– Novel Investigational Combination Regimen
is Advancing to Phase 3 and has the Potential to Become the
First Weekly Oral HIV Treatment –
Gilead Sciences, Inc. (Nasdaq: GILD) and Merck (NYSE: MRK),
known as MSD outside of the United States and Canada, today
announced new results from a Phase 2 clinical study evaluating the
investigational combination of islatravir, an investigational
nucleoside reverse transcriptase translocation inhibitor, and
lenacapavir, a first-in-class HIV-1 capsid inhibitor. These
late-breaking data were presented during an oral session at
IDWeek 2024, taking place in Los Angeles, and virtually,
from October 16-19.
At 48 weeks, the novel investigational combination maintained a
high rate (n=49; 94.2%) of viral suppression (HIV-1 RNA <50
copies/mL) in virologically suppressed adults, a secondary endpoint
of the study. Zero participants had a viral load of ≥50 copies/mL
at Week 48. Week 24 results, including the study’s primary
endpoint, were previously presented at the 31st Conference on
Retroviruses and Opportunistic Infections (CROI).
“The future of HIV treatment is person-centered, with
long-acting options tailored to help meet the needs and preferences
of people affected by HIV,” said Jared Baeten, MD, PhD, Senior Vice
President, Virology Therapeutic Area Head, Gilead Sciences. "There
is no ‘one size fits all’ approach. The complexities of HIV care
require putting people first in the development of biomedical
innovations as we keep striving to offer options for all those
living with HIV. These data presented at IDWeek demonstrate our
commitment to continuous scientific discovery aimed at further
transforming the HIV treatment landscape.”
In this open-label, active-controlled study (NCT05052996),
virologically suppressed adults (n=104) on Biktarvy® (bictegravir
50 mg/emtricitabine 200 mg/tenofovir alafenamide 25 mg tablets,
B/F/TAF) were randomly allocated in a 1:1 ratio to receive either
oral islatravir 2 mg and lenacapavir 300 mg once a week (n=52) or
to continue daily oral Biktarvy (n=52). The median age of
participants was 40 years (20-76). Eighteen percent of participants
were assigned female at birth, 50% were non-white, and 29% were
Latine.
The proportion of individuals with HIV-1 RNA <50 c/mL at Week
48 by FDA snapshot algorithm (a secondary endpoint), showed that
participants who switched to treatment with once-weekly islatravir
and lenacapavir (ISL + LEN) or continued Biktarvy maintained
comparable high rates of HIV suppression at Week 48 (94.2% v.
92.3%, respectively). No participants treated with either ISL + LEN
or Biktarvy had a viral load of ≥ 50 copies/mL at Week 48 (another
secondary endpoint).
Treatment-related-adverse events (TRAEs), as attributed by study
investigator, were experienced by 19.2% of participants (n=10/52)
in the ISL + LEN group and the most common were dry mouth (n=2/52;
3.8%) and nausea (n=2/52; 3.8%). TRAEs were reported by 5.8% of
participants in the Biktarvy group (n=3/52). No grade 3 or 4 TRAEs
related to the study drug were reported in either treatment group.
Two participants (n=2/52; 3.8%) discontinued ISL + LEN due to
adverse events unrelated to the drug. At Week 48 no significant
differences were seen between treatment groups in mean change from
baseline in CD4+ T-cell counts or absolute lymphocyte counts. No
participants discontinued due to a decrease in CD4+ T-cell or
lymphocyte counts.
“Daily single-tablet regimens have helped to transform HIV care
but can be challenging for some people to maintain. Novel HIV
treatment options that allow for less frequent oral dosing have the
potential to help support adherence, and address stigma faced by
some individuals taking daily oral therapy,” said Dr. Elizabeth
Rhee, Vice President, Global Clinical Development, Merck Research
Laboratories. “We are pleased to see these encouraging 48-week data
for this once-weekly oral combination regimen and advance to phase
3 clinical trials in collaboration with Gilead.”
Along with these most recent study results, the potent antiviral
activities, and pharmacokinetic profiles of islatravir and
lenacapavir support their continued development as an
investigational once-weekly oral combination regimen for use in
people with HIV who are virologically suppressed. This
investigational combination of weekly oral ISL 2 mg + LEN 300 mg is
being further evaluated as a fixed-dose combination regimen in two
Phase 3 studies (NCT06630286 and NCT06630299) in virologically
suppressed people with HIV.
Islatravir in combination with lenacapavir is investigational
and not approved anywhere globally. The safety and efficacy of the
combination of islatravir and lenacapavir have not been
established.
Lenacapavir is being studied in multiple ongoing early and
late-stage development programs and has the potential to offer a
diverse set of person-centric options for treatment that could
uniquely fit into the lives of people with HIV. The use of
lenacapavir for HIV treatment in virologically suppressed
individuals is investigational and not approved anywhere
globally.
Please see below for the U.S. Indication and Important Safety
Information, including Boxed Warning, for Biktarvy.
There is currently no cure for HIV or AIDS.
About Islatravir (MK-8591) and Merck’s HIV Research
Islatravir (MK-8591) is Merck’s investigational nucleoside
reverse transcriptase translocation inhibitor (NRTTI) under
evaluation in multiple ongoing early and late-stage clinical
studies in combination with other antiretrovirals for the treatment
of HIV-1. Studies with islatravir are designed to offer different
dosing options as potential daily and once-weekly treatments. For
an overview of Merck’s HIV treatment and prevention clinical
development program, please click here.
About Lenacapavir
The multi-stage mechanism of action of lenacapavir, is
distinguishable from other currently approved classes of antiviral
agents. While most antivirals act on just one stage of viral
replication, lenacapavir is designed to inhibit HIV at multiple
stages of its lifecycle.
Lenacapavir is being evaluated as a potential long-acting option
in multiple ongoing and planned early and late-stage clinical
studies in Gilead’s HIV prevention and treatment research program.
The goal is to offer both long-acting oral and injectable options
with various dosing frequencies in combination with other
antiretroviral agents for treatment or as a single agent for
prevention. This approach aims to help address the individual needs
and preferences of people with HIV and people who could benefit
from pre-exposure prophylaxis (PrEP). The use of lenacapavir for
HIV prevention is investigational and the safety and efficacy of
lenacapavir for this use has not been established.
About Merck
At Merck, known as MSD outside of the United States and Canada,
we are unified around our purpose: We use the power of leading-edge
science to save and improve lives around the world. For more than
130 years, we have brought hope to humanity through the development
of important medicines and vaccines. We aspire to be the premier
research-intensive biopharmaceutical company in the world – and
today, we are at the forefront of research to deliver innovative
health solutions that advance the prevention and treatment of
diseases in people and animals. We foster a diverse and inclusive
global workforce and operate responsibly every day to enable a
safe, sustainable and healthy future for all people and
communities. For more information, visit www.merck.com and connect
with us on X (formerly Twitter), Facebook, Instagram, YouTube and
LinkedIn.
Merck’s Commitment to HIV
For more than 35 years, Merck has been committed to scientific
research and discovery in HIV leading to scientific breakthroughs
that have helped change HIV treatment. Our work has been pioneering
in the development of new options across multiple drug classes to
help those impacted by HIV. Today, we are developing a series of
antiviral options designed to help people manage HIV and protect
people from HIV, with the goal of reducing the growing burden of
infection worldwide. We want to ensure people are not defined by
HIV and our work focuses on transformational innovations,
collaborations with others in the global HIV community, and access
initiatives aimed at the goal of helping to end the HIV epidemic
for everyone.
About Gilead Sciences
Gilead Sciences, Inc. is a biopharmaceutical company that has
pursued and achieved breakthroughs in medicine for more than three
decades, with the goal of creating a healthier world for all
people. The company is committed to advancing innovative medicines
to prevent and treat life-threatening diseases, including HIV,
viral hepatitis, COVID-19, cancer, and inflammation. Gilead
operates in more than 35 countries worldwide, with headquarters in
Foster City, Calif.
About Gilead Sciences in HIV
For 35 years, Gilead has been a leading innovator in the field
of HIV, driving advances in treatment, prevention and cure
research. Gilead researchers have developed 12 HIV medications,
including the first single-tablet regimen to treat HIV, the first
antiretroviral for pre-exposure prophylaxis (PrEP) to help reduce
new HIV infections, and the first long-acting injectable HIV
treatment medication administered twice-yearly. Our advances in
medical research have helped to transform HIV into a treatable,
preventable, chronic condition for millions of people.
Gilead is committed to continued scientific innovation to
provide solutions for the evolving needs of people affected by HIV
around the world. Through partnerships, collaborations, and
charitable giving, the company also aims to improve education,
expand access and address barriers to care, with the goal of ending
the HIV epidemic for everyone, everywhere. Gilead is recognized as
one of the leading funders of HIV-related programs in a report
released by Funders Concerned About AIDS.
IMPORTANT U.S. SAFETY INFORMATION AND INDICATION FOR THE USE
OF BIKTARVY
Biktarvy is indicated as a complete regimen for the treatment of
human immunodeficiency virus type 1 (HIV-1) infection in adults and
pediatric patients weighing at least 14 kg who have no
antiretroviral treatment history or to replace the current
antiretroviral regimen in those who are virologically-suppressed
(HIV-1 RNA less than 50 copies per mL) on a stable antiretroviral
regimen with no history of treatment failure and no known or
suspected substitutions associated with resistance to bictegravir
or tenofovir.
BOXED WARNING: POST TREATMENT ACUTE EXACERBATION OF HEPATITIS
B
- Severe acute exacerbations of hepatitis B have been reported
in patients who are coinfected 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. Closely monitor hepatic function with
both clinical and laboratory follow-up for at least several months
in patients who are coinfected with HIV-1 and HBV and discontinue
BIKTARVY. If appropriate, anti-hepatitis B therapy may be
warranted.
Contraindications
- Coadministration: Do not use BIKTARVY with dofetilide or
rifampin.
Warnings and precautions
- Drug interactions: See Contraindications and Drug
Interactions sections. Consider the potential for drug interactions
prior to and during BIKTARVY therapy and monitor for adverse
reactions.
- Immune reconstitution syndrome, including the occurrence
of autoimmune disorders with variable time to onset, has been
reported.
- New onset or worsening renal impairment: Postmarketing
cases of renal impairment, including acute renal failure, proximal
renal tubulopathy (PRT), and Fanconi syndrome have been reported
with tenofovir alafenamide (TAF)–containing products. Do not
initiate BIKTARVY in patients with estimated creatinine clearance
(CrCl) <30 mL/min except in virologically suppressed adults
<15 mL/min who are receiving chronic hemodialysis. Patients with
impaired renal function and/or taking nephrotoxic agents (including
NSAIDs) are at increased risk of renal-related adverse reactions.
Discontinue BIKTARVY in patients who develop clinically significant
decreases in renal function or evidence of Fanconi syndrome. Renal
monitoring: Prior to or when initiating BIKTARVY and during
therapy, assess serum creatinine, CrCl, urine glucose, and urine
protein in all patients as clinically appropriate. In patients with
chronic kidney disease, assess serum phosphorus.
- Lactic acidosis and severe hepatomegaly with steatosis:
Fatal cases have been reported with the use of nucleoside analogs,
including FTC and TDF. Discontinue BIKTARVY if clinical or
laboratory findings suggestive of lactic acidosis or pronounced
hepatotoxicity develop, including hepatomegaly and steatosis in the
absence of marked transaminase elevations.
Adverse reactions
- Most common adverse reactions (incidence ≥5%; all
grades) in clinical studies through week 144 were diarrhea (6%),
nausea (6%), and headache (5%).
Drug interactions
- Prescribing information: Consult the full prescribing
information for BIKTARVY for more information on Contraindications,
Warnings, and potentially significant drug interactions, including
clinical comments.
- Enzymes/transporters: Drugs that induce P-gp or induce
both CYP3A and UGT1A1 can substantially decrease the concentration
of components of BIKTARVY. Drugs that inhibit P-gp, BCRP, or
inhibit both CYP3A and UGT1A1 may significantly increase the
concentrations of components of BIKTARVY. BIKTARVY can increase the
concentration of drugs that are substrates of OCT2 or MATE1.
- Drugs affecting renal function: Coadministration of
BIKTARVY with drugs that reduce renal function or compete for
active tubular secretion may increase concentrations of FTC and
tenofovir and the risk of adverse reactions.
Dosage and administration
- Dosage: Adult and pediatric patients weighing ≥25 kg: 1
tablet containing 50 mg bictegravir (BIC), 200 mg emtricitabine
(FTC), and 25 mg tenofovir alafenamide (TAF) taken once daily with
or without food. Pediatric patients weighing ≥14 kg to <25 kg: 1
tablet containing 30 mg BIC, 120 mg FTC, and 15 mg TAF taken once
daily with or without food. For children unable to swallow a whole
tablet, the tablet can be split and each part taken separately as
long as all parts are ingested within approximately 10
minutes.
- Renal impairment: For patients weighing ≥25 kg, not
recommended in patients with CrCl 15 to <30 mL/min, or <15
mL/min who are not receiving chronic hemodialysis, or <15 mL/min
who are receiving chronic hemodialysis and have no antiretroviral
treatment history. For patients weighing ≥14 kg to <25 kg, not
recommended in patients with CrCl <30 mL/min.
- Hepatic impairment: Not recommended in patients with
severe hepatic impairment.
- Prior to or when initiating: Test patients for HBV
infection.
- Prior to or when initiating, and during treatment: As
clinically appropriate, assess serum creatinine, CrCl, urine
glucose, and urine protein in all patients. In patients with
chronic kidney disease, assess serum phosphorus.
Pregnancy and lactation
- Pregnancy: BIKTARVY is recommended in pregnant
individuals who are virologically suppressed on a stable ARV
regimen with no known substitutions associated with resistance to
any of the individual components of BIKTARVY. Lower plasma
exposures of BIKTARVY were observed during pregnancy; therefore,
viral load should be monitored closely during pregnancy. An
Antiretroviral Pregnancy Registry (APR) has been established.
Available data from the APR for BIC, FTC, or TAF show no difference
in the rates of birth defects compared with a US reference
population.
- Lactation: Individuals infected with HIV-1 should be
informed of the potential risks of breastfeeding.
Gilead Forward-Looking Statements
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 Gilead’s ability to initiate, progress or complete
clinical trials or studies within currently anticipated timelines
or at all, and the possibility of unfavorable results from ongoing
and additional clinical trials or studies, including those
involving lenacapavir; uncertainties relating to regulatory
applications and related filing and approval timelines, including
potential applications for indications currently under evaluation;
the possibility that Gilead may make a strategic decision to
discontinue development of these programs and, as a result, these
programs may never be successfully commercialized for the
indications currently under evaluation; and any assumptions
underlying any of the foregoing. These and other risks,
uncertainties and factors are described in detail in Gilead’s
Quarterly Report on Form 10-Q for the quarter ended June 30, 2024,
as filed with the U.S. Securities and Exchange Commission. These
risks, uncertainties and other factors could cause actual results
to differ materially from those referred to in the forward-looking
statements. All statements other than statements of historical fact
are statements that could be deemed forward-looking statements. The
reader is cautioned that any such forward-looking statements are
not guarantees of future performance and involve risks and
uncertainties and is cautioned not to place undue reliance on these
forward-looking statements. All forward-looking statements are
based on information currently available to Gilead, and Gilead
assumes no obligation and disclaims any intent to update any such
forward-looking statements.
Forward-Looking Statement of Merck & Co., Inc., Rahway,
N.J., USA
This news release of Merck & Co., Inc., Rahway, N.J., USA
(the “company”) includes “forward-looking statements” within the
meaning of the safe harbor provisions of the U.S. Private
Securities Litigation Reform Act of 1995. These statements are
based upon the current beliefs and expectations of the company’s
management and are subject to significant risks and uncertainties.
There can be no guarantees with respect to pipeline candidates that
the candidates will receive the necessary regulatory approvals or
that they will prove to be commercially successful. If underlying
assumptions prove inaccurate or risks or uncertainties materialize,
actual results may differ materially from those set forth in the
forward-looking statements.
Risks and uncertainties include but are not limited to, general
industry conditions and competition; general economic factors,
including interest rate and currency exchange rate fluctuations;
the impact of pharmaceutical industry regulation and health care
legislation in the United States and internationally; global trends
toward health care cost containment; technological advances, new
products and patents attained by competitors; challenges inherent
in new product development, including obtaining regulatory
approval; the company’s ability to accurately predict future market
conditions; manufacturing difficulties or delays; financial
instability of international economies and sovereign risk;
dependence on the effectiveness of the company’s patents and other
protections for innovative products; and the exposure to
litigation, including patent litigation, and/or regulatory
actions.
The company undertakes no obligation to publicly update any
forward-looking statement, whether as a result of new information,
future events or otherwise. Additional factors that could cause
results to differ materially from those described in the
forward-looking statements can be found in the company’s Annual
Report on Form 10-K for the year ended December 31, 2023 and the
company’s other filings with the Securities and Exchange Commission
(SEC) available at the SEC’s Internet site (www.sec.gov).
U.S. full Prescribing Information for Biktarvy,
including BOXED WARNING, is available at www.gilead.com.
Biktarvy, Gilead and the Gilead logo are
registered trademarks of Gilead Sciences, Inc., or its related
companies. All other marks are the property of their respective
owners.
For more information about Gilead, please visit
the company’s website at www.gilead.com, follow Gilead on X
(@Gilead Sciences) and LinkedIn, or call Gilead Public Affairs at
1-800-GILEAD-5 or 1-650-574-3000.
View source
version on businesswire.com: https://www.businesswire.com/news/home/20241019252729/en/
Meaghan Smith, Media public_affairs@gilead.com Jacquie Ross,
Investors investor_relations@gilead.com Julie Cunningham, Media
julie.cunningham@merck.com Peter Dannenbaum, Investors
peter.dannenbaum@merck.com
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