据世界卫生组织报道显示，自1981年发现和报告艾滋病以来，全球感染者累计6900万人，其中死亡人数占40％，每年约新增500多万HIV感染染病例，目前HIV/AIDS患者总数达4200多万人，若不能有效的预防控制，预计20年后HIV感染者将达2亿人。从地域上看，在撒哈拉以南的非洲地区的患者占据了70％，而病死率已达八成；在拉丁美洲和加物比地区流行率也较高，60％感染者失去生命，而亚洲也已呈现出快速蔓延的趋势。

艾滋病是由人免疫缺陷病毒（HIV）感染导致人体防御机能缺陷，而易于发生感染和肿瘤的临床综合症。HIV是单股RNA病毒，分为HIV-1和HIV-2两种。在世界范围内的HIV以HIV-1为主，占95%，HIV-2集中在西非地区。HIV病毒密码通过逆转录酶（reverse transcriptase）蛋白酶（protease）和整合酶（integrase）来表达。HIV一旦进入靶细胞，病毒RNA就在逆转录酶作用下逆转录为DNA，从而进行繁殖。因此，逆转录酶抑制剂是最早开发的抗HIV品种。最先用于临床的齐多呋啶（AZT）就是种逆转录酶抑制剂。

最近，Gilead 科技公司宣布欧洲委员会已经批准其可以对新药Eviplera进行市场推广。Eviplera是用量一日一片，用于进行成年艾滋病1型初治患者（病毒载量小于或等于10万艾滋病毒RNA拷贝/毫升）感染抗逆转病毒治疗。 欧洲委员会允许Eviplera在欧盟区27个国家进行市场商业化推广。

Eviplera 结合了Truvada的功效。Truvada是全世界最大的艾滋病药物生产商吉利德科学公司生产的一款常规药片，有助于防止同性恋或者双性恋男性感染HIV，研究显示，2004年开始作为抑制已经感染艾滋病患者病毒蔓延的药物，Truvada能够将HIV的风险降低44%。

Eviplera 是由两种核苷类逆转录酶抑制剂恩曲他滨200mg和245mg毫克替诺福韦以及Tibotec医药公司25mg利匹韦林组成的固定剂量药物。

治疗艾滋病新药Eviplera主要成分——恩曲他滨临床介绍
恩曲他滨是由美国抗病毒药物的专业开发公司Gilead Sciences公司作为抗HIV、HBV药物开发的新产品。2003年7月，恩曲他滨（Emtriva）在美国被批准用于与其它抗转录病毒药物联用于成人HIV-1感染的治疗 。Emtriva是一种最新的核苷类逆转录酶抑制剂，这也是Gilead Sciences公司所开发的继Viread（tenofovir disoproxil fumarate）之后第二个每日给药一次的治疗艾滋病的抗逆转录病毒药物。

治疗艾滋病新药Eviplera主要成分——替诺福韦临床介绍
替诺福韦是一种核苷酸类逆转录酶抑制剂，以与核苷类逆转录酶抑制剂类似的方法抑制逆转录酶，从而具有潜在的抗HIV－1的活性。本品的活性成分替诺福韦双磷酸盐可通过直接竞争性地与天然脱氧核糖底物相结合而抑制病毒聚合酶，及通过插入DNA中终止DNA链。在体外，本品可有效对抗多种病毒，包括那些对核苷类逆转录酶抑制剂耐药的毒株。

治疗艾滋病新药Eviplera主要成分——利匹韦林临床介绍
利匹韦林属于所谓的非核苷类逆转录酶抑制剂（NNRTI）类抗艾滋药物。该药物通过阻断HIV病毒复制来起作用。Edurant将用作高活性抗逆转录病毒治疗（HAART）方案的一部分，该方案旨在用来抑制血液中的艾滋病病毒量（病毒载量）。Edurant这种丸剂每日随餐服用一次。

治疗艾滋病新药Eviplera临床数据：为期48周的第二阶段双盲、主动控制、随机研究是由Tibotec公司负责的，正因为试验很好地验证了利匹韦林的药效和安全性，所以得到了欧盟的上市批准。

Eviplera–Treatment for HIV, United States of America

Eviplera is a single-pill regimen targeted at human immunodeficiency virus-1 (HIV-1). It combines the active substances emtricitabine, rilpivirine and tenofovir disoproxil.

Developed by Gilead Sciences International in collaboration with Tibotec, eviplera is approved in the US under the trade name Complera. It was approved by the European Medicines Agency in November 2011.

What human immunodeficiency virus (HIV) does to the body

HIV is responsible for causing acquired immune deficiency syndrome (AIDS) which destroys the immune system if left untreated. There are two types of the virus - HIV-1 and HIV-2. Compared to HIV-1, immunodeficiency develops at a slower rate in HIV-2 patients.

Both types of HIV damage a person's immune system by destroying blood cells called CD4 or T cells, which help the body fight diseases. People infected with HIV develop flu-like symptoms which remain for several days, while others may not show any symptoms at all. Although the symptoms may not be visible, HIV affects a person internally.

An estimated 34 million people across the world are currently living with HIV-1. There is no complete cure available for HIV.

Current treatment options available for HIV involve taking multiple medications, known as combination therapy. This treatment helps reduce the amount of HIV or viral load in a patient's body.

Combination therapy earlier involved taking nearly 20 or more pills throughout the day. The treatment options, however, have improved over the years, including coformulated medicines. These treatment methods help in simplifying the dosage regimen and reduce HIV drug resistance.

Eviplera (complera), enzyme inhibiting treatment for HIV
Emtricitabine and tenofovir disoproxil are nucleoside reverse transcriptase inhibitors (NRTIs) and rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). The three active substances are available as individual medicines - Emtriva (emtricitabine), Viread (tenofovir disoproxil fumarate) and Edurant (rilpivirine).

The active substances work by inhibiting the activity of reverse transcriptase, an enzyme produced by HIV. The enzyme multiplies and infects CD4 cells. Eviplera inhibits the enzyme and reduces the level of HIV in the blood.

It enables patients to maintain HIV at low levels in the body with a viral load = 100,000 HIV-1 RNA copies/ml.

Eviplera does not cure HIV infection or Aids but it helps in slowing the damage caused by the virus to the immune system. It also helps in preventing the development of infections and diseases associated with Aids.

Clinical trials on the combined / coformulated HIV single-pill regimen
Clinical testing of eviplera included two Phase IIa studies, one Phase IIb study and two pivotal Phase III studies.

Phase IIa studies were monotherapies conducted to confirm rilpivirine's antiviral activity. One study was conducted in 47 treatment-naive patients and the second in 36 treatment experienced patients. Both studies established the efficacy of rilpivirine, based on which the Phase IIb study was conducted.

The Phase IIb study was a randomised, active controlled, partially blind trial conducted in 368 patients. Three doses of rilpivirine were administered during a 96 week period.

Both Phase III trials of eviplera were randomised, double-blind studies. The first study, C209 (ECHO), recruited 690 patients with HIV-1 and compared eviplera with Efavirenz. Results from the study indicated that 83% patients responded to eviplera treatment when compared to 84% of patients who were administered efavirenz.

The second Phase III trial, C215 (THRIVE), recruited 678 patients and compared rilpivirine with efavirenz. The results of the study showed that 87% of the patients administered with rilpivirine responded to the treatment, compared to 83% of the patients administered with efavirenz.

Marketing commentary for HIV treatments such as eviplera
Demand for single-pill antiretroviral treatments has increased over the years due their ability to control HIV and promote patient adherence. These treatments have transformed HIV / Aids into a more manageable condition for patients.

Newer single-pill treatments are also being considered as more effective. The global market for HIV drugs is expected to grow at an average of 4.5% between 2008 and 2015. Although demand is set to grow, competition from generic and cheaper versions of expensive drugs is eroding some of the profits of big pharmaceutical companies.

Gilead's Atripla HIV drug holds nearly two-thirds share in the market. Approval of eviplera, whose patent does not expire until 2023, will further strengthen Gilead's market position.

规格与剂型
30片/瓶