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Drug

Sitagliptin Phosphate

Established medicine
ClassDipeptidyl peptidase IV inhibitorResearchOngoing clinical research
Also known as Janumet, Janumet XR, Januvia, Juvisync+3 more

Janumet, Janumet XR, Januvia, Juvisync, Steglujan, Sitagliptin, sitagliptin (as phosphate).

RxNorm621590ChEMBLCHEMBL1201174UNIITS63EW8X6F
8
Research papers
Dipeptidyl peptidase 4
Primary target
57
Regulatory events
Latest activity
beta

Recent clinical, regulatory, research and industry developments relating to this drug.

Label change: SITAGLIPTIN AND METFORMIN HYDROCHLORIDE (NDA022044)

Regulatory2026-08-11FDA

Label change: SITAGLIPTIN AND METFORMIN HYDROCHLORIDE (NDA202270)

Regulatory2026-08-11FDA

DPP-4 inhibitors sitagliptin and PF-00734,200 mitigate dopaminergic neurodegeneration, neuroinflammation and behavioral impairment in the rat 6-OHDA model of Parkinson's disease.

Research2024-04-02GeroScience

An Open-Label, Randomized Naturalistic Study to Evaluate the Incidence of Hypoglycemia Comparing Sitagliptin With Sulfonylurea Treatment in Patients With Type 2 Diabetes During Ramadan Fasting

Clinical trial2022-09-21Results posted · ClinicalTrials.gov

Label change: SITAGLIPTIN AND METFORMIN HYDROCHLORIDE (NDA022044)

Regulatory2022-06-21FDA

Label change: SITAGLIPTIN AND METFORMIN HYDROCHLORIDE (NDA202270)

Regulatory2022-06-21FDA

Exploring the Incretin Effect in People With IFG

Clinical trial2021-04-05Results posted · ClinicalTrials.gov

Sitagliptin Treatment at the Time of Hospitalization Was Associated With Reduced Mortality in Patients With Type 2 Diabetes and COVID-19: A Multicenter, Case-Control, Retrospective, Observational Study.

Research2020-09-29Diabetes care

A Randomized, Double-blind, Parallel-group, Placebo-controlled Study to Assess Efficacy, Safety and Tolerability of Sitagliptin Phosphate 100 mg as Treatment for Recurrent, Persistent or Newly Diagnosed Type 2 Diabetes After Gastric Bypass

Clinical trial2019-01-22Results posted · ClinicalTrials.gov

A Phase III, Multicenter, Randomized, Placebo-Controlled, Double-Blind Clinical Trial to Evaluate the Safety and Efficacy of the Addition of Sitagliptin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Diet/Exercise Therapy and Acarbose Monotherapy

Clinical trial2018-08-16Results posted · ClinicalTrials.gov

Efficacy and tolerability of sitagliptin monotherapy in elderly patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial.

Research2011-03-23Barzilai N · Current medical research and opinion

Efficacy and safety of sitagliptin monotherapy compared with voglibose in Japanese patients with type 2 diabetes: a randomized, double-blind trial.

Research2010-07-01Iwamoto Y · Diabetes, obesity & metabolism

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name
Sitagliptin Phosphate
Aliases & brands
JanumetJanumet XRJanuviaJuvisyncSteglujanSitagliptinsitagliptin (as phosphate)
RxNorm CUI
621590
ChEMBL ID
CHEMBL1201174
UNII
TS63EW8X6F
Primary mechanism
Dipeptidyl peptidase IV inhibitor
Regulatory jurisdictions
fda

Pharmacology & targets

1 target

Known molecular targets and mechanisms supported by curated pharmacology databases.

Dipeptidyl peptidase 4
DPP4 · P27487
INHIBITORDipeptidyl peptidase IV inhibitor

Regulatory timeline

57 events

The complete regulatory record, grouped by authority — approvals, safety advisories and label changes. Each authority shows its most recent events; expand one to read its full history.

Earliest approval
2007-03-30
Latest approval
2020-12-04
Authorities
FDA
Total events
57
fdaU.S. Food and Drug Administration· 57 events
2026-08-11Label change
Label change: SITAGLIPTIN AND METFORMIN HYDROCHLORIDE (NDA022044)
Evidence ↗
2026-08-11Label change
Label change: SITAGLIPTIN AND METFORMIN HYDROCHLORIDE (NDA202270)
Evidence ↗
2022-06-21Label change
Label change: SITAGLIPTIN AND METFORMIN HYDROCHLORIDE (NDA022044)
Evidence ↗

Data from the U.S. Food and Drug Administration (U.S. Food and Drug Administration), public domain (CC0).

Clinical trials

32 trials

The current development programme across all trial phases — status mix, phase distribution and the late-stage studies shaping the evidence base.

Development programme
CLINICALTRIALS.GOV · LIVE REGISTRY
32
registered trials across all phases
LATEST COMPLETION 2016
23
Late-stage (III+)
32
Completed
PHASE DISTRIBUTIONn = 32
Phase 17Phase 22Phase 317Phase 44Phase N / A2

Late-stage studies

Phase III+ trials still open or recently active — where late-stage evidence is being generated.

Treatment With Sitagliptin Phosphate in Patients With Reactive Hypoglycemia Secondary to Dysinsulinism. A Controlled, Randomized, Double-blind, Clinical Trial

CompletedPH IVInstituto Nacional de Ciencias Medicas y Nutricion Salvador Zubirann=202011

An Open-Label, Randomized Naturalistic Study to Evaluate the Incidence of Hypoglycemia Comparing Sitagliptin With Sulfonylurea Treatment in Patients With Type 2 Diabetes During Ramadan Fasting

CompletedPH IVKey trialMerck Sharp & Dohme LLCn=1,1472010

A 24 Week, Multicenter, Open-label Study to Evaluate the Efficacy and Safety of Adding Sitagliptin 100 mg Once Daily in Patients With T2DM Who Have Inadequate Glycemic Control on Metformin Therapy

CompletedPH IVMerck Sharp & Dohme LLCn=6082009

Study to Assess the Efficacy and Safety of Sitagliptin in Recently Diagnosed, Naive Type 2 Diabetics With Inadequate Glycemic Control on Diet and Exercise

CompletedPH IVMerck Sharp & Dohme LLCn=292008

A Phase III, Multicenter, Randomized, Placebo-Controlled, Double-Blind Clinical Trial to Evaluate the Safety and Efficacy of the Addition of Sitagliptin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Diet/Exercise Therapy and Acarbose Monotherapy

CompletedPH IIIMerck Sharp & Dohme LLCn=3802013

Recent completions

Trials that read out recently, adding to the completed evidence base.

A Randomized, Double-blind, Parallel-group, Placebo-controlled Study to Assess Efficacy, Safety and Tolerability of Sitagliptin Phosphate 100 mg as Treatment for Recurrent, Persistent or Newly Diagnosed Type 2 Diabetes After Gastric Bypass

CompletedN/ABlandine Laferreren=372016

A Phase III, Multicenter, Randomized, Placebo-Controlled, Double-Blind Clinical Trial to Evaluate the Safety and Efficacy of the Addition of Sitagliptin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Diet/Exercise Therapy and Acarbose Monotherapy

CompletedPH IIIMerck Sharp & Dohme LLCn=3802013

A Phase III, Multicenter, Double-Blind, Randomized, Active-Controlled Study to Evaluate the Safety and Efficacy of Sitagliptin Compared With Glimepiride in Elderly Patients With Type 2 Diabetes Mellitus With Inadequate Glycemic Control

CompletedPH IIIMerck Sharp & Dohme LLCn=4802012

A Phase III, Randomized, Clinical Trial to Evaluate the Safety and Efficacy of the Addition of Sitagliptin in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on a Sulfonylurea in Combination With Metformin

CompletedPH IIIMerck Sharp & Dohme LLCn=4272012

A Multicenter, Randomized, Double-Blind Study of the Co-Administration of Sitagliptin and Pioglitazone in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control

CompletedPH IIIKey trialMerck Sharp & Dohme LLCn=1,6152011

Treatment With Sitagliptin Phosphate in Patients With Reactive Hypoglycemia Secondary to Dysinsulinism. A Controlled, Randomized, Double-blind, Clinical Trial

CompletedPH IVInstituto Nacional de Ciencias Medicas y Nutricion Salvador Zubirann=202011

Research activity

8 papers

Key research shaping understanding of this drug, combining the latest publications with the most influential evidence.

Publications over time
20072024
Most influential

Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or on glimepiride and metformin.

Diabetes, obesity & metabolism · 2007 · 352 cites

Efficacy and safety of sitagliptin when added to insulin therapy in patients with type 2 diabetes.

Diabetes, obesity & metabolism · 2010 · 224 cites

Sitagliptin Treatment at the Time of Hospitalization Was Associated With Reduced Mortality in Patients With Type 2 Diabetes and COVID-19: A Multicenter, Case-Control, Retrospective, Observational Study.

Diabetes care · 2020 · 185 cites

Efficacy and safety of monotherapy of sitagliptin compared with metformin in patients with type 2 diabetes.

Diabetes, obesity & metabolism · 2010 · 123 cites

Efficacy and tolerability of sitagliptin monotherapy in elderly patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial.

Current medical research and opinion · 2011 · 107 cites

Dose-ranging efficacy of sitagliptin, a dipeptidyl peptidase-4 inhibitor, in Japanese patients with type 2 diabetes mellitus.

Endocrine journal · 2010 · 84 cites
Recent papers

DPP-4 inhibitors sitagliptin and PF-00734,200 mitigate dopaminergic neurodegeneration, neuroinflammation and behavioral impairment in the rat 6-OHDA model of Parkinson's disease.

GeroScience · 2024 · 12 cites

Sitagliptin Treatment at the Time of Hospitalization Was Associated With Reduced Mortality in Patients With Type 2 Diabetes and COVID-19: A Multicenter, Case-Control, Retrospective, Observational Study.

Diabetes care · 2020 · 185 cites

Efficacy and tolerability of sitagliptin monotherapy in elderly patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial.

Current medical research and opinion · 2011 · 107 cites

Efficacy and safety of sitagliptin when added to insulin therapy in patients with type 2 diabetes.

Diabetes, obesity & metabolism · 2010 · 224 cites

Efficacy and safety of monotherapy of sitagliptin compared with metformin in patients with type 2 diabetes.

Diabetes, obesity & metabolism · 2010 · 123 cites

Dose-ranging efficacy of sitagliptin, a dipeptidyl peptidase-4 inhibitor, in Japanese patients with type 2 diabetes mellitus.

Endocrine journal · 2010 · 84 cites
Major research themes8
Asian People2Coronavirus1Coronavirus Infections1Diabetes Mellitus, Type 21Dipeptidyl-Peptidase IV Inhibitors1Dopaminergic Neurons1Oxidopamine1Pandemics1
Journals, researchers & institutions
Top journals
  • Diabetes, obesity & metabolism4
  • Current medical research and opinion1
  • Diabetes care1
  • Endocrine journal1
  • GeroScience1
Leading researchers
  • Amatruda JM3
  • Kaufman KD3
  • Arjona Ferreira JC2
  • Goldstein BJ2
  • Guo H2
  • Iwamoto Y2
  • Luo E2
  • Nonaka K2
Leading institutions
free-text, unnormalised
  • Diabetes Center2
  • "V. Buzzi" Children's Hospital1
  • Aarhus University Hospital1
  • Boston Children's Hospital1
  • Brigham and Women's Hospital1
  • Center for Neuropsychiatric Research1

Related diseases

1 conditions

Regulator-approved indications and conditions co-mentioned with this drug across the research literature. Number shows shared papers.

Active research areas
Diabetes Mellitus, Type 22

Related drugs

2 matches

Drugs sharing diseases, protein targets and literature with this one. Ranked by graph evidence (shared targets + diseases weighted above co-mentions).

Metformin

Studied across 3 of the same disease areas as Sitagliptin Phosphate in the shared literature.

3 shared diseases1 shared paper
Glimepiride

Studied across 2 of the same disease areas as Sitagliptin Phosphate in the shared literature.

2 shared diseases1 shared paper
References & data sources
  • RxNorm (U.S. National Library of Medicine) — drug identity
  • ChEMBL (EMBL-EBI) & UniProt — pharmacology and targets
  • Europe PMC — research literature
  • ClinicalTrials.gov — clinical trials
  • Regulatory event sources are credited in the Regulatory Timeline above.