部份中文帕唑帕尼处方资料（仅供参考）
英文名称：Pazopanib Hydrochloride
商品名称：Votrient
药品名称：盐酸帕唑帕尼
原研公司：GlaxoSmithKline
化学名称：5-[ [ 4-[ ( 2, 3-二甲基-2H-吲唑-6-基)甲氨基]-2-嘧啶基]氨基] -2-甲基-苯磺酰胺盐酸盐
结构式  
剂型规格
片剂：200mg、400mg
适应症：2009年10月19日，FDA批准用于晚期肾细胞癌患者；2012年4月26日，FDA批准用于既往接受化疗的晚期软组织肉瘤患者。
用法用量：800mg口服每天1次；不和食物一起服药(至少在进餐前1小时或后2小时)。
中度肝损伤：口服200mg每天1次。严重肝损伤患者不建议使用。
作用机制：可干扰顽固肿瘤存活和生长所需的新血管生成的新型口服血管生成抑制剂，靶向作用于血管内皮生长因子受体(VEGFR)，通过抑制对肿瘤供血的新血管生成而起作用。适用于晚期肾细胞癌（一种在肾小管中发现癌细胞的肾癌类型）、软组织肉瘤(STS)、上皮性卵巢癌和非小细胞肺癌(NSCLC)的治疗。
国内外上市情况
美国：片剂200mg（2009.10.19）、400mg*2；Novartis Pharms corp*1公司持有；商品名Votrient
欧盟：片剂200mg（2010.6.14）、400mg；Novartis Europharm Limited公司持有；商品名Votrient
日本：片剂200mg（2012.11）；ノバルティス ファーマ株式会社（日本诺华）公司持有；商品名ヴォトリエント錠（http://database.japic.or.jp/pdf/newPINS/00060782.pdf）
中国进口：片剂200mg（2017.2.21）、400mg；Novartis Pharma Schweiz AG公司持有的；商品名维全特
临床优势；
1、2011年NCCN肾癌治疗指南中，帕唑帕尼作为1类证据推荐用于复发或尤法切除的Ⅳ期肾癌(透明细胞为主型)的一线治疗。盐酸帕唑帕尼作为多靶点酪氨酸激酶抑制剂对包括肾癌在内的几种肿瘤均有活性,其毒性较小且药代动力学性质良好,具有很好的市场前景及利润空间。
2、Ⅰ期临床研究培唑帕尼总体耐受性良好，对多种肿瘤组织有抗肿瘤活性。
3、Ⅱ期研究体现了培唑帕尼良好的耐受性和持久的抗肿瘤活性。
4、Ⅲ期注册临床研究结果显示，与安慰剂组相比，培唑帕尼治疗组PFS得到显著提高。
5、COMPARZ研究——头对头比较证实，培唑帕尼与舒尼替尼疗效相似但安全性和生活质量更优。。
6、PISCES研究最终表明，从患者角度考虑，在疗效相当的前提下，一线使用培唑帕尼的耐受性和生活质量均优于舒尼替尼。
Votrient国内外情况。
*1、2015年3月诺华完成从葛兰素史克收购特定的肿瘤药品和研发产品线，其中包括Votrient。
*2、美国上市的400mg撤市。 。

Votrient (pazopanib)
Company: GlaxoSmithKline
Approval Status: Approved October of 2009
Treatment for: renal cell carcinoma
Areas: Urology & Kidneys; Cancer & Oncology
General Information
Votrient (pazopanib) is a vascular epidermal growth factor receptor(VEGFR) tyrosine kinase inhibitor which acts at all three isoforms:
VEGFR-1, VEGFR-2 and VEGFR-3. VEGF is a chemical signal produced by cells that stimulates the growth of new blood vessels. It is part of
the system that restores the oxygen supply to tissues when blood circulation is inadequate. When VEGF is overexpressed, it can contribute to disease. Solid cancers need an adequete blood supply or they will not be able to grow. Hence, cancer that can express VEGF are able to grow and metastasize.
Votrient is specifically indicated for the treatment of patients with advanced renal cell carcinoma.
Votrient is supplied as a tablet designed for oral administration.
The recommended initial dose is 800 mg orally once daily without food (at least 1 hour before or 2 hours after a meal). The dose of Votrient should not exceed 800 mg.
Clinical Results
FDA Approval
The FDA approval of Votrient was based on the results of a randomized, double-blind, placebo-controlled, multicenter study in 435 subjects with locally advanced and/or metastatic RCC who had received either no prior therapy or one prior cytokine-based systemic therapy. The subjects were randomized to receive Votrient800 mg once daily or placebo once daily. The primary objective progression-free survival (PFS); the secondary endpoints included overall survival (OS), overall response rate (RR), and duration of response. The median progression free survival for the overall population was 9.2 months in the Votrient arm versus 4.2 months in the placebo group (P<0.001). The median progression free survival for the treatment-naïve subgroup was 11.1 months versus 2.8 months and in the Cytokine pre-treated subgroup 7.4 months versus 4.2 months. In the Votrient arm, there was a 30% response rate (complete response + partial response) versus 3% in the placebo arm. The median duration of response was 58.7 weeks in the Votrient arm.
Side Effects
Adverse events associated with the use of Votrient may include, but are not limited to, the following:
Diarrhea
Hypertension
Hair color change
Nausea
Fatigue
Anorexia
Vomiting
Mechanism of Action
Votrient (pazopanib) is a vascular epidermal growth factor receptor (VEGFR) tyrosine kinase inhibitor which acts at all three isoforms:
VEGFR-1, VEGFR-2 and VEGFR-3. VEGF is a chemical signal produced by cells that stimulates the growth of new blood vessels. It is part of
the system that restores the oxygen supply to tissues when blood circulation is inadequate. When VEGF is overexpressed, it can contribute to disease. Solid cancers need an adequete blood supply or they will not be able to grow. Hence, cancer that can express VEGF are able to grow and metastasize.
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20123817243021.PDF