制造商：
百时美施贵宝
药理分类：
细胞毒性T淋巴细胞抗原4（抗原- 4）阻断抗体。
活性成分（补）：
Ipilimumab 5mg/mL;为静脉注射溶液，不含防腐剂。
指示（补）：
治疗不能手术切除或转移性黑色素瘤。
药理作用：
抗原- 4是T细胞活化的负调控。 Ipilimumab结合抗原- 4和阻断了抗原- 4的配体，CD80/CD86分子的相互作用。对抗原- 4封锁已被证明增加T细胞的活化和增殖。该行动在黑色素瘤患者ipilimumab机制是间接的，可能是通过T细胞介导的抗肿瘤免疫反应。
临床试验：
的安全性和有效性进行了调查，ipilimumab一项研究中，包括以前无法手术切除或转移性黑色素瘤与一个或多个以下治疗676例：aldesleukin，达卡巴嗪，替莫唑胺，fotemustine，或卡铂。其中676例，403给予ipilimumab结合3mg/kg与不完全弗氏佐剂（gp100），137人获得ipilimumab 3mg/kg研究中胜肽疫苗，并给予gp100 136人孤独。该研究纳入与HLA - A2的唯一* 0201基因型患者，这有利于人类白细胞抗原基因疫苗的免疫介绍。肿瘤反应进行了评估在12周和24，每3个月后。肿瘤反应与客观证据在12或者使用24周的患者在16或28周的反应耐久性确认的评估，分别为。
测量结果的主要功效是在ipilimumab + gp100相比，在gp100手臂组的总生存。那些接受了ipilimumab组合+疫苗或ipilimumab独自生活了约10个月平均水平;那些仅接受疫苗谁住了6.5个月。
法律分类：
接收
成人：
静脉输注给受超过90分钟。 3mg/kg剂量为4总每3周。全心全意为中等剂量的免疫介导的反应或内分泌失调症状。完成/不良反应和接受<7.5mg强的松或相当于每天每部分的解决：可能恢复治疗。永久停止并启动全身大剂量糖皮质激素治疗严重不良反应。
儿童：
不推荐。
警告/注意事项：
永久终止条件是：持续的中度不良反应或无法降低到7.5mg剂量皮质类固醇激素或相当于一天;未能从16个星期内完成第一剂全疗程;包括严重或威胁生命的反应：腹部1）结肠炎疼痛，发热，肠梗阻，或腹膜的迹象;增加静脉输液的大便次数，大小便失禁，需要> 24小时，胃肠出血/穿孔; 2）AST或ALT> 5倍正常值上限或总胆红素> 3倍正常值上限3）史蒂文斯， Johnson综合征，毒性表皮坏死，或全层皮肤溃疡复杂的皮疹，或坏死，水泡，或出血性的表现; 4）重度运动或感觉神经病变，格林巴利综合征，重症肌无力; 5）严重的免疫介导的反应涉及任何器官系统; 6）免疫介导的眼部疾病，是没有反应局部免疫抑制治疗。为肠炎，皮炎，神经病变，内分泌失调监控;执行在基准线和在每次剂量LFTs和甲状腺测试。妊娠（目录三）。哺乳母亲：不推荐。
不良反应（补）：
疲劳，腹泻，瘙痒，皮疹，肠炎，免疫介导的不良反应（可能是严重的，致命的）。
如何提供：
单用小瓶（50毫克，200毫克）-1
最后更新：
2011年4月28日
YERVOY
Manufacturer:
Bristol-Myers Squibb
Pharmacological Class:
Cytotoxic T-lymphocyte antigen 4 (CTLA-4)-blocking antibody.
Active Ingredient(s):
Ipilimumab 5mg/mL; soln for IV infusion; preservative-free.
Indication(s):
Treatment of unresectable or metastatic melanoma.
Pharmacology:
CTLA-4 is a negative regulator of T-cell activation. Ipilimumab binds to CTLA-4 and blocks the interaction of CTLA-4 with its ligands, CD80/CD86. Blockade of CTLA-4 has been shown to augment T-cell activation and proliferation. The mechanism of action of ipilimumab in patients with melanoma is indirect, possibly through T-cell mediated anti-tumor immune responses.
Clinical Trials:
The safety and efficacy of ipilimumab were investigated in a study that included 676 patients with unresectable or metastatic melanoma previously treated with one or more of the following: aldesleukin, dacarbazine, temozolomide, fotemustine, or carboplatin. Of these 676 patients, 403 were given ipilimumab 3mg/kg in combination with an investigational peptide vaccine with incomplete Freund’s adjuvant (gp100), 137 were given ipilimumab 3mg/kg, and 136 were given gp100 alone. The study enrolled only patients with HLA-A2*0201 genotype; this HLA genotype facilitates the immune presentation of the vaccine. Assessment of tumor response was conducted at Weeks 12 and 24, and every 3 months thereafter. Patients with evidence of objective tumor response at 12 or 24 weeks had assessment for confirmation of durability of response at 16 or 28 weeks, respectively.
The major efficacy outcome measure was overall survival in the ipilimumab + gp100 arm compared to that in the gp100 arm. Those receiving the combination of ipilimumab + vaccine or ipilimumab alone lived an average of about 10 months; those who received only the vaccine lived an average of 6.5 months.
Legal Classification:
Rx
Adults:
Give by IV infusion over 90 minutes. 3mg/kg every 3 weeks for a total of 4 doses. Withhold dose for moderate immune-mediated reactions or symptomatic endocrinopathy. Complete/partial resolution of adverse reaction and receiving <7.5mg prednisone or equivalent per day: may resume treatment. Permanently discontinue and initiate systemic high-dose corticosteroids for severe adverse reactions.
Children:
Not recommended.
Warnings/Precautions:
Permanently discontinue if: persistent moderate adverse reactions or inability to reduce corticosteroid dose to 7.5mg prednisone or equivalent per day; failure to complete full treatment course within 16 weeks from first dose; severe or life-threatening reactions, including: 1) colitis with abdominal pain, fever, ileus, or peritoneal signs; increase in stool frequency and incontinence, need for IV hydration for >24 hours, GI hemorrhage/perforation; 2) AST or ALT >5X ULN or total bilirubin >3X ULN; 3) Stevens-Johnson syndrome, toxic epidermal necrolysis, or rash complicated by full thickness dermal ulceration, or necrotic, bullous, or hemorrhagic manifestations; 4) severe motor or sensory neuropathy, Guillain-Barre syndrome, or myasthenia gravis; 5) severe immune-mediated reactions involving any organ system; 6) immune-mediated ocular disease that is unresponsive to topical immunosuppressive therapy. Monitor for enterocolitis, dermatitis, neuropathy, endocrinopathy; perform LFTs and thyroid tests at baseline and before each dose. Pregnancy (Cat. C). Nursing mothers: not recommended.
Adverse Reaction(s):
Fatigue, diarrhea, pruritus, rash, colitis; immune-mediated adverse reactions (may be severe and fatal).
How Supplied:
Single-use vial (50mg, 200mg)—1