Meglitinides are a class of oral hypoglycemic agents that act as rapid-acting insulin secretagogues. They are used to treat type 2 diabetes by stimulating the release of insulin from the beta cells of the pancreas. Meglitinides are structurally similar to sulfonylureas but have a shorter duration of action, making them less likely to cause hypoglycemia. They are typically taken before meals to help control blood sugar levels after eating. Meglitinides are generally well-tolerated, but common side effects include hypoglycemia, weight gain, and gastrointestinal disturbances. The mechanism of action of meglitinides involves binding to the ATP-sensitive potassium channel (KATP) on the beta cells of the pancreas. This binding leads to depolarization of the cell membrane, opening of voltage-gated calcium channels, and subsequent release of insulin. Meglitinides have been studied extensively for their potential in treating type 2 diabetes, and they are often used in combination with other antidiabetic medications. They are also being investigated for their potential in treating other conditions such as obesity and cardiovascular disease. Research into meglitinides continues to focus on improving their safety and efficacy and exploring their potential in other disease areas.'
meglitinide: structure given in first source & in Negwer, 5th ed, #6436
ID Source | ID |
---|---|
PubMed CID | 41214 |
CHEMBL ID | 149930 |
SCHEMBL ID | 37926 |
MeSH ID | M0096461 |
Synonym |
---|
meglitinido [inn-spanish] |
meglitinidum [inn-latin] |
benzoic acid, 4-(2-((5-chloro-2-methoxybenzoyl)amino)ethyl)- |
p-(2-(5-chloro-o-anisamido)ethyl)benzoic acid |
4-(2-(5-chlor-2-methoxy-benzamido)-aethyl)benzoasaeure [german] |
4-(2-((5-chloro-2-methoxybenzoyl)amino)ethyl)benzoic acid |
hb 699 |
brn 2817215 |
meglitinide [inn] |
meglitinide |
CHEMBL149930 |
4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]benzoic acid |
54870-28-9 |
meglitinidum |
meglitinido |
unii-8v6ok1i088 |
8v6ok1i088 , |
4-(2-(5-chlor-2-methoxy-benzamido)-aethyl)benzoasaeure |
SCHEMBL37926 |
MLS006011933 |
smr004703520 |
DTXSID40203356 |
SR-01000945131-1 |
SR-01000945131-2 |
sr-01000945131 |
Z224216672 |
AKOS033822030 |
Q27271068 |
4-{2-[(5-chloro-2-methoxyphenyl)formamido]ethyl}benzoic acid |
EN300-1187992 |
Meglitinides are a group of oral hypoglycemic medications currently approved for the treatment of type 2 diabetes mellitus. Meglitinide analogues increase insulin secretion, in particular, during the early phase of insulin release.
Excerpt | Reference | Relevance |
---|---|---|
"Meglitinides are a group of oral hypoglycemic medications currently approved for the treatment of type 2 diabetes mellitus (T2DM). " | ( Efficacy and Cardiovascular Safety of Meglitinides. Fernandez, CJ; Philip, J, 2021) | 2.34 |
"Meglitinide analogues are a class of oral hypoglycaemic agents that increase insulin secretion, in particular, during the early phase of insulin release." | ( Meglitinide analogues for type 2 diabetes mellitus. Black, C; Donnelly, P; McIntyre, L; Royle, PL; Shepherd, JP; Thomas, S, 2007) | 2.5 |
Excerpt | Reference | Relevance |
---|---|---|
"Treatment with meglitinides reconstructed postprandial ghrelin secretion patterns to those of controls without diabetes. " | ( Effect of meglitinides on postprandial ghrelin secretion pattern in type 2 diabetes mellitus. Möhlig, M; Otto, B; Pfeiffer, AF; Pivovarova, O; Rudovich, N; Spranger, J; Weickert, MO, 2010) | 1.12 |
Excerpt | Reference | Relevance |
---|---|---|
"The objective of this study was to evaluate the association between hypoglycemia and antibiotics using the US Food and Drug Administration Adverse Event Reporting System (FAERS), while accounting for concomitant glucose-lowering medications including sulfonylureas and meglitinides." | ( Hypoglycemia Associated with Antibiotics Alone and in Combination with Sulfonylureas and Meglitinides: An Epidemiologic Surveillance Study of the FDA Adverse Event Reporting System (FAERS). Frei, CR; Kennedy, KE; Patek, TM; Teng, C, 2020) | 0.96 |
Excerpt | Reference | Relevance |
---|---|---|
" In this article, we review the pharmacokinetic DDIs concerning oral antidiabetics, including metformin, sulfonylureas, meglitinide analogs, thiazolidinediones and dipeptidyl peptidase-4 inhibitors, and the underlying mechanistic basis that can help to predict and prevent DDIs." | ( Drug interactions with oral antidiabetic agents: pharmacokinetic mechanisms and clinical implications. Backman, JT; Neuvonen, PJ; Niemi, M; Tornio, A, 2012) | 0.59 |
" The complex pharmacokinetic and pharmacogenetic properties and the unfavourable short and long term risk profile of glibenclamide and glimepiride raise the question whether their use can be justified any longer." | ( CYP2C metabolism of oral antidiabetic drugs--impact on pharmacokinetics, drug interactions and pharmacogenetic aspects. Beil, W; Holstein, A; Kovacs, P, 2012) | 0.38 |
Excerpt | Reference | Relevance |
---|---|---|
" Patients with T2DM are usually treated with multiple drugs, and are therefore at an increased risk of harmful drug-drug interactions (DDIs)." | ( Drug interactions with oral antidiabetic agents: pharmacokinetic mechanisms and clinical implications. Backman, JT; Neuvonen, PJ; Niemi, M; Tornio, A, 2012) | 0.38 |
Excerpt | Relevance | Reference |
---|---|---|
"In patients with type 2 diabetes mellitus, the traditional method of initiating therapy with a sulfonylurea and increasing the dosage until maximum levels are reached before adding an insulin-sensitizing agent has persisted and should be re-evaluated." | ( A comparison of agents used to manage type 2 diabetes mellitus: need for reappraisal of traditional approaches. Bell, DS, 2004) | 0.32 |
" Achieving and maintaining tight glycemic control is key to preventing development or progression of CKD; however, improving glycemic control may be limited by effects of renal impairment on the efficacy and safety of T2DM treatments, necessitating dosing adjustments and careful evaluation of contraindications." | ( Glycemic control of type 2 diabetes mellitus across stages of renal impairment: information for primary care providers. Adler, S; Tong, L, 2018) | 0.48 |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID194743 | Maximum % decrease of blood glucose (deltaBG) was observed within 4 hour after administration orally at 10 mg/kg dose to fasted adult female rats versus a control group | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26 | Repaglinide and related hypoglycemic benzoic acid derivatives. |
AID706675 | Antihyperglycemic activity in streptozotocin-induced diabetic Sprague-Dawley rat assessed as reduction in blood glucose level at 63.01 umol/kg, po after 24 hrs relative to control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Synthesis and biological investigations of nitric oxide releasing nateglinide and meglitinide type II antidiabetic prodrugs: in-vivo antihyperglycemic activities and blood pressure lowering studies. |
AID194741 | Maximum % decrease of blood glucose (deltaBG) was observed within 4 hour after administration orally at 1 mg/kg dose to fasted adult female rats versus a control group | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26 | Repaglinide and related hypoglycemic benzoic acid derivatives. |
AID194171 | Effect of the compound (50 mg/kg, po) on rat blood sugar level which was given an oral glucose load (1 g/kg) 1 hr after the administration of compound | 1984 | Journal of medicinal chemistry, Jan, Volume: 27, Issue:1 | Receptor binding sites of hypoglycemic sulfonylureas and related [(acylamino)alkyl]benzoic acids. |
AID176587 | Half-maximal effective dose was measured on rat blood glucose after administrating at 4 hr | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26 | Repaglinide and related hypoglycemic benzoic acid derivatives. |
AID706694 | Antihyperglycemic activity in streptozotocin-induced diabetic Sprague-Dawley rat assessed as reduction in blood glucose level at 63.01 umol/kg, po after 6 hrs relative to control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Synthesis and biological investigations of nitric oxide releasing nateglinide and meglitinide type II antidiabetic prodrugs: in-vivo antihyperglycemic activities and blood pressure lowering studies. |
AID706696 | Antihyperglycemic activity in streptozotocin-induced diabetic Sprague-Dawley rat assessed as reduction in blood glucose level at 63.01 umol/kg, po after 1 hr relative to control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Synthesis and biological investigations of nitric oxide releasing nateglinide and meglitinide type II antidiabetic prodrugs: in-vivo antihyperglycemic activities and blood pressure lowering studies. |
AID706695 | Antihyperglycemic activity in streptozotocin-induced diabetic Sprague-Dawley rat assessed as reduction in blood glucose level at 63.01 umol/kg, po after 3 hrs relative to control | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Synthesis and biological investigations of nitric oxide releasing nateglinide and meglitinide type II antidiabetic prodrugs: in-vivo antihyperglycemic activities and blood pressure lowering studies. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 17 (15.04) | 18.7374 |
1990's | 24 (21.24) | 18.2507 |
2000's | 42 (37.17) | 29.6817 |
2010's | 22 (19.47) | 24.3611 |
2020's | 8 (7.08) | 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 (75.88) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 3 (2.54%) | 5.53% |
Reviews | 50 (42.37%) | 6.00% |
Case Studies | 5 (4.24%) | 4.05% |
Observational | 1 (0.85%) | 0.25% |
Other | 59 (50.00%) | 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 | ||
---|---|---|---|---|---|---|---|
Incretin-based Drugs and the Risk of Heart Failure: A Multi-center Network Observational Study [NCT02456428] | 1,499,650 participants (Actual) | Observational | 2014-03-31 | Completed | |||
The Use of Incretin-based Drugs and the Risk of Acute Pancreatitis in Patients With Type 2 Diabetes [NCT02476760] | 1,417,914 participants (Actual) | Observational | 2014-03-31 | Completed | |||
The Echocardiographic Left Ventricular Functional Changes of Uncontrolled Diabetes by the Intervention of Dapagliflozin Treatment Trial (ELUCIDATE) [NCT03871621] | Phase 4 | 76 participants (Actual) | Interventional | 2019-04-01 | Completed | ||
A National, Multicenter, Prospective, Interventional, Open-label, Single-arm, 24-Week Phase IV Study to Evaluate the Effectiveness and Safety of Initiation and Titration of Insulin Glargine U300 in Insulin-naïve Patients With T2DM Inadequately Controlled [NCT02954692] | Phase 4 | 112 participants (Actual) | Interventional | 2016-11-30 | Completed | ||
A Phase 3, Open Label, Randomized, Parallel, 26 Week Treatment Study Comparing LY2605541 With Insulin Glargine as Basal Insulin Treatment in Combination With Oral Anti Hyperglycemia Medications in Asian Insulin Naïve Patients With Type 2 Diabetes Mellitus [NCT01894568] | Phase 3 | 388 participants (Actual) | Interventional | 2013-07-31 | Completed | ||
Dapagliflozin Effect in Cognitive Impairment in Stroke Trial [NCT05565976] | Phase 2/Phase 3 | 270 participants (Anticipated) | Interventional | 2020-08-01 | Recruiting | ||
The Use of Incretin-based Drugs and the Risk of Pancreatic Cancer in Patients With Type 2 Diabetes [NCT02475499] | 886,172 participants (Actual) | Observational | 2014-03-31 | Completed | |||
Efficacy in Controlling Glycaemia With Victoza® (Liraglutide) as add-on to Metformin vs. OADs as add-on to Metformin After up to 104 Weeks of Treatment in Subjects With Type 2 Diabetes Inadequately Controlled With Metformin Monotherapy and Treated in a Pr [NCT02730377] | Phase 4 | 1,991 participants (Actual) | Interventional | 2016-03-28 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |