英文药名: Sutent(Sunitinib Malate Capsules)

中文药名: 苹果酸舒尼替尼胶囊

品牌药生产厂家: Pfizer

药品介绍
Sutent Description
This medication is used to treat certain types of cancer (kidney and intestinal). Sunitinib works by stopping or slowing the growth of cancer tumors. It also works by slowing the growth of new blood vessels within the tumor.

Sutent Directions
Read the Medication Guide provided by your pharmacist before you start taking sunitinib and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
Take this medication by mouth with or without food, usually once daily for 4 weeks followed by 2 weeks off, or as directed by your doctor.
The dosage is based on your medical condition and response to therapy.
Do not increase your dose or take this medication more often without your doctor's approval. Your condition will not improve any faster, and the risk of serious side effects may be increased.
Use this medication regularly in order to get the most benefit from it. To help you remember, take it at the same time each day.
Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor instructs you otherwise. Grapefruit can increase the amount of certain medications in your bloodstream. Consult your doctor or pharmacist for more details.

Sutent Cautions
ave any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: bleeding problems, heart problems (e.g., congestive heart failure), high blood pressure, liver problems, thyroid disease.
Sunitinib may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can infrequently result in serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that require immediate medical attention. The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may affect the heart rhythm (see also Drug Interactions section). Before using sunitinib, tell your doctor or pharmacist if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).
Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using sunitinib safely.
Do not have immunizations/vaccinations without the consent of your doctor, and avoid contact with people who have recently received oral polio vaccine or flu vaccine inhaled through the nose.
To lower the chance of getting cut, bruised or injured, use caution with sharp objects like safety razors or nail cutters and avoid activities such as contact sports.
If you need to have surgery, tell your doctor or dentist that you are using this medication.
Wash your hands well to prevent the spread of infections.
This drug is not recommended for use during pregnancy. It may harm an unborn baby. If you become pregnant or think you may be pregnant, inform your doctor immediately. To avoid pregnancy, both males and females using the drug must use reliable form(s) of birth control during treatment.
It is not known whether this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

Sutent Side Effects
Upset stomach, nausea, vomiting, diarrhea, change in taste, dry/cracked/thickened skin, watering eyes, swelling around eyes, numbness/tingling of arms/legs, or tiredness may occur. In some cases, drug therapy may be necessary to prevent or relieve nausea/vomiting/diarrhea. Eating several small meals or limiting activity may help lessen some of these effects. If these effects persist or worsen, notify your doctor or pharmacist promptly.
This medication may cause patchy or complete hair loss and changes in hair/skin color. These effects are not harmful.
Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Tell your doctor immediately if any of these unlikely but serious side effects occur: headache, rash/blisters on palms of hands/soles of feet, sores/pain on the tongue/mouth, easy bruising/bleeding, swelling ankles/feet, shortness of breath, seizures, unusual weight gain, cold intolerance, pain/redness/swelling of arms or legs, unusual tiredness, black/bloody stools, vomit that looks like coffee grounds.
Seek immediate medical attention if any of these rare but very serious side effects occur: trouble breathing, severe dizziness, fainting, fast/slow/irregular heartbeat.
This medication can lower the body's ability to fight an infection. Notify your doctor promptly if you develop any signs of an infection such as fever, chills or persistent sore throat.
A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Sutent Active Ingredients

SUTENT®（苹果酸舒尼替尼）胶囊
美国首次批准：2006
 
适应症及用法
索坦是一种激酶抑制剂用于治疗表示：

胃肠道间质瘤后疾病进展或不能耐受甲磺酸伊马替尼。
晚期肾细胞癌。
 
【用法用量】
口服50毫克，每日一次，或没有食物，疗程4周，2周的时间。
为12.5毫克的剂量调整建议根据个人的安全性和耐受性。
 
剂型和优势
胶囊：12.5毫克，25毫克，50毫克

禁忌
无

警告和注意事项
有生育能力的妇女应被告知对胎儿的潜在危险，以避免怀孕。

左心室射血分数下降到低于下限正常时有发生。监测患者的充血性心脏衰竭的症状和体征。
已经观察到QT间期延长和尖端扭转型室性心动过速。发展QT间期延长的风险较高的患者慎用。当使用SUTENT，监测对治疗心电图和电解质应予以考虑。
高血压可能发生。监测血压和治疗需要。
包括肿瘤相关的出血的出血事件时有发生。执行串行完整的血球计数和体检。
甲状腺功能障碍可能发生。患者的症状和/或甲状腺功能低下或甲状腺功能亢进症的症状应该有实验室监测甲状腺功能，被视为每标准的医疗实践。
在动物实验中观察到肾上腺出血。在压力的情况下，如手术，外伤或严重感染监测肾上腺皮质功能。
 
不良反应
最常见的不良反应（≥20％）是疲劳，乏力，腹泻，恶心，粘膜炎/口腔炎，呕吐，消化不良，腹痛，便秘，高血压，皮疹，手足综合征，皮肤变色，味觉改变，厌食，和出血。

报告疑似不良反应，联系辉瑞公司在1-800-438-1985或FDA在1-800-FDA-1088或www.fda.gov / medwatch

药物相互作用
CYP3A4抑制剂：强CYP3A4抑制剂考虑减少剂量给药时，SUTENT。
CYP3A4诱导剂：考虑增加剂量给药时，SUTENT与CYP3A4诱导剂。

日期：02/2010

Sunitinib苹果酸盐是一种可以抑制多种参与肿瘤生长，血管增生以及肿瘤转移的受体酪氨酸激酶（RTKs）的小分子。Sunitinib对血小板源生长因子受体（PDGFRα和PDGFRβ）、血管内皮细胞生长因子（vEGFR1，VEGFR2和ⅦGF ；）、干细胞因子受体（KIT）、FMS样酪氨酸激酶3（n ）、集落刺激因子受体1（CSF-1R）和胶质细胞源性神经营养因子受体（RET）等活性均具有抑制作用，且其主要代谢产物的抑制效果与原药相当。Sunitinib可以抑制多种受体酪氨酸激酶（PDGFR1，VEGFR2和K1T）的磷酸化，证明其在一些癌症实验模型中可抑制肿瘤的生长和抑制癌细胞转移。体外研究表明，sunitinib可抑制受体酪氨酸激酶（PDGFR，RET，或KIT）表达异常的肿瘤细胞的生长；体内实验表明，sunitinib对PDGFRβ一和VEGFR2一依赖性肿瘤血管增生具有抑制作用。

「临床研究」

对312例癌细胞已发生转移或对甲磺酸伊马替尼耐受胃肠道间质瘤患者的研究中，在肿瘤进展时间（TTP）和无进展生存期（PFS）方面stmitinib显著优于安慰剂，其中stmitinib组TTP为27.3周，安慰剂组TTP为6.4周；sunitinib组PFS为24.1周，安慰剂组PFS为6.0周。说明stmitinib能延缓胃肠道间质瘤的生长速度。对750例转移性肾细胞癌的临床试验显示，Stmitinib更能有效阻止疾病进展，并能缩小肾细胞肿瘤的尺寸，治疗效果优于干扰素（免疫疗法）。Sunitinib组患者中位PFS达到11个月，而a一干扰素治疗组的中位PFS只有5个月；Stmitinib的客观缓解率（ORR）是 干扰素的5倍（28％ ：5％）。Sunitinib的总体耐受性好，中断治疗率低于 干扰素。另外，对其他工期和Ⅱ期临床试验中使用过stmitinib的患者随访数据显示，患者的总生存时间已延长至20个月，大大超过预期时间。

「临床评价」

Ⅲ期临床试验证实，舒尼替尼能够大大延长已对伊马替尼治疗耐药或不能耐受的胃肠道基质肿瘤患者的肿瘤进展时间（分别为6.3个月对安慰剂组的1.5个月），并显著性降低他们50%的死亡风险。舒尼替尼也已在用于治疗转移性乳腺癌和神经内分泌肿瘤等的Ⅱ期临床试验中显现出令人鼓舞的结果。舒尼替尼现正在进行单用或合用其他抗肿瘤药物用于治疗许多其他类型实体瘤，包括乳腺癌、肺癌、前列腺癌和结肠直肠癌等的大量研究。