Merck Presents First Phase 3 Data in Japanese Patients for Omarigliptin, an Investigational Once-Weekly DPP-4 Inhibitor for Type 2 Diabetes


September 17, 2014 8:31 am ET

Omarigliptin significantly reduced HbA1c levels compared to placebo

Merck (NYSE:MRK), known as MSD outside the United States and Canada,
today announced the presentation of the first data from the Phase 3
clinical development program for omarigliptin, Merck’s investigational
once-weekly DPP-4 inhibitor for the treatment of type 2 diabetes. In a
study in Japanese patients, omarigliptin provided comparable efficacy
and tolerability to Merck’s once-daily DPP-4 inhibitor JANUVIA®
(sitagliptin) 50 mg, which is the standard starting dose for sitagliptin
in Japan. Merck presented these data on omarigliptin, which has been
shown to produce sustained DPP-4 inhibition, at an oral session at the 50th
European Association for the Study of Diabetes (EASD) Annual Meeting.

“Despite advances in diabetes care in recent years, many people living
with type 2 diabetes are not at recommended blood sugar goals,” said
Peter Stein, M.D., vice president, Clinical Research, Diabetes and
Endocrinology, Merck Research Laboratories. “Merck is committed to
helping patients reduce the complexities of managing diabetes. If
approved, omarigliptin, as a once-weekly medication, could provide an
important new treatment option to help patients attain their blood sugar

Merck is supporting omarigliptin with a global clinical development
program that includes 10 Phase 3 clinical trials involving approximately
8,000 patients with type 2 diabetes. These are the first Phase 3 data
presented for omarigliptin and are the pivotal data for filing in Japan.
As previously announced, Merck plans to file for approval in Japan by
the end of 2014.

About the study

The Phase 3 double-blind, non-inferiority trial assessed the efficacy,
safety and tolerability of omarigliptin 25 mg once-weekly compared to
sitagliptin 50 mg once-daily (standard starting dose in Japan), and to
placebo. The primary efficacy endpoint was the change in HbA1c1
levels from baseline at week 24.

At baseline, randomized patients (n=414) had a mean HbA1c concentration
of 7.9, 8.0 and 8.1 percent in the omarigliptin, sitagliptin and placebo
groups, respectively. Mean fasting plasma glucose (FPG) levels were also
similar between treatment groups.

The primary objectives of the study were met, demonstrating at 24 weeks
a significant change from baseline in lowering HbA1c levels versus
placebo, while demonstrating similar efficacy to sitagliptin.

At week 24, omarigliptin significantly reduced HbA1c levels by -0.80
percent from baseline relative to placebo. The change relative to
sitagliptin was -0.02 percent and met the prespecified non-inferiority
criterion. The pre-specified criterion was based on the upper bound of
the 95 percent confidence interval (CI) being less than 0.3 percent.
Fasting and two-hour post-meal blood sugar levels also were
significantly reduced from baseline with omarigliptin and sitagliptin
compared to placebo.

There were no meaningful differences in the incidences of adverse events
with omarigliptin compared to placebo and sitagliptin. The most common
adverse event that occurred with an incidence of greater than 3 percent
in the omarigliptin group was nasopharyngitis, which occurred in 12.7
percent of those treated, compared to 30.5 percent of patients receiving
placebo and 11.0 percent of those receiving sitagliptin. Symptomatic
hypoglycemia was uncommon across all treatment groups in this study
[omarigliptin (0), sitagliptin (1), and placebo (0)]. Omarigliptin was
generally weight neutral, with a 0.04 kg mean change from baseline at
week 24.

About JANUVIA® (sitagliptin)

JANUVIA is indicated, as an adjunct to diet and exercise, to improve
glycemic control in adults with type 2 diabetes mellitus. JANUVIA should
not be used in patients with type 1 diabetes or for the treatment of
diabetic ketoacidosis. JANUVIA has not been studied in patients with a
history of pancreatitis. It is unknown whether patients with a history
of pancreatitis are at increased risk of developing pancreatitis while
taking JANUVIA. JANUVIA is contraindicated in patients with a history of
a serious hypersensitivity reaction to sitagliptin, such as anaphylaxis
or angioedema.

Selected important risk information about JANUVIA (sitagliptin) 25
mg, 50 mg and 100 mg tablets

There have been postmarketing reports of acute pancreatitis, including
fatal and nonfatal hemorrhagic or necrotizing pancreatitis, in patients
taking JANUVIA. After initiating JANUVIA, observe patients carefully for
signs and symptoms of pancreatitis. If pancreatitis is suspected,
promptly discontinue JANUVIA and initiate appropriate management. It is
unknown whether patients with a history of pancreatitis are at increased
risk of developing pancreatitis while taking JANUVIA.

Assessment of renal function is recommended prior to initiating JANUVIA
and periodically thereafter. A dosage adjustment is recommended in
patients with moderate or severe renal insufficiency and in patients
with end-stage renal disease requiring hemodialysis or peritoneal
dialysis. Caution should be used to ensure that the correct dose of
JANUVIA is prescribed.

There have been postmarketing reports of worsening renal function,
including acute renal failure, sometimes requiring dialysis. A subset of
these reports involved patients with renal insufficiency, some of whom
were prescribed inappropriate doses of sitagliptin.

When JANUVIA was used in combination with a
sulfonylurea or insulin, medications known to cause hypoglycemia, the
incidence of hypoglycemia was increased over that of placebo. Therefore,
a lower dose of sulfonylurea or insulin may be required to reduce the
risk of hypoglycemia.

The incidences (and rates) of hypoglycemia based on all reports of
symptomatic hypoglycemia were: 12.2 percent (0.59 episodes per
patient-year) for JANUVIA 100 mg in combination with glimepiride (with
or without metformin), 1.8 percent (0.24 episodes per patient-year) for
placebo in combination with glimepiride (with or without metformin),
15.5 percent (1.06 episodes per patient-year) for JANUVIA (sitagliptin)
100 mg in combination with insulin (with or without metformin), and 7.8
percent (0.51 episodes per patient-year) for placebo in combination with
insulin (with or without metformin).

There have been postmarketing reports of serious hypersensitivity
reactions in patients treated with JANUVIA, such as anaphylaxis,
angioedema and exfoliative skin conditions including Stevens-Johnson
syndrome. Onset of these reactions occurred within the first 3 months
after initiation of treatment with JANUVIA, with some reports occurring
after the first dose. If a hypersensitivity reaction is suspected,
discontinue JANUVIA, assess for other potential causes for the event,
and institute alternative treatment for diabetes.

Angioedema has also been reported with other dipeptidyl peptidase-4
(DPP-4) inhibitors. Use caution in a patient with a history of
angioedema with another DPP-4 inhibitor because it is unknown whether
such patients will be predisposed to angioedema with JANUVIA.

There have been no clinical studies establishing conclusive evidence of
macrovascular risk reduction with JANUVIA or with any other antidiabetic

In clinical studies, the adverse reactions reported, regardless of
investigator assessment of causality, in greater than or equal to 5
percent of patients treated with JANUVIA as monotherapy and in
combination therapy, and more commonly than in patients treated with
placebo, were upper respiratory tract infection, nasopharyngitis and

About Merck

Today’s Merck is a global healthcare leader working to help the world be
well. Merck is known as MSD outside the United States and Canada.
Through our prescription medicines, vaccines, biologic therapies, and
consumer care and animal health products, we work with customers and
operate in more than 140 countries to deliver innovative health
solutions. We also demonstrate our commitment to increasing access to
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Merck’s Commitment to Diabetes

Through our research initiatives, on our own and in collaboration with
others, Merck is strengthening its leadership in diabetes to deliver a
broad portfolio of solutions to help improve the management of diabetes.

Merck Forward-Looking Statement

This news release includes “forward-looking statements” within the
meaning of the safe harbor provisions of the United States Private
Securities Litigation Reform Act of 1995. These statements are based
upon the current beliefs and expectations of Merck’s management and are
subject to significant risks and uncertainties. There can be no
guarantees with respect to pipeline products that the products 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; Merck’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 Merck’s patents and other protections
for innovative products; and the exposure to litigation, including
patent litigation, and/or regulatory actions.

Merck 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 Merck’s 2013 Annual Report on Form 10-K and the company’s other
filings with the Securities and Exchange Commission (SEC) available at
the SEC’s Internet site (

Please see Prescribing Information for JANUVIA (sitagliptin) at
and Medication Guide for JANUVIA at

JANUVIA® is a registered trademark of Merck
Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc.

1 HbA1c is an estimate of a person’s average blood glucose
over a two- to three-month period.

Pam Eisele, +1 (267) 305-3558
Michael Close, +1 (267) 305-1221 or +1 (310) 617-1067
Justin Holko, +1 (908) 423-5088

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