近日，首个新类型抗HIV药物（口服CCR5-受体阻滞剂）Selzentry（maraviroc）已获美国FDA批准上市，用于治疗那些已经尝试过其他药物治疗方案并确诊其感染的HIV与CCR5受体相关的患者。

批准日期：2007年8月6日 公司：辉瑞公司

SELZENTRY（马拉维若 maraviroc）片剂

美国最初批准：2007年

肝毒性：

肝毒性：已经通过全身性过敏反应（例如，瘙痒性皮疹，嗜酸性粒细胞增多或IgE升高）报告了肝毒性。

立即评估有肝炎或过敏反应症状或体征的患者。

最近的重大变化

适用和用法：11/2009

剂量和用法：05/2010

禁忌症：05/2010

警告和注意事项：05/2010

警告和注意事项：11/2009

作用机制

Maraviroc是一种抗病毒药物[见临床药理学]。

适应症和用法

SELZENTRY是一种CCR5共同受体拮抗剂，适用于仅感染CCR5-向性HIV-1的成人的抗逆转录病毒联合治疗。

在未接受治疗的受试者中，该研究的结果显着增加[参见微生物学（12.4）临床研究（14.3）]。

适当使用SELZENTRY需要具有高度敏感性向性的向性测试。

剂量和用量

当与给定有效的CYP3A抑制剂（具有强CYP3A诱导无金），包括蛋白酶抑制剂（除替拉那韦/利托那韦），地拉韦啶150毫克，每天两次

与NRTI类药物，替拉那韦/利托那韦，奈韦拉平，雷特格韦，和其他药物有效的CYP3A抑制剂的arent每日两次CYP3A诱导或300mg

使用有效的CYP3A诱导剂，包括依法韦仑（不含有效的CYP3A抑制剂）600 mg，每日两次

剂量和给药中列出了更完整的共同给药药物清单。

肾功能不全患者可能需要调整剂量。

剂量形式和强度

片剂：150mg和300mg

禁忌症

Selzentry不宜在患有严重肾损伤或正在服用有效的CYP3A抑制剂或诱导终末期肾病（ESRD）（肌酐清除率<30 mL /分钟）一起使用。

警告和注意事项

将SELZENTRY用于既往肝功能不全或共感染病毒性乙型肝炎或丙型肝炎的患者时要谨慎。

在SELZENTRY的治疗中观察到更多的心血管事件，包括心肌缺血和/或梗塞。对心血管事件风险增加的患者慎用。

如果患者有严重肾损伤或终末期肾病（ESRD），接收发送Selzentry（不伴随CYP3A诱导剂或抑制剂）的经验体位性低血压的Selzentry剂量不宜从300 mg，每天两次，每天两次减少到150毫克。

不良反应

评论在治疗经验的受试者最常见的不良事件（> 8％的发病率）魁发生的频率高与安慰剂相比是上呼吸道感染，咳嗽，发热，皮疹，头晕。

要报告疑似不良反应，请致电1-800-438-1985联系辉瑞，或致电1-800-FDA-1088联系Pfizer或访问www.fda.gov/medwatch

药物相互作用

与CYP3A抑制剂共同给药，包括蛋白酶抑制剂（替拉那韦/利托那韦除外）和地拉夫定，将增加SEL的浓度

如何提供/存储和处理

SELZENTRY薄膜包衣片如下：

150和300mg片剂是蓝色，双凸面，椭圆形，薄膜包衣片，一面用“Pfizer”压印，另一面用“MVC 150”或“MVC 300”压印。

瓶装150毫克片剂

60粒（NDC 0069-0807-60）

瓶装300毫克片剂

60粒（NDC 0069-0808-60）

SELZENTRY薄膜包衣片应储存在25°C（77°F）; 允许的偏差在15°C至30°C（59°F至86°F）之间[见USP受控室温]。

保质期为24个月。

完整治疗资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=A94A9A2B-337B-4C13-8622-FC392194DC21

Selzentry  (maraviroc)

IMPORTANT SAFETY INFORMATION

What is the most important information I should know about SELZENTRY?

SELZENTRY can cause serious side effects including serious liver problems (liver toxicity). An allergic reaction may happen before liver problems occur. Stop taking SELZENTRY and call your healthcare provider right away if you get any of the following signs or symptoms of liver problems:

an itchy rash on your body (allergic reaction)      

your skin or the white part of your eyes  turns yellow (jaundice)                                                   

dark or “tea-colored” urine

vomiting

pain, aching, or tenderness on the right side of your stomach area

Your healthcare provider will do blood tests to check your liver before you begin treatment with SELZENTRY and as needed during treatment, and if you get a severe rash, signs and symptoms of liver problems, or an allergic reaction during treatment with SELZENTRY.

Who should not take SELZENTRY?

Do not take SELZENTRY if you have severe kidney problems or are on hemodialysis and are also taking certain other medications.

What should I tell my healthcare provider before taking SELZENTRY?

Before you take SELZENTRY, tell your healthcare provider if you:

have or have had liver problems including hepatitis B or C virus infection.

have heart problems.

have kidney problems.

have low blood pressure or take medicines to lower blood pressure.

are pregnant or plan to become pregnant. It is not known if SELZENTRY may harm your unborn baby.

are breastfeeding or plan to breastfeed. Do not breastfeed if you take SELZENTRY. You should not breastfeed if you have HIV-1 because of the risk of passing HIV-1 to your baby.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Some medicines may interact with SELZENTRY. Keep a list of your medicines to show your healthcare provider and pharmacist. You can ask your healthcare provider or pharmacist for a list of medicines that interact with SELZENTRY. Do not start taking a new medicine without telling your healthcare provider. Your healthcare provider can tell you if it is safe to take SELZENTRY with other medicines.

Your healthcare provider may need to change your dose of SELZENTRY when you take it with certain medicines.

You should not take SELZENTRY if you also take St. John’s wort.

What are the possible side effects of SELZENTRY?

SELZENTRY can cause serious side effects including:

See “What is the most important information I should know about SELZENTRY?”

Serious skin rash and allergic reactions. Severe and potentially life-threatening skin reactions and allergic reactions have been reported in some patients taking SELZENTRY. If you develop a rash with any of the following symptoms, stop using SELZENTRY and contact your doctor right away:   fever

generally ill feeling

muscle aches

blisters or sores in your mouth

blisters or peeling of the skin

redness or swelling of the eyes

swelling of the mouth or face or lips

problems breathing

yellowing of the skin or whites of your eyes

dark or tea-colored urine

pain, aching, or tenderness on the right side below the ribs

loss of appetite

nausea/vomiting

Heart problems including heart attack.

Low blood pressure when standing up (postural hypotension) can cause dizziness or fainting. You should avoid driving or operating heavy machinery if you have dizziness while taking SELZENTRY.

Changes in your immune system (Immune Reconstitution Syndrome) can happen when you start taking HIV-1 medicines. Your immune system may get stronger and begin to fight infections that have been hidden in your body for a long time. Tell your healthcare provider right away if you develop new symptoms after you start taking SELZENTRY.

Possible chance of infection or cancer. SELZENTRY affects other immune system cells and therefore may possibly increase your chance for getting other infections or cancer.

The most common side effects of SELZENTRY in adults include colds and cold-like symptoms, cough, fever, rash, bloating and gas, indigestion, constipation, and dizziness.

The most common side effects of SELZENTRY in children include vomiting, abdominal pain, diarrhea, nausea, and dizziness.

Tell your healthcare provider if you have any side effect that bothers you or that does not go away.

These are not all the possible side effects of SELZENTRY. For more information, ask your healthcare provider or pharmacist. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

SELZENTRY comes in 25-mg, 75-mg, 150-mg, and 300-mg tablets, and a 20-mg/mL oral solution. Take SELZENTRY 2 times a day. Swallow tablets whole. Do not chew the tablets. You can take SELZENTRY tablets with or without food.