imeglimin: a tetrahydrotriazine-containing oral antidiabetic
ID Source | ID |
---|---|
PubMed CID | 24812808 |
CHEMBL ID | 4297514 |
SCHEMBL ID | 2158106 |
SCHEMBL ID | 14868241 |
SCHEMBL ID | 22029979 |
MeSH ID | M0578468 |
Synonym |
---|
imeglimin [inn] |
uu226qgu97 , |
(4r)-6-(dimethylamino)-4-methyl-4,5-dihydro-1,3,5-triazin-2-amine |
775351-65-0 |
unii-uu226qgu97 |
imeglimin |
SCHEMBL2158106 |
emd-387008 |
imeglimin [who-dd] |
HY-14771 |
CS-1751 |
DTXSID50228237 |
SCHEMBL14868241 |
A914497 |
DB12509 |
Q6003719 |
(r)-n2,n2,6-trimethyl-3,6-dihydro-1,3,5-triazine-2,4-diamine |
1,3,5-triazine-2,4-diamine,1,6-dihydro-n,n,6-trimethyl-,(+)-(9ci) |
emd 387008 (r-imeglimin) hcl |
BCP11085 |
emd387008 |
emd 387008 |
NCGC00378621-02 |
emd 387008 hcl |
(4r)-6-n,6-n,4-trimethyl-1,4-dihydro-1,3,5-triazine-2,6-diamine |
CHEMBL4297514 |
SCHEMBL22029979 |
(s)-n2,n2,6-trimethyl-1,6-dihydro-1,3,5-triazine-2,4-diamine |
AKOS040745212 |
Imeglimin is a novel tetrahydrotriazine-containing drug suggested as a safe drug for glycemic management in patients with type 2 diabetes mellitus (T2DM) The details of this mechanism have not been clarified.
Excerpt | Reference | Relevance |
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"Imeglimin has been shown to have a beneficial effect on 3 key pathogenetic elements of T2DM, i.e., 1." | ( Imeglimin: a new antidiabetic drug with potential future in the treatment of patients with type 2 diabetes. Grzeszczak, W; Nowak, M, 2022) | 2.89 |
Excerpt | Reference | Relevance |
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"Imeglimin may enhance glucose-induced insulin secretion (GIIS) and inhibit apoptosis of pancreatic ß-cells leading to preserved β-cell mass by maintaining or restoring the functional and structural integrity of the mitochondria and the endoplasmic reticulum homeostasis in pancreatic β-cells." | ( Current understanding of imeglimin action on pancreatic β-cells: Involvement of mitochondria and endoplasmic reticulum homeostasis. Fauzi, M; Inagaki, N; Murakami, T; Yabe, D, 2023) | 1.93 |
Imeglimin treatment for 7 days raised the insulin secretory response to glucose by +112% (iAUC0-45 , p = 0.035) Treatment with imeglimin significantly decreased infarct size, brain edema, and neurological deficits after pMCAO.
Imeglimin is a novel tetrahydrotriazine-containing drug suggested as a safe drug for glycemic management in patients with type 2 diabetes mellitus (T2DM) There were no significant differences between imeglimin and placebo in the risk of all-cause discontinuation.
Excerpt | Reference | Relevance |
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" Pharmacokinetic parameters were determined from blood and urine; levels of all compounds were evaluated using liquid chromatography with tandem mass spectrometry." | ( Imeglimin Does Not Induce Clinically Relevant Pharmacokinetic Interactions When Combined with Either Metformin or Sitagliptin in Healthy Subjects. Bolze, S; Fouqueray, P; Perrimond-Dauchy, S, 2020) | 2 |
"To assess the pharmacokinetic and safety profile of imeglimin in Caucasian and Japanese healthy individuals." | ( Pharmacokinetics of Imeglimin in Caucasian and Japanese Healthy Subjects. Bolze, S; Chevalier, C; Fouqueray, P, 2022) | 1.3 |
No clinically significant drug-drug interaction exists between imeglimin and cimetidine. Cimetidine is a reference inhibitor of MATE1, MATE2-K, OCT1 and OCT2 transporters.
Excerpt | Reference | Relevance |
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" The objective of the study was to assess the potential drug-drug interaction between imeglimin and cimetidine, a reference inhibitor of these transporters." | ( Lack of Drug-Drug Interaction Between Cimetidine, a Renal Transporter Inhibitor, and Imeglimin, a Novel Oral Antidiabetic Drug, in Healthy Volunteers. Bolze, S; Chevalier, C; Dubourg, J; Fouqueray, P; Perrimond-Dauchy, S, 2020) | 1.01 |
"No clinically significant drug-drug interaction exists between imeglimin and cimetidine, a reference inhibitor of MATE1, MATE2-K, OCT1 and OCT2 transporters." | ( Lack of Drug-Drug Interaction Between Cimetidine, a Renal Transporter Inhibitor, and Imeglimin, a Novel Oral Antidiabetic Drug, in Healthy Volunteers. Bolze, S; Chevalier, C; Dubourg, J; Fouqueray, P; Perrimond-Dauchy, S, 2020) | 1.02 |
"A total of 714 patients received the following treatments: imeglimin monotherapy (n = 134), combination with an α-glucosidase inhibitor (n = 64), biguanide (n = 64), dipeptidyl peptidase-4 inhibitor (DPP4-I; n = 63), glinide (n = 64), glucagon-like peptide-1 receptor agonist (GLP1-RA; n = 70), sodium-glucose co-transporter-2 inhibitor (n = 63), sulphonylurea (n = 127), or thiazolidinedione (n = 65)." | ( Long-term safety and efficacy of imeglimin as monotherapy or in combination with existing antidiabetic agents in Japanese patients with type 2 diabetes (TIMES 2): A 52-week, open-label, multicentre phase 3 trial. Dubourg, J; Fouqueray, P; Grouin, JM; Kaku, K; Quinslot, D, 2022) | 1.25 |
Excerpt | Reference | Relevance |
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"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
" The imeglimine molecule is well absorbed (Tmax-4), and the half-life is 5-6 hours, is largely excreted through the kidneys, and also has no clinically significant interactions with either metformin or sitagliptin." | ( [Imeglimin: features of the mechanism of action and potential benefits]. Arapieva, AM; Bobrik, AG; Bobrik, DV; Khamitova, AD; Kuznetsov, KO; Mahmutova, EI; Nagaev, IR; Saetova, AA, 2022) | 2.15 |
Excerpt | Relevance | Reference |
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" 12-Lead Holter ECGs were recorded from 1 h before dosing until at least 24 h after each dose." | ( Absence of QTc prolongation in a thorough QT study with imeglimin, a first in class oral agent for type 2 diabetes mellitus. Bolze, S; Dubourg, J; Felices, M; Fouqueray, P; Perrimond-Dauchy, S; Voiriot, P, 2020) | 0.8 |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
[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 | 0 (0.00) | 29.6817 |
2010's | 8 (15.38) | 24.3611 |
2020's | 44 (84.62) | 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 (64.44) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 16 (29.63%) | 5.53% |
Reviews | 12 (22.22%) | 6.00% |
Case Studies | 1 (1.85%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 25 (46.30%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |