Page last updated: 2024-11-13

imeglimin

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Description

imeglimin: a tetrahydrotriazine-containing oral antidiabetic [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID24812808
CHEMBL ID4297514
SCHEMBL ID2158106
SCHEMBL ID14868241
SCHEMBL ID22029979
MeSH IDM0578468

Synonyms (29)

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

Research Excerpts

Overview

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.

ExcerptReferenceRelevance
"Imeglimin is a novel oral hypoglycemic agent that improves blood glucose levels through multiple mechanisms of action including the enhancement of glucose-stimulated insulin secretion (GSIS), however, the details of this mechanism have not been clarified. "( A novel mechanism of imeglimin-mediated insulin secretion via the cADPR-TRP channel pathway.
Dezaki, K; Funazaki, S; Hara, K; Kakei, M; Kawakami, M; Nagashima, S; Yamada, H; Yoshida, M, 2022
)
2.48
"Imeglimin is a novel tetrahydrotriazine-containing drug suggested as a safe drug for glycemic management in patients with type 2 diabetes mellitus (T2DM). "( Efficacy and safety of imeglimin in patients with type 2 diabetes mellitus: A systematic review and meta-analysis of randomized clinical trials.
Abdelhaleem, IA; Alsabbagh, FA; Ebada, MA; Eid, AM; Hussien, HM; Mohamed, NI; Salamah, HM,
)
1.88
"Imeglimin is a novel oral antidiabetic drug modulating mitochondrial functions. "( Imeglimin Is Neuroprotective Against Ischemic Brain Injury in Rats-a Study Evaluating Neuroinflammation and Mitochondrial Functions.
Borutaite, V; Cizas, P; Grigaleviciute, R; Jankeviciute, S; Pampuscenko, K; Rastenyte, D; Umbrasas, D; Zemgulyte, G, 2022
)
3.61
"Imeglimin is a first-in-class novel oral antidiabetic marketed in Japan as TWYMEEG"( Pharmacokinetics of Imeglimin in Caucasian and Japanese Healthy Subjects.
Bolze, S; Chevalier, C; Fouqueray, P, 2022
)
2.49
"Imeglimin is a new anti-diabetic drug commercialized in Japan (Twymeeg®) and has been drawing much attention in diabetes research area as well as in clinical practice. "( Imeglimin exerts favorable effects on pancreatic β-cells by improving morphology in mitochondria and increasing the number of insulin granules.
Fushimi, Y; Ikeda, T; Kaku, K; Kaneto, H; Kimura, T; Mune, T; Nakanishi, S; Nogami, Y; Obata, A; Obata, Y; Sanada, J; Shimoda, M; Yamasaki, Y, 2022
)
3.61
"Imeglimin is a novel anti-hyperglycemic drug that improves both insulin resistance and insulin secretion. "( Add-on imeglimin versus metformin dose escalation regarding glycemic control in patients with type 2 diabetes treated with a dipeptidyl peptidase-4 inhibitor plus low-dose metformin: study protocol for a multicenter, prospective, randomized, open-label, p
Atsumi, T; Cho, KY; Kameda, H; Kurihara, H; Miya, A; Miyoshi, H; Nagai, S; Nakamura, A; Nomoto, H; Takahashi, A; Takeuchi, J; Taneda, S, 2022
)
2.62
"Imeglimin is a recently launched antidiabetic drug structurally related to metformin. "( Effects of imeglimin on mitochondrial function, AMPK activity, and gene expression in hepatocytes.
Hozumi, K; Ishihara, N; Ishihara, T; Ogawa, W; Sugawara, K, 2023
)
2.74
"Imeglimin is a novel new oral compound recently approved for treating type 2 diabetes (T2D) in India. "( Efficacy and safety of imeglimin in type 2 diabetes: A systematic review and meta-analysis of randomized placebo-controlled trials.
Misra, A; Singh, A; Singh, AK; Singh, R, 2023
)
2.66
"Imeglimin is a new antidiabetic drug structurally related to metformin. "( Stimulatory effect of imeglimin on incretin secretion.
Iwasaki, Y; Ogawa, W; Ohbayashi, K; Seino, S; Sugawara, K; Takahashi, H; Yingyue, Q; Yokoi, N, 2023
)
2.67
"Imeglimin is a novel small molecular tetrahydrotriazine that has been shown to improve hyperglycemia in clinical trials among patients with type 2 diabetes. "( Safety and Efficacy of Imeglimin for Type 2 Diabetes in Patients Undergoing Dialysis.
Mima, A,
)
1.88
"Imeglimin is a novel antidiabetic drug structurally related to metformin. "( Imeglimin profoundly affects the circadian clock in mouse embryonic fibroblasts.
Abe, J; Ando, H; Fujiwara, H; Fujiwara, T; Jing, Z; Maida, Y; Mieda, M; Miura, K; Miyazaki, R; Morishige, JI; Nagata, N; Ono, M; Sakane, N; Shi, Y; Xu, P, 2023
)
3.8
"Imeglimin is an oral antidiabetic agent currently in clinical development."( Clinical pharmacology of imeglimin for the treatment of type 2 diabetes.
Brønden, A; Christensen, MB; Johansson, KS; Knop, FK, 2020
)
1.58
"Imeglimin is a promising antidiabetic agent that has shown to have significant antihyperglycemic effects in studies, although it has not been approved yet."( Molecular Mechanisms by Which Imeglimin Improves Glucose Homeostasis.
Jamialahmadi, T; Maleki, M; Sahebkar, A; Sathyapalan, T; Yaribeygi, H, 2020
)
1.57
"Imeglimin is a novel oral antidiabetic drug for treatment of type 2 diabetes that targets mitochondrial bioenergetics. "( In Vitro Investigation, Pharmacokinetics, and Disposition of Imeglimin, a Novel Oral Antidiabetic Drug, in Preclinical Species and Humans.
Clémence, C; Fouqueray, P; Sébastien, B, 2020
)
2.24
"Imeglimin is a novel oral antidiabetic drug used to treat type 2 diabetes, targeting the mitochondrial bioenergetics. "( Pharmacokinetics of Imeglimin in Subjects with Moderate Hepatic Impairment.
Bolze, S; Chevalier, C; Dubourg, J; Fouqueray, P, 2021
)
2.39
"Imeglimin is an investigational first-in-class novel oral agent for the treatment of type 2 diabetes (T2D). "( Mechanism of action of Imeglimin: A novel therapeutic agent for type 2 diabetes.
Bolze, S; Borel, AL; Fontaine, E; Fouqueray, P; Hallakou-Bozec, S; Kergoat, M; Moller, DE; Vial, G, 2021
)
2.37
"Imeglimin is a first-in-class novel drug candidate that improves glycaemia and glucose-stimulated insulin secretion in preclinical models and patients."( Imeglimin preserves islet β-cell mass in Type 2 diabetic ZDF rats.
Bolze, S; Hallakou-Bozec, S; Kergoat, M; Moller, DE, 2021
)
2.79
"Imeglimin is a novel agent currently in development to treat type 2 diabetes. "( Imeglimin: A Potential New Multi-Target Drug for Type 2 Diabetes.
Brown, C; Chastain, LM; Maggu, GA; Vuylsteke, V, 2015
)
3.3
"Imeglimin is a promising new oral antihyperglycemic agent that has been studied in clinical trials as a possible monotherapy or add-on therapy to lower fasting plasma glucose and improve hemoglobin A1c (1-3, 9). "( Imeglimin lowers glucose primarily by amplifying glucose-stimulated insulin secretion in high-fat-fed rodents.
Bolze, S; Cardone, RL; Fouqueray, P; Hallakou-Bozec, S; Kibbey, RG; Perry, RJ; Petersen, KF; Petersen, MC; Shulman, GI; Zhang, D, 2016
)
3.32

Effects

ExcerptReferenceRelevance
"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

Actions

ExcerptReferenceRelevance
"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

Treatment

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.

ExcerptReferenceRelevance
"Imeglimin treatment significantly improved glucose-stimulated insulin secretion (augmentation of the insulinogenic index) and improved glycaemia. "( Imeglimin preserves islet β-cell mass in Type 2 diabetic ZDF rats.
Bolze, S; Hallakou-Bozec, S; Kergoat, M; Moller, DE, 2021
)
3.51
"Imeglimin treatment for 7 days raised the insulin secretory response to glucose by +112% (iAUC0-45 , p = 0.035), first-phase ISR by +110% (p = 0.034) and second-phase ISR by +29% (p = 0.031). "( Imeglimin increases glucose-dependent insulin secretion and improves β-cell function in patients with type 2 diabetes.
Bolze, S; Fouqueray, P; Mari, A; Pacini, G; Roden, M, 2015
)
3.3
"Treatment with imeglimin augmented mitochondrial function, enhanced insulin secretion, promoted β-cell proliferation, and improved β-cell survival in mouse islets."( Imeglimin Ameliorates β-Cell Apoptosis by Modulating the Endoplasmic Reticulum Homeostasis Pathway.
Chew, RSE; Inoue, R; Kin, T; Kyohara, M; Li, J; Miyashita, D; Nishiyama, K; Okuyama, T; Oyadomari, S; Satoh, A; Shapiro, AMJ; Shirakawa, J; Teo, AKK; Terauchi, Y; Togashi, Y; Tsuno, T, 2022
)
2.5
"Treatment with imeglimin significantly decreased infarct size, brain edema, and neurological deficits after pMCAO."( Imeglimin Is Neuroprotective Against Ischemic Brain Injury in Rats-a Study Evaluating Neuroinflammation and Mitochondrial Functions.
Borutaite, V; Cizas, P; Grigaleviciute, R; Jankeviciute, S; Pampuscenko, K; Rastenyte, D; Umbrasas, D; Zemgulyte, G, 2022
)
2.5
"Treatment with imeglimin starting at 10 weeks not only improved their abnormal systemic glucose metabolism and visceral obesity but also their cardiac abnormalities."( Imeglimin prevents heart failure with preserved ejection fraction by recovering the impaired unfolded protein response in mice subjected to cardiometabolic stress.
Endo, J; Fukuda, K; Goto, S; Hashimoto, S; Katsumata, Y; Kitakata, H; Mizuno, E; Moriyama, H; Sano, M; Shirakawa, K, 2021
)
2.4

Toxicity

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.

ExcerptReferenceRelevance
" Safety and tolerability were assessed in both studies through adverse event recording and laboratory parameters, vital signs and electrocardiogram."( Imeglimin, a novel glimin oral antidiabetic, exhibits a good efficacy and safety profile in type 2 diabetic patients.
Fouqueray, P; Lebovitz, H; Pirags, V, 2012
)
1.82
" Imeglimin was generally well tolerated, with a safety profile comparable to placebo and no related treatment-emergent adverse events."( The efficacy and safety of imeglimin as add-on therapy in patients with type 2 diabetes inadequately controlled with sitagliptin monotherapy.
Bailey, CJ; Diamant, M; Fouqueray, P; Inzucchi, SE; Lebovitz, HE; Pirags, V; Schernthaner, G, 2014
)
1.61
" Treatment-emergent adverse events were reported for 68."( Efficacy and safety of imeglimin in Japanese patients with type 2 diabetes: A 24-week, randomized, double-blind, placebo-controlled, dose-ranging phase 2b trial.
Dubourg, J; Fouqueray, P; Grouin, JM; Ueki, K, 2021
)
0.93
"Imeglimin is a novel tetrahydrotriazine-containing drug suggested as a safe drug for glycemic management in patients with type 2 diabetes mellitus (T2DM)."( Efficacy and safety of imeglimin in patients with type 2 diabetes mellitus: A systematic review and meta-analysis of randomized clinical trials.
Abdelhaleem, IA; Alsabbagh, FA; Ebada, MA; Eid, AM; Hussien, HM; Mohamed, NI; Salamah, HM,
)
1.88
" Regarding safety profile, imeglimin was safe and tolerable with no treatment-emergent or serious adverse events."( Efficacy and safety of imeglimin in patients with type 2 diabetes mellitus: A systematic review and meta-analysis of randomized clinical trials.
Abdelhaleem, IA; Alsabbagh, FA; Ebada, MA; Eid, AM; Hussien, HM; Mohamed, NI; Salamah, HM,
)
0.74
" The percentage of patients experiencing at least one treatment emergent adverse event (TEAE) was 75."( 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
" The incidence of patients experiencing adverse events and serious adverse events was similar in the two treatment groups."( Efficacy and safety of imeglimin add-on to insulin monotherapy in Japanese patients with type 2 diabetes (TIMES 3): A randomized, double-blind, placebo-controlled phase 3 trial with a 36-week open-label extension period.
Dubourg, J; Fouqueray, P; Grouin, JM; Reilhac, C; Thang, C; Watada, H, 2022
)
1.03
" During the observation period, adverse events such as hypoglycemia, diarrhea, nausea, or vomiting were not recognized in any patient."( Safety and Efficacy of Imeglimin for Type 2 Diabetes in Patients Undergoing Dialysis.
Mima, A,
)
0.44
" Secondary outcomes included other efficacy-related outcomes, specific adverse events, and changes in body weight and lipid parameters."( Efficacy, safety and tolerability of imeglimin in patients with type 2 diabetes mellitus: A meta-analysis of randomized controlled trials.
Hagi, K; Kaku, K; Nitta, M; Ueki, K; Watada, H, 2023
)
1.18
" There were no significant differences between imeglimin and placebo in the risk of all-cause discontinuation and the proportion of patients who presented with at least one adverse event."( Efficacy, safety and tolerability of imeglimin in patients with type 2 diabetes mellitus: A meta-analysis of randomized controlled trials.
Hagi, K; Kaku, K; Nitta, M; Ueki, K; Watada, H, 2023
)
1.44

Pharmacokinetics

ExcerptReferenceRelevance
" 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

Compound-Compound Interactions

No clinically significant drug-drug interaction exists between imeglimin and cimetidine. Cimetidine is a reference inhibitor of MATE1, MATE2-K, OCT1 and OCT2 transporters.

ExcerptReferenceRelevance
" 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

Bioavailability

ExcerptReferenceRelevance
"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

Dosage Studied

ExcerptRelevanceReference
" 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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID1347411qHTS 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) Libary2020ACS 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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular 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]

Research

Studies (52)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (15.38)24.3611
2020's44 (84.62)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 64.44

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.

MetricThis Compound (vs All)
Research Demand Index64.44 (24.57)
Research Supply Index4.26 (2.92)
Research Growth Index5.08 (4.65)
Search Engine Demand Index105.54 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (64.44)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (29.63%)5.53%
Reviews12 (22.22%)6.00%
Case Studies1 (1.85%)4.05%
Observational0 (0.00%)0.25%
Other25 (46.30%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]