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英文药名：IBRANCE Capsules(palbociclib)
中文药名：帕博西尼胶囊
生产厂家：辉瑞制药
イブランスカプセル25mg／イブランスカプセル125mg
药物分类名称
抗肿瘤剂（CDK 4/6抑制剂）
批准日期：2017年12月
商標名
IBRANCE Capsules
一般名
パルボシクリブ（Palbociclib）
化学名
6-Acetyl-8-cyclopentyl-5-methyl-2-｛［5-（piperazin-1-yl）pyridin-2-yl］amino｝pyrido［2,3-d］pyrimidin-7（8H）-one
分子式
C24H29N7O2
分子量
447.53
構造式
性状
Parvociclib是一种黄色到橙色的粉末。 难溶于N，N-二甲基乙酰胺，在乙醇（99.5）和甲醇中极难溶解，难溶于水。
分配系数（log D）
0.99（pH 7.4,1-辛醇/水）
审批条件
制定药品风险管理计划并适当执行
药效药理
1.抗肿瘤作用
Parvociclib抑制来源于人乳腺癌的T47D和MCF7细胞系的增殖。 此外，在用人乳腺癌衍生的ZR-75-1细胞系皮下移植的严重联合免疫缺陷小鼠中，肿瘤生长受到抑制。
2. 作用机序
Parvociclib是对细胞周期蛋白依赖性激酶（CDK）4和6具有抑制活性的低分子量化合物。 据认为，parvociclib抑制CDK4 / 6和细胞周期蛋白D复合物的活性，通过抑制成视网膜细胞瘤（Rb）蛋白质的磷酸化来阻止细胞周期进程，并抑制肿瘤生长。
适应症
不可手术或复发性乳腺癌
用法与用量
与内分泌治疗相结合，通常125mg一天一次口服给成年人作为parvociclib连续3周饭后，随后撤回1周。 用这个循环重复管理。 另外，根据患者的状况来减轻体重。
临床结果
1. HR阳性和HER2阴性，联合国际III期试验20用于不能手术或复发的绝经后的乳腺癌患者对晚期乳腺癌无内分泌治疗史）
HR-阳性和HER2阴性，不能手术的或复发的绝经后乳腺癌666箱子没有内分泌治疗史（包括46案件日语）对称地相对于晚期乳腺癌，这种药物+来曲唑组合投与安慰剂+一项随机，双盲，平行的组间，国际联合III期临床试验研究来曲唑联合用药的有效性。在该药物中，连续口服给药125mg作为起始剂量，每天一次，持续3周，1周后，连续给药2.5mg来曲唑。
中位无进展存活为主要终点，在药物+来曲唑24.8个月，在安慰剂+来曲唑14.5个月，风险比0.576（95％置信区间：0.463,0.718;一个层另一个对数秩检验p <0.000001）延长了该药物+来曲唑组的统计学显着的无进展存活。
2.国际肝素III期试验，HR阳性和HER2阴性，靶向不可手术或复发的乳腺癌患者耐受内分泌治疗。
甲HR-阳性和HER2阴性，（绝经状态是否）不可操作或复发性乳腺癌的内分泌疗法抗性521箱子定位（包括35案件日本），并且该药物+氟维司群联合给药一项随机，双盲，平行的小组间，国际联合III期试验研究安慰剂+氟维司群组合给药的有效性。这种药物，125毫克1，每天一次，连续3周口服给药冲洗作为起始剂量后一周，氟维司群被首先施用至500mg，2周后，4周，以后每四周后。戈舍瑞林与绝经前和围绝经期患者同时使用。
在时间的中期分析点的无进展生存的显著延长（2014年12月5日截止）是观察到的初级端点，满足停止标准，如预先定义，该测试生效停产。中位无进展生存期，9.2个月药物+氟维司群组中，与安慰剂+氟维司群组中3.8个月，风险比0.422（95％置信区间：0.318,0.560;一个分层数秩在p <0.000001的情况下），在该药+氟维司群组中观察到统计学显着的无进展存活。
包装规格
胶囊
25毫克：50粒（10粒×5 PTP）
125毫克：21粒（7粒×3 PTP）
制造和销售（进口）
辉瑞公司
提示：以上中文处方资料不够完整，使用者以原处方资金料为准。
完整说明书附件：http://www.info.pmda.go.jp/go/pack/4291051M1021_1_02/
New breast cancer drug "Iburance® capsule 25mg/125 mg" is on sale
~ CDK 4/6 inhibitor approved for the first time in Japan, breast cancer therapy in Japan is a new beginning ~
Pfizer Inc. (Headquarters: Shibuya-ku, Tokyo; President: Akihisa Harada) on December 15, 2017 (Friday), on December 15, 2017, indicated the efficacy and effect of "inoperable or recurrent breast cancer" We launched tumor agent (CDK 4/6 inhibitor) "Iburance ® capsule 25 mg/125 mg" (common name: parvociclib, hereinafter "Iburance").
The 5-year survival rate of advanced and recurrent breast cancer is as low as about 30%, and development of new therapeutic drugs is a long-awaited disease. Ibbance is a drug with a novel mechanism of action to selectively inhibit the activity of cyclin dependent kinases 4 and 6 (hereinafter CDK 4/6) and cyclin D complex. In addition to directly inhibiting CDK4/6, indirect inhibition of CDK4/6 through suppression of the expression of cyclin D which is a downstream substance of the estrogen receptor is also added, when used in combination with an endocrine therapy agent, It is expected to increase the effect.
In clinical trials, high efficacy and tolerability to HR * positive and HER 2 ** negative negative patients with advanced or recurrent breast cancer are recognized, and the progression free survival time is approximately twice as long as the standard treatment Was shown.
Iburance is the world's first CDK 4/6 inhibitor approved by the US Food and Drug Administration (FDA), approved in more than 70 countries around the world including the United States, and it is used for more than 70,000 patients. As a new treatment option for advanced and recurrent breast cancer, it is hoped that this drug will become a hope for patients in Japan and their families.
* Hormone receptor
* Human epidermal growth factor receptor
Outline of Iburance®
Product name Iburance® capsule 25 mg/125 mg
Common name Parbo Ciclib
Efficacy/efficacy Inoperable or recurrent breast cancer
Usage notes related to indication/effect
1. The efficacy and safety as adjunctive therapy of this drug surgery has not been established.
2. When administering this drug, patients with hormone receptor positive and HER2 negative should be targeted.
When used in combination with a dosage/dose endocrine therapy, usually 125 mg once a day for adults is administered orally for three consecutive weeks after meals, followed by withdrawal for one week.
Repeat administration with this as one cycle. Incidentally, weight reduction is made according to the condition of the patient.
Manufacturing marketing approval acquisition date September 27, 2017
Drug Price List Date 22 November 2017
Release date December 15, 2017
Manufacturer Distributor Pfizer Inc.
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