部份中文伏立诺他处方资料（仅供参考） 【通用名称】伏立诺他 【药品名称】vorinostat Capsules 【商品名称】Zolinza 【拼音名称】Fulinuota 【主要成分】N-羟基-N'-苯基辛二酰胺 【药品性状】白色至浅橙色结晶或结晶性粉末 【适 应 症】有皮肤T细胞淋巴瘤（CTCL）患者已进展，持续或复发疾病用两种全身治疗或后皮肤的表现的治疗。 【用法用量】 1）1400mg口服每天1次有食物。 2）如患者对治疗不能耐受，剂量可能被减低至每天1次300mg与食物口服。如必要时，剂量可能进一步减低至300mg每天1次有食物每周共连续5天。 【不良反应】 最常见不良反应（发生率≥20%）是腹泻，疲乏，恶心，血小板减少，食欲不振和味觉障碍。 【注意事项】 （1）曾报道肺栓塞和深静脉血栓形成。监视患者相关的体征和症状。 （2）曾发生剂量相关血小板减少和贫血和可能需要调整剂量或终止。 （3）曾报道胃肠道功能紊乱（如，恶心，呕吐和腹泻）。患者可能需要止吐药，止泻药和液体和电解质替代（防止脱水）。 （4）有轻度和中度肝受损患者应谨慎治疗。 （5）曾观察到高血糖。调整饮食和/或可能需要治疗葡萄糖增加。 （6）在基线时和治疗期间定期监视电解质。 （7）监视血细胞计数和化学测试，包括电解质，葡萄糖和血清肌酐，治疗的头2个月期间每2周和其后每月。 （8）曾报道Zolinza和其他HDAC抑制剂同时使用（如，丙戊酸[valproicacid]）严重血小板减少和胃肠道出血。监视血小板计数。 （9）当妊娠妇女给药时可能发生胎儿危害。应忠告妇女对胎儿潜在危害。     【禁    忌】严重肝损伤。 【药理毒理】 体外研究表明，伏立诺他在纳摩尔级浓度（IC 50<86nmol/L）即可抑制HDAC 1、HDAC 2和HDAC 3（Ⅰ型）以及HDAC 6（Ⅱ型）酶活性。在某些癌细胞内，抑制过量的HDAC酶可激活正常细胞活性的基因。伏立诺他降低HDAC活性有助于减缓或中止癌细胞生长的基因激活。 【孕妇及哺乳用药】 终止药物。 【药物过量】 对ZOLINZA药物过量的治疗无专门资料。 【贮    藏】 贮存在20-25°C(68-77°F)，外出允许15-30°C (59-86°F)间。 【有 效 期】 24个月 【包装规格】 ZOLINZA 100MG CAPS DPSH 120/EA  VORINOSTAT  MERCK HUMAN HEALTH DIVISION  00006-0568-40         ZOLINZA CAP 100MG 120 DS  VORINOSTAT  MERCK SHARP & DOHME  00006-0568-40 【企业名称】默克公司 完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=cd86ee78-2781-468b-930c-3c4677bcc092 ZOLINZA(vorinostat) Capsules Zolinza Combination Treatments Offer Benefit For Multiple Myeloma Patients The 2009 American Society of Hematology (ASH) Meeting showcased several presentations on Zolinza (vorinostat), a histone deacetylase inhibitor developed by Merck Pharmaceuticals that is currently investigated for the treatment of multiple myeloma. Zolinza alters the way a cancer cell’s DNA creates proteins, which is important in cancer treatment because such a drug can slow down cell proliferation, minimize mutations in DNA and control cell death. Zolinza With Revlimid And Dexamethasone Preliminary data from an ongoing Phase 1 study suggest that the combination treatment of Zolinza, Revlimid (lenalidomide) and dexamethasone (Decadron) is safe and active in relapsed and refractory multiple myeloma patients. Researchers have enrolled 28 patients with relapsed or refactory myeloma to determine the maximum tolerated dose of the combination treatment. They are also studying the safety and efficacy of the combination treatment The participants have received five escalating dosages of Zolinza, Revlimid and dexamethasone for at least eight cycles of treatment. Twenty five of the 28 enrolled patients have been evaluated with regard to the efficacy of the treatment. Of those 25 patients, 21 (84%) have seen an improvement in their disease. The overall response rate is 64 percent. Twenty-four patients have experienced at least one side effect, with the most common being diarrhea, fatigue, neutropenia (low white blood cell count) and thrombocytopenia (low platelet count). One dose-limiting toxicity has been observed at the highest dose level. Six additional patients were escalated to that dose level. No additional dose-limiting toxicities have been observed since then. The maximum tolerated dose has therefore not been reached yet. Researchers continue to investigate the combination treatment to further evaluate the efficacy and safety of this treatment. Zolinza With Doxil And Velcade Results from another Phase 1 study that was presented at the ASH meeting show that Zolinza in combination with Doxil (pegylated liposomal doxorubicin) and Velcade (bortezomib) is safe and efficacious in patients with relapsed and refractory multiple myeloma. Nine patients (median age of 56) with relapsed or refractory myeloma enrolled in this study, receiving 1.3mg/m² of Velcade on days 1, 4, 8, and 11, and 30mg/m² of Doxil on day 4 of treatment. In addition, they were given escalating doses of Zolinza once daily on days 4 through 11 of a 3-week cycle. Three patients received 200 mg of Zolinza, four received 300 mg and two were given 400 mg. Six out of seven evaluable patients responded to the treatment. One patient experienced a complete response, one patient went into very good partial remission and the remaining four experienced partial remission. Common side effects included fatigue, diarrhea, nausea, vomiting and peripheral neuropathy (nerve damage in the extremities that can cause pain and tingling sensations). Three patients required dose reductions due to the side effects. Blood-related side effects included neutropenia (low white blood cell count), lymphopenia (low lymphocyte count), and thrombocytopenia (low platelet count). Researchers point out that they will have to consider side effects when determining the optimal dose for the Phase 2 study. Zolinza With Velcade Preliminary results from an ongoing Phase 1 trial suggest that extended treatment of Velcade in combination with Zolinza shows long-term activity in patients with relapsed and refractory myeloma. The study sequentially enrolled 34 patients with relapsed or refractory multiple myeloma. They received escalating doses of Zolinza (200 or 400 mg) for at least eight treatment cycles. Plus, they either were given 0.7 or 0.9 mg/m2 of Velade on days 4, 8, 11 and 15, or 0.9, 1.1 or 1.3 mg/m2 of Velcade on days 1, 4, 8 and 11. Patients received 20 mg of oral dexamethasone (Decadron) on days 1-4 and 9-12 of each cycle if their disease progressed. Nine patients have completed the study through twelve or more treatment cycles so far. Of these nine patients, five patients have experienced a partial response, two have had a minimal response, and two have been given the diagnosis of a stable disease. All of the nine patients experienced mild to moderate side effects, most commonly diarrhea, nausea and fatigue. Seven out of the nine patients have discontinued the treatment because their disease has progressed. The median time to progression was 294 days. Based on these preliminary results, the study authors feel that the Zolinza/Velcade combination treatment could provide long-term responses to relapsed/refractory myeloma patients. 皮肤癌新药Zolinza（vorinostat）获FDA批准 日前，美国食品药品管理局（FDA）批准了一种治疗皮肤癌新药Zolinza（vorinostat）胶囊。用于治疗皮肤T细胞淋巴瘤（CTCL），该药可用于皮肤癌持续恶化、其他药物治疗期间或以后复发。该药由美国默克公司生产。   皮肤T细胞淋巴瘤（CTCL）发病率较低，全美每年每100万人中约有3人诊断为CTCL。多数CTCL患者为男性，平均年龄50岁。根据相关法规，FDA按照罕见病治疗药物审批程序批准Zolinza，目的在于激励制药公司投资开发每年影响约20万美国人的罕见性疾病。   Zolinza的安全性和有效性的证据来自两项临床试验，其中包括对接受其他药物治疗后又复发的107名CTCL患者。按皮肤损伤评分等级的改善确定的标准分析，接受Zolinza治疗的30%患者有所改善，疗效平均持续168天。最常见的严重不良反应为肺栓塞、脱水、深度静脉血栓和贫血。常见的不良反应有胃肠症状（包括腹泻，恶心，食欲减退，呕吐和便秘）；疲惫，寒战和味觉障碍。动物实验结果显示，孕妇禁用该药。