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glisentide (glisentide / glipentide / Staticum)

✓ Approved

Uriach · KCNJ11 · 小分子

什么是 glisentide？

glisentide 是一种小分子，由Uriach研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名glisentide, glipentide, Staticum
公司Uriach
药物类别小分子
分子靶点KCNJ11, ABCC8
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Uriach

作用机制

分子靶点

glisentide 作用于 2 个分子靶点：

KCNJ11potassium inwardly rectifying channel subfamily J member 11 (BIR, HHF2)
ABCC8ATP binding cassette subfamily C member 8 (MRP8, SUR1delta2)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

glisentide 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
InvestigationsGlucose tolerance test abnormal✓ Approved

相关研究文献

PubMedPloS one2024-11-15

Repurposing of drug candidates against Epstein-Barr virus: Virtual screening, docking computations, molecular dynamics, and quantum mechanical study.

Ibrahim Mahmoud A A MAA, Hassan Alaa M A AMA, Mohamed Eslam A R EAR, Mekhemer Gamal A H GAH et al.

Epstein-Barr virus (EBV) was the first tumor virus identified in humans, and it is mostly linked to lymphomas and cancers of epithelial cells. Nevertheless, there is no FDA-licensed drug feasible for this ubiquitous EBV viral contagion. EBNA1 (Epstein-Barr nuclear antigen 1) plays several roles in the replication and transcriptional of latent gene expression of the EBV, making it an attractive druggable target for the treatment of EBV-related malignancies. The present study targets EBV viral reactivation and upkeep by inhibiting EBNA1 utilizing a drug-repurposing strategy. To hunt novel EBNA1 inhibitors, a SuperDRUG2 database (> 4,600 pharmaceutical ingredients) was virtually screened utilizing docking computations. In accordance with the estimated docking scores, the most promising drug candidates then underwent MDS (molecular dynamics simulations). Besides, the MM-GBSA approach was applied to estimate the binding affinities between the identified drug candidates and EBNA1. On the basis of MM-GBSA//200 ns MDS, bezitramide (SD000308), glyburide (SD001170), glisentide (SD001159), and glimepiride (SD001156) unveiled greater binding affinities towards EBNA1 compared to KWG, a reference inhibitor, with ΔGbinding values of -44.3, -44.0, -41.7, -40.2, and -32.4 kcal/mol, respectively. Per-residue decomposition analysis demonstrated that LYS477, ASN519, and LYS586 significantly interacted with the identified drug candidates within the EBNA1 binding pocket. Post-dynamic analyses also demonstrated high constancy of the identified drug candidates in complex with EBNA1 throughout 200 ns MDS. Ultimately, electrostatic potential and frontier molecular orbitals analyses were performed to estimate the chemical reactivity of the identified EBNA1 inhibitors. Considering the current outcomes, this study would be an adequate linchpin for forthcoming research associated with the inhibition of EBNA1; however, experimental assays are required to inspect the efficiency of these candidates.

PMID 39546470
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PubMedPharmaceuticals (Basel, Switzerland)2024-06-27

Approved and Commercialized Antidiabetic Medicines (Excluding Insulin) in Seven European Countries-A Cross-Sectional Comparison.

Atănăsoie Ana-Maria AM, Ancuceanu Robert Viorel RV, Krajnović Dušanka D, Waszyk-Nowaczyk Magdalena M et al.

Diabetes mellitus is a complex, multifactorial, progressive condition with a variety of approved therapeutic options. The purpose of this study was to offer an overview of the authorized antidiabetic medicines (excluding insulin) compared with marketed products in seven European countries. Data were obtained from primary sources, including the websites of national authorities and directly from specialists in the countries of interest. The range of marketed medicines compared with the authorized group was assessed in terms of active pharmaceutical ingredients (>60% in Bulgaria, France, Serbia), brand names (>70% in Bulgaria, the Czech Republic, Romania, Serbia, Spain), pharmaceutical forms (>60% in all countries), strengths (>60% in Bulgaria, the Czech Republic, Romania, Serbia, Spain), marketing authorization holder (≥50% in all countries) and the status of medicine. Spain was found to have the highest number of products based on most of these attributes. Over 90% of authorized medicines had a pharmacy price in Serbia. Regarding the newer class of GLP-1 receptor agonists, a retail price for all approved substances was available in Bulgaria, Romania, Serbia, and Spain. Only one brand name with one concentration was found available for some agents, being susceptible to drug shortages: glibenclamide (Romania, Serbia, Spain), glipizide (the Czech Republic, Poland, Romania, Spain), glisentide (Spain), acarbose (the Czech Republic), sitagliptin (Bulgaria, Poland), vildagliptin (the Czech Republic, Poland) and saxagliptin (the Czech Republic, France, Romania, Serbia). An overview of the national and international therapeutic options may allow competent authorities and health professionals to take rapid measures in case of supply problems or health crises.

PMID 38931460
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PubMedJournal of pharmaceutical and biomedical analysis2002-08-23

Investigation of the effects of grinding and co-grinding on physicochemical properties of glisentide.

Mura P P, Cirri M M, Faucci M T MT, Ginès-Dorado J M JM et al.

The purpose of the present study was to investigate the possibility of improving the dissolution properties of glisentide, a poorly water-soluble antidiabetic drug, by grinding in a high energy micromill, alone or in mixture with polyvinylpyrrolidone (PVP). Conventional and modulated differential scanning calorimetry (DSC, MDSC), thermogravimetry (TGA), X-ray powder diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), hot-stage FT-IR thermomicroscopy and scanning electron microscopy (SEM) were used to characterize the drug solid state, whereas its dissolution rates were determined according to the dispersed amount method. The techniques utilized enabled exclusion of polymorphism phenomena as a consequence of mechanical treatment, and revealed a progressive drug amorphization during grinding. In particular, MDSC allowed a clear determination of the glass transition temperature of the amorphous drug, enabling separation of glass transition from enthalpic relaxation. The amorphous state of the ground drug was the main responsible factor for the obtained 100% dissolution efficiency increase in comparison with the untreated drug. Further significant increases in dissolution properties, directly related to the polymer content in the mixture, were obtained by co-grinding with PVP, whose presence clearly favored drug amorphization, allowing a strong reduction of time and frequency of grinding necessary for obtaining complete drug amorphization.

PMID 12191707
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PubMedInternational journal of pharmaceutics1999-09-16

Evidence for polymorphism in glisentide.

Zornoza A A, de Nó C C, Martín C C, Goñi M M MM et al.

The polymorphism of glisentide has been investigated. Three polymorphs (I, II, III) have been prepared by recrystallization from different solvents and other polymorphic form (IV) was obtained by heating polymorph III at 100 degrees C. In addition, two 1:1 stoichiometric solvates containing carbon tetrachloride and dioxane have been crystallized and finally, an amorphous solid has been obtained. It has been observed that the polarity of the recrystallisation solvent and its ability to form hydrogen bonds have a great influence on the polymorphism of glisentide. The different solid forms of glisentide have been characterized using X-ray diffraction analysis, differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), IR spectroscopy and optical microscopy. The recrystallization of polymorph I in melted form II and also the transition of form III-IV have been detected by DSC and X-ray diffraction analysis.

PMID 10486438
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PubMedThe Journal of pharmacy and pharmacology1992-11-01

In-vitro protein binding interaction between a metabolite of triflusal, 2-hydroxy-4-trifluoromethylbenzoic acid and other drugs.

Mis R R, Ramis J J, Conte L L, Forn J J

2-Hydroxy-4-trifluoromethylbenzoic acid (HTB) is the main active metabolite of triflusal, an antiplatelet drug. The in-vitro binding of HTB to human serum was studied in the presence of different drugs. The results indicate that no statistically significant changes are observed in the HTB binding in the presence of caffeine, theophylline, glisentide, enalapril, cimetidine or warfarin. The free fraction of HTB increases significantly in the presence of the non-steroidal anti-inflammatory drugs studied: diclofenac, ibuprofen, indomethacin, naproxen, piroxicam and salicylic acid. At high concentrations, HTB displaces these anti-inflammatory drugs and also glisentide and warfarin from their protein binding sites.

PMID 1361542
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