马拉维若片(商品名：Selzentry)是l0余年来首个新一类口服HIV治疗药。剂量规格：马拉维若150mg／片，300mg／片。Selzentry在治疗曾用其它药物治疗过的特异类型HIV感染患者时，遏止病毒进入白细胞，显著减少病毒携带量和增加T细胞计数。

马拉维若是称作CCR5拮抗剂类药的第一个．阻断病毒进入T细胞主要途径的CCR5共同受体。

本品在R5病毒进入T细胞前将其阻止在细胞外表面，而不是像所有其它已上市的所有HIV口服药作用于细胞内的病毒。

美国FDA批准马拉维若片上市是基于双盲安慰剂对照临床研究的安全性和有效性结果。选择了1076例患者临床研究，尽管患者先前采用其它HIV药物治疗过，但他们血中仍带有HIV病毒。
加速批准可让优于现有治疗严重或威胁生命疾病药物的新品尽早获准上市。本品批准是基于24周的双盲对照MOTIVATE临床研究数据，美国FDA常规批准马拉维若上市则需要长期的研究报告。

在临床研究中．马拉维若片组因不良反应停药率(3．8％)与OBT加安慰剂组停药率(3．8％)相似。本品常见的不良反应是咳嗽、发热、上呼吸道感染、药疹、肌肉骨骼症状、腹痛和眩晕。

SELZENTRY（maraviroc）片剂，薄膜包衣

最初美国批准：2007

最近的重大变化

黑框警告，肝

警告和注意事项，肝损伤2011年7月
 
适应症
SELZENTRY是一个CCR5联合受体拮抗剂结合CCR5的嗜性HIV-1感染的成年人中的抗逆转录病毒治疗表示。

更多与SELZENTRY治疗科目经历病毒学失败和发展拉米夫定耐药与efavirenz相比。
取向高度敏感的取向分析测试需要的SELZENTRY的适当使用。
 
剂量和用法
当CYP3A的强有力的抑制剂包括PIS（除tipranavir /利托那韦），地拉韦啶，150毫克（有或没有强有力的CYP3A的诱导剂）每天两次
与NRTI的tipranavir /利托那韦，奈韦拉平，拉替拉韦，和其他不属于烈性CYP3A的抑制剂或CYP3A的诱导剂，300毫克的药物每天两次

与强大的CYP3A的诱导剂包括依非韦伦（没有一个强有力的CYP3A抑制剂），600毫克每天两次

一个更完整的清单，联合用药的药物剂量和给药方法上市。

肾功能不全患者可能需要调整剂量。

剂型和优势

片剂：150毫克和300毫克
 
禁忌
SELZENTRY不应该被用于严重肾功能不全或终末期肾脏病（ESRD）患者（肌酐清除率<30毫升/分钟）正在有力CYP3A的抑制剂或诱导剂。

注意事项：
伴随着肝损伤严重皮疹或全身过敏性反应，包括潜在的威胁生命的事件已报告。治疗期间SELZENTRY和在其他时间点开始临床肝实验室指标包括ALT，AST和胆红素应事先获得。如果皮疹或肝炎或过敏反应发展的症状或体征，肝实验室参数进行监测，并应考虑停药。管理SELZENTRY预现有的肝功能不全或病毒B型肝炎或C共同感染患者时谨慎使用
更多的心血管事件，包括心肌缺血和/或心肌梗死，观察治疗经验的受试者谁收到SELZENTRY。使用在心血管事件的风险增加患者慎用。
如果患者有严重肾功能不全或终末期肾脏疾病（ESRD）患者接受SELZENTRY（没有伴随CYP3A的诱导剂或抑制剂）体验体位性低血压;的SELZENTRY剂量应减少从300毫克至150毫克，每日两次，每日两次。
 
不良反应
治疗经验的科目（发生率> 8％）与安慰剂相比，在更高的频率发生的最常见的不良事件是上呼吸道感染，咳嗽，发热，皮疹，头晕。

报告疑似不良反应，1-800-FDA-1088或www.fda.gov / medwatch欢跃医疗致电1-877-844-8872或FDA

药物相互作用

CYP3A的抑制剂，包括蛋白酶抑制剂（除tipranavir /利托那韦）和地拉韦啶合用会增加的SELZENTRY浓度。

合用CYP3A的诱导剂，包括依非韦伦，可能会降低的SELZENTRY浓度。

在特殊人群中使用

SELZENTRY应该只用于孕妇潜在的好处，如果证明对胎儿的潜在危险。
有没有在儿科病人提供的数据，因此，SELZENTRY不应在<16岁的患者使用。

日期：11/2011

SELZENTRY

Basic Informations
Selzentry is a CCR5-blocking entry inhibitor manufactured by ViiV Healthcare. It was approved by the U.S. Food and Drug Administration (FDA) in August 2007. Selzentry is approved for treatment-experienced people who have HIV strains that are resistant to multiple antiretroviral drugs and for people with drug-sensitive HIV strains, such as those starting antiretroviral therapy for the first time.
In countries other than the U.S., maraviroc will be approved and sold under the brand name Celsentri.
Selzentry binds to a protein on the membrane of CD4 cells (CD4 cells) called CCR5. Once it does this, HIV cannot successfully attach itself to the surface of CD4 cells, and is thus prevented from infecting healthy cells.
Selzentry must be combined with other HIV drugs.
In addition to Selzentry's proven antiviral efficacy, it continues to be studied for its immune-based therapy potential, notably its effects on CD4 cell counts and inflammation.
Selzentry is available in 150 mg and 300 mg tablets and must be taken twice a day. Because of interactions with other medications, including some used to treat HIV, the Selzentry dose will need to be carefully determined:
CYP3A inhibitors: If Selzentry is combined with protease inhibitors (with the exception of Aptivus [tipranavir] plus Norvir [ritonavir]); the NNRTI Rescriptor (delavirdine); the antibiotics Biaxin (clarithromycin), Ketek (telithromycin), Nizoral (ketoconazole), or Sporanox (itraconazole); or the antidepressant Serzone (nefazodone), the correct dose is one 150 mg tablet twice a day.
CYP3A Inducers: If Selzentry is combined with the NNRTI Sustiva (efavirenz); the anticonvulsant (anti-seizure) medications Tegretol (carbamazepine), or phenobarbital; or the antibiotic Rifadin (rifampin), the correct dose is two 300mg tablets twice a day.
Other Medications: If Selzentry is combined with Aptivus/Norvir; the NNRTI Viramune (nevirapine); the entry inhibitor Fuzeon (enfuvirtide); any nucleoside reverse transcriptase inhibitors (without CYP3A inhibitors); the antibiotic Bactrim or Septra (TMP/SMX); or the sedative Versed (midazolam), the correct dose is one 300 mg tablet twice a day.
Selzentry holds promise for HIV-positive patients who no longer respond to other HIV drugs. Because Selzentry targets HIV differently than most currently available antiretrovirals, chances are that many people living with the virus?regardless of which drugs have failed them in the past?will likely benefit from using Selzentry. Two large clinical trials have determined that Selzentry, when combined with other drugs, is effective for patients whose virus has adapted to other HIV drugs used in the past. However, Selzentry worked best when it was combined with at least two other drugs that the virus was sensitive to (patients who used Selzentry in combination with drugs that their virus was highly resistant to did not experience decreases in their viral load for very long). For this reason, it is best to use drug-resistance testing to determine which drugs your virus is sensitive to; the results will show which antiretrovirals are best to combine with Selzentry.
Selzentry is also approved for people with HIV that have no, or limited, resistance to other available antiretroviral drugs. Selzentry is not considered a "preferred" or "alternative" option for first-time treatment takers by the U.S. Department of Health and Human Services in its HIV treatment guidelines. Instead, the DHHS considers Selzentry?combined with Combivir (zidovudine and lamivudine)?to be an "acceptable option but more definitive data are needed."
Drugs Interactions
Selzentry is broken down (metabolized) by the liver, like many medications used to treat HIV and AIDS. This means that Selzentry can interact with other medications. While it is not expected that the drug will lower or raise the levels of any other medications in the body, studies have shown that other drugs can affect levels of Selzentry in the body.
At the time of Selzentry's approval in August 2007, there were no known "contraindications," meaning that there are no known medications that must be avoided while taking Selzentry.
Anticonvulsants, such as Tegretol (carbamazepine), Luminal (phenobarbital), and Dilantin (phenytoin), can decrease the amount of Selzentry in the bloodstream.
Other HIV drugs can interact with Selzentry. Some HIV medications are "CYP3A inhibitors," meaning that they slow the ability of certain enzymes that are responsible for metabolizing, or breaking down, Selzentry in the body. Some HIV medications are "CYP3A inducers," meaning that they can speed up the metabolism of Selzentry in the body. Still others do not have a significant effect on CYP3A enzymes. The dose of Selzentry will need to be adjusted, depending on which HIV medications are being used.
Selzentry can interact with some medications used to treat TB, MAC, and other bacterial infections. Rifadin (rifampin) can decrease Selzentry levels, meaning that the Selzentry dose (provided that CYP3A inhibitors are not being used as well) should be 600 mg (two 300 mg tablets) twice a day. Biaxin (clarithromycin) increases Selzentry levels, requiring a Selzentry dose of one 150 mg tablet twice a day.
Selzentry can interact with some medications used to treat thrush (candidiasis) and other fungal infections. Nizoral (ketoconazole) and Sporanox (itraconazole) can increase Selzentry levels in the bloodstream. If these medications are used, the Selzentry dose should be one 150 mg tablet twice a day.
Other medications, including those known to have a strong inhibitory effect on CYP3A enzymes, can interact with Selzentry and may require dosing adjustments. Tell your doctors and pharmacists about all medicines you take. This includes those you buy over-the-counter and herbal or natural remedies. Bring all your medicines when you see a doctor, or make a list of their names, how much you take, and how often you take them. Your doctor can then tell you if you need to change the dosages of any of your medications.
People with kidney problems may need to adjust their Selzentry dose when they combine it with other medications. Both those that increase and decrease CYP3A enzymes, and a host of other medications that include Aptivus with Norvir, Viramune, Isentress, Fuzeon and all nucleoside reverse transcriptase inhibitors (NRTIs).
Side Effects
The most common side effects associated with Selzentry therapy in clinical trials involving treatment-experienced patients were cough, fever, colds, rash, muscle and joint pain, stomach pain, and dizziness.
Although there hasn't been an overall increase in serious liver problems in patients treated with Selzentry in clinical trials, liver toxicity has been seen in some patients using the drug. Certain allergy-like signs and symptoms?for example, rash, an increase in the number of eosinophils (a type of white blood cell) or elevated IgE antibodies?prior to the development of liver toxicity may occur. If these signs or symptoms occur while taking Selzentry, patients should be evaluated immediately.
People with severe kidney problems and end-stage kidney disease should not take Selzentry if they are also taking other medication that affects levels of the CYP3A liver enzyme.
In clinical trials, more cardiovascular events, including heart attacks, were seen in patients receiving Selzentry as compared to placebo. In turn, the manufacturer and the FDA are recommending that the drug be used with caution in patients at increased risk for cardiovascular events.

Because Selzentry blocks the CCR5 coreceptor located on some immune system cells, there is a theoretical risk of developing infections and cancers. However, rates of infections and cancer were no higher among patients receiving Selzentry, versus those receiving placebo, in year-long clinical trials.