KENILWORTH, N.J. & NEW YORK--(BUSINESS WIRE)-- Merck (NYSE:MRK), known as MSD outside the United States and Canada, and Pfizer Inc. (NYSE:PFE), today announced that the U.S. Food and Drug Administration (FDA) has approved STEGLATROTM (ertugliflozin) tablets, an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor, and the fixed-dose combination STEGLUJAN™ (ertugliflozin and sitagliptin) tablets.

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STEGLATRO is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. STEGLUJAN is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both ertugliflozin and sitagliptin is appropriate. STEGLATRO and STEGLUJAN are not recommended in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis. STEGLUJAN 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 for the development of pancreatitis while using STEGLUJAN. STEGLATRO and STEGLUJAN are contraindicated in patients with severe renal impairment, end-stage renal disease or on dialysis, or with a history of a serious hypersensitivity reaction to ertugliflozin. STEGLUJAN is also contraindicated in patients with a history of a serious hypersensitivity reaction to sitagliptin (such as anaphylaxis or angioedema). Additional safety information can be found below.

These FDA approvals are supported by seven Phase 3 studies of approximately 4,800 patients. STEGLATRO was studied as monotherapy and in combination with metformin and/or sitagliptin, as well as with insulin and a sulfonylurea, in adults with type 2 diabetes and moderate renal impairment. “In clinical trials, treatment with STEGLATRO resulted in significant A1C reductions when used alone or in combination with sitagliptin,” said Juan Pablo Frias, M.D., president and principal investigator, National Research Institute, Los Angeles. “This is important, as A1C-lowering is a key component of diabetes management, and many of my adult patients may need multiple medications to help manage their condition.”

“Merck welcomes the opportunity to provide adult patients with type 2 diabetes and their physicians these new medicines to help lower A1C, building on over a decade of experience with our diabetes portfolio and reflecting our continued commitment to diabetes research and patient care,” said Keith Kaufman, M.D., vice president, global clinical development and therapeutic area head for diabetes, endocrinology and women’s health, Merck Research Laboratories.

Diabetes is a chronic, progressive disease affecting approximately 30 million Americans (90 to 95 percent have type 2 diabetes). About one-third of adults with type 2 diabetes in the U.S. are not at their A1C goal.

“There remains a need to help adults with type 2 diabetes improve their glycemic control, and as the prevalence of the disease continues to rise, we are pleased to offer additional treatment options to these patients and the healthcare providers who treat them,” said James Rusnak, M.D., Ph.D., senior vice president and chief development officer, internal medicine, Pfizer Global Product Development.

One of the studies supporting the FDA approvals was VERTIS SITA2, a 26-week double-blind, placebo-controlled study. VERTIS SITA2 evaluated STEGLATRO (ertugliflozin) compared to placebo in 463 patients with type 2 diabetes inadequately controlled (baseline A1C of 7.0-10.5%) on background metformin (≥1,500 mg/day) and sitagliptin (100 mg/day). Patients were randomized to STEGLATRO 5 mg, STEGLATRO 15 mg or placebo administered once daily, in addition to continuation of background metformin and sitagliptin therapy. In the study, STEGLATRO provided significant additional A1C reductions on top of metformin plus sitagliptin of 0.7 percent and 0.8 percent, respectively, for the 5 and 15 mg doses, compared with 0.2 percent for placebo (p<0.001, for both comparisons), which was the study’s primary endpoint.

In this study, STEGLATRO significantly reduced body weight by 6.6 pounds with the 5 mg dose and 6.2 pounds with the 15 mg dose, on top of metformin plus sitagliptin, compared with 2.2 pounds with placebo. Baseline body weight was 193.1 pounds, 190.9 pounds and 190.6 pounds for the 5 mg, 15 mg and placebo groups, respectively. The difference from placebo was -4.2 pounds for STEGLATRO 5 mg (95% CI: -5.7, -2.9) and -4.0 pounds for STEGLATRO 15 mg (95% CI: -5.3, -2.6). STEGLATRO 5 mg and 15 mg were also associated with significant reductions in fasting plasma glucose (25.7 mg/dL and 32.1 mg/dL, respectively, vs. 6.5 mg/dL for placebo; p<0.001, for both comparisons). Baseline fasting plasma glucose levels were 167.7 mg/dL, 171.7 mg/dL and 169.6 mg/dL for the 5 mg, 15 mg and placebo groups, respectively. Significant reductions in systolic blood pressure were also observed for STEGLATRO (3.8 mmHg for 5 mg and 4.5 mmHg for 15 mg, vs. 0.2 mmHg for placebo). Baseline systolic blood pressure values were 132.1 mmHg, 131.6 mmHg and 130.2 mmHg for the 5 mg, 15 mg and placebo groups, respectively. For systolic blood pressure, the difference from placebo was -3.7 mmHg for STEGLATRO (ertugliflozin) 5 mg (95% CI: -6.1, -1.2) and -4.3 mmHg for STEGLATRO 15 mg (95% CI: -6.7, -1.9). STEGLATRO is not indicated for weight loss or hypertension.

STEGLATRO causes intravascular volume contraction. Symptomatic hypotension may occur after initiating STEGLATRO, particularly in patients with impaired renal function (estimated glomerular filtration rate [eGFR] less than 60 mL/min/1.73 m2), elderly patients (≥65 years), patients with low systolic blood pressure or patients on diuretics. Before initiating STEGLATRO, volume status should be assessed and corrected if indicated. Monitor for signs and symptoms after initiating therapy. Additional safety information can be found below.

In addition to STEGLATRO and STEGLUJAN (ertugliflozin and sitagliptin), the only fixed-dose combination of an SGLT2 inhibitor and the dipeptidyl peptidase-4 (DPP-4) inhibitor sitagliptin, the FDA also approved the fixed-dose combination SEGLUROMETTM (ertugliflozin and metformin hydrochloride). SEGLUROMET is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus who are not adequately controlled on a regimen containing ertugliflozin or metformin, or in patients who are already treated with both ertugliflozin and metformin. SEGLUROMET is not recommended in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis. The labeling for SEGLUROMET contains a boxed warning for lactic acidosis. SEGLUROMET is contraindicated in patients with severe renal impairment, end-stage renal disease or on dialysis, acute or chronic metabolic acidosis, including diabetic ketoacidosis, or a history of a serious hypersensitivity reaction to SEGLUROMET, ertugliflozin or metformin hydrochloride. Additional safety information is found below.

STEGLATRO is available in 5 mg and 15 mg tablets. STEGLUJAN combines 5 mg or 15 mg of ertugliflozin with 100 mg of sitagliptin. SEGLUROMET combines 2.5 mg or 7.5 mg of ertugliflozin with 500 mg or 1,000 mg of metformin hydrochloride.

Merck-Pfizer Collaboration and Product Availability

In 2013, Merck and Pfizer announced that they entered into a worldwide collaboration, except Japan, for the co-development and co-promotion of ertugliflozin. The Merck sales force will exclusively promote STEGLATRO and the two fixed-dose combination products in the United States. Merck and Pfizer will share potential revenues and certain costs on a 60/40 percent basis, respectively, and Pfizer may be entitled to additional milestone payments.

Merck has established a list price (Wholesale Acquisition Cost) of $8.94 per day for STEGLATRO, $17.45 per day for STEGLUJAN and $8.94 per day for SEGLUROMET. Wholesale acquisition costs do not include discounts that may be paid on the products. STEGLATRO (ertugliflozin) and STEGLUJAN (ertugliflozin and sitagliptin) are expected to be available in pharmacies in January 2018. SEGLUROMET (ertugliflozin and metformin hydrochloride) is expected to be available in February 2018.