ViiV HIV新药Tivicay获加拿大批准

兰素史克（GSK）和辉瑞（Pfizer）合资公司ViiV Healthcare 11月4日宣布，HIV新药Tivicay（dolutegravir，50mg片剂）已获加拿大卫生部批准，该药为HIV整合酶链转移抑制剂，旨在与其他抗逆转录病毒药物联合用药，用于HIV-1成人感染者和体重大于40千克的12岁及以上儿童感染者的治疗。

此前，Tivicay于2013年8月12日，获FDA批准，与其他抗逆转录病毒制剂联合用于既往已治疗过、或初治HIV-1成人和12岁及以上体重至少40千克儿童感染者。

支持Tivicay新药申请的数据，包括多个非临床研究、临床药理学研究、以及4个关键性III期临床试验的数据。

Tivicay的服用，无需药代动力学助推剂，可空腹或与食物一起服用，并且可在一天的适合时间服用。

关于III期临床项目：

SPRING-2：在822例HIV感染者中开展，评价了每天1次Tivicay与每天2次raltegravir（拉替拉韦）与一种固定剂量双NRTI疗法联合治疗的疗效。48周时，含Tivicay方案有88%的患者实现病毒学抑制（HIV-1 RNA<50 c/ml），含raltegravir方案为86%，达到了10%的非劣性标准。

SINGLE：在833例初治HIV感染者中开展，评价了每天1次Tivicay+阿巴卡韦/拉米夫定相对于单一片剂Atripla的疗效。48周时，含Tivicay方案有88%的患者实现病毒学抑制（HIV-1 RNA<50 c/ml），Atripla方案为81%，数据具有统计学显着差异。Tivicay方案组有2%患者因不良事件中止治疗，Atripla方案组为10%。

SAILING：在719例经当前疗法治疗失败但未使用整合酶抑制剂治疗的患者中开展，评价了每天1次Tivicay和每天2次raltegravir（拉替拉韦）结合一种背景方案（2种制剂，其中至少1种完全活性剂）的疗效。24周时，含Tivicay方案有79%的患者实现病毒学抑制（HIV-1 RNA<50 c/ml），含raltegravir方案为70%，数据具有统计学显着差异。

VIKING-3：在183例正在接受治疗、且HIV已对数类HIV药物（包括整合酶抑制剂雷特格韦和/或elvitegravir）的成人感染者中开展。该项研究中，背景方案中添加Tivicay治疗7天后，HIV RNA水平下降达1.4 log10 c/ml。24周时，添加Tivicay方案有63%的患者实现病毒学抑制（HIV-1 RNA<50 c/ml）。

批准Tivicay用于12岁及以上、体重至少40千克儿童的适应症，是基于一项多中心、开发标签试验的安全性、药代动力学、药效评价数据。该项研究在既往未接受过整合酶抑制剂治疗的患者中开展。

Dolutegravir是日服一次的药物，在III期临床试验中表现强劲，达到了与默沙东（Merck & Co）HIV/AIDS药物Isentress相匹敌的疗效。Isentress日服2次，这2者均为HIV整合酶的抑制剂，这是一类对抗HIV/AIDS的新型药物，能够阻止HIV病毒进入细胞。

分析师预计，dolutegravir有望成为年销售额达数十亿美元的重磅药物，同时将成为吉利德科学（Gilead Sciences）相关药物的强有力竞争者。

ViiV医疗保健公司是葛兰素史克（GSK）和辉瑞（Pfizer）于2009年联合成立的HIV/AIDS药物研发公司，目前，GSK持有ViiV 76.5%的股份，辉瑞持有10%的股份，日本盐野义（Shionogi）持有10%的股份。

英文原文：ViiV Healthcare receives approval for Tivicay? (dolutegravir) in Canada for the treatment of HIV

MISSISSAUGA, ON , Nov. 4, 2013 /CNW/ - ViiV Healthcare has received approval in Canada for Tivicay? (dolutegravir) 50-mg tablets, an Integrase Strand Transfer Inhibitor indicated for use in combination with other antiretroviral agents for the treatment of human immunodeficiency virus (HIV) infection in adults and children 12 years of age and older and weighing at least 40 kg.1

"HIV is a complicated and devastating disease," said Gregory Reinaud, General Manager Canada , ViiV Healthcare. "Through ongoing research, our singular focus is to support people living with HIV by providing new treatment options. The life expectancy of Canadians living with HIV has never been higher, and so the choice of long-term treatment is more sensitive and challenging than ever. Today's Health Canada approval of Tivicay demonstrates ViiV Healthcare's absolute commitment to the HIV/AIDS response both globally and here at home."

Since HIV reporting began in Canada in 1985, a total of 74,174 Canadians have been diagnosed with HIV.2 According to a 2010 survey, of those people being treated for HIV, over one-third (36%) in North America did not like how their medicines made them feel.3

The data submitted in support of the use of Tivicay included results from a comprehensive program of non-clinical studies, clinical pharmacology studies, and four pivotal phase III clinical trials that covered the HIV treatment spectrum, and included data in children aged 12 years and older. Canadian trial sites were located in Vancouver , Calgary , Edmonton , Winnipeg , Hamilton , Toronto , Ottawa and Montreal . Tivicay was used without a pharmacokinetic boosting agent. Tivicay can be taken with or without food and at any time of the day.

"In many regimens, the differentiating component is the third agent. Tivicay provides a new opportunity for healthcare professionals to choose the right regimen for their patients, providing a focal point around which to individualize therapy," said Dr John Pottage , Chief Medical Officer, ViiV Healthcare. "HIV treatment should not be a 'one-size fits all' paradigm."

The indication in children aged 12 years and older is based on an evaluation of safety, pharmacokinetics and efficacy of a once-daily Tivicay-based regimen through 24 weeks in a multi-centre, open-label trial in patients who had not previously been treated with integrase inhibitors.1

"As HIV has become a chronic disease, and people now are living for a long time with the disease, we know that new medicines will always be needed. At ViiV Healthcare we listen to patients and physicians to truly understand the unmet needs in HIV. Today's approval of Tivicay is the first medicine from the ViiV Healthcare pipeline, and I look forward to seeing the future developments of our HIV science," said Pottage.

About Tivicay? (dolutegravir)

Tivicay is an integrase inhibitor indicated for use in combination with other antiretroviral agents for the treatment of HIV in adults and children aged 12 years and older.1 Integrase inhibitors block HIV replication by preventing the viral DNA from integrating into the genetic material of human immune cells (T-cells).1 This step is essential in the HIV replication cycle and is also responsible for establishing chronic infection.1

It is available as a small, yellow, 50-mg tablet and can be taken with or without food, and at any time of the day.1

Tivicay is the first new treatment delivered globally and in Canada by ViiV Healthcare.

About ViiV Healthcare

ViiV Healthcare is a global specialist HIV company established in November 2009 by GlaxoSmithKline (GSK.L) and Pfizer (PFE) dedicated to delivering advances in treatment and care for people living with HIV. Shionogi joined as a 10% shareholder in October 2012 . The company's aim is to take a deeper and broader interest in HIV/AIDS than any company has done before and take a new approach to deliver effective and new HIV medicines, as well as support communities affected by HIV.