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Linagliptin

Phase 3

Diabetes Mellitus, Type 2 | Small molecule | Metabolic |Eli Lilly and Company|Last Updated: Sep 19, 2024

Success Probability

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Trial Design

RandomizedDouble-BlindACTIVE_CONTROLLEDBiomarker
Total Trials11
Total Enrollment11,124

FDA Designations

No designations recorded

Clinical trial landscape

Linagliptin · 11 trials · 1 indication

Phase 3 11
NCT01204294Comprehensive Add on Study in JapanDiabetes Mellitus, Type 2
COMPLETED574 Analytics
NCT0118301330 Week Parallel Group Comparison Study of Linagliptin + Pioglitazone (5+15, 5+30 and 5+45 mg) qd Versus Respective Monotherapies, Followed by a Comparison of 5mg+30mg and 5mg+45mg Versus Respective Monotherapies in Type 2 Diabetes for up to 54 WeeksDiabetes Mellitus, Type 2
COMPLETED936 Analytics
NCT01084005Efficacy and Safety of Linagliptin in Elderly Patients With Type 2 DiabetesDiabetes Mellitus, Type 2
COMPLETED241 Analytics
NCT01087502Safety and Efficacy of Linagliptin in Type-2-diabetes Mellitus Patients With Moderate to Severe Renal ImpairmentDiabetes Mellitus, Type 2
COMPLETED241 Analytics
NCT00954447Efficacy and Safety of Linagliptin in Combination With Insulin in Patients With Type 2 DiabetesDiabetes Mellitus, Type 2
COMPLETED1,263 Analytics
NCT02453555Empagliflozin Add on to Linagliptin Study in Japanese Patient With Type 2 Diabetes MellitusDiabetes Mellitus, Type 2
COMPLETED275 Analytics
NCT01734785Safety and Efficacy of the Combination of Empagliflozin and Linagliptin Compared to Linagliptin Alone Over 24 Weeks in Patients With Type 2 DiabetesDiabetes Mellitus, Type 2
COMPLETED607 Analytics
NCT01243424CAROLINA: Cardiovascular Outcome Study of Linagliptin Versus Glimepiride in Patients With Type 2 DiabetesDiabetes Mellitus, Type 2
COMPLETED6,103 Analytics
NCT01214239Efficacy and Safety Study of Linagliptin (5 mg Administered Orally Once Daily) Over 24 Weeks, in Drug naïve or Previously Treated Type 2 Diabetic Patients With Insufficient Glycaemic ControlDiabetes Mellitus, Type 2
COMPLETED300 Analytics
NCT01215097Efficacy and Safety Study of Linagliptin (5 mg Administered Orally Once Daily) Over 24 Weeks in Type 2 Diabetic Patients With Insufficient Glycaemic Control Despite Metformin TherapyDiabetes Mellitus, Type 2
COMPLETED306 Analytics
PHASE3COMPLETED
Comprehensive Add on Study in Japan
Diabetes Mellitus, Type 2Unlock trial analytics
PHASE3COMPLETED
30 Week Parallel Group Comparison Study of Linagliptin + Pioglitazone (5+15, 5+30 and 5+45 mg) qd Versus Respective Monotherapies, Followed by a Comparison of 5mg+30mg and 5mg+45mg Versus Respective Monotherapies in Type 2 Diabetes for up to 54 Weeks
Diabetes Mellitus, Type 2Unlock trial analytics
PHASE3COMPLETED
Efficacy and Safety of Linagliptin in Elderly Patients With Type 2 Diabetes
Diabetes Mellitus, Type 2Unlock trial analytics
PHASE3COMPLETED
Safety and Efficacy of Linagliptin in Type-2-diabetes Mellitus Patients With Moderate to Severe Renal Impairment
Diabetes Mellitus, Type 2Unlock trial analytics
PHASE3COMPLETED
Efficacy and Safety of Linagliptin in Combination With Insulin in Patients With Type 2 Diabetes
Diabetes Mellitus, Type 2Unlock trial analytics
PHASE3COMPLETED
Empagliflozin Add on to Linagliptin Study in Japanese Patient With Type 2 Diabetes Mellitus
Diabetes Mellitus, Type 2Unlock trial analytics
PHASE3COMPLETED
Safety and Efficacy of the Combination of Empagliflozin and Linagliptin Compared to Linagliptin Alone Over 24 Weeks in Patients With Type 2 Diabetes
Diabetes Mellitus, Type 2Unlock trial analytics
PHASE3COMPLETED
CAROLINA: Cardiovascular Outcome Study of Linagliptin Versus Glimepiride in Patients With Type 2 Diabetes
Diabetes Mellitus, Type 2Unlock trial analytics
PHASE3COMPLETED
Efficacy and Safety Study of Linagliptin (5 mg Administered Orally Once Daily) Over 24 Weeks, in Drug naïve or Previously Treated Type 2 Diabetic Patients With Insufficient Glycaemic Control
Diabetes Mellitus, Type 2Unlock trial analytics
PHASE3COMPLETED
Efficacy and Safety Study of Linagliptin (5 mg Administered Orally Once Daily) Over 24 Weeks in Type 2 Diabetic Patients With Insufficient Glycaemic Control Despite Metformin Therapy
Diabetes Mellitus, Type 2Unlock trial analytics

Study Endpoints

Primary Endpoints

Incidence of Adverse Events (AEs)
The first drug administration through 7 days after the last drug administration, up to 382 days

The number of patient with any AEs, patients with severe AE, patients with AEs leading to discontinuation of trial drug, and patients with Hypoglycaemic events

Change From Baseline in HbA1c After 30 Weeks of Treatment.
Baseline and 30 weeks

HbA1c is measured as a percentage. The change from baseline is the Week 30 HbA1c minus the baseline HbA1c.

HbA1c Change From Baseline to Week 24
Baseline and week 24

HbA1c is measured as a percentage. Thus, this change from baseline reflects the Week 24 HbA1c percent minus the baseline HbA1c percent. Means are treatment adjusted for baseline HbA1c and prior use of insulin.

HbA1c Change From Baseline to Week 12
Baseline and week 12

HbA1c is measured as a percentage. Thus, this change from baseline reflects the Week 12 HbA1c percent minus the baseline HbA1c percent. Means are treatment adjusted for baseline HbA1c, renal function impairment and prior use of antidiabetic agents.

Change From Baseline in HbA1c After 24 Weeks
Baseline and 24 weeks

HbA1c is measured as a percentage. Adjusted for treatment, baseline HbA1c, categorical renal function impairment and concomitant Oral antidiabetic drugs (OAD)

Change of Glycosylated Haemoglobin A1c (Glycosylated Haemoglobin A1c After 24 Weeks of Double-blind Treatment From Baseline)
Baseline and 24 week

Change from baseline in Glycosylated haemoglobin A1c (HbA1c) at Week 24 was calculated as: HbA1c at Week 24 - HbA1c at baseline. Baseline is referred to the last observed measurement prior to the administration of randomized trial medication. Adjusted mean (Least square mean) and its standard error (SE) is presented.

HbA1c Change From Baseline After 24 Weeks Double-blind Randomized Treatment
Baseline and 24 weeks

Change from baseline in Glycated haemoglobin (HbA1c) \[%\] after 24 weeks of treatment with double-blind trial medication. Baseline was defined as the last observation before the first intake of any double-blind randomised trial medication. The term 'baseline' was not used to refer to measurements before the administration of open-label medication.

The First 3-point Major Adverse Cardiovascular Events (3P-MACE)
From randomization until individual day of trial completion, up to 432 weeks

The first occurrence of any of the following Clinical Event Committee (CEC) confirmed adjudicated components of the primary composite endpoint: CV death (including fatal stroke and fatal myocardial infarction (MI)), non-fatal MI (excluding silent MI), or nonfatal stroke is presented.

HbA1c Change From Baseline at Week 24
Baseline and at week 24

Means are treatment adjusted for baseline HbA1c and previous anti-diabetic medication.

Change From Baseline in HbA1c (Glycosylated Hemoglobin) After 24 Weeks
baseline, 24 weeks

Glycosylated hemoglobin is reported as a percentage of the total hemoglobin

Secondary Endpoints

Glycosylated Haemoglobin A1c (HbA1c)
Baseline and 52 weeks
Occurrence of Cumulative Treat to Target Efficacy Response, of HbA1c Under Treatment of < 7.0% After 30 Weeks of Treatment
Baseline and 30 weeks
Occurrence of Cumulative Treat to Target Efficacy Response, of HbA1c Under Treatment of < 6.5% After 30 Weeks of Treatment
Baseline and 30 weeks
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Bigu+LinaEXPERIMENTALbiguanide plus linagliptin
Glin+LinaEXPERIMENTALglinide plus linagliptin
Glit+LinaEXPERIMENTALglitazone plus linagliptin
SU+LinaEXPERIMENTALsulfonylurea plus linagliptin
A-GI+LinaEXPERIMENTALalpha-glucosidase inhibitor plus linagliptin
SU+MetACTIVE_COMPARATORsulfonylurea plus metformin
A-GI+MetACTIVE_COMPARATORalpha-glucosidase inhibitor plus metformin
Pioglitazone 15 mgACTIVE_COMPARATORPioglitazone Capsules 15 mg once daily
Pioglitazone 30 mgACTIVE_COMPARATORPioglitazone Capsules 30 mg once daily
Pioglitazone 45 mgACTIVE_COMPARATORPioglitazone Capsules 45 mg once daily
Linagliptin 5mgACTIVE_COMPARATORLinagliptin 5mg Tablets once daily
Linagliptin 5mg / Pioglitazone 15 mgEXPERIMENTALLinagliptin 5mg / Pioglitazone 15 mg Tablets once daily
Linagliptin 5mg / Pioglitazone 30 mgEXPERIMENTALLinagliptin 5mg / Pioglitazone 30 mg Tablets once daily
Linagliptin 5mg / Pioglitazone 45 mgEXPERIMENTALLinagliptin 5mg / Pioglitazone 45 mg Tablets once daily
linagliptinEXPERIMENTALpatients receive linagliptin 5 mg tablets once daily
placeboPLACEBO_COMPARATORpatients receive placebo tablets matching linagliptin 5 mg once daily
GlimepirideACTIVE_COMPARATORPlacebo patients switch to glimepiride after 12 weeks (40 weeks treatment)
Empagliflozin + linagliptin low doseEXPERIMENTALpatient to receive one tablet once daily
Empagliflozin + linagliptin high doseEXPERIMENTALpatient to receive one tablet once daily
Linagliptin placeboPLACEBO_COMPARATOR -
Empagliflozin + linagliptin high dose placeboPLACEBO_COMPARATOR -
Empagliflozin + linagliptin low dose placeboPLACEBO_COMPARATOR -
glimepiride 1-4 mg QDACTIVE_COMPARATORpatient to receive glimepiride 1-4 mg or linagliptin placebo tablet Quaque die (QD)

Interventions

NameTypeDescription
LinagliptinDRUGLinagliptin once daily
MetforminDRUGMetformin twice or three time per day
Pioglitazone 15 mgDRUGPioglitazone Capsules 15 mg once daily for 30 weeks followed by Pioglitazone Capsules 30 mg once daily for up to 54 weeks
Pioglitazone 45 mgDRUGPioglitazone Capsules 30 mg once daily for 6 weeks followed by Pioglitazone Capsules 45 mg once daily for up to 78 weeks
Pioglitazone 30 mgDRUGPioglitazone Capsules 30 mg once daily for up to 84 weeks
Linagliptin 5mg / Pioglitazone 45 mg FDCDRUGLinagliptin 5mg low dose / Pioglitazone 30 mg Tablets once daily for 6 weeks followed by Linagliptin 5mg low dose / Pioglitazone 45 mg FDC Tablets once daily for up to 78 weeks
Linagliptin 5mg / Pioglitazone 30 mg FDCDRUGLinagliptin 5mg low dose / Pioglitazone 30 mg FDC Tablets once daily for up to 84 weeks
Linagliptin 5mgDRUGLinagliptin 5mg Tablets low dose once daily for 30 weeks followed by Linagliptin 5mg low dose / Pioglitazone 30 mg FDC Tablets once daily for up to 54 weeks
Linagliptin 5mg / Pioglitazone 15 mg FDCDRUGLinagliptin 5mg low dose / Pioglitazone 15 mg FDC Tablets once daily for 30 weeks followed by Linagliptin 5mg low dose / Pioglitazone 30 mg FDC Tablets once daily for up to 54 weeks
placeboDRUGpatients receive placebo matching linagliptin 5 mg once daily
GlimepirideDRUG1-4 mg daily after 12 weeks
Empagliflozin placebo + linagliptin placebo low doseDRUGMatching placebo empagliflozin + linagliptin
Empagliflozin + linagliptin low doseDRUGtablet
Linagliptin placeboDRUGMatching placebo linagliptin
Empagliflozin + linagliptin high doseDRUGtablet
Empa + lina highdose placeboDRUG -
Empagliflozin + LinagliptinDRUGFixed dose combination.
Empagliflozin placebo + Linagliptin placeboDRUGMatching Empagliflozin + Linagliptin low dose
glimepiride placeboDRUGglimepiride placebo
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Eligibility Criteria

Age Range20 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites43

Inclusion criteria: 1. Diagnosis of type 2 diabetes mellitus 2. Male and female patients on diet and exercise regimen who are treated with one antidiabetic drug Exclusion criteria: 1. Myocardial infarction, stroke, transient ischemic attack, or pulmonary embolism 2. Impaired hepatic function 3. G...

Countries:JapanUnited StatesEstoniaGermanyLatviaSpainUnited KingdomAustraliaCanadaDenmarkNetherlandsSwedenFinlandIsraelNew ZealandSlovakiaArgentinaBelgiumBrazilCzechiaGreeceItalyMexicoNorwayPeruRussiaSouth KoreaTaiwanEl SalvadorFranceBulgariaChileColombiaGeorgiaHong KongHungaryIndiaIrelandMalaysiaPhilippinesPortugalRomaniaSerbiaSouth AfricaSwitzerlandTunisiaUkraineChina
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Frequently asked questions about Linagliptin

What is Linagliptin used for?

Linagliptin is a small molecule drug being developed for Type 2 Diabetes Mellitus and has been studied in healthy subjects. It is in Phase 3 clinical development by Eli Lilly and Company. The drug has been evaluated in 11 completed trials with a total enrollment of 11,124 participants.

How does Linagliptin work?

Linagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that works by blocking the enzyme DPP-4, which degrades incretin hormones. This increases active incretin levels, helping to regulate blood glucose by enhancing insulin secretion and reducing glucagon release in a glucose-dependent manner.

Who makes Linagliptin?

Linagliptin is being developed by Eli Lilly and Company, a pharmaceutical company traded on the NYSE under the ticker symbol LLY. The drug is in Phase 3 clinical development for Type 2 Diabetes Mellitus.

What phase is Linagliptin in?

Linagliptin is in Phase 3 clinical development. It is an investigational drug and has not been approved by regulatory authorities. The drug has completed 11 clinical trials, with no active trials currently ongoing.

What clinical trials is Linagliptin in?

Linagliptin has been studied in 11 completed clinical trials. Notable trials include NCT01204294, a Phase 3 study in Japan for Type 2 Diabetes Mellitus, and several Phase 1 bioequivalence studies in healthy subjects, such as NCT02084082 and NCT02121509, which tested fixed-dose combination tablets with metformin.

Is Linagliptin the same as Tradjenta?

Linagliptin is the generic name for the drug marketed as Tradjenta. It is a DPP-4 inhibitor used for the treatment of Type 2 Diabetes Mellitus. The drug is being developed by Eli Lilly and Company and is currently in Phase 3 clinical trials.