部分中文Esmya处方资料（仅供参考）

美国：华生制药公司启动Esmya®Ⅲ期临床试验
美国最新消息，华生制药公司近日宣布将启动Ⅲ期临床试验，以评估Esmya®治疗患有贫血的子宫肌瘤患者的疗效和安全性。

子宫肌瘤(uterine fibroids)多无症状，少数表现为阴道出血，腹部触及肿物以及压迫症状等。Esmya®是一种口服是一种选择性孕酮受体调节剂，而III期临床试验是一项多中心、随机、双盲等的对照研究，共招募300名18-50岁之间的子宫肌瘤患者，受试患者将随机接受日服一次10毫克Esmya®或安慰剂的治疗方案，试验将持续3个月月经周期，借以评估Esmya®的安全性、疗效性以及药动力学参数。

据悉，早于2010年12月华生制药宣布便与匈牙利的吉瑞大药厂公司达成独家许可协议，将共同负责Esmya®在美国和加拿大地区的研发与推广。根据协议，华生制药将支付给吉瑞大药厂1,700万美元的特许权使用费，从而获得Esmya®在美国和加拿大的销售权，此外华生还将支付一笔里程碑付款。

华生公司预计该项Ⅲ期临床试验将于2013财年第四季度结束，届时公司将向美国食品和药物管理局(U.S. Food and Drug Administration， 简称FDA)提交Esmya®的新药上市申请。而5毫克Esmya®片已于2010年2月份获得欧洲委员会的批准用于治疗中度至中度子宫肌瘤，该批准意味着Esmya®可在所有欧盟成员国内使用，Esmya®将在一个月内在欧洲部分国家上市，而欧洲地区对Esmya®的研究结果将刊登在近期的新英格兰医学杂志(New England Journal of Medicine)上。此外，基于欧洲方面的临床结果，华生制药将于2012年中期向加拿大卫生部提交Esmya®的新药申请。

沃特森开始III期Esmya用于贫血子宫肌瘤临床试验
沃特森医药公司开始Esmya（醋酸乌利司他）III期临床试验，评估其用于患有贫血的子宫肌瘤患者的药效和安全性。

Esmya是一种口服活性睾丸酮受体调节剂，能够定向阻断睾丸酮受体。

III阶段研究共招募300名18-50岁之间的子宫肌瘤患者，设置了多中心、随机、双盲等的对照，目的是评估其安全性和药效。

研究中患者将随机接受醋酸乌利司他和安慰剂的治疗，要在三个连续月经周期内每日服用一次。

沃特森全球运营副总裁Fred Wilkinson说：“美国的研究现在已经提上日程，我们希望这次III期研究真够看到手术前血红素浓度的改善，以及贫血症状的减缓。”

欧洲委员会先前已经批准5毫克Esmya片用于治疗中重度子宫纤维化。
公司计划于2013年4季度完成III期研究，届时将向美国食品药监局（FDA）提交新药申请。

Esmya: new pre-operative treatment option for uterine fibroids
Esmya (ulipristal acetate) has been launched for the pre-operative treatment of moderate to severe symptoms of uterine fibroids in women of reproductive age.
 
The active ingredient of Esmya, ulipristal acetate, is also licensed for use as an emergency contraceptive (EllaOne)

PHARMACOLOGY
Ulipristal acetate is an orally-active synthetic progesterone receptor modulator with a tissue-specific partial progesterone antagonist effect. It exerts a direct action on fibroids, reducing their size by inhibiting cell proliferation and inducing apoptosis.1

CLINICAL STUDIES
In the PEARL I study, women with symptomatic fibroids, excessive uterine bleeding and anaemia were randomised to receive daily treatment for up to 13 weeks with ulipristal acetate 5mg (n=96), 10mg (unlicensed dose; n=98) or placebo (n=48). All patients received oral iron supplementation.2

At 13 weeks, control of uterine bleeding was observed in 91% of women receiving the 5mg dose, 92% of those receiving the 10mg dose and 19% of those on placebo (p<0.001 for both doses vs placebo). Amenorrhoea was reported in 73%, 82% and 6% of women respectively, and occurred within 10 days in the majority of those who received ulipristal acetate. Fibroid volume decreased with ulipristal acetate 5mg and 10mg but increased slightly with placebo: median changes of -21%, -12% and +3%, respectively.2

In the non-inferiority PEARL II study, 307 women with symptomatic fibroids and excessive uterine bleeding were randomised to receive 3 months of daily therapy with ulipristal acetate (5mg or 10mg) or monthly intramuscular injections of leuprorelin (3.75mg).3

At 13 weeks, uterine bleeding was controlled in 90% of patients receiving 5mg ulipristal acetate, 98% of those receiving 10mg ulipristal acetate and in 89% of those receiving leuprorelin. Median times to amenorrhoea were 7 days with 5mg ulipristal acetate, 5 days with 10mg ulipristal acetate and 21 days with leuprorelin. Moderate to severe hot flushes were more common with leuprorelin than ulipristal acetate (p<0.001).3

Esmya：ulipristal
What is Esmya?
Esmya is a medicine that contains the active substance ulipristal acetate. It is available as tablets (5 mg).

What is Esmya used for?
Esmya is used before surgery to treat moderate to severe symptoms of uterine fibroids, which are noncancerous (benign) tumors of the womb (uterus). Esmya is used in adult women who have not yet reached menopause.

This medicine can only be obtained with a prescription.

How is Esmya used?
Esmya is taken by mouth and the recommended dose is one tablet daily. Treatment can last for up to three months and it should be started during the first week of the menstrual cycle (period bleeding).

How does Esmya work?
The active substance in Esmya, ulipristal acetate, is a ‘selective progesterone receptor modulator’. It acts by blocking the receptor of a hormone in the body called progesterone, which is involved in controlling the growth of the lining of the womb. In some women, progesterone may promote the growth of fibroids, which may cause symptoms such as heavy uterine bleeding (bleeding from the womb during or outside the menstrual period), anaemia (low red blood cell counts, due to bleeding) and abdominal pain (such as period pain or pain in the belly area). When progesterone activity is blocked, fibroid cells stop dividing and eventually die, which reduces the size of the fibroids and reduces the symptoms caused by them.

How has Esmya been studied?
The effects of Esmya were first tested in experimental models before being studied in humans.

Two main studies involving 549 women with symptomatic uterine fibroids were carried out with Esmya. In both studies the treatment lasted for three months.

One study investigated the effects of Esmya compared with placebo (a dummy treatment) in adult women with heavy uterine bleeding and anaemia who were to undergo surgery to remove the fibroids. Iron supplements were also given to all the patients to help treat anaemia. The main measures of effectiveness were reductions in heavy bleeding and associated anaemia, as well as the size of the fibroids.

The second main study investigated the effects of Esmya in comparison with another medicine used to treat fibroids, leuprorelin. The main measure of effectiveness was the ability of the treatment to reduce heavy uterine bleeding.

What benefit has Esmya shown during the studies?
Esmya was shown to improve the symptoms of women with uterine fibroids.

In the first study, 91.5% of women taking Esmya had reduced menstrual bleeding compared with 18.8% of women taking placebo. The size of the fibroids was also smaller in women treated with Esmya than in those who received the placebo.

In the second study, Esmya was as effective as leuprorelin in reducing heavy uterine bleeding, as 90.3% of women treated with Esmya had reduced bleeding compared with 89.1% of women treated with leuprorelin.

What is the risk associated with Esmya?
The most common side effects with Esmya (seen in more than 1 in 10 patients) are amenorrhea (absence of menstrual period), endometrial thickening (thickening of the lining of the womb) and hot flush. For the full list of all side effects reported with Esmya, see the package leaflet.

Esmya must not be used in women who are hypersensitive (allergic) to ulipristal acetate or any of the other ingredients. It must not be used in women who are pregnant or breastfeeding, have bleeding from the genital region of unknown cause or for reasons other than uterine fibroids, or have cancer of the womb, cervix (the neck of the womb), ovary or breast. Treatment with Esmya should not be longer than three months. See the package leaflet for full details.

Why has Esmya been approved?
The CHMP concluded that Esmya was shown to be effective in reducing bleeding and anaemia as well as the size of the fibroids. There were no major safety concerns. Although endometrial thickening was seen in some patients, it normally disappears after treatment. Therefore, the CHMP concluded that the benefits of Esmya outweigh its risks and recommended that it be granted marketing authorisation. The Committee restricted treatment to three months due to the lack of longer-term data.

What measures are being taken to ensure the safe use of Esmya?
The company that markets Esmya will ensure that doctors who are expected to prescribe this medicine receive educational material containing important safety information about Esmya, including recommendations for monitoring and managing endometrial changes that occur with Esmya treatment.

Other information about Esmya
The European Commission granted a marketing authorisation valid throughout the European Union for Esmya on 23 February 2012.

For more information about treatment with Esmya, read the package leaflet (also part of the EPAR) or contact your doctor or pharmacist.

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原产地英文商品名:
ESMYA 5MG/TAB 28TABS/BOX
原产地英文药品名:
ULIPRISTAL ACETATE
中文参考商品译名:
ESMYA 5毫克/片 28片/盒
中文参考药品译名:
醋酸乌利司他
生产厂家中文参考译名:
Preglem
生产厂家英文名:
Preglem