European Commission Approves Gilead’s Vitekta™, an Integrase Inhibitor for the Treatment of HIV-1 Infection

  European Commission Approves Gilead’s Vitekta™, an Integrase Inhibitor for
  the Treatment of HIV-1 Infection

Business Wire

FOSTER CITY, Calif. -- November 18, 2013

Gilead Sciences, Inc. (Nasdaq: GILD) today announced that the European
Commission has granted marketing authorization for Vitekta™ (elvitegravir 85
mg and 150 mg) tablets, an integrase inhibitor for the treatment of HIV-1
infection in adults without known mutations associated with resistance to
elvitegravir. Vitekta is indicated for use as part of HIV treatment regimens
that include a ritonavir-boosted protease inhibitor. Vitekta interferes with
HIV replication by blocking the virus from integrating into the genetic
material of human cells. In clinical trials, Vitekta was effective in
suppressing HIV among patients with drug-resistant strains of HIV.

“Vitekta offers people with HIV who have failed prior therapy or who have
developed drug resistance an important new treatment option,” said Norbert
Bischofberger, PhD, Executive Vice President, Research and Development and
Chief Scientific Officer, Gilead Sciences. “Vitekta is only the second
integrase inhibitor to become available in the European Union. Today’s
approval exemplifies Gilead’s ongoing commitment to meeting the evolving needs
of people living with HIV.”

Vitekta has been approved in two doses: an 85 mg tablet is indicated for use
with the ritonavir-boosted protease inhibitors atazanavir 300 mg and lopinavir
400 mg; and a 150 mg tablet is indicated for use with the ritonavir-boosted
protease inhibitors darunavir 600 mg and fosamprenavir 700 mg. The approval is
supported by 96-week data from a Phase 3 study (Study 145) in which Vitekta
dosed once daily was found to be non-inferior to the integrase inhibitor
raltegravir dosed twice daily, each administered with a background regimen
that included a fully active ritonavir-boosted protease inhibitor and a second
antiretroviral agent. Patients enrolled in the trial were required to have
genotypic HIV drug resistance or at least six months of treatment experience
with two or more different classes of antiretrovirals.

Vitekta was well tolerated in clinical studies and most adverse reactions were
mild to moderate. The most common adverse reactions (all grades) observed were
diarrhea (7.1 percent) and nausea (4 percent); please see additional Important
Safety Information below.

Vitekta is also a component of Gilead’s Stribild^® (elvitegravir 150
mg/cobicistat 150 mg/emtricitabine 200 mg/tenofovir disoproxil fumarate 300
mg), a once-daily single tablet regimen for HIV that was approved in the
United States in August 2012 for treatment-naïve adults and by the European
Commission in May 2013 for adults who are treatment-naïve or who have no known
mutations associated with resistance to any of the three antiretroviral agents
in Stribild. Gilead submitted a new drug application to the U.S. Food and Drug
Administration (FDA) for Vitekta as a single agent in June 2012 and received a
Complete Response Letter in April 2013. Gilead is working on resubmitting the
application to the FDA.

About Vitekta

Vitekta was licensed by Gilead from Japan Tobacco Inc. (JT) in March 2005.
Under the terms of Gilead’s agreement with JT, Gilead has exclusive rights to
develop and commercialize Vitekta as a single agent in all countries of the
world, excluding Japan, where JT retains rights.

Indication and Important Safety Information about Vitekta

Vitekta co-administered with a ritonavir-boosted protease inhibitor and with
other antiretroviral agents, is indicated for the treatment of human
immunodeficiency virus-1 (HIV-1)infection in adults who are infected with
HIV-1 without known mutations associated with resistance to elvitegravir.

Elvitegravir-resistant viruses show cross-resistance to the integrase strand
transfer inhibitor raltegravir in most cases. Elvitegravir has a relatively
low genetic barrier to resistance. Therefore, whenever possible, Vitekta
should be administered with a fully active ritonavir-boosted protease
inhibitor and a second fully active antiretroviral agent to minimise the
potential for virologic failure and the development of resistance.

Elvitegravir is primarily metabolised by CYP3A. Co-administration of Vitekta
with strong CYP3A inducers (including St.John’s wort [Hypericum perforatum],
rifampicin, carbamazepine, phenobarbital and phenytoin) is contraindicated.
Co-administration of Vitekta with moderate CYP3A inducers (including, but not
limited to, efavirenz and bosentan) is not recommended.

Due to the need for co-administration of Vitekta with a ritonavir-boosted
protease inhibitor, prescribers should consult the Summary of Product
Characteristics of the co-administered protease inhibitor and ritonavir for a
description of contraindicated medicinal products and other significant
drug-drug interactions that may cause potentially life-threatening adverse
reactions or loss of therapeutic effect and possible development of
resistance.

Atazanavir/ritonavir and lopinavir/ritonavir have been shown to significantly
increase the plasma concentrations of elvitegravir. When used in combination
with atazanavir/ritonavir and lopinavir/ritonavir, the dose of Vitekta should
be decreased from 150mg once daily to 85mg once daily. Vitekta must be used
in combination with a ritonavir-boosted protease inhibitor. Vitekta should not
be used with a protease inhibitor boosted by another agent as dosing
recommendations for such combinations have not been established. Boosting
elvitegravir with an agent other than ritonavir may result in suboptimal
plasma concentrations of elvitegravir and/or the protease inhibitor leading to
loss of therapeutic effect and possible development of resistance.

Vitekta should not be used in combination with products containing
elvitegravir or pharmacokinetic boosting agents other than ritonavir.

Female patients of childbearing potential should use either a hormonal
contraceptive containing at least 30µg ethinylestradiol and containing
norgestimate as the progestagen or should use an alternative reliable method
of contraception. Co-administration of elvitegravir with oral contraceptives
containing progestagens other than norgestimate have not been studied and,
therefore, should be avoided. Patients using oestrogens as hormone replacement
therapy should be clinically monitored for signs of oestrogen deficiency.

Elvitegravir has not been studied in patients with severe hepatic impairment
(Child-Pugh ClassC). No dose adjustment of Vitekta is required in patients
with mild (Child-Pugh ClassA) or moderate hepatic impairment (Child-Pugh
ClassB).

Immune Reactivation Syndrome has been reported in patients treated with
combination therapy.

Vitekta contains lactose. Consequently, patients with rare hereditary problems
of galactose intolerance, the Lapp lactase deficiency, or glucose-galactose
malabsorption should not take this medicinal product.

About Gilead Sciences

Gilead Sciences is a biopharmaceutical company that discovers, develops and
commercializes innovative therapeutics in areas of unmet medical need. The
company's mission is to advance the care of patients suffering from
life-threatening diseases worldwide. Headquartered in Foster City, California,
Gilead has operations in North and South America, Europe and Asia Pacific.

Forward-Looking Statement

This press release includes forward-looking statements, within the meaning of
the Private Securities Litigation Reform Act of 1995, that are subject to
risks, uncertainties and other factors, including the risk that physicians may
not see advantages of Vitekta over other HIV therapies and may therefore be
reluctant to prescribe the product. In addition, pending marketing
applications for Vitekta in the United States and other regions may not be
approved or approval may be delayed, and marketing approvals, if granted, may
have significant limitations on their use. These risks, uncertainties and
other factors could cause actual results to differ materially from those
referred to in the forward-looking statements. The reader is cautioned not to
rely on these forward-looking statements. These and other risks are described
in detail in Gilead’s Quarterly Report on Form 10-Q for the quarter ended
September 30, 2013, as filed with the U.S. Securities and Exchange Commission.
All forward-looking statements are based on information currently available to
Gilead, and Gilead assumes no obligation to update any such forward-looking
statements.

 EU Summary of Product Characteristics for Vitekta and Stribild are available
                       at http://www.ema.europa.eu/ema/

 U.S. full prescribing information for Stribild, including BOXED WARNING, is
                         available at www.gilead.com.

    Vitekta and Stribild are trademarks or registered trademarks of Gilead
                                Sciences, Inc.

For more information on Gilead Sciences, please visit the company’s website at
  www.gilead.com, follow Gilead on Twitter (@GileadSciences) or call Gilead
             Public Affairs at 1-800-GILEAD-5 or 1-650-574-3000.

Contact:

Gilead Sciences, Inc.
Patrick O’Brien, Investors, 650-522-1936
Arran Attridge, Media (EU), +44 (208) 587-2477
Cara Miller, Media (US), 650-522-1616
 
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