制造商：
安进公司
药理分类：
破骨细胞抑制因子（RANKL抑制剂）
活性成分（S）：
denosumab的120mg/vial（70mg/mL）为SC INJ soln，不含防腐剂。
指示（S）：
预防骨相关事件与来自实体瘤骨转移患者（SRE）。不预防与多发性骨髓瘤SRE。
药理：
在与骨转移实体瘤患者，在破骨细胞活性增加，是骨病理调停。这增加破骨细胞的活性是由一种叫做刺激受体激活核因子kappa - B配体，或RANKL的物质。 denosumab的是一种单克隆抗体，它把人类RANKL。它可以阻止RANKL与其受体相互作用，从对破骨细胞及其前体的表面，从而抑制破骨细胞的形成，功能和生存。
临床试验：
的安全性和疗效Xgeva在骨骼相关事件预防与实体瘤骨转移患者（如病理性骨折，放射治疗骨，骨手术，或脊髓压缩）进行了评估，三个随机，双盲，主动对照试验比较，这种药物唑来膦酸。在每次试验中，主要结果测量是为了显示与denosumab的时间到第一骨骼相关事件（SRE）非劣性相比，唑来膦酸。如果主要终点（非劣性）达成，时间到第一SRE和时间，第一届和以后SRE次要终点是测试的优越性。
参加试验1晚期乳腺癌和骨转移患者。试用2报读从实体瘤骨转移，前列腺癌或乳腺癌相比，多发性骨髓瘤或其他成人。试用3收纳阉割性前列腺癌骨转移的患者。
Xgeva延迟时间先SRE以下随机相比，在乳腺癌骨转移或阉割性前列腺癌患者的唑来膦酸。在骨转移，由于其他实体瘤或由于多发性骨髓瘤溶骨性病变，Xgeva是在拖延不劣于随机分组后的第一时间SRE唑来膦酸。
总生存率和无进展生存期之间的所有三项试验武器相似，但死亡率较高的Xgeva在与多发性骨髓瘤患者分组，因此，它不应该在这些患者中使用。
法律分类：
接收
成人：
由SC INJ给到上臂，大腿或腹部。 120毫克，每4周一次。
儿童：
不推荐（牙列与骨骼的生长和干扰）。
警告/注意事项：
在开始纠正低钙血症，保证充足的每日钙，镁，Vit.D摄入，ESP。在肾功能不全（肌酐清除率<30mL/min）。监视器钙，磷，在（如严重肾功能不全，接受透析）患者易患镁的水平。监测的颚骨坏死。不要在治疗前和定期的基线口试和预防性牙科。保持良好的口腔卫生。治疗期间避免侵入性牙科手术。妊娠（Cat.C）。护理母亲：避免（可能会损害乳腺发育/哺乳期）。
交互（S）：
同时服用的药物，可以降低钙的水平;监控。
不良反应（S）：
疲劳，乏力，低磷血症，胃肠不适，呼吸困难，颌骨，骨坏死严重低钙血症。
注：
鼓励妇女谁成为治疗怀孕期间Xgeva报名参加Amgen的妊娠监察计划。要登记电话：（800）77 - AMGEN。
如何提供：
单用小瓶（1.7mL）-1
FDA批准地诺单抗预防癌症相关骨损伤
美国FDA于 11月19日批准地诺单抗（denosumab，商品名Xgeva）用以预防癌症已经转移并且损害骨质的肿瘤患者骨骼相关事件（SREs）。所谓骨骼相关事件包括癌症所致骨折和疼痛。地诺单抗这一获准适用人群不包括多发性骨髓瘤或其它血癌患者。
骨转移是癌症患者疼痛和难受的重要原因，影响患者的生活质量。地诺单抗具有与现已获准的减少肿瘤骨骼并发症药物不同的作用机制。三项随机-双盲的临床研究证实了地诺单抗的安全性和疗效，总共有5723名患者参与研究。这些研究在乳腺癌（研究1）、前列腺癌（研究2）以及多种其它癌症（研究3）患者身上对地诺单抗与唑来膦酸作了比较。这些研究旨在测定由于癌症，患者最终出现骨折或脊髓压迫，或为控制疼痛需要进行放射或手术治疗间隔的时间。在乳腺癌或前列腺癌患者中，地诺单抗延迟SREs优于唑来膦酸。前列腺癌患者中SREs延迟时间中位值21个月，唑来膦酸为17个月。
乳腺癌患者唑来膦酸使SREs延迟的中位时间为26个月，而地诺单抗没有达到这一水平。在其它实体瘤患者中，地诺单抗和唑来膦酸使SREs延迟的中位时间不相上下。受试者主要的实体瘤为非小细胞肺癌、多发性骨髓瘤、肾癌以及小细胞肺癌。
诺单抗最严重的不良反应为低钙血症和颚骨坏死。
今年6月1日FDA批准注射用地诺单抗（denosumab）治疗有高骨折风险的绝经后妇女骨质疏松症，其所用商品名Prolia。
XGEVA
Manufacturer:
Amgen, Inc.
Pharmacological Class:
Osteoclast inhibitor (RANKL inhibitor)
Active Ingredient(s):
Denosumab 120mg/vial (70mg/mL); soln for SC inj; preservative-free.
Indication(s):
Prevention of skeletal-related events (SRE) in patients with bone metastases from solid tumors. Not for preventing SRE with multiple myeloma.
Pharmacology:
In patients with solid tumors with osseous metastases, an increase in osteoclast activity is a mediator of bone pathology. This increased osteoclast activity is stimulated by a substance called receptor activator of nuclear factor kappa-B ligand, or RANKL. Denosumab is a monoclonal antibody that binds to human RANKL. It prevents RANKL from interacting with its receptors on the surfaces of osteoclasts and their precursors, thereby inhibiting osteoclast formation, function, and survival.
Clinical Trials:
The safety and efficacy of Xgeva in the prevention of skeletal-related events (eg, pathologic fracture, radiation therapy to bone, surgery to bone, or spinal cord compression) in patients with bone metastases from solid tumors were evaluated in three randomized, double-blind, active-controlled trials that compared this drug to zoledronic acid. In each trial, the main outcome measure was to show noninferiority of time-to-first skeletal-related event (SRE) with denosumab as compared to zoledronic acid. If primary endpoint (noninferiority) was reached, secondary endpoints for Time to First SRE and Time to First and Subsequent SRE were tested for superiority.
Trial 1 enrolled patients with advanced breast cancer and bone metastasis. Trial 2 enrolled adults with bone metastasis from solid tumors, other than prostate or breast cancer, or with multiple myeloma. Trial 3 enrolled patients with castrate-resistant prostate cancer and bone metastasis.
Xgeva delayed the time to first SRE following randomization as compared to zoledronic acid in patients with breast or castrate-resistant prostate cancer with osseous metastases. In patients with bone metastasis due to other solid tumors or lytic lesions due to multiple myeloma, Xgeva was noninferior to zoledronic acid in delaying time to first SRE after randomization.
Overall survival and progression-free survival were similar between arms in all three trials, but mortality was higher with Xgeva in a subgroup of patients with multiple myeloma; therefore, it should not be used in these patients.
Legal Classification:
Rx
Adults:
Give by SC inj into upper arm, upper thigh, or abdomen. 120mg once every 4 weeks.
Children:
Not recommended (interferes with bone growth and dentition).
Warnings/Precautions:
Correct hypocalcemia before starting; ensure adequate daily calcium, magnesium, and Vit.D intake, esp. in renal impairment (CrCl<30mL/min). Monitor calcium, phosphorus, magnesium levels in susceptible patients (eg, severe renal impairment, receiving dialysis). Monitor for osteonecrosis of the jaw. Do baseline oral exam and preventive dentistry before and regularly during therapy. Maintain good oral hygiene. Avoid invasive dental procedures during treatment. Pregnancy (Cat.C). Nursing mothers: avoid (may impair mammary gland development/lactation).
Interaction(s):
Concomitant drugs that can lower calcium levels; monitor.
Adverse Reaction(s):
Fatigue, asthenia, hypophosphatemia, GI upset, dyspnea, osteonecrosis of jaw, severe hypocalcemia.
Notes:
Encourage women who become pregnant during Xgeva treatment to enroll in Amgen’s Pregnancy Surveillance program. To enroll call (800) 77-AMGEN.
How Supplied:
Single-use vial (1.7mL)—1
Last Updated:
12/23/2010