简介:
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。
Indication
VOTRIENT is a prescription medicine used to treat people with advanced renal cell cancer (RCC).
It is not known if VOTRIENT is safe and effective in children under 18 years of age.
Important Safety Information
Before taking VOTRIENT, tell your healthcare provider if you have or had liver problems. Some people may develop liver damage while taking VOTRIENT. VOTRIENT can cause serious liver problems including death. Your healthcare provider will do blood tests to check your liver before you start and while you take VOTRIENT. Tell your healthcare provider right away if you have yellow eyes or skin, dark urine, tiredness, nausea or vomiting, loss of appetite, pain in the right upper side of your stomach area, or if you bruise easily. Your healthcare provider may need to prescribe a lower dose of VOTRIENT for you or tell you to stop taking VOTRIENT if you develop liver problems during treatment.
•VOTRIENT may cause irregular or fast heartbeat or fainting.
•VOTRIENT may cause heart failure; a condition where your heart does not pump as well as it should and may result in shortness of breath.
•Heart attack and stroke can happen with VOTRIENT and may cause death. Tell your healthcare provider if you have heart problems. Call your healthcare provider right away if you have chest pain or pressure, pain in your arms, back, neck or jaw, shortness of breath, numbness or weakness on one side of your body, trouble talking, headache, or dizziness.
•VOTRIENT may cause blood clots, which may form in a vein, especially in your legs. Pieces of a blood clot may travel to your lungs. This may be life-threatening and cause death. Call your healthcare provider right away if you have new chest pain, trouble breathing or sudden shortness of breath, leg pain, and swelling of the arms and hands, or legs and feet, a cool or pale arm or leg.
•Thrombotic microangiopathy (TMA) including thrombotic thrombocytopenia purpura (TTP) and hemolytic uremic syndrome (HUS) is a condition involving blood clots that can happen while taking VOTRIENT. TMA is accompanied by a decrease in red blood cells and cells that are involved in clotting. TMA may harm organs such as the brain and kidneys.
•VOTRIENT may cause bleeding problems, which may be severe and cause death. Tell your healthcare provider before taking VOTRIENT if you have a history of abnormal bleeding. If you experience unusual bleeding, bruising, or wounds that do not heal, call your healthcare provider right away.
•VOTRIENT may cause a tear (called a perforation) in the stomach or intestinal wall. Fatal perforations have occurred. VOTRIENT may also cause an abnormal connection between two parts of your gastrointestinal system (called a fistula). Call your healthcare provider if you experience pain or swelling in the stomach area, vomiting blood, or black sticky stools.
•Reversible Posterior Leukoencephalopathy Syndrome (RPLS) is a condition that can happen while taking VOTRIENT that may cause death. Symptoms may include headaches, seizures, lack of energy, confusion, high blood pressure, loss of speech, blindness or changes in vision, and problems thinking.
•High blood pressure can happen with VOTRIENT, including a sudden and severe rise in blood pressure which may be life-threatening. These blood pressure increases usually happen in the first several months of treatment. Blood pressure should be well controlled before starting VOTRIENT. Your healthcare provider should test your blood pressure within 1 week of starting treatment with VOTRIENT and should check it often during treatment. Get medical help right away if you have symptoms of a severe increase in blood pressure, such as severe chest pain, severe headache, blurred vision, confusion, nausea and vomiting, severe anxiety, shortness of breath, or seizures, or if you pass out (become unconscious).
•VOTRIENT may cause thyroid problems. Your healthcare provider should test your thyroid function during treatment with VOTRIENT.
•VOTRIENT may affect wound healing. Tell your doctor if you had recent surgery (within the last 7 days) or are going to have surgery.
•VOTRIENT may cause you to have too much protein in your urine. Your healthcare provider will check you for this problem. If there is too much protein in your urine, your healthcare provider may tell you to stop taking VOTRIENT.
•Serious infections can happen with VOTRIENT and can cause death. Call your healthcare provider if you experience fever; cold symptoms, such as runny nose or a sore throat that does not go away; flu symptoms, such as cough, feeling tired, and body aches; pain when urinating; or cuts, scrapes, or wounds that are red, warm, swollen, or painful.
•When used in combination with some other anti-cancer therapies, VOTRIENT has caused increased toxicity and even death. Tell your healthcare provider about all of the medicines you are taking, including other anti-cancer therapies.
•VOTRIENT may harm an unborn baby (cause birth defects). Do not become pregnant while taking VOTRIENT. If you do become pregnant, tell your healthcare provider right away.
•A collapsed lung can happen with VOTRIENT (called pneumothorax). This may cause shortness of breath. Call your healthcare provider right away if you experience shortness of breath.
The most common side effects in people with advanced renal cell carcinoma who take VOTRIENT include:
◦diarrheaDiarrheaFrequent and watery bowel movements.
◦high blood pressure
◦hair color changes
◦nausea (feeling sick to your stomach) or vomiting
◦loss of appetite
Tell your healthcare provider right away if you have any side effects.
VOTRIENT may affect the way other medicines work and other medicines may affect how VOTRIENT works. Tell your healthcare provider about all the medicines you take, including prescription and nonprescription medicines and herbal and dietary supplements.
Do not eat grapefruit or drink grapefruit juice during treatment with VOTRIENT because it may affect how VOTRIENT works.
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