linagliptin / Generic mfg. - LARVOL DELTA

Real-World Data on Severe Cutaneous Adverse Reactions to Drugs. (PubMed, Pharmaceuticals (Basel)) - "The top five drugs involved in SCARs were dupilumab (2.14%, n = 244), piperacillin and beta-lactamase inhibitor (2.0%, n = 227), pembrolizumab (1.98%, n = 225), levofloxacin (1.95%, n = 222), and linagliptin (1.93%, n = 220). The strongest signals were detected for linagliptin (PRR = 15.37, 95% CI: 13.54-17.44; ROR = 17.24, 95% CI: 14.95-19.88), followed by clindamycin (PRR = 12.44, 95% CI: 10.89-14.21; ROR = 13.62, 95% CI: 11.77-15.77) and by piperacillin and beta-lactamase inhibitor (PRR = 10.02, 95% CI: 8.86-11.43; ROR = 10.81, 95% CI: 9.42-12.40). Pharmacovigilance databases facilitate the identification of diverse phenotypes of SCARs and the list of culprit drugs. The accumulated data serve as a valuable tool to enhance clinical practice outcomes and strengthen overall healthcare monitoring."

Journal • Real-world evidence • Allergy • Eosinophilia • Immunology • Oncology • Steven-Johnson Syndrome

Green evaluation of human plasma levels of metformin, linagliptin, and empagliflozin using HPLC and HPTLC methods: a pharmacokinetic study. (PubMed, BMC Chem) - "The validated methods were successfully applied to a pharmacokinetic study in healthy volunteers, yielding mean Cmax values of 877.5 ± 162.2 ng/mL (MEF), 576 ± 87.5 ng/mL (EMP), and 680.8 ± 7.9 ng/mL (LIN), with Tmax values of 2.42 ± 0.38, 1.5 ± 0.61, and 5.3 ± 0.52 h, respectively. The obtained pharmacokinetic parameters were consistent with reported literature, confirming the reliability and clinical applicability of the proposed green bioanalytical methods."

Journal • PK/PD data

Endogenous GIP signaling is indispensable for DPP-4 inhibitor-mediated metabolic control in mice. (PubMed, J Diabetes Investig) - "Endogenous GIP signaling is essential for both glucose-lowering and anti-obesity actions of DPP-4 inhibitors in mice. GLP-1 elevation alone is insufficient to compensate for GIP receptor deficiency. These findings refined the mechanistic understanding of DPP-4 inhibitors, highlighted the physiological importance of GIP, and suggested context-dependent metabolic actions of incretins."

Journal • Preclinical • Genetic Disorders • Obesity

Dual blockade of DPP-4 and CXCL12/CXCR4 axes synergistically protects podocytes in lupus nephritis. (PubMed, Front Pharmacol) - "MRL/lpr lupus-prone mice were treated with the DPP-4 inhibitor linagliptin, either alone or in combination with the CXCL12/CXCR4 axis antagonist AMD3100. Combined DPP-4 and CXCL12/CXCR4 axis inhibition synergistically enhanced podocyte protection and attenuated renal inflammation, fibrosis, and oxidative stress in lupus nephritis. These findings support dual blockade as a promising therapeutic strategy for LN."

Journal • Diabetes • Fibrosis • Glomerulonephritis • Immunology • Inflammation • Inflammatory Arthritis • Lupus • Lupus Nephritis • Metabolic Disorders • Nephrology • Renal Disease • Systemic Lupus Erythematosus • CXCL12 • CXCR4 • FN1 • NLRP3 • NOX4 • NPHS1

Case report: Epidermolysis bullosa acquisita following dipeptidyl peptidase-4 inhibitor therapy and complicated by immune thrombocytopenic purpura. (PubMed, Front Immunol) - "A 68-year-old Japanese man with type 2 diabetes and chronic renal dysfunction, treated with linagliptin, developed widespread tense blisters with mucosal involvement...Despite corticosteroids, cyclosporine, pulse therapy, and intravenous immunoglobulin, the disease remained refractory...This is the first reported case of EBA following DPP-4 inhibitor therapy complicated by ITP. It highlights the therapeutic challenges of EBA and the potential for systemic autoimmune manifestations beyond the skin in patients receiving DPP-4 inhibitors."

Journal • Bullous Pemphigoid • Chronic Kidney Disease • Dermatology • Dermatopathology • Diabetes • Hematological Disorders • Immune Thrombocytopenic Purpura • Immunology • Infectious Disease • Metabolic Disorders • Nephrology • Pneumonia • Renal Disease • Respiratory Diseases • Thrombocytopenia • Thrombocytopenic Purpura • Type 2 Diabetes Mellitus

Deubiquitinase inhibitors: Targeting SARS-CoV-2 papain-like protease with antiviral efficacy in a murine model. (PubMed, FEBS J) - "Among the identified compounds, flupenthixol, lithocholic acid, teneligliptin, and linagliptin markedly inhibited the proteolytic activity of purified PLpro and demonstrated potent antiviral effects against SARS-CoV-2 infection in a dose-dependent manner. Additionally, oral and intraperitoneal treatments with linagliptin increased survival, reduced lung viral load, and ameliorated histopathological damage in a mouse-adapted model of SARS-CoV-2 infection. This study demonstrates for the first time that using DUB inhibitors that target the proteolytic activity of PLpro can simultaneously reinstate the host's immune response against SARS-CoV-2, highlighting the potential of this two-pronged therapeutic approach."

Journal • Preclinical • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases • Targeted Protein Degradation

Trends in Adverse Event Reports of Dipeptidyl Peptidase-4 Inhibitor-Associated Pemphigoid in Japan. (PubMed, Drugs Real World Outcomes) - "The number of reported DPP-4 inhibitor-associated pemphigoid events increased after the revised precautions of package inserts for DPP-4 inhibitors were released."

Adverse events • Journal • Diabetes • Immunology • Metabolic Disorders • Type 2 Diabetes Mellitus

Comparative Effect of SGLT2 Inhibitors and GLP-1 Agonists on Glycemic Control in Type 2 Diabetes Mellitus. (PubMed, J Pharm Bioallied Sci) - "They were randomly given either empagliflozin, Canagliflozin, Dapagliflozin, Ertugliflozin, Bexagliflozin, Sotagliflozin (an SGLT2 inhibitor) or liraglutide, Sitagliptin, Saxagliptin, Linagliptin, Alogliptin, Vildagliptin (n GLP-1 receptor agonist) to consume for 24 weeks. But GLP-1 agonists are better at helping people lose weight and keep their hearts healthy, so they are also a fantastic choice for people who have these problems. It's crucial to consider what each patient needs and what could go wrong while establishing treatment plans for them."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Cardiovascular Disease and Diabetes: A New Challenge in the Treatment and Management. (PubMed, Int J Mol Sci) - "The latest classes of glucose-lowering drugs introduced in the clinical practice are DPP4 inhibitors (sitagliptin, saxagliptin, vildagliptin, linagliptin, and alogliptin), GLP-1 receptor agonists (semaglutide, liraglutide, albiglutide, dulaglutide, exenatide, and lixenatide), and SGLT-2 inhibitors (empaglifozin, canaglifozin, and dapaglifozin). Multiple lines of evidence show that all these new drugs associated with the treatment of diabetic disease have the same effectiveness as the traditional antidiabetic drugs, and excellent cardiovascular safety, highlighting their potential in significantly reducing major cardiovascular events and mortality. The aim of our review is to summarise the clinical efficacy of these recently introduced drugs to optimise treatment strategies, especially in the early phase of diabetic disease."

Journal • Review • Cardiovascular • Diabetes • Metabolic Disorders

Evaluation of the anti-hyperglycemic, anti-hyperlipidemic, cardioprotective and anti-inflammatory effects of a xanthine-based dipeptidyl peptidase-4 inhibitor and diosmin in NA/STZ-induced diabetic rats. (PubMed, Arch Physiol Biochem) - "Additionally, inflammatory markers, including TNF-α and IL-1β, were significantly reduced, highlighting the anti-inflammatory properties of linagliptin and diosmin. the findings suggest that linagliptin and diosmin exert strong anti-hyperglycemic, anti-hyperlipidemic, cardioprotective, and anti-inflammatory effects in diabetic rats; the combined treatment effect was the most potent."

Journal • Preclinical • Cardiovascular • Diabetes • Inflammation • Metabolic Disorders • IL1B • TNFA

Incretin effect is sufficient for glucose control in developing rats. (PubMed, J Endocrinol) - "Standard therapeutic doses of linagliptin and liraglutide did not influence the blood glucose concentrations of 2-week-old pups, and no hypoglycemia developed. Furthermore, neither a DPP-4 inhibitor nor a GLP-1 receptor agonist induced hypoglycemia as an adverse effect. Therefore, incretin hormones may be safe therapeutic targets for hyperglycemia in preterm infants."

Journal • Preclinical • Diabetes • Hypoglycemia

Linagliptin-Induced Bullous Pemphigoid: A Case Report and Comprehensive Literature Review. (PubMed, Cureus) - "Bullous pemphigoid (BP) is an autoimmune blistering disorder predominantly affecting the elderly, presenting significant management challenges, especially in patients with multimorbidity and polypharmacy. Furthermore, we comprehensively review the current evidence for emerging biological and targeted therapies (e.g., rituximab, dupilumab, omalizumab, and intravenous immunoglobulin) in BP management, highlighting their potential role in reducing corticosteroid dependence and improving outcomes in frail, comorbid patients. This case underscores the importance of the prompt recognition of drug-induced BP, individualized treatment plans considering comorbidities, and the growing promise of novel therapeutic strategies."

Journal • Alzheimer's Disease • Bullous Pemphigoid • Cardiovascular • Chronic Kidney Disease • CNS Disorders • Dementia • Dermatology • Dermatopathology • Diabetes • Hypertension • Immunology • Metabolic Disorders • Nephrology • Renal Disease

DPP-4 inhibitor linagliptin modulates myocardial metabolism in a model of coronary artery disease. (PubMed, JTCVS Open) - "Linagliptin shifted myocardial metabolism pointing to enhanced ketone utilization, upregulation of the TCA cycle, and reductions in free fatty acid oxidation, glycolysis, and lactate production. These findings suggest a potential cardioprotective role for linagliptin via metabolic manipulation under ischemic conditions, warranting further investigation."

Journal • Cardiovascular • Coronary Artery Disease • Myocardial Ischemia

PACAP: A promising disease-modifying target for Alzheimer's disease. (PubMed, Life Sci) - "We also consider how established drugs (metformin, linagliptin, and statins) might provide a degree of neuroprotection in part-seeking through PACAP-related pharmacology. Taken together, the cumulative available evidence places PACAP not only as yet another promising therapeutic candidate but rather as a master regulator of neuroprotection, tackling AD's multifaceted nature. Restoration of PACAP signaling is a very distinct method to intervene in disease development, which offers immeasurable benefit in comparison to symptom relief treatment."

Journal • Review • Alzheimer's Disease • CNS Disorders • Inflammation • ADCYAP1 • APP

Morpheus Lung: A Study Of Multiple Immunotherapy-Based Treatment Combinations In Participants With Metastatic Non-Small Cell Lung Cancer (Morpheus- Non-Small Cell Lung Cancer) (clinicaltrials.gov) - P1/2 | N=314 | Completed | Sponsor: Hoffmann-La Roche | Active, not recruiting ➔ Completed

Trial completion • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • PD-L1

Comparative analysis of dapagliflozin and linagliptin in managing type 2 diabetes mellitus and heart failure: A retrospective study. (PubMed, Medicine (Baltimore)) - "All patients received standard anti-HF therapy in combination with metformin. Both dapagliflozin and linagliptin effectively improve glycemic control and cardiac function in patients with T2DM and HF, with favorable safety profiles. However, dapagliflozin appears to confer additional benefits in improving cardiac function, potentially due to its unique pharmacological mechanism."

Clinical • Journal • Observational data • Retrospective data • Cardiovascular • Congestive Heart Failure • Diabetes • Heart Failure • Metabolic Disorders • Type 2 Diabetes Mellitus • FGF23

MORPHEUS-EC: A Study of Multiple Immunotherapy-Based Treatment Combinations in Patients With Locally Advanced Unresectable or Metastatic Gastric or Gastroesophageal Junction Cancer (G/GEJ) or Esophageal Cancer (Morpheus-Gastric and Esophageal Cancer) (clinicaltrials.gov) - P1/2 | N=214 | Completed | Sponsor: Hoffmann-La Roche | Active, not recruiting ➔ Completed | N=410 ➔ 214

Enrollment change • Trial completion • Esophageal Adenocarcinoma • Esophageal Cancer • Gastric Adenocarcinoma • Gastric Cancer • Gastroesophageal Junction Adenocarcinoma • Oncology • Solid Tumor • HER-2 • PD-L1 • TIGIT

Comparing the effectiveness of Linagliptin vs. Sitagliptin in patients with Type 2 Diabetes Mellitus (ASHP 2025) - No abstract available

Clinical • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Repurposing DPP-4 inhibitors as anticancer agents in KRAS-mutated pancreatic ductal adenocarcinoma. (PubMed, BMC Pharmacol Toxicol) - "Overall, we report that Sitagliptin and Linagliptin have significant anticancer potential towards KRAS-mutated PDAC. Furthermore, we recommend repurposing of more drugs to examine their anti-cancer potential towards these aggressive cancers and to overcome clinical resistance in the near future."

Journal • Diabetes • Metabolic Disorders • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Type 2 Diabetes Mellitus • KRAS • MIA

Dipeptidyl Peptidase 4 Inhibitors: Novel Therapeutic Agents in the Management of Type II Diabetes Mellitus. (PubMed, Pharmacoepidemiol Drug Saf) - "DPP-4 inhibitors remain effective and well-tolerated options for managing T2DM."

Journal • Review • Diabetes • Hypoglycemia • Metabolic Disorders • Type 2 Diabetes Mellitus

Mechanically robust PVA/SA semi-IPN hydrogels for highly effective temperature-triggered linagliptin delivery. (PubMed, Phys Chem Chem Phys) - "The hydrogel system demonstrated temperature-responsive release kinetics: minimal release occurred at low temperatures, while rapid, sustained release was achieved at physiological temperature, reaching a cumulative release efficiency of up to 85.17%, which was highly beneficial for the storage and application of drug-loaded hydrogels. This study presents a hydrogel platform with effectively integrated material robustness, temperature-triggered drug delivery and high-efficiency loading and release of LIN, which showcases significant potential as a novel therapeutic material for diabetic wound healing."

Journal • Musculoskeletal Diseases • Orthopedics

Linagliptin Attenuates Kidney Cancer in Rats via AMPK Activation and Suppression of YAP/TAZ/HIF-1α Signaling. (PubMed, Eur J Pharm Sci) - "This study investigated the renoprotective action of linagliptin compared to doxorubicin against thioacetamide (TAA) and diethyl nitrosamine (DEN)-induced renocarcinogenesis in a rat model. These findings demonstrate that linagliptin, especially at 6 mg/kg/day, exhibits significant renoprotective activities through multifarious mechanisms involving antioxidant action and regulation of key molecular pathways. The present study presents evidence for the potential therapeutic application of linagliptin in renal manifestations of renocarcinogenesis."

Journal • Preclinical • Genito-urinary Cancer • Inflammation • Kidney Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor • CASP3 • HIF1A • PCNA • STAT3

Dipeptidyl peptidase-4 inhibitors and diabetic retinopathy in type 2 diabetes: A network meta-analysis of randomized clinical trials. (PubMed, J Diabetes Complications) - "Current randomized evidence indicates class-level neutrality of DPP-4 inhibitors on DR incidence, with no dose-response signal. Choice among gliptins may therefore be guided primarily by glycemic efficacy, safety, and participant characteristics rather than retinal risk."

Clinical • Journal • Retrospective data • Review • Diabetes • Diabetic Retinopathy • Metabolic Disorders • Retinal Disorders • Type 2 Diabetes Mellitus

Exploring the Evidence for Personalized Pharmacotherapy in Type 2 Diabetes-A Systematic Review. (PubMed, J Pers Med) - " We systematically searched PubMed, Scopus, and Web of Science for studies published from the earliest available records to 18 August 2025 using the following Boolean search terms: "miRNA AND gliclazide", "miRNA AND glibenclamide", "miRNA AND gliquidone", "miRNA AND glimepiride", "mirRNA AND metformin", "miRNA AND pioglitazone", "miRNA AND rosiglitazone", "miRNA AND sitagliptin", "miRNA AND vildagliptin", "miRNA AND alogliptin", "miRNA and saxagliptin", "miRNA AND linagliptin", "miRNA AND liraglutide", "miRNA and dulaglutide", "miRNA AND semaglutide", "miRNA AND tirzepatide", "miRNA AND lixisenatide", "miRNA AND empagliflozin", "miRNA AND dapagliflozin", miRNA AND insulin glargine", "miRNA AND insulin detemir", "miRNA AND insulin degludec", "miRNA AND..."

Journal • Review • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

ON TARGET DM: Comparison of Type 2 Diabetes Pharmacotherapy Regimens (clinicaltrials.gov) - P=N/A | N=241981 | Completed | Sponsor: Kaiser Permanente | Recruiting ➔ Completed | Trial completion date: Aug 2025 ➔ Mar 2025

Trial completion • Trial completion date • Cardiovascular • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus