文药名: Promacta (Eltrombopag Olamine Tablets) 中文药名: 艾曲波帕片 生产厂家: Glaxo Smith Kline(葛兰素史克) 药品介绍 艾曲波帕是首个FDA获准治疗成人慢性ITP患者的口服非肽类血小板生成素受体激动剂,用于治疗经糖皮质激素类药物、免疫球蛋白治疗无效或脾切除术后慢性特发性血小板减少性紫癜(ITP)患者的血小板减少。 美国FDA批准葛兰素史克公司的艾曲波帕片(Promacta)上市,用于治疗经糖皮质激素类药物、免疫球蛋白治疗无效或脾切除术后慢性特发性血小板减少性紫癜(ITP)患者的血小板减少。 由葛兰素史克(GSK)公司开发的小分子血小板生成素受体激动剂eltrombopag( Promacta /Revolade)则为一种治疗慢性ITP的口服新药,其作用机制与Amgen公司开发的同类产品romiplostim(即Nplate,已在欧美、澳大利亚和加拿大报批) 相似, 即促进血小板产生, 但eltrombopag是通过结合于血小板生成素受体跨膜区及刺激巨核细胞(一种骨髓细胞,可产生血小板)增殖和分化而发挥作用,为每日1次口服产品;后者却是一种血小板生成刺激型Fc肽融合蛋白,靶向血小板生成素受体的天然结合域,通过激活补体而起作用,为1周1次皮下注射用产品。血小板生成素受体为骨髓细胞的生长和成熟所必需,对血小板数的增加起着极为重要的作用。一般认为,血小板数低于5万/μL时具出血高风险, 正常的血小板数应为15万/μL~40万/μL。 GSK公司曾于2007年在美国佐治亚州亚特兰大举行的美国血液学会会议上报告了EXTEND试验的初步阳性结果,该项试验为一Ⅲ期延长期临床试验,旨在评价eltrombopag长期使用的安全性和有效性。94名受试的ITP患者中有61人治疗前的血小板数低于3万/μL;受试者的中值治疗期为151 d,最长治疗期为333 d;开始剂量为50 mg/d, 3周后可增至75mg/d,直至疗效降低。结果发现,血小板数低于3万/μL的受试者经本品治疗后,有73%的人血小板数达5 万/μL 或以上,其血小板数中值达14. 35万/μL;本品耐受性良好,常见不良反应仍为头痛, 13%的受试者出现一种严重不良反应。 最近, eltrombopag已获美国FDA肿瘤药物咨询委员会(ODAC)的一致“可获准”推荐,用于短期治疗那些先前曾接受过治疗的ITP患者,尽管FDA还有些许保留意见。在芝加哥举行的2008年美国临床肿瘤学会(ASCO)年度会议上,本品获得了ODAC成员16∶0的赞成票,因为最新的临床数据已表明本品短期用于ITP具有良好的风险-疗效比。但他们也表示,希望在本品获准上市前,出台一项适宜的强效风险处置方案。若本品获准上市,它将成为用于慢性ITP患者以升高血小板数的首个短期口服治疗药。 Eltrombopag短期使用的重要意义在于,可使那些需要外科或牙科手术的ITP患者血小板数升高,因为低血小板数者具过度失血高风险,不宜手术。 美国FDA的主要关注点是,一旦本品获准短期使用,势必导致本品非适应证的长期使用,因为ITP为一种慢性疾病,而在本品的若干项短期临床试验中已暴露出安全性问题,包括停药后的出血风险和肝毒性,且来自无对照的长期EXTEND试验的中期临床数据也显示本品可能导致骨髓纤维化。GSK公司则声称,本品停药后虽会重现血小板减少,但并未伴有临床意义的出血增加,而出现的肝胆实验室检查指标异常也一般较轻且可逆。 PROMACTA Generic Name for PROMACTAEltrombopag (as olamine) 25mg, 50mg; tabs. Legal Classification:Rx Pharmacological Class for PROMACTAThrombopoietin receptor agonist. Manufacturer of PROMACTAGlaxoSmithKline Pharmaceuticals Indications for PROMACTAThrombocytopenia due to chronic immune (idiopathic) thrombocytopenic purpura (ITP) in adults who have had an insufficient response to corticosteroids, immunoglobulins, or splenectomy. Adult dose for PROMACTATake on empty stomach. Initially 50mg once daily. Moderate to severe hepatic impairment or East Asian ancestry: initially 25mg once daily. Titrate to maintain platelet count ≥50x109/L; max 75mg once daily. Adjust dose based on platelet count: see literature. Children's dosing for PROMACTANot recommended. Warnings/Precautions for PROMACTAMonitor CBC, platelet count, and peripheral blood smears for cytopenias and abnormal morphologies; discontinue if no increase in platelet count occurs after 4 weeks at max dose, or if excessive increase in platelet count occurs (eg, >400x109/L), or if evidence of bone marrow fibrosis occurs (eg, cytopenias, nucleated RBCs). Monitor liver function closely before, during, and after treatment (see literature); discontinue if ALT >3xULN and is progressive or persistent for ≥4 weeks, or if it occurs with evidence of hepatic injury; reinitiation of therapy: not recommended; if restarted, use lower dose and monitor carefully. Do baseline eye exam; monitor for cataracts. Thromboembolism risk factors. Myelodysplastic syndromes. Renal impairment. Pregnancy (Cat.C). Nursing mothers: not recommended. Interactions for PROMACTADo not take within 4 hours of food/drugs containing polyvalent cations (eg, Fe+2, Ca+2, Al+2, Mg+2, Se+2, Zn+2). May potentiate substrates of organic anion transporter polypeptide 1B1 (eg, benzylpenicillin, most statins, methotrexate, nateglinide, repaglinide, rifampin); monitor and consider reducing their doses. May be potentiated by strong inhibitors of CYP1A2 (eg, ciprofloxacin, fluvoxamine) or CYP2C8 (eg, gemfibrozil, trimethoprim), and with moderate or strong inhibitors of UGT1A1 or UGT1A3. Adverse Reactions for PROMACTANausea, vomiting, menorrhagia, myalgia, paresthesia, cataract, ecchymosis, thrombocytopenia, increased ALT/AST, conjunctival hemorrhage, increased risk of hematologic malignancies; thrombotic events with excessive increases in platelet counts; worsened thrombocytopenia after discontinuation. Notes for PROMACTANote: Physicians, pharmacies, and patients must enroll in Promacta Cares program. Register pregnant patients taking eltrombopag by calling (888) 825-5249. How is PROMACTA supplied?Tabs—30 通用名称PROMACTA |
艾曲波帕片|Promacta (Eltrombopag Olamine Tablets)简介:
文药名: Promacta (Eltrombopag Olamine Tablets)
中文药名: 艾曲波帕片
生产厂家: Glaxo Smith Kline(葛兰素史克)
药品介绍
艾曲波帕是首个FDA获准治疗成人慢性ITP患者的口服非肽类血小板生成素受 ... 责任编辑:admin |
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