and has the potential to prevent more unwanted pregnancies.
  Ulipristal acetate was developed by HRA Pharmaceuticals, Inc., and was marketed by the Food and Drug Administration (FDA) in August 2010 under the trade name Ella. It could be used for the protection of unprotected sex or for the pregnancy prevention in the known or suspected contraceptive failure situation within 120h. Ulipristal acetate is a selective progesterone receptor modulator; and mainly it can take effect by inhibiting the ovulation and plays an emergency contraceptive effect. The study found that Ulastatal acetate was more effective than levonorgestrel in suppressing vomiting after dosing before the estimated ovulation day. And it consequently suggests that Ulatastatin acetate might have a stronger emergency contraceptive effectiveness.
  
  Figure 1 for the structure of ulcaritin acetate;

• Pharmacological action

  Ulinastal acetate is a progesterone agonist/antagonist that inhibits or delays the ovulation; however, changes in the endometrium may also be a cause of efficacy.
  Ulinastal acetate belongs to the category of selective progesterone receptor modulator, and it has partial agonistic action to progesterone receptor antagonism and partial agonism. It binds to progesterone receptors in the human body and prevents progesterone receptor binding. The efficacy of Ulinastal acetate depends on the time of administration in the menstrual cycle. Administration during the mid-follicular hyperplasia would suppress follicle formation and decrease the estradiol concentrations. And the administration during the in the peak period of follicular hyperplasia can delay the breakdown of follicles from 5 to 9 days. Although early luteal phase of administration cannot significantly delay the endometrial maturation, it can reduce the thickness of the endometrium within 0.6±2.2mm（average value ±SD）.;

• Pharmacokinetics

  Absorption: The highest fasting plasma concentrations of 20 women reached 176 ng/ mL and 69ng/ mL after 0.9 and 1 hour of using ulipristal acetate and active metabolite (mono-demethyl-ulipristal acetate) in single bolus medication.  And mono palmitoyl-ulipristal acetate was lower by 40% to 45% compared with the high-fat breakfast. And ompared with the fasting state, and the delayed tmax (delayed from median 0.75 h to 3 h) with an average AUC0-∞ of 20% to 25% higher. These differences are not expected to impair the efficacy or safety of Ulinastal acetate. Therefore, Ulatastatin acetate can take effect in both situation: with or without food.
  Distribution: This product has a high binding rate (> 94%) with plasma protein, high-density lipoprotein, α-1-acid glycoprotein and albumin.
  Metabolism: Ulipristal acetate could be metabolized to mono-desmethyl and bis-nor-metabolites. In vitro data indicates that single demethyl metabolites are pharmacologically active, mainly due to CYP3A4 mediated.
  Excretion: The terminal half-life of ulipristal acetate in plasma after a single dose of Ulistatta 30 mg would be estimated to (32.4 ± 6.3) hours.
  The pharmacological effects, pharmacokinetics, market prospect and patent intellectual property rights of oral emergency contraceptive Ulinastal acetate were edited by Xiao Nan from Chemical book.;

• market prospect

  Emergency contraception, also known as after-birth control pills, is a kind of contraceptive for women of childbearing age in the situation od non-protective intercourse or contraceptive failure after the use of contraception to prevent accidental pregnancy.
  At present, the most widely used emergency contraceptive is levonorgestrel (1evonorgestre1), which is used at intervals of 12hours each serving one piece (0.75mg) or a single taking of two pieces(1.5mg). However, levonorgestrel was only approved for using as an emergency contraceptive only 72 hours (3days) after unprotected intercourse or contraceptive failure. Even though, the efficacy of levonorgestrel emergency contraception will be significantly reduced with the delay of treatment time; it is recommended that it should better used in unprotected intercourse or contraceptive failure within 12h after the start of medication.
  In May 2009, the European Union approved a new emergency contraceptive ulipristal acetate, also called as Ella One, which is not only allowed to be taken within 120 hours (5 days) of unprotected intercourse or contraceptive failure, but the  emergency contraceptive efficacy would not delay and decline with the medication time.
  Ulastat is one of the first oral contraceptives approved worldwide to be administered within 120 hours of unprotected intercourse or contraceptive failure, which has the potential to prevent more unwanted pregnancies than levonorgestrel. As a new oral emergency contraceptive, Ulinastal acetate can not only be used within 120 hours after unprotected intercourse, but the efficacy of emergency contraception would not decrease with the delay of administration, and it is safe and durable as well. Compared with the most commonly used emergency contraceptive levonorgestrel, Ulinastal acetate is more suitable for clinical use, and it has the potential to prevent more unwanted pregnancies.;

• intellectual property rights

  The original research manufacturer in China has already applied for a patent for Ulinastal acetate tablets and its indications as well as for its indications. However, it has not been authorized yet. There are not any intellectual property barriers.;

• Other clinical researches

  February 2, 2012, The New England Journal of Medicine published two clinical trials found that Ulinastal acetate has an excellent effect in the treatment of uterine fibroids. The results show that Ulinastal acetate is as effective as leuprolide in controlling uterine fibroid bleeding, reducing the volume of myoma and comforting the pain;
  According to statistics, about a quarter of women have suffered from uterine fibroids symptoms. Leuprolide acetate, a gonadotropin-releasing hormone (GnRH) agonist, has been approved for preoperative treatment of uterine fibroids since its approval in 1995. Ulinastal acetate can successfully challenge leuprolide and it becomes become a new choice for preoperative uterine fibroids drug therapy. Let’s wait for the post-trial to reveal the answer.;

• References

  [1] Shilpa P. Jadav, Dinesh M. Parmar (2012) Ulipristal acetate, a progesterone receptor modulator for emergency contraception, J Pharmacol Pharmacother, 3, 109-111
  [2] Ulipristal acetate for fibroids, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5155051/
  [3] Elena Rosato, Manuela Farris, Carbo Bastianeli (2015) Mechanism of Action of Ulipristal Acetate for Emergency Contraception: A Systematic Review, Front Pharmacol, 6, 315
  [4] https://www.glowm.com/Critical_current_issue/page/5 ;

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