GLEEVEC Rx 
 Generic Name and Formulations:
Imatinib (as mesylate) 100mg, 400mg; tabs.

Company:
Novartis Pharmaceuticals Corp

Indications for GLEEVEC:
Kit (CD117) (+) unresectable and/or metastatic malignant GI stromal tumors (GIST). Adjuvant treatment of adults following complete gross resection of Kit (CD117) (+) GIST.

Adult Dose for GLEEVEC:
Take with food and water. May disperse tab in water or apple juice and take promptly. ≥18yrs: GIST: 400mg once daily; up to 800mg daily (given as 400mg twice daily) may be considered if clinically indicated. Adjuvant GIST treatment: 400mg once daily; 36 months of treatment recommended (see full labeling). If severe non-hematologic reactions develop: interrupt dose; resume at a lower dose in hepatic dysfunction. Severe hepatic impairment: reduce dose by 25%. Renal or hematologic reactions: see full labeling. Potent CYP3A4 inducers (eg, rifampin): increase imatinib dose by at least 50%.

Children's Dose for GLEEVEC:
Not recommended.

Pharmacological Class:
Signal transduction inhibitor.

Warnings/Precautions:
Hepatic or renal impairment. Immunosuppressed. Monitor weight and for fluid retention regularly; CBCs weekly for 1st month, bi-weekly for 2nd month, then periodically (eg, every 2–3 months); liver function at baseline then monthly or as needed. Monitor for tumor lysis syndrome; correct clinically significant dehydration and treat high uric acid levels before initiating therapy. Monitor growth in children. Cardiovascular disease. Elderly. Avoid pregnancy (Cat.D); nursing mothers: not recommended; see full labeling.

Interactions:
Potentiated by CYP3A4 inhibitors (eg, azole antifungals, macrolides). Antagonized by CYP3A4 inducers (eg, dexamethasone, phenytoin, phenobarbital, carbamazepine, St. John's wort, rifampin). May potentiate drugs metabolized by CYP3A4 (eg, acetaminophen, benzodiazepines, dihydropyridine calcium channel blockers, cyclosporine, pimozide, statins), CYP2D6, or CYP2C9 (use heparin instead of warfarin).

Adverse Reactions:
GI disturbances, edema (may be severe), bleeding, muscle cramps, fever, pain, rash (may be severe; eg, erythema multiforme, Stevens-Johnson syndrome), fatigue, dizziness, blurred vision, somnolence, headache, cough, arthralgia/myalgia, dyspnea, hypokalemia, night sweats, anorexia, pruritus, neutropenia, thrombocytopenia, weight gain, renal or hepatotoxicity, immunosuppression, hypothyroidism in thyroidectomy patients undergoing levothyroxine replacement (monitor TSH levels); rare: severe CHF, left ventricular dysfunction.

Metabolism:
Hepatic (CYP3A4, 1A2, 2D6, 2C9, 2C19); 95% protein bound.

Elimination:
Fecal (primarily), renal.

Generic Availability:
NO

How Supplied:
100mg—90

400mg—30
美国FDA批准Gleevec为儿童急性淋巴细胞性白血病 
2012年1月 25日美国食品和药品监督管理局(FDA)批准Gleevec (伊马替尼[imatinib])一种新使用为治疗儿童新诊断有Philadelphia染色体阳性 (Ph+)急性淋巴细胞性白血病(ALL)。
ALL是儿童最常见型癌症，每年影响约2,900儿童，和如不治疗进展迅速。有Ph+ ALL儿童有致被称为酪氨酸激酶蛋白遗传异常刺激骨髓制造太多不成熟白血细胞。与感染斗争所需健康白血细胞留下较少空间。
Gleevec，一种酪氨酸激酶抑制剂，阻断促进癌细胞发展蛋白。应与化疗联用治疗有Ph+ ALL儿童。
FDA的药物评价和研究中心血液学和肿瘤产品室主任Richard Pazdur，M.D.说：“我们很高兴为儿童的癌症药物数正在上升”“今天的批准是FDA，儿童肿瘤组和美国国家癌症研究所之间连续不断相互作用为美国有癌症儿童提供新和更佳治疗的结果。”
在一项由美国国家癌症研究所主办儿童肿瘤组进行的临床试验中确定Gleevec的这个新适应证的安全性和有效性。试验纳入儿童和年轻成年1岁和以上有非常高危ALL，被定义为在治疗5年内患者有大于45%机会经受其疾病并发症。92例有Ph+ ALL患者被纳入试验和被分为5个治疗组，各组连续接受格列卫治疗与化疗联用一个更大的时间。
50例Ph+ ALL患者接受Gleevec 最长时间，而这些70%患者4年内不经历复发或死亡(无事件生存)。结果还显示随着Gleevec与化疗联用治疗时间增加患者死亡减低。
有Ph+ ALL儿童用Gleevec与化疗联用治疗观察到最常见副作用包括感染斗争血细胞被称为嗜中性水平减低；血小板水平减低，它有助于血液凝固；肝毒性；和感染。
在2001年Gleevec被授予加速批准治疗有原始母细胞危象，加速相或慢性相Ph+慢性粒性白血病(CML)干扰素α治疗失败的患者。批注治疗几种情况，最近正规批准治疗 approval to treat children 新诊断有Ph+ CML (2011)儿童和正规批准治疗已被手术切除的成年Kit(CD117)-阳性胃肠道间质肿瘤(GIST) (2012)。
Gleevec由总部设在新泽西州的东汉诺威，Novartis上市。