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 详细处方信息以本药内容附件PDF文件（2011112021090122.pdf）的“原文Priscribing Information”为准
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部分中文替莫瑞林处方资料（仅供参考）

Egrifta获准治疗艾滋病患者脂肪代谢障碍
2010年11月10日，美国食品药品管理局（FDA）宣布批准 Egrifta用于治疗艾滋病（AIDS）患者脂肪代谢障碍。患有此疾病的患者体内会产生过剩的脂肪，分布于体内各处，尤其是肝脏、胃和其他腹部器官周围区域。该症状的出现与许多抗逆转录病毒类AIDS治疗药物的使用有关。
Egrifta是FDA批准的首个脂肪代谢障碍治疗药物，属于人生长激素释放因子（GRF）类药物，给药方式为每日注射一次。
FDA药品审评与研究中心药物审评二室主任、M.D.、M.P.H Curtis Rosebraugh说，“FDA意识到了需要有一些措施用于治疗AIDS患者的脂肪代谢障碍。该疾病患者体内的过剩脂肪可能会引起其他的健康问题，并且会对患者的生命质量产生影响，因此有一些措施能够对这些症状进行安全有效的治疗是十分重要的。”
目前尚未进行Egrifta能否降低心血管风险及是否能够改善抗逆转录病毒药物顺应性相关研究。
共纳入了816名艾滋病病毒HIV感染成年男性和女性的两项临床试验对Egirfta的疗效进行了评估，这些纳入的患者均存在脂肪代谢障碍和腹部脂肪过剩症状。在816名患者中，543名接受Egrifta治疗，为期26周，同时设立安慰剂组进行了对照。在两项试验中，根据电脑断层扫描结果，得知与安慰剂组相比，接受Egrifta治疗的患者腹部脂肪均出现了更大程度的减少。一些患者报告称自我感觉有所改善。
在这些研究中，最常见的不良反应包括关节痛、注射部位皮肤发红和出疹（红疹和瘙痒）、腹痛、肿胀、肌肉痛（肌痛）。同时，Egrifta组患者血糖控制恶化的情况多于安慰剂组。
Egrifta由位于加拿大蒙特利尔的Theratechnologies公司研发，由Rockland, Mass.-based EMD Serono在美国上市。

药物名称：替莫瑞林[Egrifta(tesamorelin)]

适应症：HIV感染者腹部脂肪过量

公司：Theratechnologies

批准日期：2010年11月10日

药品类型：小分子药物

简要说明：腹部脂肪代谢障碍是一种与使用治疗HIV感染的多种抗病毒药物有关的疾病。一天一次注射替莫瑞林用于减少人类免疫缺陷病毒(HIV)感染者腹部过多的脂肪(腹部脂肪过量)。Egrifta是通过诱导内源性生长激素(GH)的释放来发挥作用。采用Egrifta治疗可刺激GH分泌和增加血清胰岛素样生长因子I(IGF-I)的水平。

Contraindications
•Disruption of the hypothalamic-pituitary axis due to hypophysectomy, hypopituitarism or pituitary tumor/surgery, head irradiation or head trauma
•Active malignancy (either newly diagnosed or recurrent). Any preexisting malignancy should be inactive and its treatment complete prior to instituting therapy with EGRIFTA®
•Known hypersensitivity to tesamorelin and/or mannitol
•Women who are pregnant; if pregnancy occurs, discontinue EGRIFTA® therapy

Warnings and Precautions
•Neoplasms: For patients with a history of non-malignant neoplasms, EGRIFTA® therapy should be initiated after careful evaluation of the potential benefit of treatment. For patients with a history of treated and stable malignancies, EGRIFTA® therapy should be initiated only after careful evaluation of the potential benefit of treatment relative to the risk of re-activation of the underlying malignancy. In addition, the decision to start treatment with EGRIFTA® should be considered carefully based on the increased background risk of malignancies in HIV-positive patients
•Elevated IGF-1: EGRIFTA® stimulates GH production and increases serum IGF-1. Given that IGF-1 is a growth factor and the effect of prolonged elevations in IGF-1 levels on the development or progression of malignancies is unknown, IGF-1 levels should be monitored closely during EGRIFTA® therapy. Careful consideration should be given to discontinuing EGRIFTA® in patients with persistent elevations of IGF-1 levels (eg, >3 SDS), particularly if the efficacy response is not robust (eg, based on visceral adipose tissue changes measured by waist circumference or CT scan). During the clinical trials, patients were monitored every three months. Among patients who received EGRIFTA® for 26 weeks, 47.4% had IGF-1 levels greater than 2 standard deviation scores (SDS), and 35.6% had SDS >3, with this effect seen as early as 13 weeks of treatment. Among those patients who remained on EGRIFTA® for a total of 52 weeks, at the end of treatment 33.7% had IGF-1 SDS >2 and 22.6% had IGF-1 SDS >3
•Fluid Retention: Fluid retention may occur during EGRIFTA® therapy and is thought to be related to the induction of GH secretion. It manifests as increased tissue turgor and musculoskeletal discomfort resulting in a variety of adverse reactions (eg, edema, arthralgia, carpal tunnel syndrome) which are either transient or resolve with discontinuation of treatment
•Glucose Intolerance: EGRIFTA® treatment may result in glucose intolerance. Patients treated with EGRIFTA® are at an increased risk of developing diabetes (HbA1c ≥ 6.5%). In clinical trials at week 26, a greater percentage of patients had elevated HbA1c (≥6.5%) in the EGRIFTA® group than in the placebo group (4.5% vs 1.3%). Glucose status should be carefully evaluated prior to initiating EGRIFTA® treatment and monitored periodically for changes in glucose metabolism to diagnose those who develop impaired glucose tolerance or diabetes. Caution should be exercised in treating patients with EGRIFTA® if they develop these conditions and discontinuation of treatment should be considered in patients who do not show a clear efficacy response as judged by the degree of reduction in visceral adipose tissue by waist circumference or CT scan measurements. Since EGRIFTA® increases IGF-1, patients with diabetes who are receiving ongoing treatment with EGRIFTA® should be monitored at regular intervals for potential development or worsening of retinopathy
•Hypersensitivity Reactions: Hypersensitivity reactions may occur in patients treated with EGRIFTA®. Hypersensitivity reactions occurred in 3.6% of patients with HIV-associated lipodystrophy treated with EGRIFTA® in the Phase 3 clinical trials. These reactions included pruritis, erythema, flushing, urticaria, and other rash. In cases of suspected hypersensitivity reactions, patients should be advised to seek prompt medical attention and treatment with EGRIFTA® should be discontinued immediately
•Injection Site Reactions: EGRIFTA® treatment may cause injection site reactions, including injection site erythema, pruritus, pain, irritation, and bruising. The incidence of injection site reactions was 24.5% in EGRIFTA®-treated patients and 14.4% in placebo-treated patients during the first 26 weeks of treatment in the Phase III clinical trials. For patients who continued EGRIFTA® for an additional 26 weeks, the incidence of injection site reactions was 6.1%. In order to reduce the incidence of injection site reactions, it is recommended to rotate the site of injection to different areas of the abdomen
•Acute Critical Illness: Increased mortality in patients with acute critical illness due to complications following open heart surgery, abdominal surgery or multiple accidental trauma, or those with acute respiratory failure has been reported after treatment with pharmacologic amounts of growth hormone. EGRIFTA® has not been studied in patients with acute critical illness. Since EGRIFTA® stimulates growth hormone production, careful consideration should be given to discontinuing EGRIFTA® in critically ill patients

Drug Interactions
•Cytochrome P450-Metabolized Drugs: Co-administration of EGRIFTA® with simvastatin, a sensitive CYP3A substrate, showed that EGRIFTA® had no significant impact on the pharmacokinetic profiles of simvastatin in healthy subjects. Because tesamorelin stimulates GH production, careful monitoring is advisable when EGRIFTA® is administered in combination with other drugs known to be metabolized by CYP450 liver enzymes

Immunogenicity
•Antibody formation may occur with the use of therapeutic peptide products. Anti-tesamorelin IgG antibodies were detected in approximately half of patients treated with EGRIFTA® and generally disappeared over time after discontinuation of treatment. Antibodies did not appear to impact the efficacy of EGRIFTA®

Use in Specific Populations
•Nursing Mothers: Because of both the potential for HIV-1 infection transmission and serious adverse reactions in nursing infants, mothers receiving EGRIFTA® should be instructed not to human milk-feed
•Pediatric Use: Safety and effectiveness in pediatric patients have not been established. EGRIFTA® should not be used in children with open epiphyses, among whom excess GH and IGF-1 may result in linear growth acceleration and excessive growth
•Geriatric Use: There is no information on the use of EGRIFTA® in patients greater than 65 years of age with HIV and lipodystrophy
•Renal and Hepatic Impairment: Safety, efficacy, and pharmacokinetics of EGRIFTA® in patients with renal or hepatic impairment have not been established

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 详细处方信息以本药内容附件PDF文件（2011112021090122.pdf）的“原文Priscribing Information”为准
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