英文药名：LEUPLIN PRO FOR INJECTION KIT（Leuprorelin Acetate）

中文药名：醋酸亮丙瑞林注射用试剂盒

生产厂家：武田化学工业

リュープリンPRO注射用キット22.5mg

治疗类别名称
LH-RH注1）衍生物
注1）LH-RH：促黄体激素释放激素
微胶囊型缓释性制剂
商標名
LEUPLIN PRO FOR INJECTION KIT 22.5mg
化学構造式

一般名
リュープロレリン酢酸塩（Leuprorelin Acetate）〔JAN〕
化学名
5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide monoacetate
分子式
C59H84N16O12・C2H4O2
分子量
1269.45
性状
醋酸亮丙瑞林是白色至淡黄色粉末。非常易溶于水或乙酸（100），可溶于甲醇，微溶于乙醇（99.5）。它是吸湿性的。
条件批准
在建立药品风险管理计划的顶部，要正确使用。
药效药理
1. 作用机序
醋酸亮丙瑞林的重复给药是LH-RH或高剂量的高活性的LH-RH衍生物，首次剂量瞬时垂体后立即 - 观察性腺系统刺激作用（急性效应）后，下在垂体降低生产和促性腺激素释放。此外，它降低了反应性睾丸和促性腺激素卵巢，降低睾酮，雌二醇产生能力（慢性效应）。
磷酸盐的亮丙瑞林的LH释放活性为约100倍，LH-RH，垂体 - 性腺功能的抑制效果比LH-RH更强。柳是醋酸亮丙瑞林是高活性的LH-RH衍生物，垂体 - 强原因性腺功能抑制作用，醋酸亮丙瑞林，它是对蛋白水解酶的​​高电阻与LH-RH相比例如通过对LH-RH受体的高亲和性。另外，由于这种药物是持续释放制剂，它导致有效地降低了睾丸和卵巢释放醋酸亮丙瑞林在血液中的所有时间的反应性，垂体 - 显示性腺功能抑制作用。
2. 性激素浓度的抑制作用
(1) 血清睾酮浓度是由一个单一皮下给药下面可持续去势水平降低至24周的患者的前列腺癌，它是观察药物去势动作。
(2) 血清雌二醇浓度在乳腺癌患者绝经前通过一次在24周皮下施用通常低于绝经水平，识别的卵巢功能抑制动作，通常是排卵被抑制，月经停止。
适应病症
前列腺癌，绝经前乳腺癌
用法用量
以原处方为准
包装规格
22.5mg*1套件
制造厂商
武田化学工业有限公司
完整资料附件：http://www.info.pmda.go.jp/go/pack/2499407G4029_1_03/
Takeda's "Leuplin® PRO for Injection Kit 22.5 mg" Now Available for the Treatment of Prostate Cancer/Premenopausal Breast Cancer in Japan
Osaka, Japan, December 15, 2015—Takeda Pharmaceutical Company Limited ("Takeda") today announced that “Leuplin® PRO for Injection Kit 22.5 mg” (hereafter 24-week depot formulation), the 24-week depot formulation of “Leuplin®” (generic name: leuprorelin acetate; hereafter “Leuplin”), is now available in Japan for the treatment of prostate cancer and premenopausal breast cancer.
Leuplin is an LH-RH agonist that consistently stimulates the pituitary gland, resulting in suppressed production of male/female hormone. Leuplin is used as a treatment for hormone-dependent diseases such as prostate cancer and premenopausal breast cancer, and it is currently available in the United States, Europe, and Asia. The 24-week depot formulation becomes available for the first time in the world for the treatment of premenopausal breast cancer.
The 24-week depot formulation can maintain stable blood concentration by sustained release using Takeda's unique microcapsule formulation technology through 24 weeks with a single injection. The new formulation providing sustained efficacy over a 24-week period will be a valuable addition to the available dosing options and provides the added benefit of less frequent dosing thus helping reduce the burden of treatment for patients with prostate cancer and premenopausal breast cancer.
“Given the high unmet needs that remain among patients with prostate cancer and premenopausal breast cancer, we have continued the Research and Development with our drug delivery for Leuplin even after its launch in Japan in 1992,” said Masato Iwasaki, Ph.D., Director and President, Japan Pharma Business Unit of Takeda. “We are confident that the new 24-week depot formulation will help ease the various burden of treatment for patients with prostate cancer and premenopausal breast cancer”.
Overview of the 24-week depot formulation

Brand name	Leuplin® PRO for Injection Kit 22.5 mg
Generic name	Leuprorelin acetate
Indications	Prostate cancer Premenopausal breast cancer
Dosage and administration	Usually, for adults, 22.5 mg of Leuprorelin Acetate is subcutaneously administered once every 24 weeks. When using Leuplin® PRO, it should be used after suspending it completely by transferring the whole quantity of the vehicle into the powder part, by pressing the plunger rod, with the injection needle held upward, with caution against foaming.