2010年6月17日，诺华公司与美国食品药品管理局(FDA)宣布，Tasigna (尼罗替尼)已获准扩大治疗指征。新批准令允许该药用于治疗新诊断的费城染色体阳性的慢性期慢性髓系白血病(Ph+ CP-CML)。

FDA最初于2007年10月批准Tasigna用于治疗病情已进展或无法耐受其他治疗(其中包括伊马替尼)的成人Ph+ CP-CML患者。Tasigna是Bcr-Abl蛋白的强效选择性抑制剂，而Bcr-Abl蛋白是导致Ph+ CP-CML患者癌细胞生成的罪魁祸首。该药也是与格列卫耐药相关的Bcr-Abl突变的广谱抑制剂。

Tasigna对这项扩大的治疗指征有效，此结果来自经证实的血液学和未经证实的细胞遗传学反应率。研究数据已发表于6月17日出版的《新英格兰医学杂志》(摘要)。目前尚无对照试验证实该药有改善疾病相关症状或提高生存率等临床收益。

最常见的与应用Tasigna相关的3或4级不良事件主要是血液学改变，其中包括中性粒细胞减少。所观察到的胆红素水平、肝功能试验、脂肪酶、血糖升高大多为暂时性的，随着时间的推移可恢复。最常见的非血液学药物相关的不良事件为皮疹、瘙痒、恶心、疲乏、头痛、便秘及腹泻，其中大多数不良事件为轻至中度。

Tasigna应慎用于心脏病未得到控制或很严重的患者以及既往曾出现或可能出现QTc延长的患者。可能包括异常低钾或低镁的患者、先天性长QT综合征患者以及接受抗心律失常药或其他可能导致QT延长药物的患者。在应用Tasigna之前必须纠正低钾或低镁。最好密切监测其对QTc间期的影响，推荐在Tasigna初始治疗前做基线超声心动图检查。

Tasigna不得在进餐时服用，应于进餐后至少2 h以后服用。另外，用药后至少1 h内不得进食任何食物。

Tasigna

Generic name: Nilotinib

What is Tasigna?

Tasigna is used treat the chronic phase and accelerated phase of Philadelphia chromosome-positive chronic myelogeneous leukemia (CML) in patients resistant to previous therapy.

What is the most important information I should know about Tasigna?

Tasigna can cause QT prolongation (irregular heart beat) and sudden death. It can also suppress the bone marrow, hence reducing the body's ability to fight infections, and may cause anemia and bleeding.

Who should not take Tasigna?

Do not take Tasigna if you have low potassium or low magnesium levels.

What should I tell my doctor before I take the first dose of Tasigna?

Tell your doctor about all prescription, over-the-counter, and herbal medications you are taking before beginning treatment with Tasigna. Also talk to your doctor about your complete medical history, especially if you had a history of heart problems (including irregular heartbeat or QTc prolongation), liver problems, pancreatitis, low blood levels of potassium or magnesium, or a severe problem with lactose or other blood sugars.

What is the usual dosage?

The information below is based on the dosage guidelines your doctor uses. Depending on your condition and medical history, your doctor may prescribe a different regimen. Do not change the dosage or stop taking your medication without your doctor's approval.

Adults: The usual dosage of Tasigna is 400 milligrams (mg) twice daily.

How should I take Tasigna?

Take Tasigna twice a day, 12 hours apart.

Do not take Tasigna with food. Take Tasigna at least 2 after eating and then wait at least 1 hour before eating again.

What should I avoid while taking Tasigna?

Do not open Tasigna capsules. Do not drink grapefruit juice, eat grapefruit, or take any supplements containing grapefruit extract.

What are possible food and drug interactions associated with Tasigna?

If Tasigna is used with certain other drugs, the effects of either could be increased, decreased, or altered. It is especially important to check with your doctor before combining Tasigna with the following: ketoconazole, rifampicin, or any drug that prolongs QTc (check with your doctor or pharmacist).

What are the possible side effects of Tasigna?

Side effects cannot be anticipated. If any develop or change in intensity, tell your doctor as soon as possible. Only your doctor can determine if it is safe for you to continue taking this drug.

Side effects may include: irregular heartbeat, liver damage, fluid retention, inflammation of the pancreas, rash, nausea, headache, itching, diarrhea, constipation

Can I receive Tasigna if I am pregnant or breastfeeding?

Avoid Tasigna during pregnancy and breastfeeding.

What should I do if I miss a dose of Tasigna?

If you miss a dose, take your next dose as scheduled. Do not take 2 doses at once.

How should I store Tasigna?

Store at room temperature.