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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
linagliptin : A xanthine that is 7H-xanthine bearing (4-methylquinazolin-2-yl)methyl, methyl, but-2-yn-1-yl and 3-aminopiperidin-1-yl substituents at positions 1, 3, 7 and 8 respectively (the R-enantiomer). Used for treatment of type II diabetes. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| Flora | Rank | Flora Definition | Family | Family Definition |
|---|---|---|---|---|
| Ione | genus | [no description available] | Orchidaceae | A plant family of the order Asparagales. All members of the orchid family have the same bilaterally symmetrical flower structure, with three sepals, but the flowers vary greatly in color and shape.[MeSH] |
| ID Source | ID |
|---|---|
| PubMed CID | 10096344 |
| CHEMBL ID | 237500 |
| CHEBI ID | 68610 |
| SCHEMBL ID | 160188 |
| MeSH ID | M0554626 |
| Synonym |
|---|
| HY-10284 |
| 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1h-purine-2,6-dione |
| ondero |
| linagliptin |
| bi-1356-bs |
| trazenta |
| bi-1356 |
| trajenta |
| tradjenta |
| bdbm50228403 |
| (r)-8-(3-aminopiperidin-1-yl)-7-(but-2-ynyl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1h-purine-2,6(3h,7h)-dione |
| bi 1356 |
| bi-1356bs |
| CHEMBL237500 , |
| bs 1356 bs |
| chebi:68610 , |
| bs-1356-bs |
| bi 1356 bs |
| D09566 |
| linagliptin (jan/usan/inn) |
| tradjenta (tn) |
| 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)- |
| linagliptin [usan:inn:jan] |
| hsdb 8204 |
| (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 |
| 3x29zej4r2 , |
| unii-3x29zej4r2 |
| linagliptin (bi-1356) |
| 8-[(3r)-3-amino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1h-purine-2,6-dione |
| 668270-12-0 |
| AKOS015951179 |
| ione |
| AKOS015995251 |
| BCP9000854 |
| BCPP000185 |
| NCGC00346655-01 |
| linagliptin component of trijardy xr |
| linagliptin [mi] |
| linagliptin [mart.] |
| 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)- |
| linagliptin [inn] |
| trijardy xr component linagliptin |
| linagliptin [orange book] |
| jentadueto component of linagliptin |
| linagliptin [jan] |
| linagliptin [usan] |
| linagliptin component of glyxambi |
| linagliptin [vandf] |
| glyxambi component linagliptin |
| linagliptin component of jentadueto |
| linagliptin [who-dd] |
| (r)-8-(3-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methylquinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione |
| 8-[(3r)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1h-purine-2,6-dione |
| CS-0637 |
| S3031 |
| c25h28n8o2 |
| gtpl6318 |
| 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione |
| DB08882 |
| smr004701306 |
| MLS006010217 |
| SCHEMBL160188 |
| AB01563307_01 |
| AB01563307_03 |
| (r)-8-(3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1h-purine-2,6(3h,7h)-dione |
| J-519354 |
| EX-A076 |
| AC-8761 |
| (r)-8-(3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-3,7-dihydro-1h-purine-2,6-dione |
| SW219813-1 |
| 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1h-purine-2,6-d |
| AS-35080 |
| mfcd14635356 |
| 1233245-11-8 |
| 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(r)-aminopiperidin-1-yl)xanthine |
| LTXREWYXXSTFRX-QGZVFWFLSA-N |
| 1-[(4-methyl-quinazolin-2yl) methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(r) amino-piperidin-1-yl]-xanthine |
| 1-[(4-methylquinazolin-2-yl)methyl]-3-methyl-7-(2-butin-1-yl)-8-(3-(r)-aminopiperidin-1-yl)-xanthine |
| 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(r)aminopiperidin-1-yl)xanthine |
| 1-[(4-methylquinazolin-2-yl)-methyl]-3-methyl-7-(2-butin-1-yl)-8-(3-(r)-aminopiperidin-1-yl)-xanthine |
| BCP02462 |
| Q909745 |
| linagliptin; (r)-8-(3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1h-purine-2,6(3h,7h)-dione |
| 8-[(3r)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3- methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1h-purine-2,6-dione |
| linaglitpin |
| AMY8953 |
| CCG-269463 |
| NCGC00346655-02 |
| 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1h-purine-2,6-d ione |
| BL164627 |
| DTXSID201021653 |
| 8-[(3r)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,3,6,7-tetrahydro-1h-purine-2,6-dione |
| EN300-6481354 |
| Z2235801970 |
| linagliptin (mart.) |
| a10bh05 |
| linagliptine |
| linagliptinum |
| linagliptina |
| 8-((3r)-3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-3,7-dihydro-1h-purine-2,6-dione |
Linagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor used for the treatment of type 2 diabetes, with additional beneficial effects for the kidney. It suppresses the rapid degradation of endogenous glucagon-like peptide-1 (GLP-1)
Linagliptin has a low oral bioavailability due to intestinal degradation and low permeability. It has a protective role on endothelial function in patients with type 2 diabetes with moderate hyperglycemia.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Linagliptin has a low oral bioavailability due to intestinal degradation and low permeability." | ( Architecting novel multilayer nanosponges for co-administration of two drugs managing high-risk type II diabetes mellitus patients suffering from cardiovascular diseases. Abdelmalak, NS; Hammad, RW; Latif, R; Sanad, RA, 2022) | 1.44 |
| "Linagliptin has a xanthine-based structure, a difference that might account for some of the pharmacological differences observed with linagliptin versus other dipeptidyl-peptidase-4 inhibitors." | ( Pharmacokinetic and pharmacodynamic evaluation of linagliptin for the treatment of type 2 diabetes mellitus, with consideration of Asian patient populations. Ceriello, A; Inagaki, N, 2017) | 1.43 |
| "Linagliptin has a protective role on endothelial function in patients with type 2 diabetes with moderate hyperglycemia." | ( Linagliptin improves endothelial function in patients with type 2 diabetes: A randomized study of linagliptin effectiveness on endothelial function. Hirose, T; Iga, R; Kanda, E; Kobayashi, Y; Kumashiro, N; Miyagi, M; Shigiyama, F; Uchino, H, 2017) | 2.62 |
| "Linagliptin has a unique PK/pharmacodynamic (PD) profile and is the first DPP-4 inhibitor with a nonrenal elimination route." | ( Linagliptin for the treatment of type 2 diabetes (pharmacokinetic evaluation). Scheen, AJ, 2011) | 2.53 |
| "Linagliptin also has a favorable safety profile; nasopharyngitis is one of the more common observed side effects." | ( Linagliptin: the newest dipeptidyl peptidase-4 inhibitor for type 2 diabetes mellitus. Aletti, R; Cheng-Lai, A, ) | 2.3 |
| "Linagliptin has a long terminal half-life (>100 hours); however, its accumulation half-life is much shorter (approximately 10 hours), accounting for the rapid attainment of steady state." | ( Clinical pharmacokinetics and pharmacodynamics of linagliptin. Friedrich, C; Graefe-Mody, U; Retlich, S, 2012) | 1.35 |
| "Linagliptin has been studied in combination with the most commonly used classes of antihyperglycemic medications, with demonstrated efficacy and a safety profile comparable to placebo." | ( Use of the dipeptidyl peptidase-4 inhibitor linagliptin in combination therapy for type 2 diabetes. Lajara, R, 2012) | 1.36 |
Linagliptin might inhibit the N-terminal degradation of the transcobalamin receptor CD320. It did not increase the risk of adverse kidney outcomes or hospitalization for heart failure across age groups.
Linagliptin treatment significantly reduced the hazard of kidney disease events by 16% compared with placebo (HR, 0.84; 95% CI,. 0.72-0.97; P=0.02) Linagli leptin treatment in the BMVEC was able to reduce TLR2 expression in cells from both diabetic and nondiabetic rats.
Linagliptin, when added to ongoing insulin treatment in patients with type 2 diabetes, improves glycemic control and has a neutral impact on major adverse CV events. Overall, the safety profile of linagli leptin in this patient group was comparable to that of placebo, with comparable incidence of adverse events.
Linagliptin is the most recently launched gliptin, with a unique pharmacokinetic (PK) profile. It is now also available as a fixed-dose combination (FDC) with metformin.
Linagliptin and its combination with metformin successfully ameliorated diabetic osteoporosis in HFD-fed mice possibly through modulation of BMP-2 and sclerostin. We used a panel of stably and transiently transfected cell lines to elucidate the carrier-mediated transport processes that are involved in linagli leptin disposition in vivo.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Patients with type 2 diabetes mellitus (T2DM) are generally treated with many pharmacological compounds and are exposed to a high risk of drug-drug interactions." | ( Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions. Scheen, AJ, 2010) | 0.36 |
| " We used a panel of stably and transiently transfected cell lines to elucidate the carrier-mediated transport processes that are involved in linagliptin disposition in vivo and to assess the potential for drug-drug interactions (DDIs)." | ( Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. Ebner, T; Ishiguro, N; Kishimoto, W; Schaefer, O; Shimizu, H, 2013) | 0.83 |
| "The effects of the dipeptidyl peptidase-4 (DPP-4) inhibitor, linagliptin, alone and in combination with voglibose or exendin-4, on glycaemic control and body weight were assessed in an animal model of type 2 diabetes." | ( Effect of linagliptin, alone and in combination with voglibose or exendin-4, on glucose control in male ZDF rats. Cheetham, SC; Headland, KR; Jones, RB; Klein, T; Mark, M; Vickers, SP, 2014) | 1.05 |
| " Interestingly, treatment with linagliptin and its combination with metformin significantly reverted the impaired bone architecture, BMD, and positively modulated bone turnover biomarkers, while metformin alone did not exhibit any significant improvement." | ( Linagliptin in Combination With Metformin Ameliorates Diabetic Osteoporosis Through Modulating BMP-2 and Sclerostin in the High-Fat Diet Fed C57BL/6 Mice. Nirwan, N; Vohora, D, 2022) | 2.45 |
| "Linagliptin and its combination with metformin successfully ameliorated diabetic osteoporosis in HFD-fed mice possibly through modulation of BMP-2 and sclerostin." | ( Linagliptin in Combination With Metformin Ameliorates Diabetic Osteoporosis Through Modulating BMP-2 and Sclerostin in the High-Fat Diet Fed C57BL/6 Mice. Nirwan, N; Vohora, D, 2022) | 3.61 |
| "To probe into the efficacy of Yishen Huashi granules combined with linagliptin tablets in the treatment of type 2 diabetic nephropathy (DN) and its effect on blood glucose and renal function in patients." | ( Efficacy of Yishen Huashi Granules Combined with Linagliptin Tablets on Blood Glucose and Renal Function in Patients with Type 2 Diabetic Nephropathy. Duan, M; Li, D; Meng, J; Wang, R; Zhang, P, 2022) | 1.21 |
Linagliptin has a low oral bioavailability due to intestinal degradation. Two studies evaluated the role of P-gp-mediated transport in the bioavailability and intestinal secretion of linaglipt in rats. The oral bio availability of linAGliptin estimated with this model is approximately 30%.
Linagliptin is suitable for once-daily dosing in a broad range of patients with type 2 diabetes mellitus. In vitro inhibition of renal-specific DPP-4 activity was more sustained in Sprague Dawley rats after exposure to linaglipt than it was after sitaglipton. Compared to patients with vildagli leptin-associated BP, those with linaglisptin- associated BP were managed by higher dosage of systemic corticosteroids.
| Role | Description |
|---|---|
| EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor | An EC 3.4.14.* (dipeptidyl- and tripeptidyl-peptidases) inhibitor that specifically inhibits dipeptidyl peptidase-4 (EC 3.4.14.5). |
| hypoglycemic agent | A drug which lowers the blood glucose level. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| quinazolines | Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives. |
| aminopiperidine | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 28.8601 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Dipeptidyl peptidase 9 | Bos taurus (cattle) | IC50 (µMol) | 100.0000 | 0.6800 | 0.6800 | 0.6800 | AID1501063 |
| Dipeptidyl peptidase IV | Porphyromonas gingivalis | IC50 (µMol) | 10.0000 | 1.3000 | 1.3000 | 1.3000 | AID1501058 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 0.3000 | 0.0001 | 1.7740 | 10.0000 | AID1631916 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0001 | 1.7536 | 10.0000 | AID1305313 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0000 | 2.0151 | 10.0000 | AID1305313 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | IC50 (µMol) | 0.2967 | 0.0000 | 1.4039 | 10.0000 | AID1631916; AID304455; AID646546 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 100.0000 | 0.0004 | 0.9086 | 10.0000 | AID1129903 |
| Dipeptidyl peptidase 4 | Homo sapiens (human) | IC50 (µMol) | 0.0008 | 0.0001 | 0.4444 | 10.0000 | AID1305311; AID1501061; AID1581626; AID1631905; AID1801383; AID1802590; AID1915713; AID1917944; AID304453; AID331175; AID646406; AID749996 |
| Prolyl endopeptidase | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0011 | 1.9896 | 9.7500 | AID1129903; AID748310 |
| Prolyl endopeptidase FAP | Mus musculus (house mouse) | IC50 (µMol) | 0.3700 | 0.0660 | 0.1884 | 0.3700 | AID1129901; AID748314 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 30.0000 | 0.0009 | 1.9014 | 10.0000 | AID646415 |
| Prolyl endopeptidase FAP | Homo sapiens (human) | IC50 (µMol) | 0.0799 | 0.0120 | 1.1589 | 5.8300 | AID1305312; AID688691 |
| Dipeptidyl peptidase 8 | Homo sapiens (human) | IC50 (µMol) | 80.0000 | 0.0019 | 2.6532 | 10.0000 | AID1305314; AID1501062; AID688693 |
| Dipeptidyl peptidase 9 | Homo sapiens (human) | IC50 (µMol) | 55.0000 | 0.0001 | 1.4207 | 10.0000 | AID1305315; AID688690 |
| Solute carrier family 22 member 8 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 4.9300 | 7.3900 | 9.9200 | AID1219117 |
| Dipeptidyl peptidase 2 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0002 | 0.9316 | 6.6000 | AID1305313; AID1501064; AID688688 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0500 | 2.3797 | 9.7000 | AID1219118 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Dipeptidyl peptidase 4 | Homo sapiens (human) | Kd | 0.0027 | 0.0000 | 0.0080 | 0.0285 | AID1631907; AID1631913 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1219133 | Permeability assessed as human P-glycoprotein-mediated transport of apical to basolateral side in pig LLC-PK1 cells by measuring nontransporter-related passive membrane permeability by Transwell experiment/liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219112 | Inhibition of human P-glycoprotein expressed in pig LLC-PK1 cells assessed as reduction of [3H]digoxin substrate transport from basolateral to apical side by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1631908 | Binding affinity to human recombinant DPP4 (39 to 766 residues) assessed as association rate constant by surface plasmon resonance analysis | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1219121 | Ratio of unbound Cmax to IC50 for P-glycoprotein (unknown origin) expressed in HEK293 cells | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219149 | Drug uptake assessed as OCTN1 (unknown origin)-mediated drug uptake expressed in HEK293 cells by liquid scintillation counting relative to control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID749996 | Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | Synthetic approaches to the 2011 new drugs. |
| AID304455 | Displacement of [N-methyl-3H]scopolamine from human recombinant muscarinic M1 receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1219127 | Ratio of unbound Cmax to IC50 for OATP1B1 (unknown origin) expressed in HEK293 cells | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1305311 | Inhibition of human DPP4 preincubated for 30 mins followed by Gly-Pro-AMC addition measured for 50 mins by continuous fluorescence assay | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1305313 | Inhibition of QPP (unknown origin) preincubated for 30 mins followed by Nle-Pro-AMC addition measured for 50 mins by continuous fluorescence assay | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1219172 | Permeability assessed as human P-glycoprotein-mediated transport across basolateral to apical side expressed in pig LLC-PK1 cells at 500 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1581626 | Inhibition of human DPP4 in pH 7.4 Tris buffer using AP-7-ATFMC as substrate preincubated for 15 mins followed by substrate addition by microplate reader analysis | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities. |
| AID304456 | Clearance in rat at 5 mg/kg, po and 5 mg/kg, iv | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID331175 | Inhibition of DPP4 in human Caco-2 cells after 1 hr | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11 | 3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors. |
| AID1219124 | Ratio of unbound Cmax to IC50 for OCT1 (unknown origin) expressed in HEK293 cells | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID304468 | Inhibition of plasma DPP4 activity in rhesus monkey at 1 mg/kg, po after 7 hrs | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1501064 | Inhibition of DPP2 (unknown origin) | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling. |
| AID1219162 | Inhibition of OATP1B3 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]CCK8 substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID304463 | Total mean residence time in cynomolgus monkey at 5 mg/kg, po | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1501063 | Inhibition of bovine DPP9 | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling. |
| AID1219144 | Drug uptake assessed as OAT3 (unknown origin)-mediated drug uptake expressed in HEK293 cells by liquid scintillation counting relative to control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219148 | Drug uptake assessed as OCT1 (unknown origin)-mediated drug uptake expressed in HEK293 cells by liquid scintillation counting relative to control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219118 | Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]E217betaG substrate uptake by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID304467 | Inhibition of plasma DPP4 activity in Beagle dog at 1 mg/kg, po after 7 hrs | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1631924 | Invivo binding affinity to DPP4 in mouse plasma at >100 nM relative to control | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID646542 | Clearance in rat at 1 mg/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. |
| AID1631920 | Invivo binding affinity to DPP4 in human plasma at <1 nM relative to control | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1631916 | Inhibition of M1 receptor (unknown origin) | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1219153 | Inhibition of OCT1 (unknown origin) expressed in HEK293 cells assessed as reduction of [14C]metformin substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID304472 | Reduction in plasma glucose excursion in db/db C57BL/KSJ mouse at 0.1 mg/kg, po by oral glucose tolerance test | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID646420 | Cmax in rat | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. |
| AID1631927 | Renal clearance in DPP4 knockout mouse at 0.01 mg/kg, iv | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1219110 | Inhibition of human P-glycoprotein expressed in pig LLC-PK1 cells assessed as reduction of [3H]digoxin substrate transport by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID748314 | Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold. |
| AID1219152 | Drug uptake assessed as OCT2 (unknown origin)-mediated drug uptake expressed in HEK293 cells by liquid scintillation counting in presence of 10 mM cimetidine OCT inhibitor | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID614482 | Ratio of Kinact/Ki for CYP3A4 in human liver microsomes | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | 2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivatio |
| AID1581625 | Inhibition of human DPP4 in pH 7.4 Tris buffer using AP-7-ATFMC as substrate preincubated for 15 mins followed by substrate addition by microplate reader analysis relative to control | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities. |
| AID646546 | Inhibition of M1 receptor | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. |
| AID748312 | Inhibition of DPP9 in bovine testis using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold. |
| AID1219160 | Inhibition of OAT4 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]E-sul substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219119 | Unbound Cmax in human at 5 mg, po | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219134 | Permeability assessed as human P-glycoprotein-mediated transport of basolateral to apical side in pig LLC-PK1 cells by measuring nontransporter-related passive membrane permeability by Transwell experiment/liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID304461 | Clearance in cynomolgus monkey at 5 mg/kg, po and 1.5 mg/kg, iv | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID688687 | Selectivity ratio of IC50 for DPP8 to IC50 for human DPP4 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1219114 | Inhibition of human BCRP expressed in MDCK2 cells assessed as reduction of [3H]E-sul substrate transport up to 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1501059 | Selectivity index, ratio of IC50 for human DPP4 to IC50 for Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling. |
| AID1385533 | Anti-obesity activity in db/db mouse model assessed as reduction in triglyceride levels in liver at 20 mg/kg, po administered daily for 6 weeks | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of 4-Benzyloxybenzo[ d]isoxazole-3-amine Derivatives as Highly Selective and Orally Efficacious Human Sphingomyelin Synthase 2 Inhibitors that Reduce Chronic Inflammation in db/ db Mice. |
| AID1305312 | Inhibition of FAP (unknown origin) preincubated for 20 mins followed by Nle-Pro-AMC addition measured for 40 mins by continuous fluorescence assay | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1129902 | Inhibition of DPP4 purified from human seminal plasma using Gly-Pro-p-nitroanilide as substrate by spectrophotometry | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID1219143 | Drug uptake assessed as OAT1 (unknown origin)-mediated drug uptake expressed in HEK293 cells by liquid scintillation counting relative to control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1501057 | Inhibition of Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli at 100 uM using Gly-Pro-p-nitroanilide as substrate relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling. |
| AID1305315 | Inhibition of DPP9 (unknown origin) preincubated for 20 mins followed by Gly-Pro-AMC addition measured for 50 mins by continuous fluorescence assay | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID1219157 | Inhibition of OCT2 (unknown origin) expressed in HEK293 cells assessed as reduction of [ethyl 1-14C]TEA substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1385535 | Anti-obesity activity in db/db mouse model assessed as reduction in LDL-C levels in liver at 20 mg/kg, po administered daily for 6 weeks | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of 4-Benzyloxybenzo[ d]isoxazole-3-amine Derivatives as Highly Selective and Orally Efficacious Human Sphingomyelin Synthase 2 Inhibitors that Reduce Chronic Inflammation in db/ db Mice. |
| AID1631913 | Binding affinity to human recombinant DPP4 (39 to 766 residues) at 5 uM by isothermal titration calorimetry | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1395907 | Elimination half life in human | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID304457 | Volume of distribution at steady state in rat at 5 mg/kg, po and 5 mg/kg, iv | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1129901 | Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID1219125 | Ratio of unbound Cmax to IC50 for OCT2 (unknown origin) expressed in HEK293 cells | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1631915 | Binding affinity to human recombinant DPP4 (39 to 766 residues) at 50 uM in presence of 7-benzyl-8-(piperazin-1-yl)-1H-purine-2,6(3H,7H)-dione by isothermal titration calorimetry | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1631925 | Invivo binding affinity to DPP4 in Fischer rat plasma at >100 nM relative to control | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1129904 | Inhibition of DPP9 purified from bovine testes using Ala-Pro-p-nitroanilide as substrate by spectrophotometry | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID1219132 | Permeability assessed as human P-glycoprotein-mediated active membrane transport by measuring basolateral to apical side expressed in pig LLC-PK1 cells by Transwell experiment/liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219169 | Permeability assessed as human P-glycoprotein-mediated transport across apical to basolateral side expressed in pig LLC-PK1 cells at 2 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID304469 | Aqueous solubility at pH 7.4 | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1219163 | Inhibition of OCTN1 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]ergothioneine substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID304464 | Half life in cynomolgus monkey at 5 mg/kg, po | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1219161 | Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]E217betaG substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219158 | Inhibition of OAT1 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]PAH substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1631909 | Binding affinity to human recombinant DPP4 (39 to 766 residues) assessed as dissociation rate constant by surface plasmon resonance analysis | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID646407 | Permeability from apical side to basal side of human Caco2 cells | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. |
| AID688691 | Inhibition of FAPalpha | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1219159 | Inhibition of OAT3 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]E-sul substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219146 | Drug uptake assessed as OATP1B1 (unknown origin)-mediated drug uptake expressed in HEK293 cells by liquid scintillation counting relative to control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID688685 | Selectivity ratio of IC50 for FAPalpha to IC50 for human DPP4 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID304474 | Inhibition of plasma DPP4 activity in db/db C57BL/KSJ mouse at 1 mg/kg, po after 30 mins of glucose administration | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID304466 | Inhibition of plasma DPP4 activity in Han Wistar rat at 1 mg/kg, po after 7 hrs | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1219126 | Ratio of unbound Cmax to IC50 for OAT3 (unknown origin) expressed in HEK293 cells | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1129905 | Inhibition of DPP2 purified from human seminal plasma using Lys-Ala-p-nitroanilide as substrate by spectrophotometry | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID1631922 | Invivo binding affinity to DPP4 in Fischer rat plasma at <1 nM relative to control | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID688689 | Inhibition of DPP4 in human plasma using Gly-Pro-AMC as substrate by fluorimetric analysis | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1631921 | Invivo binding affinity to DPP4 in mouse plasma at <1 nM relative to control | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1631910 | Binding affinity to human recombinant DPP4 (39 to 766 residues) assessed as residence time on target by surface plasmon resonance analysis | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1501062 | Inhibition of DPP8 (unknown origin) | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling. |
| AID1631905 | Inhibition of human recombinant DPP4 (39 to 766 residues) using Ala-Pro-AFC as substrate incubated for 1 hr by fluorescence assay | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1219151 | Drug uptake assessed as OCT2 (unknown origin)-mediated drug uptake expressed in HEK293 cells by liquid scintillation counting relative to control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID646408 | Efflux ratio of permeability across human Caco2 cells | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. |
| AID1219136 | Permeability assessed as human P-glycoprotein-mediated transport across basolateral to apical side expressed in pig LLC-PK1 cells by measuring membrane permeability time by Transwell experiment/liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1688640 | Antidiabetic activity in ICR mouse assessed as reduction in blood glucose AUC at 2 mg/kg, po administered as single dose followed by glucose challenge measured upto 120 mins by OGTT relative to control | |||
| AID304473 | Reduction in plasma glucose excursion in db/db C57BL/KSJ mouse at 1 mg/kg, po by oral glucose tolerance test | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID304475 | Dissociation constant, pKa corresponding to the protonation of the primary amino group | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1385534 | Anti-obesity activity in db/db mouse model assessed as reduction in NEFA levels in liver at 20 mg/kg, po administered daily for 6 weeks | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Discovery of 4-Benzyloxybenzo[ d]isoxazole-3-amine Derivatives as Highly Selective and Orally Efficacious Human Sphingomyelin Synthase 2 Inhibitors that Reduce Chronic Inflammation in db/ db Mice. |
| AID304459 | Half life in rat at 5 mg/kg, po | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1631923 | Invivo binding affinity to DPP4 in human plasma at >100 nM relative to control | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID304462 | Volume of distribution at steady state in cynomolgus monkey at 5 mg/kg, po and 1.5 mg/kg, iv | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID688686 | Selectivity ratio of IC50 for DPP9 to IC50 for human DPP4 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1219145 | Drug uptake assessed as OAT4 (unknown origin)-mediated drug uptake expressed in HEK293 cells by liquid scintillation counting relative to control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219128 | Efflux ratio assessed as human P-glycoprotein-mediated of permeability ratio of basolateral to apical side over apical to basolateral side expressed in pig LLC-PK1 cells at 2 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219120 | Protein binding in plasma (unknown origin) | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1915713 | Inhibition of DPP4 (unknown origin) | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Therapeutic progression of quinazolines as targeted chemotherapeutic agents. |
| AID1219154 | Inhibition of OCT1 (unknown origin) expressed in HEK293 cells assessed as reduction of [ethyl 1-14C]TEA substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID304465 | Oral bioavailability in cynomolgus monkey at 5 mg/kg | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1219147 | Drug uptake assessed as OATP1B3 (unknown origin)-mediated drug uptake expressed in HEK293 cells by liquid scintillation counting relative to control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219117 | Inhibition of OAT3 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]E-sul substrate uptake by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1917944 | Inhibition of human DPP4 using Gly-Pro-AMC as substrate incubated for 30 mins by continuous fluorescent assay | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Proline based rationally designed peptide esters against dipeptidyl peptidase-4: Highly potent anti-diabetic agents. |
| AID304453 | Inhibition of human DPP4 in Caco-2 cells by fluorescene assay | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID304460 | Oral bioavailability in rat at 5 mg/kg | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1631911 | Inhibition of DPP4 in human CaCo2 cells assessed as dissociation rate constant using Ala-Pro-AFC as substrate preincubated for 1 hr followed by substrate addition by fluorescence assay | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1219123 | Ratio of drug uptake in human intestine at 5 mg, po to IC50 for P-glycoprotein (unknown origin) expressed in HEK293 cells | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219156 | Inhibition of OCT2 (unknown origin) expressed in HEK293 cells assessed as reduction of [14C]metformin substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219130 | Permeability assessed as human P-glycoprotein-mediated of transport of basolateral to apical side expressed in pig LLC-PK1 cells by Transwell experiment/liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID646406 | Inhibition of human C-terminal step-tagged DPP4 expressed using baculovirus system | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. |
| AID304470 | Distribution coefficient, log D at pH 7.4 | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID304454 | Inhibition of human hERG current at 1 uM | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID646415 | Inhibition of human ERG by dofetilide binding assay | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. |
| AID1219122 | Drug uptake in human intestine at 5 mg, po | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1129906 | Selectivity index, ratio of IC50 for recombinant human PREP purified from Escherichia coli to IC50 for recombinant mouse FAP purified from HEK293 cell supernatant | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID1501056 | Inhibition of Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli at 10 uM using Gly-Pro-p-nitroanilide as substrate relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling. |
| AID1631928 | Lipophilicity, log D of the compound at pH 7.4 | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1631926 | Renal clearance in wild type mouse at 0.01 mg/kg, iv | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1219155 | Inhibition of OCT2 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]MPP+ substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1127773 | Inhibition of plasma DPP4 (unknown origin) after 24 hrs | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else? |
| AID688690 | Inhibition of DPP9 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1631919 | Cmax in human plasma at 5 mg | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID748313 | Inhibition of DPP4 in human seminal plasma using Gly-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold. |
| AID1501061 | Inhibition of human DPP4 | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling. |
| AID1129903 | Inhibition of recombinant human PREP purified from Escherichia coli using Z-Gly-Pro-p-nitroanilide as substrate by spectrophotometry | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID1219164 | Inhibition of OCTN2 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]carnitine substrate uptake at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219131 | Permeability assessed as human P-glycoprotein-mediated active membrane transport by measuring apical to basolateral side expressed in pig LLC-PK1 cells by Transwell experiment/liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219170 | Permeability assessed as human P-glycoprotein-mediated transport across apical to basolateral side expressed in pig LLC-PK1 cells at 500 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID646544 | Oral bioavailability in rat | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. |
| AID1219129 | Permeability assessed as human P-glycoprotein-mediated transport across apical to basolateral side expressed in pig LLC-PK1 cells by Transwell experiment/liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1631907 | Binding affinity to human recombinant DPP4 (39 to 766 residues) by surface plasmon resonance analysis | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16 | Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
| AID1305314 | Inhibition of recombinant DPP8 (unknown origin) preincubated for 20 mins followed by Ala-Pro-AFC addition measured for 40 mins by continuous fluorescence assay | 2016 | ACS medicinal chemistry letters, May-12, Volume: 7, Issue:5 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
| AID748311 | Inhibition of DPP2 in human seminal plasma using Lys-Ala-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold. |
| AID688688 | Inhibition of human DPP2 using Lys-Ala-AMC as substrate by fluorimetric analysis | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1219111 | Maximal inhibition of human P-glycoprotein expressed in pig LLC-PK1 cells assessed as reduction of [3H]digoxin substrate transport at 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID646421 | AUC in rat | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3 | Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. |
| AID748310 | Inhibition of human recombinant PREP expressed in Escherichia coli using Z-Gly-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold. |
| AID1219135 | Permeability assessed as human P-glycoprotein-mediated transport across apical to basolateral side expressed in pig LLC-PK1 cells by measuring membrane permeability time by Transwell experiment/liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID304471 | Dissociation constant, pKa corresponding to the protonation of the quinazoline | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1219171 | Permeability assessed as human P-glycoprotein-mediated transport across basolateral to apical side expressed in pig LLC-PK1 cells at 2 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID1219113 | Inhibition of human MRP2 expressed in MDCK2 cells assessed as reduction of [3H]E217betaG substrate transport up to 100 uM by liquid scintillation counting | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID688693 | Inhibition of DPP8 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
| AID1219150 | Drug uptake assessed as OCTN2 (unknown origin)-mediated drug uptake expressed in HEK293 cells by liquid scintillation counting relative to control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods. |
| AID304458 | Total mean residence time in rat at 5 mg/kg, po | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| AID1501058 | Inhibition of Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli using Gly-Pro-p-nitroanilide as substrate | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID1802590 | DPP-4 Activity Assay from Article 10.1016/j.bioorg.2017.02.004: \\Design and synthesis of quinazoline-3,4-(4H)-diamine endowed with thiazoline moiety as new class for DPP-4 and DPPH inhibitor.\\ | 2017 | Bioorganic chemistry, 04, Volume: 71 | Design and synthesis of quinazoline-3,4-(4H)-diamine endowed with thiazoline moiety as new class for DPP-4 and DPPH inhibitor. |
| AID1801383 | In vitro Assay for Inhibition of DPP-4 from Article 10.1111/cbdd.12560: \\Design, Synthesis and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel DPP-4 Inhibitors.\\ | 2015 | Chemical biology & drug design, Oct, Volume: 86, Issue:4 | Design, Synthesis and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel DPP-4 Inhibitors. |
| AID1345443 | Human dipeptidyl peptidase 4 (S9: Prolyl oligopeptidase) | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26 | 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 13 (2.24) | 29.6817 |
| 2010's | 393 (67.76) | 24.3611 |
| 2020's | 174 (30.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (98.67) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 149 (24.92%) | 5.53% |
| Reviews | 96 (16.05%) | 6.00% |
| Case Studies | 25 (4.18%) | 4.05% |
| Observational | 13 (2.17%) | 0.25% |
| Other | 315 (52.68%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Bioequivalence of a Low Strength Fixed Dose Combination Tablet of Empagliflozin/Linagliptin/Metformin Extended Release Compared to the Free Combination of Empagliflozin, Linagliptin, and Metformin Extended Release Tablets Following Oral Administration in [NCT03629054] | Phase 1 | 30 participants (Actual) | Interventional | 2018-08-27 | Completed | ||
| Evogliptin Versus Linagliptin for the Effect on Albuminuria in Patients With Type 2 Diabetes and Renal Insufficiency: a Multicenter, Randomised, Double-blind, Active-controlled, Non-inferiority Trial [NCT03667300] | Phase 2 | 209 participants (Actual) | Interventional | 2017-03-16 | Completed | ||
| Efficacy and Safety of Empagliflozin Compared With Linagliptin in New-onset Diabetes Mellitus After Kidney Transplantation [NCT03642184] | Phase 4 | 6 participants (Actual) | Interventional | 2018-07-14 | Terminated(stopped due to Difficult in enrolling suitable participants) | ||
| RACELINES: Renal Actions of Combined Empagliflozin and LINagliptin in Type 2 diabetES [NCT03433248] | Phase 4 | 66 participants (Actual) | Interventional | 2017-11-09 | Active, not recruiting | ||
| Bioequivalence of a Fixed Dose Combination Tablet of Empagliflozin/Linagliptin/Metformin Extended Release Compared to the Free Combination of Empagliflozin, Linagliptin, and Metformin Extended Release Tablets Following Oral Administration in Healthy Male [NCT03259490] | Phase 1 | 30 participants (Actual) | Interventional | 2017-08-31 | Completed | ||
| Relative Bioavailability of Two FDC Tablet Strengths of Empagliflozin/Linagliptin/Metformin Extended Release Compared to the Free Combination of Empagliflozin, Linagliptin and Metformin Extended Release Following Oral Administration in Healthy Male and Fe [NCT02821910] | Phase 1 | 50 participants (Actual) | Interventional | 2016-07-20 | Completed | ||
| A Phase 4, Monocenter, Randomized, Double-blind, Comparator-controlled, Parallel-group, Mechanistic Intervention Trial to Assess the Effect of 8-week Treatment With the Dipeptidyl Peptidase-4 Inhibitor (DPP-4i) Linagliptin Versus the Sulfonylurea (SU) Der [NCT02106104] | Phase 4 | 48 participants (Actual) | Interventional | 2014-03-31 | Completed | ||
| A Randomized, Open-label, Single Dose, 3x3 Partial Replicated Crossover Study to Evaluate the Pharmacokinetics and Safety/Tolerability Between a Fixed Dose Combination of Fimasartan 120 mg/Linagliptin 5 mg and Co-administration of Fimasartan 120 mg and Li [NCT03609294] | Phase 1 | 67 participants (Actual) | Interventional | 2018-07-18 | Completed | ||
| Pharmacokinetics and Pharmacodynamics of Multiple 5 mg Doses of BI 1356 p.o. Given Once Daily Compared to Multiple 2.5 mg Doses Given Twice Daily in Healthy Male and Female Volunteers. A Monocentric, Open Label, Cross-over Trial [NCT02173652] | Phase 1 | 16 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
| A Randomised, Double-blind, Placebo-controlled, Multiple Dose Phase II Study of BI 1356 BS (0.5 mg, 2.5 mg, and 10 mg in Tablet q.d. Administered Orally for 28 Days) to Evaluate Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics in Japanese Pati [NCT02183324] | Phase 2 | 72 participants (Actual) | Interventional | 2007-02-28 | Completed | ||
| Relative Bioavailability of Digoxin After Co-administration of Multiple Oral Doses of Digoxin (0.25 mg qd) and Multiple Oral Doses of BI 1356 (5 mg qd) Compared to the Bioavailability of Multiple Oral Doses of Digoxin (0.25 mg qd) Alone in Healthy Male an [NCT02183402] | Phase 1 | 20 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| Assessment of Dose Proportionality of Different Dose Strengths of Linagliptin Tablets After Oral Administration to Healthy Male and Female Volunteers in an Open, Randomised, Multiple-dose, Three-period Crossover, Phase I Trial [NCT02183480] | Phase 1 | 12 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| Relative Bioavailability of Two Fixed Dose Combination Tablets of Linagliptin 5 mg/Pioglitazone 45 mg Compared With Single Linagliptin 5 mg and Pioglitazone 45 mg Tablets Administered Together to Healthy Male and Female Subjects (Open, Randomised, Single [NCT02183636] | Phase 1 | 39 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
| Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Rising Oral Doses of BI 1356 BS as a Solution at Dose Levels 2.5 -5 mg and Tablets at Dose Levels 25 - 600 mg Administered to Healthy Male Subjects. A Randomised, Double-blind, Placebo- [NCT02173665] | Phase 1 | 64 participants (Actual) | Interventional | 2004-10-31 | Completed | ||
| Relative Bioavailability of Both BI 1356 and Pioglitazone After Co-administration Compared to the Bioavailability of Multiple Oral Doses of BI 1356 10 mg qd Alone and Pioglitazone 45 mg qd Alone in Healthy Male and Female Volunteers (an Open Label, Random [NCT02183337] | Phase 1 | 20 participants (Actual) | Interventional | 2007-02-28 | Completed | ||
| Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Multiple Oral Doses (2.5, 5, and 10 mg q.d. for 28 Days) of BI 1356 BS as Tablet in Patients With Type 2 Diabetes (Randomised, Double-blind, Placebo-controlled Within the Dose Groups) [NCT02183415] | Phase 1 | 77 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
| Relative Bioavailability of a 5 mg BI 1356 Tablet Administered With and Without Food to Healthy Male and Female Subjects in an Open, Randomised, Single Dose, Two-way Crossover, Phase I Trial [NCT02183493] | Phase 1 | 32 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
| Bioequivalence of a 2.5 mg Linagliptin / 1000 mg Metformin Fixed-dose Combination Tablet Compared With Single Linagliptin 2.5 mg and Metformin 1000 mg Tablets Administered Together in Healthy Male and Female Volunteers (an Open-label, Randomised, Single D [NCT02221401] | Phase 1 | 96 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| Prevalence of Contrast Nephropathy in Type 2 Diabetes Patients With Microalbuminuria [NCT03470454] | 40 participants (Actual) | Observational [Patient Registry] | 2018-07-01 | Completed | |||
| A Phase I Clinical Trial to Evaluate Pharmacokinetic Interactions and Safety Between Fimasartan and Linagliptin in Healthy Male Volunteers [NCT03250052] | Phase 1 | 39 participants (Actual) | Interventional | 2017-08-14 | Completed | ||
| Effects of Linagliptin in Addition to Empagliflozin on Islet Cell Physiology and Metabolic Control in Patients With Type 2 Diabetes Mellitus on Stable Metformin Treatment [NCT02401880] | Phase 4 | 89 participants (Actual) | Interventional | 2015-05-31 | Completed | ||
| A Phase III, Randomised, Double-blind, Parallel Group, 24-week Study to Evaluate Efficacy and Safety of Once Daily Empagliflozin 10 mg and Linagliptin 5 mg Fixed Dose Combination Compared With Empagliflozin 10 mg Plus Placebo and a 52-week Study to Evalua [NCT02489968] | Phase 3 | 880 participants (Actual) | Interventional | 2015-05-12 | Completed | ||
| Relative Bioavailability of a 2.5 mg Linagliptin / 1000 mg Metformin Fixed Dose Combination Tablet Administered With and Without Food to Healthy Male and Female Subjects in an Open, Randomised, Single-dose, Two-way Crossover, Phase I Trial [NCT02223026] | Phase 1 | 32 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| A Comparative Clinical Study Evaluating the Efficacy of Empagliflozin or Linagliptin as an Alternative to Metformin for Treatment of Polycystic Ovary Syndrome in Egyptian Women [NCT05200793] | Phase 4 | 75 participants (Anticipated) | Interventional | 2021-12-07 | Recruiting | ||
| A Randomized Double-blind Study to Evaluate the Effect of Linagliptin on Pancreatic Beta Cell Function and Insulin Sensitivity in Patients With Type 2 Diabetes Mellitus on Metformin Monotherapy [NCT02097342] | Phase 4 | 30 participants (Anticipated) | Interventional | 2013-12-31 | Recruiting | ||
| A Phase III, Randomised, Double-blind, Placebo-controlled, Parallel Group, Efficacy and Safety Study of Linagliptin, Administered Orally Once Daily, in Combination With Insulin Therapy for 24 Weeks in Chinese Type 2 Diabetes Mellitus Patients With Insuffi [NCT02897349] | Phase 3 | 206 participants (Actual) | Interventional | 2016-09-30 | Completed | ||
| Rotation for Optimal Targeting of Albuminuria and Treatment Evaluation: A Rotation Study of Different Albuminuria Lowering Drug Classes to Study Individual Drug Response in Diabetes [NCT03504566] | Phase 4 | 0 participants (Actual) | Interventional | 2017-11-15 | Withdrawn(stopped due to Registered and published incorrectly) | ||
| Relative Bioavailability of Multiple Doses BI 10773 50 mg and Linagliptin 5 mg After Concomitant Administration Compared to Multiple Doses of BI 10773 50 mg and Linagliptin 5mg Administered Alone to Healthy Male Volunteers (an Open-label, Randomised, Cros [NCT02172222] | Phase 1 | 16 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| The Effect of Combination of Mosapride and Dipeptidyl Peptidase-4 (DPP-4) Inhibitor on Plasma Concentration of Incretin Hormones [NCT02180334] | Phase 4 | 12 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
| Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Rising Doses (0.5 mg to 10 mg) of BI 1356 BS as Formulation for Intravenous Administration in Healthy Male Volunteers. A Randomised, Single-blind, Placebo-controlled Trial, Including a [NCT02183298] | Phase 1 | 36 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
| Pharmacokinetics and Pharmacodynamics of BI 1356 5 mg Once Daily in Male and Female Subjects With Different Degrees of Liver Impairment (Child Pugh Classification A-C) as Compared to Male and Female Healthy Subjects (a Non-blinded, Parallel Group Study of [NCT02183376] | Phase 1 | 33 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| Pharmacokinetics of Single and Multiple Oral Doses of 5 mg BI 1356 in Healthy Chinese Volunteers [NCT02183532] | Phase 1 | 12 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| Investigation of the Metabolism and Pharmacokinetics of 10 mg [14C] BI 1356 Administered Orally Compared to 5 mg [14C] BI 1356 Administered Intravenously in Healthy Male Volunteers in an Open Label, Single-dose and Parallel Study Design [NCT02183610] | Phase 1 | 12 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
| Single-center, Open, Randomized, Single-dose, Crossover Bioequivalence Study Evaluating the Use of the Subject Formulation, Empagliflozin And Linagliptin Tablets, Versus the Reference Formulation, Empagliflozin And Linagliptin Tablets (Glyxambi®), in Heal [NCT05956522] | Phase 1 | 106 participants (Actual) | Interventional | 2022-07-01 | Completed | ||
| Effect of Linagliptin on Intestinal Triglyceride-rich-lipoprotein Metabolism in Type 2 Diabetic Patients [NCT02280174] | Phase 4 | 20 participants (Anticipated) | Interventional | 2014-09-30 | Recruiting | ||
| An Open, Two-period, Fixed-sequence, Phase I Trial to Evaluate the Effect of Multiple Doses of BI 1356 on the Multiple-dose Pharmacokinetics of a Combination of Ethinylestradiol and Levonorgestrel [NCT02175394] | Phase 1 | 18 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Multiple Rising Oral Doses (1, 2.5, 5, 10 and 25 mg q.d. for 12 Days) of BI 1356 BS as Powder in the Bottle (PIB) in Patients With Type 2 Diabetes (Randomised, Double-blind, Placebo-controlled [NCT02183350] | Phase 1 | 47 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
| Relative Bioavailability of BI 1356 and Glyburide After Concomitant Administration of Multiple Oral Doses of BI 1356 5 mg Once Daily and a Single Oral Dose of Glyburide 1.75 mg Compared With the Bioavailability of BI 1356 and Glyburide After Each Treatmen [NCT02183428] | Phase 1 | 20 participants (Actual) | Interventional | 2008-05-31 | Completed | ||
| Bioavailability of Both BI 1356 BS and Metformin After Co-administration Compared to the Bioavailability of Multiple Oral Doses of BI 1356 BS 10 mg Daily Alone and Metformin 850 mg Three Times a Day Alone in Healthy Male Volunteers (an Open-label, Randomi [NCT02183506] | Phase 1 | 16 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
| An Open Label, Two-period, Fixed Sequence, Phase 1 Trial to Evaluate the Effect of Multiple Doses of Rifampicin on the Multiple-dose Pharmacokinetics of Linagliptin [NCT02183584] | Phase 1 | 16 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
| Pharmacokinetics, Pharmacodynamics, Safety and Tolerability of Single and Multiple 5 mg Doses of Linagliptin Tablets in Patients With Different Degrees of Renal Impairment in Comparison to Subjects With Normal Renal Function in a Monocentric, Open, Parall [NCT02191228] | Phase 1 | 51 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| Bioequivalence of a 2.5 mg Linagliptin / 500 mg Metformin Fixed Dose Combination Tablet Compared With Single Linagliptin 2.5 mg and Metformin 500 mg Tablets Administered Together in Healthy Male and Female Volunteers (an Open-label, Randomised, Single-dos [NCT02221414] | Phase 1 | 95 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| Effect of Empagliflozin Versus Linagliptin on Glycemic Outcomes, Renal Outcomes and Body Composition in Renal Transplant Recipients With Diabetes Mellitus: Randomized Controlled Trial [NCT06098625] | 200 participants (Anticipated) | Interventional | 2023-11-10 | Not yet recruiting | |||
| A Double-blind, Randomised, Placebo-controlled, Parallel Group Trial to Evaluate the Efficacy and Safety of Empagliflozin and Linagliptin Over 26 Weeks, With a Double-blind Active Treatment Safety Extension Period up to 52 Weeks, in Children and Adolescen [NCT03429543] | Phase 3 | 175 participants (Actual) | Interventional | 2018-03-20 | Completed | ||
| 12 Week Randomised Double-blind BI 1356 2.5 mg Bid vs 5 mg qd add-on to Metformin [NCT01012037] | Phase 2 | 491 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
| Open Label, Randomized, Single Dose, Two-way Crossover Bioequivalence Study of Linagliptin From Prevaglip 5 mg Tablets (Eva Pharma, Egypt) and Trajenta 5 mg Tablets (Boehringer Ingelheim International GmbH, Germany) [NCT02857946] | Phase 1 | 24 participants (Actual) | Interventional | 2016-02-29 | Completed | ||
| A 4-week, Randomized, Double Blind, Double Dummy, Placebo Controlled, Parallel Group Study Comparing the Influence of BI 1356 (5 mg) and Sitagliptin (100 mg) Administered Orally Once Daily on Various Biomarkers in Type 2 Diabetic Patients [NCT00716092] | Phase 2 | 121 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| The Role of Glucagon in the Effects of Dipeptidyl Peptidase-4 Inhibitors and Sodium-glucose Co-transporter-2 Inhibitors [NCT02792400] | 24 participants (Actual) | Interventional | 2016-05-31 | Completed | |||
| A Pilot Study to Assess the Efficacy of Linagliptin as an Adjunct in Schizophrenia Patients [NCT01943019] | Phase 1 | 1 participants (Actual) | Interventional | 2013-08-31 | Terminated(stopped due to Inability to obtain patients) | ||
| Bioavailability of BI 1356 After Single Oral Administration of 5 mg BI 1356 Given as Tablet Formulation TF IIb Relative to Tablet Formulation TF II and Tablet Formulation iFF in Healthy Male Volunteers (an Open Label, Randomised, Single-dose, Three-way Cr [NCT02183363] | Phase 1 | 24 participants (Actual) | Interventional | 2007-02-28 | Completed | ||
| Relative Bioavailability of a Single Oral Dose of BI 1356 (5 mg) After Co-administration With Multiple Oral Doses of Ritonavir (200 mg Bid for 3 Days) Compared to the Bioavailability of a Single Oral Dose of BI 1356 (5 mg) Alone in Healthy Male Volunteers [NCT02183441] | Phase 1 | 12 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| A Randomized, Open, Controlled, Parallel Group Study of Adding Linagliptin to Control Glycemic Variability and HbA1c in Peritoneal Dialysis Patients With Type 2 Diabetes(PDPD) With Premixed Insulin Therapy [NCT03320031] | Phase 4 | 232 participants (Anticipated) | Interventional | 2017-06-03 | Recruiting | ||
| Linagliptin as a Modulator of Vascular Inflammation in Patients With Type 2 Diabetes Mellitus [NCT02077309] | Phase 3 | 4 participants (Actual) | Interventional | 2014-08-31 | Terminated(stopped due to bad recruitment of suitable participants, just 4 patients in one year) | ||
| A Phase Ib/II, Open-Label, Multicenter, Randomized Umbrella Study Evaluating The Efficacy And Safety Of Multiple Immunotherapy-Based Treatment Combinations In Patients With Metastatic Non-Small Cell Lung Cancer (Morpheus-Lung) [NCT03337698] | Phase 1/Phase 2 | 470 participants (Anticipated) | Interventional | 2018-01-02 | Recruiting | ||
| [NCT02092597] | Phase 4 | 42 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
| An Open-label, Randomized, Single-dose Crossover Study to Evaluate the Pharmacokinetics, Safety and Tolerability of IN-C009 in Healthy Subjects [NCT05066516] | Phase 1 | 48 participants (Actual) | Interventional | 2020-06-25 | Completed | ||
| Early Prevention of Diabetes Complications in People With Hyperglycaemia in Europe: e-PREDICE Study [NCT03222765] | 1,000 participants (Anticipated) | Interventional | 2015-03-15 | Recruiting | |||
| Bioequivalence of a Fixed Dose Combination Tablet of Empagliflozin/Linagliptin Compared With the Free Combination of Empagliflozin Tablet and Linagliptin Tablet in Healthy Male and Female Subjects (an Open-label, Randomised, Single-dose, Crossover Study) [NCT02758171] | Phase 1 | 56 participants (Actual) | Interventional | 2016-05-17 | Completed | ||
| Relative Oral Bioavailability of a Fixed Dose Combination Tablet of BI 1356 2.5 mg / Metformin 1000 mg, Compared With Single BI 1356 2.5 mg and Metformin 1000 mg Tablets Administered Together to Healthy Male and Female Subjects in an Open, Randomised, Sin [NCT02173639] | Phase 1 | 20 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
| Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Rising Oral Doses (1 to 10 mg) and Multiple Rising Oral Doses (2.5 to 10 mg Once Daily for 12 Days) of BI 1356 BS in Healthy Male Volunteers (a Randomised, Double-blind, Placebo Contro [NCT02183311] | Phase 1 | 56 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
| Relative Bioavailability of a Single Oral Dose of Warfarin (10 mg qd) After Coadministration With Multiple Oral Doses of BI 1356 (5 mg qd) Compared to the Bioavailability of a Single Oral Dose of Warfarin (10 mg qd) Alone in Healthy Male Volunteers (an Op [NCT02183389] | Phase 1 | 18 participants (Actual) | Interventional | 2008-05-31 | Completed | ||
| Assessment of the Effect of 5 mg and 100 mg of BI 1356 as Single Dose on the QT Interval in Healthy Female and Male Subjects. A Randomised, Placebo Controlled, Double-blind, Four-way Crossover Study With Moxifloxacin as Positive Control [NCT02183467] | Phase 1 | 44 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| Relative Bioavailability of 1 mg and 10 mg BI 1356 BS as Powder in the Bottle (PIB) Reconstituted With 0.1% Tartaric Acid Compared to 1 mg and 10 mg BI 1356 BS as Tablets as Single Oral Administration in Healthy Male Volunteers (Separately at Each Dose Le [NCT02180503] | Phase 1 | 24 participants | Interventional | 2005-08-31 | Completed | ||
| The Effect of Multiple Oral Doses of BI 1356 BS as Tablets Once Daily for Six Days on the Pharmacokinetics, Safety and Tolerability of Multiple Oral Doses of 40 mg Simvastatin Given Once Daily for 20 Days and on the Pharmacokinetics of Its Metabolite Simv [NCT02183623] | Phase 1 | 20 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
| Effect of Empagliflozin Versus Linagliptin on Glycemic Outcomes, Renal Outcomes and Body Composition in Renal Transplant Recipients With Diabetes Mellitus: Randomized Controlled Trial (EmLina Renal Trial) [NCT06095492] | 200 participants (Anticipated) | Interventional | 2023-10-30 | Recruiting | |||
| A Phase III, Randomised, Double Blind, Placebo Controlled Parallel Group 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 a Therapy of Metfor [NCT00996658] | Phase 3 | 278 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
| Bioequivalence of a 2.5 mg Linagliptin / 850 mg Metformin Fixed Dose Combination Tablet Compared With Single Linagliptin 2.5 mg and Metformin 850 mg Tablets Administered Together in Healthy Male and Female Volunteers (an Open-label, Randomised, Single-dos [NCT02220647] | Phase 1 | 96 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| The Effect of Sodium-Glucose Cotransporter 2 Inhibitors on Advanced Glycation End Products [NCT02768220] | Phase 4 | 0 participants (Actual) | Interventional | 2017-12-01 | Withdrawn(stopped due to no funding) | ||
| Effects of the Dipeptidyl Peptidase-4 (DPP-4) Inhibitor Linagliptin on Left Ventricular Myocardial DYsfunction in Patients With Type 2 DiAbetes Mellitus and Concentric Left Ventricular Geometry [NCT02851745] | Phase 3 | 188 participants (Actual) | Interventional | 2015-07-31 | Completed | ||
| Effect of Linagliptin on Incretin Axis in Type 1 Diabetes [NCT02725502] | 20 participants (Anticipated) | Interventional | 2013-07-31 | Recruiting | |||
| A Randomised, Double-blind, Placebo-controlled Parallel Group Efficacy and Safety Study of BI 1356 (5 mg) Administered Orally Once Daily Over 24 Weeks, With an Open-label Extension to One Year (Placebo Patients Switched to BI 1356), in Type 2 Diabetic Pat [NCT00602472] | Phase 3 | 1,058 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| A Randomised, Double-blind, Placebo-controlled Parallel Group Efficacy and Safety Study of BI 1356 (One Dose, e.g. 5 mg), Administered Orally Once Daily Over 24 Weeks, With an Open Label Extension to 80 Weeks (Placebo Patients Switched to BI 1356), in Typ [NCT00601250] | Phase 3 | 701 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| A Phase IIA , Multi-center, Randomized, Double-blind, Placebo and Positive Drug Parallel Control Study of TQ-F3083 Capsules With Different Doses in Subjects With Type 2 Diabetes Mellitus [NCT03986073] | Phase 2 | 120 participants (Anticipated) | Interventional | 2020-01-01 | Recruiting | ||
| Effect of Low Dose Combination of Linagliptin and Metformin to Improve Pancreatic Beta Cell Function, Insulin Resistance and Cardiovascular Function in Patients With Prediabetes and Overweight/Obesity: Randomizer Clinical Trial [NCT04134650] | Phase 3 | 34 participants (Anticipated) | Interventional | 2019-09-01 | Recruiting | ||
| A Phase III Randomised, Double-blind, Placebo-controlled Parallel Group Study to Compare the Efficacy and Safety of Twice Daily Administration of the Free Combination of BI 1356 2.5 mg + Metformin 500 mg, or of BI 1356 2.5 mg + Metformin 1000 mg, With the [NCT00798161] | Phase 3 | 857 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| A Double-blind Phase III Study to Evaluate the Efficacy of BI 1356 5 mg and 10 mg vs. Placebo for 12 Weeks and vs. Voglibose 0.6 mg for 26 Weeks in Patients With Type 2 Diabetes Mellitus and Insufficient Glycaemic Control, Followed by an Extension Study t [NCT00654381] | Phase 3 | 561 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| A Phase III Randomised, Double-blind, Placebo-controlled, Parallel Group Efficacy and Safety Study of Linagliptin (5 mg), Administered Orally Once Daily for at Least 52 Weeks in Type 2 Diabetic Patients in Combination With Basal Insulin Therapy [NCT00954447] | Phase 3 | 1,263 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
| Comparison of Type 2 Diabetes Pharmacotherapy Regimens Using Targeted Learning [NCT05073692] | 270,000 participants (Anticipated) | Observational | 2021-07-01 | Recruiting | |||
| A Randomised, Double-blind, Placebo Controlled, Parallel Group 24 Week Study to Assess the Efficacy and Safety of BI 1356 (5 mg) in Combination With 30 mg Pioglitazone (Both Administered Orally Once Daily), Compared to 30 mg Pioglitazone Plus Placebo in D [NCT00641043] | Phase 3 | 389 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
| A Randomised, Double-blind Parallel Group Study to Compare the Efficacy and Safety of Initial Combination Therapy With Linagliptin 5 mg + Pioglitazone 15 mg, 30 mg, or 45 mg, vs. Monotherapy With Pioglitazone (15 mg, 30 mg, or 45 mg) or Linagliptin 5 mg O [NCT01183013] | Phase 3 | 936 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
| A Phase IIIb, 24-week, Randomised, Placebo-controlled, Double-blinded, Efficacy and Safety Study of Linagliptin (BI 1356) in Black/African American Patients With Type 2 Diabetes With a MTT Sub-study [NCT01194830] | Phase 3 | 234 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| Roux-en-Y Gastric Bypass for BMI 27-32 Type 2 Diabetes vs Best Medical Treatment [NCT02041234] | Phase 4 | 40 participants (Anticipated) | Interventional | 2014-02-28 | Completed | ||
| A Randomized, db, Placebo Controlled Parallel Group Efficacy and Safety Study Over 24 Weeks in T2D Patients in China [NCT01214239] | Phase 3 | 300 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
| Relative Bioavailability Investigations of a 25 mg BI 10773 / 5 mg Linagliptin Fixed Dose Combination (FDC) Tablet (Formulation A1) Including the Comparison With Its Mono-components, the Comparison With a Second FDC Tablet (Formulation A3), and the Invest [NCT01189201] | Phase 1 | 42 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
| A Phase Ib/II, Open-Label, Multicenter, Randomized, Umbrella Study Evaluating the Efficacy and Safety of Multiple Immunotherapy-Based Treatment Combinations in Patients With Locally Advanced Unresectable or Metastatic Gastric or Gastroesophageal Junction [NCT03281369] | Phase 1/Phase 2 | 410 participants (Anticipated) | Interventional | 2017-10-13 | Active, not recruiting | ||
| An Open Label, Phase I Trial to Investigate the Pharmacokinetics and Pharmacodynamics of Linagliptin (BI 1356) 5 mg After Single and Multiple Oral Administration in Patients With Type 2 Diabetes Mellitus of African American Origin for 7 Days [NCT00935220] | Phase 1 | 41 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| Effect of Linagliptin + Metformin on Glucose Metabolism and Pancreatic Beta Cell Function in Patients With Prediabetes Who do Not Achieve Normoglycemia After 12 Months of Treatment With Metformin Alone [NCT04088461] | Phase 4 | 31 participants (Actual) | Interventional | 2016-09-30 | Completed | ||
| Effect of Linagliptin Therapy on Myocardial Diastolic Function in Patients With Type 2 Diabetes Mellitus [NCT01888796] | Phase 3 | 8 participants (Actual) | Interventional | 2013-09-30 | Terminated(stopped due to bad recruitment of suitable participants, just 8 patients in one year) | ||
| EFFECTS OF LINAGLIPTIN ON ACTIVE GLP-1 CONCENTRATIONS IN SUBJECTS WITH RENAL IMPAIRMENT [NCT01903070] | Phase 4 | 99 participants (Actual) | Interventional | 2013-07-11 | Completed | ||
| A Randomised Double-blind, Active-controlled Parallel Group Efficacy and Safety Study of BI 1356 ( 5.0 mg, Administered Orally Once Daily) Compared to Glimepiride Over Two Years in Type 2 Diabetic Patients With Insufficient Glycaemic Control Despite Metfo [NCT00622284] | Phase 3 | 1,560 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| A Randomised, db, Placebo-controlled, Parallel Group Efficacy and Safety Study of BI 1356 (5mg), Administered Orally Once Daily for 18 Weeks Followed by a 34 Week Double-blind Extension Period (Placebo Patients Switched to Glimepiride) in Type 2 Diabetic [NCT00740051] | Phase 3 | 227 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
| A Randomized, Double-blind, Placebo-controlled, Five Parallel Group Study Investigating the Efficacy and Safety of BI 1356 BS (0.5 mg, 2.5 mg and 5.0 mg Administered Orally Once Daily) Over 12 Weeks in Drug Naive and Treated Patients With Type 2 Diabetes [NCT00328172] | Phase 2 | 302 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
| A Randomised, Double-blind, Placebo-controlled, Five Parallel Groups Study Investigating the Efficacy and Safety of BI 1356 BS (1 mg, 5 mg and 10 mg Administered Orally Once Daily) Over 12 Weeks as add-on Therapy in Patients With Type 2 Diabetes and Insuf [NCT00309608] | Phase 2 | 333 participants (Actual) | Interventional | 2006-04-30 | Completed | ||
| Linagliptin Plus Insulin for Hyperglycemia Immediately After Renal Transplantation: A Comparative Study [NCT03970668] | 28 participants (Actual) | Observational | 2016-01-01 | Completed | |||
| Effects of Linagliptin on Endothelial- , Renal-, and Retinal Function in Comparison to Placebo in Patients With Hypertension and Albuminuria [NCT02376075] | Phase 3 | 43 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| A Multicenter,Randomized, Placebo-controlled, Parallel Group, Double-blind, Phase IIIb Study to Evaluate the Safety and Efficacy After 12 Weeks Administration of Gemigliptin and Placebo in Type 2 Diabetes Mellitus Patients With Moderate or Severe Renal Im [NCT01968044] | Phase 3 | 132 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
| A Regulatory Requirement Non-interventional Study to Monitor the Safety and Effectiveness of Esgliteo (Empagliflozin/Linagliptin, 10/5mg, 25/5mg) in Korean Patients With Type 2 Diabetes Mellitus [NCT05130463] | 684 participants (Actual) | Observational | 2022-03-22 | Active, not recruiting | |||
| Off taRget Effects of Linagliptin monothErapy on Arterial Stiffness in Early Diabetes [NCT02015299] | Phase 3 | 45 participants (Actual) | Interventional | 2014-03-31 | Completed | ||
| A Phase III Randomised, Double Blind, Placebo-controlled, Parallel Group, Efficacy and Safety Study of Linagliptin (5 mg) Administered Orally Once Daily Over 24 Weeks in Type 2 Diabetic Patients (Age >= 70 Years) With Insufficient Glycaemic Control( HbA1c [NCT01084005] | Phase 3 | 241 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
| A Randomized, Open-label, Multiple-dose, Crossover Phase I Clinical Study to Evaluate DW1029M Influence the Pharmacokinetic Profiles of Linagliptin After Oral Administration in Healthy Male Volunteer [NCT02212782] | Phase 1 | 12 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
| A Phase III, Randomised, Double-blind, Placebo-controlled Parallel Group Safety and Efficacy Study of Linagliptin (5 mg Administered Orally Once Daily) Over 12 Weeks Followed by a 40 Week Double-blind Extension Period (Placebo Patients Switched to Glimepi [NCT01087502] | Phase 3 | 241 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
| Effect of the Combination of Dipeptidyl Peptidase-4 Inhibitor (DPP4i) and Insulin in Comparison to Insulin on Metabolic Control and Prognosis in Hospitalized Patients With COVID-19 [NCT04542213] | Phase 3 | 70 participants (Actual) | Interventional | 2020-08-01 | Completed | ||
| An Open Label, Randomised, Parallel Group Safety and Efficacy Study of Linagliptin (5 mg Administered Orally Once Daily) Over 52 Weeks in Patients With Type 2 Diabetes Mellitus and Insufficient Glycaemic Control Despite Background Mono-therapy With an App [NCT01204294] | Phase 3 | 574 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| A Randomised, Double-blind, Placebo-controlled, Parallel Group Dose-finding Study of Linagliptin (1 and 5 mg Administered Orally Once Daily) Over 12 Weeks in Children and Adolescents, From 10 to 17 Years of Age, With Type 2 Diabetes Mellitus [NCT01342484] | Phase 2 | 40 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
| A Randomised, Double-blind, Placebo-controled Parallel Group Efficacy and Safety Study of BI 1356 (5 mg Administered Orally Once Daily) Over 24 Weeks, in Drug Naive or Previously Treated (6 Weeks Washout) Type 2 Diabetic Patients With Insufficient Glycemi [NCT00621140] | Phase 3 | 503 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| Effect of a Quadruple Therapy on Pancreatic Islet Function, Insulin Resistance and Cardiovascular Function in Patients With Mixed Prediabetes and Obesity: Randomized Clinical Trial [NCT04131582] | Phase 3 | 34 participants (Anticipated) | Interventional | 2019-09-01 | Recruiting | ||
| A Non-interventional Study of Patient Medication Adherence and Treatment Effectiveness Among New Users of Linagliptin and Acarbose in the Real-world Clinical Setting in China [NCT04180813] | 85 participants (Actual) | Observational | 2020-03-04 | Terminated(stopped due to Study enrollment did not meet expectation.) | |||
| Extension Study Linagliptin 2.5 mg Bid + Metformin 500 or 1000 mg Bid Versus Metformin 1000 mg Bid [NCT00915772] | Phase 3 | 567 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| A Randomized, Double-blind, Placebo-controlled Parallel Group Efficacy and Safety Study of BI 1356 (5 mg Administered Orally Once Daily) Over 18 Weeks in Type 2 Diabetic Patients With Insufficient Glycaemic Control (HbA1c 7.0-10%) Despite Background Thera [NCT00819091] | Phase 3 | 245 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| Safety in Type 2 Diabetic Patients With Severe Chronic Renal Impairment, 5 mg BI 1356 vs. Placebo, DB, Parallel Group, Randomized, Insulin Background Inclusive [NCT00800683] | Phase 3 | 133 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| A Multicentre, International, Randomised, Parallel Group, Double Blind Study to Evaluate Cardiovascular Safety of Linagliptin Versus Glimepiride in Patients With Type 2 Diabetes Mellitus at High Cardiovascular Risk. [NCT01243424] | Phase 3 | 6,103 participants (Actual) | Interventional | 2010-11-11 | Completed | ||
| A Randomized, Double-blind, Placebo-controlled Parallel Group Efficacy and Safety Study of BI 1356 Over 24 Weeks in T2D Patients With Insufficient Glycaemic Control Despite Metformin Therapy [NCT01215097] | Phase 3 | 306 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
| ELMI - Prospective, Randomized, Controlled, Parallel-arm Study to Assess the Effects of the Combined Therapy of Empagliflozin and Linagliptin Compared to Metformin and Insulin Glargine on Renal and Vascular Changes in Type 2 Diabetes [NCT02752113] | Phase 3 | 101 participants (Actual) | Interventional | 2016-04-30 | Completed | ||
| A Prospective, Randomized, Open Label, Parallel, 12-month Study to Explore and Evaluate the Therapeutic Effects ofLiraglutide, Empagliflozin and Linagliptin on the Cognitive Function, Olfactory Function, and Odor-induced Brain Activation in T2DM Patients [NCT05313529] | 324 participants (Anticipated) | Interventional | 2022-10-08 | Recruiting | |||
| The Efficacy and Safety of Sodium-glucose Co-transporter 2 Inhibitor or Dipeptidyl Peptidase 4 Inhibitor Added to Premix Insulin Injection Twice Daily in Uncontrolled Type 2 Diabetes Patients [NCT03458715] | Phase 4 | 120 participants (Anticipated) | Interventional | 2017-09-21 | Recruiting | ||
| Glucose Metabolism in South Asian Women With IGT or IFG. DIAbetes in South Asians - DIASA 3: A 12-week Intervention Trial With Oral Antidiabetic Medication to Improve Hepatic and Whole Body Insulin Sensitivity [NCT04662866] | Phase 2 | 64 participants (Anticipated) | Interventional | 2021-02-10 | Recruiting | ||
| Efficacy and Safety of Dipeptidyl Peptidase-4 Inhibitors in Diabetic Patients With Established COVID-19 [NCT04371978] | Phase 3 | 64 participants (Actual) | Interventional | 2020-10-01 | Terminated(stopped due to End of COVID-19 outbreak in Israel) | ||
| Investigation of the Effect of Food on the Bioavailability of Empagliflozin / Linagliptin Fixed Dose Combination Tablet in an Open, Randomised, Single Dose, Two Way Cross-over Study in Healthy Japanese Male Subjects [NCT02815644] | Phase 1 | 22 participants (Actual) | Interventional | 2016-07-15 | Completed | ||
| Relative Bioavailability of Two Newly Developed Extended Release FDC Tablet Strengths (5mg/1000mg and 2.5 mg/750 mg) of Linagliptin/Metformin Extended Release Compared With the Free Combination of Linagliptin and Metformin Extended Release in Healthy Subj [NCT01845077] | Phase 1 | 72 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
| Effect of Linagliptin in Comparison With Glimepiride as Add on to Metformin on Postprandial Beta Cell Function, Postprandial Metabolism and Oxidative Stress in Patients With Type 2 Diabetes Mellitus [NCT01547104] | Phase 4 | 40 participants (Anticipated) | Interventional | 2012-04-30 | Recruiting | ||
| Research on Optimal Strategy of Hypoglycemic Therapy for Cirrhosis With Diabetes [NCT05641337] | Phase 3 | 184 participants (Anticipated) | Interventional | 2022-10-01 | Recruiting | ||
| A Single Dose Comparative Bioavailability Study of Linagliptin/Metformin hydrochloride2.5mg/500mg Combination Tablets Versus Linagliptin 2.5mg Tablets Administered With Glucophage 500mg Tablets Under Fasting Conditions [NCT01383356] | Phase 1 | 58 participants (Actual) | Interventional | 2011-06-30 | Completed | ||
| Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study [NCT05220917] | 781,430 participants (Anticipated) | Observational | 2021-08-01 | Active, not recruiting | |||
| Two-way Crossover Study in Healthy Male and Female Subjects to Evaluate the Bioequivalence of Jentadueto® (Two Fixed Dose Combination Tablets of Linagliptin 2.5 mg and Metformin 500 mg) Compared With the Free Combination of Linagliptin 5 mg and Metformin [NCT01947153] | Phase 1 | 36 participants (Actual) | Interventional | 2013-11-30 | Completed | ||
| A Randomized, Open Label, Parallel-group, Non-inferiority, Active-controlled, Phase Ⅳ Study to Evaluate the Efficacy and Safety of Teneligliptin Versus Linagliptin in Type 2 Diabetes Mellitus Patients [NCT03011177] | Phase 4 | 168 participants (Actual) | Interventional | 2017-01-31 | Completed | ||
| Bioequivalence of a Fixed Dose Combination Tablet of Linagliptin 5 mg / Pioglitazone 30 mg Compared With Its Mono-components in Healthy Male and Female Subjects (an Open-label, Randomised, Single-dose, Replicate Design Study With Two Treatments in Four Cr [NCT01276327] | Phase 1 | 64 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| A Randomized Controlled Study Comparing a DPP4 Inhibitor (Linagliptin) and Basal Insulin (Glargine) in Long-Term Care Residents With Type 2 Diabetes [NCT02061969] | Phase 4 | 140 participants (Actual) | Interventional | 2014-04-25 | Completed | ||
| Linagliptin Inpatient Trial: A Randomized Controlled Trial on the Safety and Efficacy of Linagliptin (Tradjenta®) Therapy for the Inpatient Management of General Surgery Patients With Type 2 Diabetes [NCT02004366] | Phase 4 | 295 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
| Rapid Effects of the DPP-4 Inhibitor Linagliptin on Monocyte Polarization and Endothelial Progenitor Cells in Type 2 Diabetic Patients With and Without Chronic Renal Failure. A Randomized Cross-over Trial Versus Placebo [NCT01617824] | Phase 4 | 45 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
| Association of Fasting GLP-1 Level With the Effect of Linagliptin After an Oral Glucose Tolerance Test in Prediabetes and Type 2 Diabetes Mellitus [NCT05290506] | Phase 3 | 50 participants (Actual) | Interventional | 2020-08-01 | Completed | ||
| Effects of Linagliptin on Renal Endothelium Function in Patients With Type 2 Diabetes [NCT01835678] | Phase 3 | 65 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| A Phase III Randomised, Double-blind, Double-dummy, Parallel Group Study to Compare the Efficacy and Safety of Twice Daily Administration of the Fix Dose Combination of Linagliptin 2.5 mg + Metformin 500 mg, or of Linagliptin 2.5 mg + Metformin 1000 mg, W [NCT01708902] | Phase 3 | 876 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| A Phase III Randomized, Double-blind, Parallel Group Study to Evaluate the Efficacy and Safety of Once Daily Oral Administration of BI 10773 25 mg/Linagliptin 5 mg and BI 10773 10 mg/Linagliptin 5 mg Fixed Dose Combination Tablets Compared With the Indivi [NCT01422876] | Phase 3 | 1,405 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
| The Effect of TRADJENTA ® (LINAGLIPTIN) on Inflammation, Oxidative Stress and Insulin Resistance in Obese Type 2 Diabetes Subjects [NCT02372630] | Phase 4 | 40 participants (Actual) | Interventional | 2014-05-23 | Completed | ||
| Effects of DPP4 Inhibition on COVID-19 Patients With Type 2 Diabetes [NCT04341935] | Phase 4 | 0 participants (Actual) | Interventional | 2021-06-30 | Withdrawn(stopped due to Logistical challenges amid COVID-19 pandemic and lack of financial support) | ||
| Replication of the CARMELINA Diabetes Trial in Healthcare Claims [NCT03936036] | 101,830 participants (Actual) | Observational | 2017-09-22 | Completed | |||
| Use of Combination Empagliflozin/Linagliptin or Dapagliflozin/Saxagliptin vs Empagliflozin or Dapagliflozin Alone, Subclinical Inflammation of the Genito-urinary Tract and Risk of Infections. [NCT04735042] | 60 participants (Anticipated) | Observational | 2020-10-07 | Recruiting | |||
| A Phase 1 Clinical Trial to Compare and Evaluate the Safety and Pharmacokinetic Characteristics After Administration of Fixed-dose Combination of DW6013 and Loose Combination of Each Component in Healthy Adult Volunteers in Fed Condition [NCT05874180] | Phase 1 | 31 participants (Actual) | Interventional | 2023-01-09 | Completed | ||
| A Phase 1 Clinical Trial to Compare and Evaluate the Safety and Pharmacokinetic Characteristics After Administration of Fixed-dose Combination of DW6013 and Loose Combination of Each Component in Healthy Adult Volunteers in Fast Condition [NCT05874167] | Phase 1 | 50 participants (Actual) | Interventional | 2022-08-08 | Completed | ||
| Safety and Efficacy of Linagliptin Therapy in the Setting of Internal Medicine Department Type 2 Diabetes Mellitus [NCT03051243] | Phase 3 | 60 participants (Anticipated) | Interventional | 2017-10-01 | Not yet recruiting | ||
| A Randomised, Double-blind, Double-dummy, Active-comparator Controlled Study Investigating the Efficacy and Safety of Linagliptin Co-administered With Metformin QD at Evening Time Versus Metformin BID Over 14 Weeks in Treatment Naive Patients With Type 2 [NCT01438814] | Phase 4 | 689 participants (Actual) | Interventional | 2011-11-30 | Completed | ||
| A Multicenter, Randomized, Double-blind, Active-contrelled, Parallel-group, Phase IV Clinical Trial to Investigate the Effect on Blood Glucose of Evogliptin After Oral Administration in Patiend With Type 2 Diabetes [NCT02974504] | Phase 4 | 207 participants (Actual) | Interventional | 2016-09-30 | Completed | ||
| Investigating the Protective Effect of Newer Antidiabetic Drugs on Cognitive Decline in Diabetic Patients [NCT05347459] | 100 participants (Anticipated) | Observational | 2022-03-02 | Recruiting | |||
| Role of Linagliptin in Improving Renal Failure by Improving CD34+ Stem Cell Number, Function and Gene Expression in Renal Function Impaired Type 2 Diabetes Patients. [NCT02467478] | Phase 4 | 31 participants (Actual) | Interventional | 2015-04-30 | Completed | ||
| CORDIALLY® - CEE: Characteristics of Patients With Type 2 Diabetes Treated With Modern Antidiabetic Drugs. A Real World Data Collection of Patient Baseline Characteristics, Treatment Patterns and Comorbidities in Central Eastern European (CEE) Countries [NCT03807440] | 4,083 participants (Actual) | Observational | 2019-08-26 | Completed | |||
| Bioequivalence of a Fixed Dose Combination Tablet of Linagliptin/Metformin Extended Release (5 mg/1000 mg) Compared With the Free Combination of Linagliptin and Metformin Extended Release Tablets in Healthy Subjects (an Open-label, Randomised, Single Dose [NCT02084082] | Phase 1 | 68 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
| Effects of Linagliptin on Endothelial Function and Global Arginine Bioavailability Ratio in Coronary Artery Disease Patients With Early Diabetes [NCT02350478] | Phase 4 | 49 participants (Actual) | Interventional | 2013-07-31 | Completed | ||
| A Phase III, Randomised, Double-blind, Parallel Group, 52 Week Study to Evaluate Efficacy and Safety of Once Daily Empagliflozin and Linagliptin Fixed Dose Combination Compared With Linagliptin Plus Placebo in Japanese Type 2 Diabetes Mellitus Patients Wi [NCT02453555] | Phase 3 | 275 participants (Actual) | Interventional | 2015-05-14 | Completed | ||
| A Multicenter, Randomized, Double-Blind, Active-Controlled Trial of the Efficacy and Safety of Adding HSK7653 to Metformin in Chinese Patients With Type 2 Diabetes and Inadequate Glycaemic Control [NCT04564872] | Phase 3 | 465 participants (Actual) | Interventional | 2020-11-13 | Completed | ||
| Continuous Glucose Monitoring to Assess Glycemia in Chronic Kidney Disease - Changing Glucose Management [NCT02608177] | 3 participants (Actual) | Interventional | 2015-11-30 | Completed | |||
| Real World Glycemic Effectiveness of Linagliptin Among Type 2 Diabetes Mellitus Adults by Age and Renal Function [NCT03338803] | 11,001 participants (Actual) | Observational | 2017-11-21 | Completed | |||
| Bioequivalence of Metformin Under Fed Conditions After Administration of a 2.5 mg Linagliptin / 500 mg Metformin Fixed Dose Combination Tablet Compared With Single Linagliptin 2.5 mg and Metformin 500 mg Tablets Administered Together in Healthy Male and F [NCT01581931] | Phase 1 | 32 participants (Actual) | Interventional | 2012-04-30 | Completed | ||
| Characterisation of Fixed Dose Combination Tablets of Linagliptin 2.5 mg/Metformin 850 mg or Linagliptin 2.5 mg/Metformin 500 mg and Relative Oral Bioavailability Compared With Single Linagliptin 2.5 mg and Metformin 850 mg or 500 mg Tablets Administered [NCT01540487] | Phase 1 | 48 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
| A 24-week, Randomized, Double-blind, Active-controlled, Parallel Group Trial to Assess the Superiority of Oral Linagliptin and Metformin Compared to Linagliptin Monotherapy in Newly Diagnosed, Treatment-naïve, Uncontrolled Type 2 Diabetes Mellitus Patient [NCT01512979] | Phase 4 | 316 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
| Bioequivalence of a Fixed Dose Combination Tablet of Linagliptin/Metformin Extended Release (2.5 mg/1000 mg) Compared With the Free Combination of Linagliptin and Metformin Extended Release Tablets in Healthy Subjects (an Open-label, Randomised, Single Do [NCT02084056] | Phase 1 | 74 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
| Linagliptin and Mesenchymal Stem Cells: A Pilot Study [NCT02442817] | Phase 4 | 10 participants (Actual) | Interventional | 2015-03-02 | Completed | ||
| [NCT01969084] | Phase 4 | 45 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
| A Regulatory Requirement Non Interventional Study to Monitor the Safety and Effectiveness of Trajenta (Linagliptin, 5 mg, q.d) in Korean Patients With Type 2 Diabetes Mellitus(SELINA Study) [NCT01707147] | 3,219 participants (Actual) | Observational | 2012-11-16 | Completed | |||
| Randomized, Double-blind, Multicenter, National, Phase III Clinical Trial to Evaluate the Efficacy and Safety of Lima Association in the Control of Type II Diabetes Mellitus [NCT03766750] | Phase 3 | 0 participants (Actual) | Interventional | 2021-12-31 | Withdrawn(stopped due to Sponsor decision) | ||
| A Post-Marketing Surveillance Study on the Safety, Tolerability and Efficacy of Linagliptin Among Filipino Patients With Type 2 Diabetes Mellitus [NCT01826370] | 678 participants (Actual) | Observational | 2012-05-31 | Terminated | |||
| A Phase IIIb, Multicenter, Multinational, Randomized, Double-blind, Placebo Controlled, Parallel Group Study to Evaluate the Glycemic and Renal Efficacy of Once Daily Administration of Linagliptin 5 mg for 24 Weeks in Type 2 Diabetes Patients, With Micro- [NCT01792518] | Phase 3 | 360 participants (Actual) | Interventional | 2013-02-28 | Completed | ||
| A Regulatory Requirement Non Interventional Study to Monitor the Safety and Effectiveness of Trajenta Duo® (Linagliptin/Metformin HCl, 2.5 mg/500 mg, 2.5 mg/850 mg and 2.5 mg/1000 mg, b.i.d) in Korean Patients With Type 2 Diabetes Mellitus [NCT01903356] | 724 participants (Actual) | Observational | 2013-07-11 | Completed | |||
| Relative Bioavailability of Two Different Batches of a 2.5 mg Linagliptin / 1000 mg Metformin Fixed Dose Combination Tablet (FDC) in Healthy Male and Female Volunteers (an Open-label, Randomised, Single Dose, Two-way Crossover, Phase I Trial) [NCT01216397] | Phase 1 | 40 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| National, Multicenter, Randomized, Double-blind, Triple-dummy, Phase III Clinical Trial to Evaluate the Efficacy and Safety of Madalena Association in the Treatment of Type II Diabetes Mellitus. [NCT04670666] | Phase 3 | 270 participants (Anticipated) | Interventional | 2023-08-31 | Not yet recruiting | ||
| CARMELINA: A Multicenter, International, Randomized, Parallel Group, Double-blind, Placebo-controlled, Cardiovascular Safety and Renal Microvascular Outcome Study With Linagliptin, 5 mg Once Daily in Patients With Type 2 Diabetes Mellitus at High Vascular [NCT01897532] | Phase 4 | 6,991 participants (Actual) | Interventional | 2013-07-10 | Completed | ||
| A Phase III, Randomized, Double-blind, Parallel Group Study to Evaluate the Efficacy and Safety of Linagliptin 5 mg Compared to Placebo, Administered as Oral Fixed Dose Combination With Empagliflozin 10 mg or 25 mg for 24 Weeks, in Patients With Type 2 Di [NCT01778049] | Phase 3 | 708 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| Effect of Linagliptin + Metformin vs Metformin Alone on the Role of Pancreatic Islet Function, Insulin Resistance and Markers of Cardiovascular Risk in Patients With Prediabetes: Randomized Clinical Trial [NCT03004612] | Phase 4 | 144 participants (Actual) | Interventional | 2016-01-31 | Completed | ||
| A Phase III, Randomised, Double-blind, Parallel Group, 24 Week Study to Evaluate Efficacy and Safety of Once Daily Empagliflozin 10 mg and 25 mg Compared to Placebo, All Administered as Oral Fixed Dose Combinations With Linagliptin 5 mg, in Patients With [NCT01734785] | Phase 3 | 607 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| Randomized, Three Period Cross Over, Double Blind, Double Dummy Study in Type 2 Diabetic Patients to Assess the Endothelial Effects of Linagliptin, Glimepiride and Placebo Therapy for 28 Days ('ENDOTHELINA') [NCT01703286] | Phase 1 | 42 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| A 24 Week Randomized, Double-blind, Placebo-controlled, Parallel Group, Efficacy and Safety Trial of Once Daily Linagliptin, 5 Milligrams Orally, as Add on to Basal Insulin in Elderly Type 2 Diabetes Mellitus Patients With Insufficient Glycaemic Control [NCT02240680] | Phase 4 | 302 participants (Actual) | Interventional | 2014-09-23 | Completed | ||
| Association of Clinical Covariates With Non-insulin Diabetes Medication Initiation Using Electronic Medical Records (EMR) [NCT02140645] | 166,613 participants (Actual) | Observational | 2014-05-31 | Completed | |||
| An Individualized treatMent aPproach for oldER patIents: A Randomized, Controlled stUdy in Type 2 Diabetes Mellitus (IMPERIUM) [NCT02072096] | Phase 4 | 192 participants (Actual) | Interventional | 2014-02-28 | Terminated(stopped due to The trial was terminated per protocol because of lack of feasibility.) | ||
| Bioequivalence of a Fixed Dose Combination Tablet of Linagliptin/Metformin Extended Release (2.5 mg/750 mg) Compared With the Free Combination of Linagliptin and Metformin Extended Release Tablets in Healthy Subjects (an Open-label, Randomised, Single Dos [NCT02121509] | Phase 1 | 74 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| National, Multicenter, Randomized, Double-blind, Triple-dummy, Phase III Clinical Trial to Evaluate the Efficacy and Safety of LID104 in the Treatment of Type II Diabetes Mellitus [NCT05886088] | Phase 3 | 597 participants (Anticipated) | Interventional | 2024-02-29 | Not yet recruiting | ||
| A One-year Randomized Controlled Trial Evaluating the Impact of Pioglitazone Versus Linagliptin on Bone Turnover Markers [NCT02429232] | Phase 4 | 160 participants (Anticipated) | Interventional | 2015-10-31 | Not yet recruiting | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||