Gilead Receives Approval in Canada for BIKTARVY™ (bictegravir, emtricitabine, tenofovir alafenamide) for the Treatment of HIV-1 Infection

  • In clinical trials, BIKTARVY demonstrated high efficacy, and a high
    barrier to resistance
  • BIKTARVY offers a demonstrated tolerability profile, and few
    drug-drug interactions
  • BIKTARVY is the smallest INSTI-based triple-therapy single tablet
    regimen available

MISSISSAUGA, Ontario–(BUSINESS WIRE)–Gilead Sciences Canada, Inc. (Gilead Canada) today announced that Health
Canada has granted a Notice of Compliance (NOC) for Biktarvy™
(bictegravir 50mg/emtricitabine 200mg/tenofovir alafenamide 25mg,
BIC/FTC/TAF), a once-daily single tablet regimen (STR) for the treatment
of HIV-1 infection. BIKTARVY combines the potency of a novel integrase
strand transfer inhibitor (INSTI) bictegravir, with the demonstrated
safety and efficacy profile of the Descovy® (FTC/TAF) dual
nucleoside reverse transcriptase inhibitor (NRTI) backbone, and is the
smallest INSTI-based triple-therapy STR available. BIKTARVY is Gilead’s
third DESCOVY-based STR approved in Canada in the past three years.

BIKTARVY is indicated as a complete regimen for the treatment of HIV-1
infection in adults with no known substitution associated with
resistance to the individual components of BIKTARVY. No dosage
adjustment is required in patients with estimated creatinine clearance
greater than or equal to 30 mL per minute.

“To help support the long-term health of people living with HIV, it is
ideal that treatment regimens deliver both durable viral suppression and
a demonstrated tolerability profile,” said Dr. Jason Brunetta,
Operations and Finance Director at Maple Leaf Research, a treating
physician at Maple Leaf Medical Clinic, and a Principal Investigator on
BIKTARVY clinical trials. “In clinical trials through 48 weeks, BIKTARVY
has shown high efficacy and zero resistance. With convenient dosing and
few pre-screening or ongoing monitoring requirements, BIKTARVY will
simplify treatment initiation, and follow-up, over time.”

The approval of BIKTARVY is supported by data from four ongoing Phase 3
studies: Studies 1489 and 1490 in treatment-naïve HIV-1 infected adults,
and Studies 1844 and 1878 in virologically suppressed adults. These
trials are comprised of a diverse population of 2,414 participants,
including a wide range of adult age groups and races/ethnicities.
BIKTARVY met its primary objective of non-inferiority at 48 weeks across
all four studies. Through 48 weeks, no participants in any of the four
studies failed BIKTARVY with treatment-emergent virologic resistance, no
patients discontinued BIKTARVY due to renal adverse events and there
were no cases of proximal renal tubulopathy or Fanconi syndrome. The
most common adverse reactions in patients taking BIKTARVY were diarrhea,
nausea and headache.

In Study 1489, a total of 629 treatment-naïve adults with HIV were
randomized 1:1 to receive BIKTARVY or abacavir/dolutegravir/lamivudine
(600/50/300mg) (ABC/DTG/3TC) once daily. At Week 48, 92 per cent
(n=290/314) of patients taking BIKTARVY and 93 per cent (n=293/315) of
patients taking ABC/DTG/3TC achieved the primary endpoint of HIV-1 RNA
<50 c/mL. In Study 1490, a total of 645 treatment-naïve adults with HIV were randomized 1:1 to receive BIKTARVY or DTG+FTC/TAF. At Week 48, 89 per cent (n=286/320) of patients taking BIKTARVY and 92 per cent (n=302/325) of patients taking DTG+FTC/TAF achieved the primary endpoint of HIV-1 RNA <50 c/mL.

In Study 1878, a total of 577 virologically suppressed (HIV-1 RNA <50 c/mL) adults with HIV taking regimens of a boosted protease inhibitor (bPI; atazanavir or darunavir) plus a dual-NRTI backbone (ABC/3TC or FTC/tenofovir disoproxil fumarate) were randomized 1:1 to continue their bPI regimen or to switch to open-label coformulated BIKTARVY once daily. At the primary endpoint of Week 48, switching to BIKTARVY was non-inferior to continuing on a bPI regimen with 2 per cent of patients in each group having HIV-1 RNA ≥50 c/mL; the proportion of patients with HIV-1 RNA <50 c/mL was 92 per cent in the BIKTARVY arm and 89 per cent in the bPI arm, according to FDA snapshot algorithm.

In Study 1844, a total of 563 virologically suppressed adults with HIV
taking a regimen containing abacavir, dolutegravir and lamivudine
(600/50/300mg) (ABC/DTG/3TC) were randomized 1:1 in a blinded fashion to
continue a once-daily fixed-dose combination of ABC/DTG/3TC or to switch
to BIKTARVY, to evaluate the efficacy and safety of switching from a
regimen to BIKTARVY. Through Week 48, BIKTARVY was found to be
statistically non-inferior to ABC/DTG/3TC with a numerically lower
incidence of mild or moderate study drug-related adverse events and no
treatment-emergent resistance.

“Gilead Canada is committed to improving care and simplifying therapy
for people living with HIV. We continue to invest in research in
next-generation treatments, including the ultimate goal of therapies
that could potentially cure HIV infection in patients,” said Kennet
Brysting, General Manager, Gilead Canada. “We are pleased to offer
BIKTARVY, our latest triple-therapy treatment, which brings together the
potency of an integrase inhibitor with guideline-recommended dual-NRTI
backbone of DESCOVY in a once-daily single tablet regimen.”

Additional clinical trials of BIKTARVY are ongoing, including a
dedicated study in women, as well as a study in adolescents and children
living with HIV.

BIKTARVY does not cure HIV infection or AIDS.

Important Safety Information

BIKTARVY has serious warnings and precautions in its product label
including the risk of post-treatment acute exacerbation of hepatitis B
in patients who are co-infected with HIV-1 and HBV and have discontinued
products containing emtricitabine (FTC) and/or tenofovir disoproxil
fumarate (TDF), and may occur with discontinuation of BIKTARVY. Prior
to, or when initiating BIKTARVY, healthcare professionals should test
for hepatitis B virus infection, and closely monitor hepatic function
with both clinical and laboratory follow-up for at least several months
in patients who are co-infected with HIV-1 and HBV and discontinue
BIKTARVY. Patients with chronic hepatitis B or C and treated with
antiretroviral therapy are at increased risk for severe hepatic adverse
events.

BIKTARVY should not be co-administered with any other antiretroviral
products including those containing bictegravir, emtricitabine and
tenofovir alafenamide, or those containing lamivudine or tenofovir
disproxil fumarate. BIKTARVY should not be administered with adefovir
dipivoxil.

For all important safety information, including contraindications,
additional warnings and precautions, adverse reactions and drug
interactions, please see the Canadian Product Monograph at www.gilead.ca.

About Gilead Sciences

Gilead Sciences, Inc. (Gilead) 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. Gilead has operations
in more than 35 countries worldwide, with headquarters in Foster City,
California. Gilead Sciences Canada, Inc. is the Canadian affiliate of
Gilead Sciences, Inc., and was established in Mississauga, Ontario, in
2006.

For nearly 30 years, Gilead has been a leading innovator in the field of
HIV, driving advances in treatment, prevention, testing and linkage to
care, and cure research. Today, it’s estimated that more than 10 million
people living with HIV globally receive antiretroviral therapy provided
by Gilead or one of the company’s manufacturing partners.

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 the benefits of prescribing BIKTARVY and the
possibility of unfavorable results from additional clinical trials
involving BIKTARVY. 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
March 31, 2018, 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.

Canadian Product Monograph for BIKTARVY™, including Boxed Warning, is
available at
www.gilead.ca.

BIKTARVY, DESCOVY, Gilead, and the Gilead logo are trademarks of
Gilead Sciences, Inc., or its related companies.

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.

Contacts

FOR MORE INFORMATION IN CANADA:
Gilead Sciences Canada, Inc.
Karen
M. Chow, 905-363-8083
National Stakeholder Relations and
Communications