部分中文阿尼芬净处方资料（仅供参考）

名称：阿尼芬净注射液（ERAXIS，ANIDULAFUNGIN）

商品名：Eraxis

藥品中文名：助黴飛注射劑

开发与上市厂商
本品由美国礼来公司研制，2006年12月在美国首次上市。

适应证
本品适用于下列真菌感染：①念珠菌血症及其他类型的念珠菌感染（腹腔脓肿、腹膜炎）；②食管念珠菌病。
药理作用
本品为半合成棘球白素，具有抗真菌活性，能抑制真菌中葡聚糖合成酶，从而抑制真菌细胞壁的主要成分1，3-β-D-葡聚糖的生成。体外试验显示，本品具有抗白念珠菌、光滑念珠菌、近平滑念珠菌和热带念珠菌活性。免疫正常或受抑的全身性感染小鼠和兔子肠胃外给予本品，能有效对抗白念珠菌感染。免疫受抑兔口咽／食管感染模型试验显示，对耐氟康唑白念珠菌感染，本品可降低真菌负荷。健康成人个体静脉内使用本品一日，次，连续10天，本品全身暴露．量与剂量成比例，且个体间差异很小（变异系数＜25％）。
本品静脉给药分布t1/2为0.5～1小时，分布容积为 30～50L，本品血浆蛋白结合率高，超过99%。
未观察到本品的肝代谢。本品为非细胞色素 P450(CYP450)同工酶底物、诱导剂或抑制剂，因此本品与经由CYP450同工酶代谢的药物几无相互作用。
单剂临床研究中，健康个体使用14C标记的本品， 9天内约30%剂量的放射性物质随粪便排出，用药6天后本品血药浓度跌至检测下限以下，用药8周后血液、尿液和粪便中回收的放射性物质可忽略不计。

临床评价
一项随机双盲Ⅲ期临床研究在256例念珠菌血症和（或）其他类型侵袭性念珠菌病患者中评价了本品的安全性和疗效。患者随机一日，次静脉内使用本品（200mg负荷量，随后100mg维持量）或氟康唑（800mg 负荷量，随后400mg维持量），持续至少14天，但不超过42天。两组患者在静脉用药治疗至少，0天后可转用口服氟康唑。结果，本品组和氟康唑组静脉用药治疗的平均持续时间分别为14和11天，两组均有33例患者转用口服治疗，口服治疗平均持续时间本品组为7天，氟康唑组为5天，全部治疗结束后本品组和氟康唑组治愈率分别为74.0%和56.8％。

一项纳入601例食管念珠菌病患者的双盲双模拟随机Ⅲ期临床研究，300例患者静脉注射本品（第，天负荷量100mg,随后一日50mg）、301例患者口服氟康唑（第 1天负荷量200mg，随后一日100mg）。
内窥镜检查治疗成功率（治愈：内窥镜检查等级为0；或改善：相对基线下降，个等级或以上），本品组为97.4%，氟康唑组为98.7%。本品组治愈（等级 =0）者204例（88.3%），氟康唑组为221例（93.6%）。经内窥镜检查证实结束治疗后2周，本品组有120例复发（53.3%），显著多于氟康唑组的45例（19.3%）。
治疗结束时，临床治疗成功率（包括吞咽痛／吞咽困难和胸骨后疼痛的临床症状治愈或改善），本品组为 99.1％，氟康唑组为99.6％。白念珠菌感染者的微生物学治疗成功率，本品组为87.7%，氟康唑组为94.6%；除白念珠菌外其他念珠菌感染者，本品组和氟康唑组的治疗成功率分别为83.3%和 87.5％。

不良反应
在念珠菌血症／其他念珠菌感染患者中进行的 3项研究评价了本品（1OOmg）的疗效和安全性，结果显示，发生率≥2.0%的治疗相关不良反应，本品组主要为腹泻、肝功能受损、低血钾以及深静脉血栓形成。
另一项随机双盲对照Ⅲ期临床研究评价了本品和氟康唑对食管念珠菌病患者的疗效和安全性，结果显示，发生率＞1.0%的治疗相关不良反应，本品组主要为血液和淋巴系统损害，如恶心呕吐、发热、肝功能受损、头痛、皮疹和静脉炎等。
注意事项
已知对本品或本品任一组分，或其他棘球白素过敏者禁用。

接受本品治疗的健康志愿者和患者可出现肝功能检测指标异常，故应对接受本品治疗出现肝功能异常者进行监测，并评估继续治疗的风险和效益。

用法与用量

对于念珠菌血症和其他念珠菌感染（腹腔脓肿，腹膜炎），本品推荐剂量为第1天予负荷量200mg，此后维持剂量100mg，一日1次。一般而言，抗真菌治疗应在最后1次培养阳性后持续治疗至少14天。

对于食管念珠菌病患者，本品推荐剂量为第1天负荷量1 OOmg,此后50mg,一日1次。患者应接受最少 14天治疗，症状消除至少7天。治疗持续时间可根据患者的临床反应确定。

制剂
本品为冻干粉针剂（静脉输注用），每瓶装规格有50和100mg两种。

注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
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原产地英文商品名:
ERAXIS(WATER DIL) 100mg/vial
原产地英文药品名:
ANIDULAFUNGIN
中文参考商品译名:
助霉飞(DIL水) 100毫克/瓶
中文参考药品译名:
阿尼芬净
生产厂家中文参考译名:
辉瑞
生产厂家英文名:
PFIZER

------------------------------------------------------
原产地英文商品名:
ERAXIS(WATER DIL) 50mg/vial
原产地英文药品名:
ANIDULAFUNGIN
中文参考商品译名:
助霉飞(DIL水) 50毫克/瓶
中文参考药品译名:
阿尼芬净
生产厂家中文参考译名:
辉瑞
生产厂家英文名:
PFIZER

------------------------------------------------------
原产地英文商品名:
ERAXIS 100mg/vial
原产地英文药品名:
ANIDULAFUNGIN
中文参考商品译名:
助霉飞 100毫克/瓶
中文参考药品译名:
阿尼芬净
生产厂家中文参考译名:
辉瑞
生产厂家英文名:
PFIZER

------------------------------------------------------
原产地英文商品名:
ERAXIS 50mg/vial
原产地英文药品名:
ANIDULAFUNGIN
中文参考商品译名:
助霉飞 50毫克/瓶
中文参考药品译名:
阿尼芬净
生产厂家中文参考译名:
辉瑞
生产厂家英文名:
PFIZER

------------------------------------------------------

Eraxis (anidulafungin)
Company: Pfizer
Approval Status: Approved February 2006
Treatment for: Fungal infections
Areas: Immunology/Infectious Diseases

General Information
Eraxis (anidulafungin) is an echinocandin semi-synthetic lipopetide, designed to eradicate fungal infections through disruption of enzyme synthesis pathways in these cells without affecting human tissues.

Eraxis is specifically indicated for the treatment of several types of fungal infections: Candidemia; intra-abdominal abscess and peritonitis caused by Candida species; and esophageal candidiasis. The drug has not been studied for the treatment of Candida related endocarditis, osteomyelitis, or meningitis, and efficacy in the treatment of neutropenic patients has not been fully established.

Eraxis is supplied as a lyophilized powder for reconstitution and injection. The recommended initial dose of the drug for the treatment of Candidemia/additional Candida infections is a single loading dose of 200 mg Eraxis on day 1, followed by 100 mg daily thereafter, until clinical response is observed (generally through at least 14 days after the last positive fungal culture). For esophageal candidiasis, recommended dosing is a single loading dose of 100 mg on day 1, followed by 50 mg daily thereafter for at least 14 days and at least 7 days following the resolution of symptoms.

Clinical Results
FDA Approval
Candidemia/Additional Candida Infections
Approval of Eraxis for the treatment of Candidemia and additional Candida infections was based on a phase III trial. This randomized, double-blind, controlled study treated 256 patients with candidemia and/or other forms of invasive candidiasis. Subjects received a fixed dose regimen of either Eraxis (200 mg loading dose/100 mg daily maintenance dose) or fluconazole (800 mg loading dose/400 mg daily maintenance dose) via intravenous infusion for 14 to 42 days. Patients from either arm were permitted to transfer to oral fluconazole following at least 10 days of IV therapy and a negative blood culture. At the end of IV treatment, treatment 75.6% of subjects receiving Eraxis achieved global clinical success, vs. 60.2% for fluconazole. Superiority was maintained at the end of all treatment, (74.0% global success, vs. 56.8%, respectively), and at 2-week (64.6% vs. 49.2%) and 6-week (55.9% vs. 44.1%) follow-ups. All-cause mortality during the study (22.8% vs. 31.4%) all cause mortality during study therapy (7.9% vs. 14.4%), and mortality attributed to Candida (1.6% vs. 4.2%) all showed reductions for Eraxis relative to fluconazole.

Esophageal Candidiasis
Approval of Eraxis for the treatment of esophageal candidiasis was based on a double-blind, double-dummy, randomized phase III trial. 601 subjects were randomized to receive Eraxis (100 mg loading dose/50 mg daily maintenance dose) or fluconazole (200 mg loading dose/100 mg daily maintenance dose) via intravenous infusion. Treatment was administered for a minimum of 14 days, and for 7 days following the resolution of symptoms, through a maximum of 21 days. In both treatment groups, median time to resolution of symptoms was 5 days, and median duration of therapy was 14 days. Endoscopic success (the combined rate of clinical improvement and cure) at the end of therapy (the trial's primary endpoint) was 97.4% for Eraxis and 98.7% for fluconazole; this included cure rates of 88.3% vs. 93.6%, respectively, and improvement rates of 9.1% vs. 5.1%. At 2-weeks post-treatment subjects receiving Eraxis experienced significantly more endoscopically-documented relapses (53.3%) than subjects receiving fluconazole (19.3%).

Ongoing Study Commitments
Deferred pediatric study under PREA for the treatment of candidemia and other forms of Candida infections (intra-abdominal abscess and peritonitis) in pediatric patients ages zero months to sixteen years of age.
Final Report Submission: February 17, 2011

Side Effects
Adverse events associated with the use of Eraxis may include, but are not limited to, the following:
Diarrhea
Hypokalemia
Liver Enzyme Abmormalities
Headache
Rash
Neutropenia
Nausea

Mechanism of Action
Anidulafungin is a semi-synthetic echinocandin designed to inhibit glucan synthase, an enzyme present in fungal (but not mammalian) cells. Inhibition of glucan synthase disrupts formation of 1,3-ß-D-glucan, an essential component of the fungal cell wall.

Additional Information
For additional information regarding Eraxis or Candida fungal infections, please visit the Eraxis web page.