A Phase III, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter Clinical Trial to Evaluate the Efficacy and Safety of the Initial Combination of Ertugliflozin (MK-8835/PF-04971729) With Sitagliptin in the Treatment of Subjects With T2DM With Inadequate Glycemic Control on Diet and Exercise

This is a study to evaluate the efficacy and safety of ertugliflozin (MK-8835/PF-04971729) in combination with sitagliptin in the treatment of participants with Type 2 diabetes mellitus (T2DM) with inadequate glycemic control on diet and exercise. The primary hypothesis of the study is that ertugliflozin plus sitagliptin is more effective in lowering of hemoglobin A1C (HbA1C) than placebo.

Start Date23 Sep 2014

Sponsor / Collaborator

Merck Sharp & Dohme Corp.

[+1]

100 Clinical Results associated with Ertugliflozin/Sitagliptin Phosphate

100 Translational Medicine associated with Ertugliflozin/Sitagliptin Phosphate

100 Patents (Medical) associated with Ertugliflozin/Sitagliptin Phosphate

Literatures (Medical) associated with Ertugliflozin/Sitagliptin Phosphate

01 Mar 2018·DrugsQ1 · MEDICINE

Ertugliflozin: First Global Approval

Q1 · MEDICINE

Review

Author: Markham, Anthony

Ertugliflozin (Steglatro™) is an orally active sodium glucose co-transporter type 2 inhibitor being developed by Merck and Pfizer as a treatment for type 2 diabetes mellitus (T2DM). Ertugliflozin as monotherapy and in combination with various other antidiabetic drugs was associated with improvements in glycaemic control and secondary outcome measures in the VERTIS phase III clinical trial program. Ertugliflozin and fixed-dose combinations of ertugliflozin and metformin (Segluromet™) and ertugliflozin and sitagliptin (Steglujan™) have recently been approved by the US FDA as an adjunct to diet and exercise to improve glycaemic control in adults with T2DM. These products have also received a positive opinion from the EU Committee for Medicinal Products for Human Use (CHMP). This article summarizes the milestones in the development of ertugliflozin leading to its first approval for T2DM.

Drugs of today (Barcelona, Spain : 1998)Q4 · MEDICINE

Ertugliflozin for the treatment of type 2 diabetes

Q4 · MEDICINE

Review

Author: Razdan, K ; Sharma, R ; Kuhad, A

Sodium/glucose cotransporter 2 (SGLT2) is exclusively expressed in the S1 and S2 segments of proximal convoluted tubules and accounts for roughly 90% of glucose reabsorption. Ertugliflozin, a highly selective and reversible SGLT2 inhibitor, is the latest addition to the gliflozin class of SGLT2 inhibitors for the treatment of type 2 diabetes mellitus (T2DM). It was granted approval by the U.S. Food and Drug Administration (FDA) in December 2017 for treatment of T2DM as a monotherapy, and as part of two separate fixed-dose combination therapies with sitagliptin (Steglujan) and metformin (Segluromet). Ertugliflozin demonstrated roughly 100% bioavailability following a single dose of 15 mg. It also has a longer half-life (16.6 hours) than presently available gliflozins, which translates into single daily dosing and dose reduction allowing for patient compliance. This review will focus on the preclinical pharmacology, pharmacokinetics, clinical efficacy and safety of ertugliflozin.

News (Medical) associated with Ertugliflozin/Sitagliptin Phosphate

29 Aug 2025

·www.einpresswire.com

July - September 2021 | Potential Signals of Serious Risks/New Safety Information Identified by the FDA Adverse Event Reporting System (FAERS)

Ajovy (fremanezumab-vfrm) Emgality (galcanezumab-gnlm) Nurtec ODT (rimegepant) Ubrelvy (ubrogepant) Vyepti (eptinezumab-jjmr) Hypertension The "Warnings and Precautions", "Adverse Reactions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in March 2025 to include information about the risk of hypertension. Example: Ajovy labeling Apriso (mesalamine) Asacol (mesalamine) Asacol HD (mesalamine) Azulfidine (sulfasalazine) Azulfidine EN-Tabs (sulfasalazine) Canasa (mesalamine) Colazal (balsalazide disodium) Delzicol (mesalamine) Dipentum (osalazine sodium) Giazo (balsalazide disodium) Lialda (mesalamine) Rowasa (mesalamine) Pentasa (mesalamine) Severe cutaneous adverse reactions The Warnings and Precautions section of the labeling was updated November 2021 to include severe cutaneous adverse reactions. Example: Delzicol labeling Avastin (bevacizumab) Mvasi (bevacizumab-awwb) Zirabev (bevacizumab-bvzr) Pancreatitis FDA determined that no action is necessary at the time based on available information. Avastin (bevacizumab) Mvasi (bevacizumab-awwb) Zirabev (bevacizumab-bvzr) Anaphylactic shock The "Warnings and Precautions" section of the labeling was updated between September 2022 and February 2023 to include anaphylactoid/anaphylactic reactions. Example: Avastin labeling Ayvakit (avapritinib) Photosensitivity reaction The "Warnings and Precautions", "Adverse Reactions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in March 2023 to include information about photosensitivity. Ayvakit labeling Azacitidine Onureg (azacitidine) Vidaza (azacitidine) Generic products containing azacitidine Pericarditis The "Adverse Reactions" section of the labeling was updated between September 2022 and June 2023 to include pericarditis. Example: Vidaza labeling FDA determined that no action is necessary at the time based on available information for Onureg. Bavencio (avelumab) Imfinzi (durvalumab) Libtayo (cemiplimab-rwlc) Keytruda (pembrolizumab) Opdivo (nivolumab) Tecentriq (atezolizumab) Yervoy (ipilimumab) Tumour lysis syndrome FDA determined that no action is necessary at the time based on available information. Cymbalta (duloxetine hydrochloride) Drizalma Sprinkle (duloxetine hydrochloride) Generic products containing duloxetine hydrochloride Anosmia, Hyposmia This issue is posted as two individual newly identified safety signal (NISS) entries in the January-March 2022 quarter, to reflect the focus on the potential signals of anosmia and hyposmia, separately. Darzalex (daratumumab) Darzalex Faspro (daratumumab and hyaluronidase-fihj) Blood stem cell transplant failure FDA determined that no action is necessary at the time based on available information. Dipeptidyl peptidase-4 (DPP-4) inhibitors Glyxambi (empagliflozin and linagliptin) Janumet (metformin hydrochloride and sitagliptin phosphate) Janumet XR (metformin hydrochloride and sitagliptin phosphate) Jentadueto (linagliptin and metformin hydrochloride) Jentadueto XR (linagliptin and metformin hydrochloride) Kazano (alogliptin and metformin hydrochloride) Kombiglyze XR (metformin hydrochloride and saxagliptin) Nesina (alogliptin) Onglyza (saxagliptin) Oseni (alogliptin and pioglitazone) Steglujan (ertugliflozin and sitagliptin) Tradjenta (linagliptin) Trijardy XR (empagliflozin, linagliptin and metformin hydrochloride) Qtern (saxagliptin and dapagliflozin) Generic products containing dipeptidyl peptidase-4 inhibitors Tubulointerstitial nephritis The "Adverse Reactions" section of the labeling was updated between March 2022 and June 2022 for products containing alogliptin and sitagliptin to include tubulointerstitial nephritis. Example: Janumet labeling FDA determined that no action is necessary for products containing linagliptin and saxagliptin at the time based on available information. *An administrative error resulted in the omission of Januvia from the list of product names after the initial quarterly report was posted. Dupixent (dupilumab) Angioedema The "Warnings and Precautions" and "Adverse Reactions" sections of the labeling were updated in December 2021 to include angioedema. Dupixent labeling Glucagon-like peptide-1 (GLP-1) analogues Adlyxin (lixisenatide) Bydureon (exenatide) Bydureon BCise (exenatide) Byetta (exenatide) Ozempic (semaglutide) Rybelsus (semaglutide) Saxenda (liraglutide) Soliqua 100/33 (insulin glargine and lixisenatide injection) Trulicity (dulaglutide) Victoza (liraglutide) Wegovy (semaglutide) Xultophy 100/3.6 (insulin degludec and liraglutide injection) Generic products containing glucagon-like peptide-1 analogues Gallbladder related disorders The "Warnings and Precautions", "Adverse Reactions", and "Patient Counseling Information" sections of the GLP-1 analogues labeling were updated between March 2022 and June 2022 to include information about acute gallbladder disease. Example: Adlyxin labeling FDA has determined that the last approved labeling for Saxenda and Wegovy is adequately labeled for acute gallbladder disease, and that no further regulatory action is needed at this time. Gonadotropin releasing hormone (GnRH) analogues Fensolvi (leuprolide acetate) Lupron Depot-PED (leuprolide acetate) Supprelin LA (histrelin acetate) Synarel (nafarelin acetate) Triptodur (triptorelin) Idiopathic intracranial hypertension The "Warnings", "Precautions", and "Adverse Reactions" sections of the labeling were updated in April 2022 to include idiopathic intracranial hypertension. Example: Fensolvi labeling Jakafi (ruxolitinib phosphate) Herpes simplex virus (HSV) reactivation and/or disseminated HSV The "Dosage and Administration", "Warnings and Precautions", and "Adverse Reactions" sections of the labeling were updated in January 2023 to include information about herpes simplex and herpes zoster infections. Jakafi labeling Ibrance (palbociclib) Kisqali (ribociclib) Kisqali Femara Co-Pack (letrozole and ribociclib) Embolic and thrombotic events, venous The "Adverse Reactions" section of the Ibrance labeling was updated in December 2024 to include venous thromboembolism. Ibrance labeling FDA determined that no action is necessary at the time for Kisqali and Kisqali Femara Co-Pack based on available information. Ocrevus (ocrelizumab) Myocardial infarction FDA determined that no action is necessary at the time based on available information. Potassium Chloride Product preparation error The “Warnings” section of the labeling was updated in December 2022 to include information about fatal cardiac adverse reactions with intravenous administration of undiluted potassium chloride. Praxbind (idarucizumab) Wrong dose errors The carton labeling and "Dosage and Administration" sections of the labeling were revised in February 2022 to clarify the number of vials included in each carton and the recommended dosing. Praxbind labeling Qbrexza (glycopyrronium tosylate) Accidental exposure to product The container label, carton labeling, "Dosage and Administration", "Warnings and Precautions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in October 2022 to include information about accidental exposure. Qbrexza labeling Qbrexza (glycopyrronium tosylate) Urinary retention The “Warnings and Precautions”, “Adverse Reactions”, and “Patient Counseling Information” sections of the labeling were updated in October 2022 to include information about new or worsening urinary retention. Qbrexza labeling Sodium-glucose cotransporter-2 (SGLT-2) inhibitors Farxiga (dapagliflozin) Glyxambi (empagliflozin and linagliptin) Invokamet (canagliflozin and metformin hydrochloride) Invokamet XR (canagliflozin and metformin hydrochloride) Invokana (canagliflozin) Jardiance (empagliflozin) Qtern (saxagliptin and dapagliflozin) Steglatro (ertugliflozin) Steglujan (ertugliflozin and sitagliptin) Segluromet (ertugliflozin and metformin hydrochloride) Synjardy (empagliflozin and metformin hydrochloride) Synjardy XR (empagliflozin and metformin hydrochloride) Trijardy XR (empagliflozin, linagliptin and metformin hydrochloride) Xigduo XR (dapagliflozin and metformin) Generic products containing sodium-glucose cotransporter-2 (SGLT-2) inhibitors Tubulointerstitial nephritis FDA determined that no action is necessary at the time based on available information. Somatostatin Receptor Imaging Agents Detectnet (copper Cu-64 dotatate injection) Gallium Dotatoc (GA 68) Octreoscan (Indium In 111 Pentetreotide) Netspot (Gallium GA 68 Dotatate) Hypersensitivity The "Warnings and Precautions" and "Adverse Reactions" sections of the labeling were updated in December 2021 to include hypersensitivity reactions. Example: Netspot labeling Stromectol (ivermectin) Generic products containing ivermectin Off label use FDA determined that no action is necessary at the time based on available information. Stromectol (ivermectin) Generic products containing ivermectin Neurotoxicity The "Warnings", "Adverse Reactions", and "Overdosage" sections of the labeling were updated in March 2022 to include neurotoxicity. Example: Stromectol labeling Sunosi (solriamfetol hydrochloride) Hypersensitivity FDA determined that no action is necessary at the time based on available information. Vivitrol (naltrexone) Incorrect route of product administration The container label (vial), carton labeling, "Dosage and Administration", "Warnings and Precautions", and "Description", sections of the labeling were revised in September 2022 to emphasize the appropriate route and site of administration. Vivitrol labeling Xcopri (cenobamate) Psychiatric disorders The "Adverse Reactions" section of the labeling was updated in June 2022 to include psychiatric disorders. Xcopri labeling Legal Disclaimer: EIN Presswire provides this news content "as is" without warranty of any kind. We do not accept any responsibility or liability for the accuracy, content, images, videos, licenses, completeness, legality, or reliability of the information contained in this article. If you have any complaints or copyright issues related to this article, kindly contact the author above.

Drug Approval

10 Aug 2022

·www.biospace.com

Merck’s Blockbuster Diabetes Drug Sitagliptin Found Contaminated with Potential Carcinogen

Katherine Welles The FDA will still allow continued distribution of sitagliptin containing NTTP with an acceptable intake limit of 37 ng per day and up to 246.7 ng per day. FDA updated the dosage limits of Sitagliptin. (Courtesy of Katherine Welles/Getty Images) The U.S. Food and Drug Administration announced Tuesday that certain samples of sitagliptin were contaminated with the nitrosamine Nitroso-STG-19 (NTTP). Sitagliptin is the main compound in Merck’s blockbuster type 2 diabetes drug Januvia. The regulatory body said it will allow continued distribution of sitagliptin even if the nitrosamine impurities are present at levels above the acceptable intake limits. This is to prevent a drug shortage and ensure that people with diabetes can continue to access their medicines. The FDA has set a daily acceptable intake limit of 37 ng per day but is expanding this to an interim threshold of 246.7 ng per day. As per agency scientists, this higher limit poses only a minimal additional risk of cancer compared to the stricter cut-off. Sitagliptin, dispensed only through prescriptions, helps control blood sugar levels in people suffering from type 2 diabetes mellitus. Because this condition can overload the bloodstream with too much glucose, eventually leading to complications in the circulatory and nervous systems, it can prove dangerous to cut off medication in patients. The FDA recommends that physicians continue to prescribe sitagliptin as appropriate. In a statement to Bloomberg , Merck confirmed that it has “recently detected a nitrosamine identified as NTTP in some batches of our sitagliptin-containing medicines.” Aside from Januvia, the company has also detected impurity in certain batches of Janumet, which combines sitagliptin with metformin, and Steglujan, containing both sitagliptin and ertugliflozin. All three drugs are indicated for type 2 diabetes. The company is working with health authorities across the globe and is implementing additional quality control mechanisms to meet the FDA’s interim thresholds of NTTP. “We remain confident in the safety, efficacy and quality of our sitagliptin-containing medicines,” Merck said. “No significant impact on supply of these medicines for patients is anticipated.” Januvia and Janumet are Merck’s best-selling drugs, behind only its melanoma medicine Keytruda (pembrolizumab) and its HPV vaccine Gardasil. In the second quarter of 2022, Januvia and Janumet delivered combined earnings of more than $1.2 billion, a mild decline of 2% from the same period the year prior. Merck lost market exclusivity for Januvia and Janumet in China earlier this year and is expected to face the same challenge in the European Union in September. Still, the news of impurities in its top assets dealt a blow to the company. Its shares dropped by 1.9% after the FDA’s announcement. NTTP falls under a class of compounds called nitrosamine. Some nitrosamines, such as nitrosodimethylamine (NDMA) and N-nitrosodiethylamine, have shown carcinogenic activity in animal studies. No such data is yet available for NTTP, however, and the FDA’s move to flag this impurity as a safety concern in sitagliptin may be a decision to err on the side of caution. In 2018, the agency detected unacceptable levels of NDMA in valsartan, an angiotensin II receptor blocker used to control high blood pressure and treat heart failure. This set off a years-long investigation process that also found unacceptable levels of NDMA in other commonly used drugs, such as the heartburn medications ranitidine and nizatidine. In early 2020, the FDA also found certain batches of metformin, another diabetes drug, to be contaminated with NDMA, though at acceptable levels. In February 2021, the agency published a comprehensive guidance document to help drug manufacturers detect, prevent and address unacceptable levels of nitrosamine contaminations in their products.

Vaccine

10 Aug 2022

·www.biospace.com

Merck's Blockbuster Diabetes Drug Found Contaminated with Potential Carcinogen

Courtesy of Katherine Welles/Getty Images The U.S. Food and Drug Administration announced Tuesday that certain samples of sitagliptin were contaminated with the nitrosamine Nitroso-STG-19 (NTTP). Sitagliptin is the main compound in Merck's blockbuster type 2 diabetes drug Januvia. The regulatory body said it will allow continued distribution of sitagliptin even if the nitrosamine impurities are present at levels above the acceptable intake limits. This is to prevent a drug shortage and ensure that people with diabetes can continue to access their medicines. The FDA has set a daily acceptable intake limit of 37 ng per day but is expanding this to an interim threshold of 246.7 ng per day. As per agency scientists, this higher limit poses only a minimal additional risk of cancer compared to the stricter cut-off. Sitagliptin, dispensed only through prescriptions, helps control blood sugar levels in people suffering from type 2 diabetes mellitus. Because this condition can overload the bloodstream with too much glucose, eventually leading to complications in the circulatory and nervous systems, it can prove dangerous to cut off medication in patients. The FDA recommends that physicians continue to prescribe sitagliptin as appropriate. In a statement to Bloomberg, Merck confirmed that it has "recently detected a nitrosamine identified as NTTP in some batches of our sitagliptin-containing medicines." Aside from Januvia, the company has also detected impurity in certain batches of Janumet, which combines sitagliptin with metformin, and Steglujan, containing both sitagliptin and ertugliflozin. All three drugs are indicated for type 2 diabetes. The company is working with health authorities across the globe and is implementing additional quality control mechanisms to meet the FDA's interim thresholds of NTTP. "We remain confident in the safety, efficacy and quality of our sitagliptin-containing medicines," Merck said. "No significant impact on supply of these medicines for patients is anticipated." Januvia and Janumet are Merck's best-selling drugs, behind only its melanoma medicine Keytruda (pembrolizumab) and its HPV vaccine Gardasil. In the second quarter of 2022, Januvia and Janumet delivered combined earnings of more than $1.2 billion, a mild decline of 2% from the same period the year prior. Merck lost market exclusivity for Januvia and Janumet in China earlier this year and is expected to face the same challenge in the European Union in September. Still, the news of impurities in its top assets dealt a blow to the company. Its shares dropped by 1.9% after the FDA's announcement. NTTP falls under a class of compounds called nitrosamine. Some nitrosamines, such as nitrosodimethylamine (NDMA) and N-nitrosodiethylamine, have shown carcinogenic activity in animal studies. No such data is yet available for NTTP, however, and the FDA's move to flag this impurity as a safety concern in sitagliptin may be a decision to err on the side of caution. In 2018, the agency detected unacceptable levels of NDMA in valsartan, an angiotensin II receptor blocker used to control high blood pressure and treat heart failure. This set off a years-long investigation process that also found unacceptable levels of NDMA in other commonly used drugs, such as the heartburn medications ranitidine and nizatidine. In early 2020, the FDA also found certain batches of metformin, another diabetes drug, to be contaminated with NDMA, though at acceptable levels. In February 2021, the agency published a comprehensive guidance document to help drug manufacturers detect, prevent and address unacceptable levels of nitrosamine contaminations in their products.

Vaccine

100 Deals associated with Ertugliflozin/Sitagliptin Phosphate

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	A10BD24	-

R&D Status

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	United States	Merck Sharp & Dohme Corp.	19 Dec 2017

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02226003 (CTgov)	Phase 3	Diabetes Mellitus, Type 2	291	Ertugliflozin+Sitagliptin (Ertugliflozin 5 mg + Sitagliptin 100 mg)	mvxgxyrgfu(zczgerowjq) = zyoxebydid gcmqrgmkeu (ygvvenjlxd, czxtcfafzc - yhxrjkssvj) View more	-	07 Apr 2017
				Ertugliflozin+Sitagliptin (Ertugliflozin 15 mg + Sitagliptin 100 mg)	mvxgxyrgfu(zczgerowjq) = kloelgfuky gcmqrgmkeu (ygvvenjlxd, gxqwltrnqw - zbtsqtoccm) View more

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Hiro LS Researcher

The AI Search Engine Built to Accelerate Biopharma Decisions

Search across billion-scale life sciences data to uncover signals, validate evidence, and act with confidence.

Ask any biopharma research question→

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, Patsnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Discover Synapse Data Servers

Synapse data is now integrated into the PatSnap LS Model Context Protocol (MCP) service. Customize your LLM agent now using our MCP server!

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis