TheraRadar
Data updated: May 26, 2026

ZITUVIO (sitagliptin)

Dipeptidyl Peptidase 4 Inhibitors Genetically Validated Trial Activity: Declining 5 active trials
Metabolic Approved 2023-10-18

Zituvio (sitagliptin) is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It is not recommended for use in patients with type 1 diabetes. Use in patients with a history of pancreatitis has not been studied, and it is unknown if these patients are at an increased risk for developing pancreatitis while on this medication.

Source: FDA Label • ZYDUS LIFESCIENCES • Dipeptidyl Peptidase 4 Inhibitor

How ZITUVIO Works

Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that slows the inactivation of incretin hormones, including GLP-1 and GIP. By increasing and prolonging active incretin levels, the drug stimulates insulin synthesis and release from pancreatic beta cells and reduces glucagon secretion from pancreatic alpha cells. These effects are glucose-dependent, occurring primarily when blood glucose levels are normal or elevated, ultimately leading to reduced hepatic glucose production and improved glucose homeostasis.

Development Insights

Merck Sharp & Dohme LLC conducting 29 trials (14%)
100 indications explored (Broad Platform)
type 2 diabetes mellitus (57 trials)
diabetes mellitus, type 2 (50 trials)
type 2 diabetes (21 trials)
1
Indication
--
Phase 3 Trials
2
Years on Market

Details

Status
Prescription
First Approved
2023-10-18
Patent Cliff
2035

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Patent cliff and revenue data

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Routes
ORAL
Dosage Forms
TABLET

Companies

Active Ingredient: SITAGLIPTIN

ZITUVIO Approval History

2024
2025
2026
Original
New Indication
New Form
Label Update
3 FDA actions from 2023 to 2023
Oct 2023 ORIGINAL
New Ingredient · Type 2 - New Active Ingredient

What ZITUVIO Treats

1 indications

ZITUVIO is approved for 1 conditions since its original approval in 2023. These indications span multiple therapeutic areas including oncology, immunology, and more.

  • Type 2 Diabetes
Source: FDA Label

ZITUVIO Target & Pathway

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Target

GLP-1 (Glucagon-Like Peptide-1) Incretin Receptor

A hormone released after eating that stimulates insulin secretion, suppresses glucagon, slows gastric emptying, and promotes satiety. GLP-1 receptor agonists mimic these effects, improving blood sugar control and promoting weight loss in diabetes and obesity.

What's emerging in ZITUVIO's indications

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Phase 3 candidates targeting molecules with no FDA-approved drug, in indications ZITUVIO treats. First-in-class if their pivotal trials read out positive.

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Clinical Trial Registry

213 trials
Trial Sponsor ID Phase Status Title
NCT07003542 CASE2325 Ph 2 recruiting A Phase 2 and Pharmacodynamic Study of Sitagliptin in Patients With Progressive Grade 4 Gliomas
NCT07567781 M25-744 Ph 1 recruiting A Phase 1 Study to Assess the Effect of ABBV-722 on Midazolam, Digoxin, Pitavastatin, Metformin, and Sitagliptin Drug Levels in Healthy Adults.
NCT07541781 202512310 Ph 1 not yet recruiting Sitagliptin in Recurrent/Progressive Grade 4 Glioma
NCT06246799 STUDY00000139 R01DK097554 Ph 3 recruiting Comparative Effectiveness of Two Initial Combination Therapies in Patients With Recent Onset Diabetes
NCT06851962 EPHIC-DIA2 EPHIC-DIA2 2025-520686-46-00 Ph 4 active not recruiting Impact of Pharmacogenetic-Guided Treatment on Type 2 Diabetes.
NCT06263673 results posted 23-008183 Ph 4 completed Anti-Diabetic Medications to Fight PD and LBD
NCT02650427 HCC-DPPIV C15-41 2015-002968-17 Ph 1 completed A Pilot Study to Evaluate the Safety of a 3 Weeks Sitagliptin Treatment in HCC Patients Undergoing Liver Resection
NCT03738878 results posted IRB#170762 Ph 4 terminated Mechanism(s) Underlying Hypotensive Response to ARB/NEP Inhibition - Aim 1
NCT04409795 2019-76 Ph 2, Ph 3 completed Oral Hypoglycemic Therapy for Monogenic Variant Carriers of the Joslin Medalist Study
NCT02512523 HD_TEN_PH42014 Ph 4 completed Exploratory Study to Compare the Effects of Tenelia® or Januvia® on Glucose Variability in add-on to Metformin (CGMS Study)
NCT06054815 DA1241_NASH_IIa Ph 2 completed Study to Evaluate the Efficacy and Safety of DA-1241 in Subjects With Presumed NASH
NCT04017832 PIONEER 12 results posted NN9924-4309 U1111-1188-1256, 2018-002589-38 Ph 3 completed A Research Study Comparing a New Medicine Oral Semaglutide to Sitagliptin in People With Type 2 Diabetes
NCT04304261 ESCDP ESCDP Ph 3 completed Effects of SGLT2i on the Cognitive Function in T2DM Patient (ESCDP)
NCT05895201 CTO-IUSCCC-0778 Ph 1, Ph 2 withdrawn High-Dose Post-Transplant Cyclophosphamide, Bortezomib, and Sitagliptin for the Prevention of GVHD
NCT00936663 results posted 0254-09-FB Ph 4 terminated Using Sitagliptin as a Treatment to Prevent New Onset Diabetes After Kidney Transplantation
NCT05219409 SITA-one 01/2022 Ph 2, Ph 3 not yet recruiting Effects of Sitagliptin in Relatives of T1D Patients
NCT03790839 HMM0111 Ph 1 completed Drug Interaction Study Between Dorzagliatin and Sitagliptin
NCT01928199 results posted 201306111 50669 Ph 4 completed Efficacy Study of Sitagliptin to Prevent New-onset Diabetes After Kidney Transplant
NCT03101930 results posted IRB# 170213 Ph 4 completed Cardiovascular Effects of GLP-1 Receptor Activation
NCT03076112 B-1612/375-004 Ph 3 completed Efficacy of Ipragliflozin Compared With Sitagliptin in Uncontrolled Type 2 Diabetes With Sulfonylurea and Metformin
NCT01485614 results posted 0431-083 2011-002528-42, MK-0431-083 Ph 3 completed Study to Assess Safety & Efficacy of Sitagliptin as Initial Oral Therapy for Treatment of Type 2 Diabetes Mellitus in Pediatric Participants. (MK-0431-083)
NCT02607865 PIONEER 3 results posted NN9924-4222 2015-001351-71, U1111-1168-4339 Ph 3 completed Efficacy and Long-term Safety of Oral Semaglutide Versus Sitagliptin in Subjects With Type 2 Diabetes
NCT02849080 PIONEER 7 results posted NN9924-4257 2015-005593-38, U1111-1177-5103 Ph 3 completed Efficacy and Safety of Oral Semaglutide Using a Flexible Dose Adjustment Based on Clinical Evaluation Versus Sitagliptin in Subjects With Type 2 Diabetes Mellitus.
NCT05266404 D1683C00014 2021-005104-35 Ph 1 completed Phase 1 Bioequivalence Study of Dapagliflozin/Sitagliptin FDC vs Loose Combination of Single Components
NCT02338921 Triple_3 Ph 4 completed Triple Combination Therapy in Type 2 Diabetic Patients Who Had Inadequate Glycemic Control With Combination Therapy
NCT00790205 TECOS results posted 0431-082 2008_523, 2008-006719-20 Ph 3 completed Sitagliptin Cardiovascular Outcomes Study (MK-0431-082)
NCT02917031 MEASURE-HF results posted D1680C00016 Ph 4 completed Mechanistic Evaluation of Glucose-lowering Strategies in Patients With Heart Failure
NCT02956044 results posted THR-1442-C-453 Ph 1 completed Interaction of Bexagliflozin With Metformin, Glimepiride and Sitagliptin
NCT03115112 results posted THR-1442-C-423 Ph 3 completed Safety and Efficacy of Bexagliflozin Compared to Sitagliptin as Add-on Therapy to Metformin in Type 2 Diabetes Subjects
NCT03893526 NEPT2D NEPT2D Ph 4 completed Effect of Neprilysin on Glucagon-Like Peptide-1 in Patients With Type 2 Diabetes
NCT03061214 SUSTAIN results posted NN9535-4114 U1111-1149-0432, CTR20161003 Ph 3 completed Efficacy and Safety of Semaglutide Once-weekly Versus Sitagliptin Once-daily as add-on to Metformin in Subjects With Type 2 Diabetes (SUSTAIN - CHINA MRCT)
NCT00627744 BEGAMI BEGAMI Ph 4 completed Beta-cell Function in Glucose Abnormalities and Acute Myocardial Infarction
NCT03646721 DA1241_DM_Ib Ph 1 completed A Study to Evaluate the Safety, Tolerability, PK and PD of DA-1241 in Healthy Male Subjects and Subjects With T2DM
NCT02683525 results posted IUSCC-0522 Ph 2 completed Sitagliptin for Prevention of Acute Graft Versus-Host Disease After Allogeneic Hematopoietic Stem Cell Transplantation
NCT00860288 CLAF237B2224 Ph 2, Ph 3 completed Efficacy and Long-Term Safety of Vildagliptin as Add-on Therapy to Metformin in Patients With Type 2 Diabetes
NCT00770081 CLAF237A23138E1 Ph 3 completed Safety and Tolerability of Vildagliptin Versus Sitagliptin in Patients With Type 2 Diabetes and Severe Renal Insufficiency (28-week Extension Study)
NCT01619332 CLEZ763X2201 Ph 1, Ph 2 completed Clinical Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of LEZ763
NCT00616811 CLAF237A23138 Ph 3 completed Safety and Tolerability of Vildagliptin Versus Sitagliptin in Patients With Type 2 Diabetes and Severe Renal Insufficiency
NCT03108521 results posted 2015SZ0182 Ph 4 completed SNP Study of DPP-4 and GLP-1R in Chinese People (Including Diabetes Patients)
NCT01991197 DIP results posted DPIDM-2012-01 2012-005505-51 Ph 2 completed Dipeptidyl Peptidase-4 Inhibition in Psoriasis Patients With Diabetes (DIP): A Randomized Clinical Trial.
NCT02536248 results posted JANU-INF Ph 3 completed Sitagliptin Therapy and Kinetics of Inflammatory Markers
NCT02122380 results posted 131969 K23HL119602-01A1 Ph 4 completed The Effect of Dipeptidyl Peptidase 4 Inhibition on Growth Hormone Secretion in Women With Polycystic Ovarian Syndrome
NCT02043054 LYDIA 0398 2012-002422-78, U1111-1131-8802 Ph 3 completed Effects of Liraglutide in Young Adults With Type 2 DIAbetes (LYDIA)
NCT02556918 SITA-CABGDM results posted IRB00082180 Ph 4 completed Sitagliptin for Hyperglycemia in Patients With T2DM Undergoing Cardiac Surgery
NCT02920918 results posted HM20007043 28431754DIATBD Ph 4 completed Treatment of Diabetes in Patients With Systolic Heart Failure
NCT02173457 CMAS CGZ302 Ph 3 completed Study of Chiglitazar Compare With Sitagliptin in Type 2 Diabetes Patients
NCT02111096 results posted 15286 I1R-MC-GLDJ, 2013-004275-12 Ph 2 terminated A Study of LY2409021 in Participants With Type 2 Diabetes Mellitus
NCT02072096 IMPERIUM results posted 14842 F3Z-MC-IOQL, 2013-001473-24 Ph 4 terminated A Comparison of Two Treatment Strategies in Older Participants With Type 2 Diabetes Mellitus (T2DM)
NCT02743260 PHENTRA_2015_KPUK Ph 4 completed Drug Transporter Interaction Study PHENTRA_2015_KPUK
NCT02330406 REASON ICE_2014_01R Ph 4 completed Randomized Evaluation of Anagliptin Versus Sitagliptin On Low-density lipoproteiN Cholesterol in Diabetes Trial

Showing 50 of 213 trials

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Active Pipeline

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Ongoing clinical trials by development phase

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Key Completed Trials

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Completed studies with published results, ranked by significance

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Trial Timeline

Full development history with FDA approval milestones

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Understanding FDA Approval Types
Count Type What it means
- ORIG Original approval - drug first enters market
- SUPPL - Efficacy New indication (new disease/condition approved)
- SUPPL - Labeling Label text changes (warnings, dosing updates)
- SUPPL - Manufacturing Production changes (new facility)
- SUPPL - Chemistry Formulation changes (new dosage strength)

Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.

ZITUVIO FDA Label Details

Indications & Usage

FDA Label (PDF)

ZITUVIO is indicated for the treatment of Type 2 Diabetes.

View full patent landscape →
1 OB patents · 1 families · 7 international docs across 5 countries

ZITUVIO Patents & Exclusivity

Latest Patent: Feb 2035

Patents (1 active)

US10925871 Expires Feb 25, 2035
Source: FDA Orange Book

Pro Intelligence Preview

Deep insights for ZITUVIO

Revenue Insights

  • Quarterly revenue tracking
  • Historical trend analysis

Patent Timeline

  • Cliff: 2035
  • 9 active patents

Trial Analysis

  • 213 total trials
  • Stage: Declining

Competitive Landscape

  • 20 similar drugs
  • Same target/indication analysis
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Data Sources

Data sourced from official FDA and NIH databases. Click links to verify on original sources.

How We Calculate These Metrics

Trial Activity Stage

Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.

Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.

  • Growth: High proportion of early-phase trials (Phase 1/2), active development
  • Expansion: Significant Phase 3 activity, approaching or pursuing approvals
  • Mature: Substantial Phase 4 post-marketing studies
  • Stable: Mixed phase distribution, steady development
  • Declining: Low active trial ratio, reduced R&D investment