Linagliptin

A purine and quinazoline derivative that functions as an INCRETIN and DIPEPTIDYL-PEPTIDASE IV INHIBTOR. It is used as a HYPOGLYCEMIC AGENT in the treatment of TYPE II DIABETES MELLITUS.

Also Known As:

(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione; 1H-purine-2,6-dione, 8-((3r)-3-amino-1-piperidinyl)-7-(2-butynyl)-3,7-dihydro-3-methyl-1-((4-methyl-2-quinazolinyl)methyl)-; BI 1356; BI-1356; BI1356; Tradjenta; Trajenta; 1356, BI

Networked: 575 relevant articles (92 outcomes, 221 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Purines: 651
      - Linagliptin: 575
    - Quinazolines: 402
      - Linagliptin: 575

Experts

1.	Klein, Thomas: 38 articles (01/2021 - 01/2011)
2.	Woerle, Hans-Juergen: 38 articles (01/2018 - 06/2010)
3.	Patel, Sanjay: 34 articles (09/2017 - 01/2012)
4.	von Eynatten, Maximilian: 32 articles (09/2021 - 01/2012)
5.	Johansen, Odd Erik: 22 articles (09/2021 - 01/2012)
6.	Woerle, H-J: 20 articles (01/2016 - 12/2010)
7.	Rosenstock, Julio: 19 articles (09/2021 - 08/2012)
8.	Zinman, Bernard: 16 articles (09/2021 - 07/2013)
9.	Marx, Nikolaus: 14 articles (09/2021 - 07/2013)
10.	Cooper, Mark E: 13 articles (09/2021 - 11/2013)

Related Diseases

1.	Type 2 Diabetes Mellitus (MODY) 03/01/2011 - "To assess the safety and efficacy of the potent and selective dipeptidyl peptidase-4 inhibitor linagliptin 5 mg when given for 24 weeks to patients with type 2 diabetes who were either treatment-naive or who had received one oral antidiabetes drug (OAD). " 03/26/2011 - "In two double-blind, multicentre trials (n >350 evaluable patients/trial) in adult patients with inadequately controlled type 2 diabetes mellitus, oral linagliptin monotherapy (5 or 10 mg once daily) was significantly more effective than placebo in improving glycaemic control and several parameters of pancreatic function, with placebo-corrected adjusted mean changes in glycosylated haemoglobin (HbA(1c)) levels of -0.69% to -0.88% after 12 or 24 weeks. " 09/01/2014 - "Linagliptin significantly improved hyperglycaemia in patients with type 2 diabetes both with and without the TCF7L2 gene diabetes risk alleles. " 02/01/2015 - "Linagliptin is considered to be effective for patients with type 2 diabetes and renal impairment in the present analysis performed at our institution." 09/10/2012 - "However, clinical data currently available indicate that linagliptin is an effective and generally well tolerated treatment option for use in patients with type 2 diabetes, including those with renal impairment for whom other antihyperglycaemia agents require dosage adjustment or are not suitable."
2.	Hypoglycemia (Reactive Hypoglycemia) 02/01/2022 - "Severe hypoglycemia had slightly descended incidence, whereas insignificant difference was shown in the linagliptin cohorts in contrast to placebo cohorts (OR=0.95, 95 % CI: 0.68, 1.32, p=0.76). " 05/15/2021 - "Notably, linagliptin inhibited the colonic DPP-4 activity and upregulated the expression of intestinotrophic GLP-2 without incurring hypoglycemia in animals. " 05/01/2020 - "Overall, no new safety findings were identified for linagliptin, and no increased risk of hypoglycemia was observed for linagliptin versus placebo. " 12/01/2017 - "The degree of hypoglycemia in klotho-/- mice was less in linagliptin group than in control group, as estimated by the findings of OGTT. " 11/01/2016 - "Among subjects with hepatic disorders, 13.5% and 14.8% of the linagliptin and placebo groups, respectively, reported drug-related adverse events while 10.4% and 15.9%, respectively, reported hypoglycemia. "
3.	Weight Gain 01/01/2021 - "Linagliptin monotherapy was effective, without producing hypoglycaemia or weight gain." 04/01/2013 - "These findings provide evidence for the safety and tolerability of oral linagliptin at either 5 or 10 mg for up to 52 weeks for the treatment of Japanese patients with T2DM, without clinically relevant increase in the risk of hypoglycaemia or weight gain." 02/01/2012 - "As other molecules belonging to this pharmacological class, linagliptin improves blood glucose control of type 2 diabetic patients, without increasing hypoglycaemic risk, without promoting weight gain and with a good clinical and biological tolerance profile. " 05/01/2013 - "Consistent with other members of its class, the benefits of linagliptin also include a low risk of hypoglycemia and weight gain. " 09/01/2012 - "The overall tolerability of linagliptin was similar to that of placebo, with a low risk for hypoglycemia and no significant weight gain. "
4.	Body Weight (Weight, Body) 06/05/2023 - "Linagliptin increased mortality and heart/body weight ratio in mice with HF. " 12/01/2017 - "Thus, linagliptin significantly prevented body weight loss in klotho-/- mice. " 12/01/2017 - "Body weight of klotho-/- mice was greater in linagliptin group than in control group (11.1 ± 0.3 vs 9.9 ± 0.3 g; P < 0.01), which was associated with greater gastrocnemius muscle weight (P < 0.01) and greater kidney weight (P < 0.05) in linagliptin group. " 01/01/2016 - "No meaningful changes in mean (±sd) body weight were noted in either group [week 52: linagliptin, -0.5 (±3.2) kg; placebo, 0.0 (±3.1) kg]. " 03/01/2015 - "By Week 52, changes (SE) in mean body weight were similar in both groups (linagliptin -0.67 [0.26] kg, placebo -0.38 [0.25] kg). "
5.	Hyperglycemia 11/01/2014 - "This pooled analysis found that linagliptin was well tolerated and significantly improved hyperglycemia in a clinically challenging population of patients with long-standing T2DM (>10 years). " 01/01/2017 - "Linagliptin effectively reduced hyperglycemia in Asian patients with uncontrolled T2D, irrespective of age, BMI, renal function, or ethnic subgroups, and was well tolerated. " 10/01/2016 - "This post-hoc analysis supports that linagliptin achieved clinically meaningful improvements in hyperglycemia in patients with diverse clinical characteristics. " 04/01/2020 - "Therefore, linagliptin may be considered as a therapeutic treatment for stroke patients with mild hyperglycemia." 01/01/2019 - "Linagliptin is a dipeptidyl peptidase-4 inhibitor which is clinically approved to reduce hyperglycemia in type 2 diabetes. "

Related Drugs and Biologics

1.	Metformin (Glucophage)
2.	Glucose (Dextrose)
3.	Insulin (Novolin)
4.	Dipeptidyl-Peptidase IV Inhibitors
5.	glimepiride (Amarel)
6.	Glucagon-Like Peptide 1 (GLP 1)
7.	Hypoglycemic Agents (Hypoglycemics)
8.	Antioxidants
9.	Enzymes
10.	empagliflozin

Related Therapies and Procedures

1.	Therapeutics
2.	Glycemic Control
3.	Oral Administration
4.	Injections
5.	Renal Dialysis (Hemodialysis)