acarbose / Generic mfg. - LARVOL DELTA

In silico drug repurposing targeting fusion and nucleoprotein of human metapneumovirus: A step toward pandemic preparedness. (PubMed, Indian J Pharmacol) - "The study highlights mobocertinib, rutin, and levetiracetam as promising repurposed drugs against HMPV. While mobocertinib exhibited the strongest predicted binding affinity, levetiracetam demonstrated the best pharmacokinetic profile, making it a particularly viable candidate for further experimental validation. These results validate the usefulness of in silico drug repurposing in addressing unmet antiviral needs and warrant preclinical studies to evaluate therapeutic efficacy."

Journal

Synthesis and characterization of indole-3-butyric acid-based hydrazones: from multifunctional enzyme inhibition to therapeutic potential for drug development. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "The thiophene-based compound exhibited potent acetylcholinesterase inhibition (IC50 1.95 ± 10.79 μM), surpassing the standard donepezil (IC50 4.53 ± 0.13 μM), and demonstrated effective α-amylase inhibition (IC50 0.99 ± 2.6 μM), comparable to acarbose (IC50 4.21 ± 0.27 μM). This compound also showed pronounced cytotoxicity against HeLa (96.31%, IC50 49.2 ± 0.02 μM) and PC-3 (97.42%, IC50 41.1 ± 0.11 μM) cell lines in comparison with standard doxorubicin (HeLa 98.7%, IC50 1.13 ± 0.18 μM and PC-3 80.8%, IC50 1.18 ± 0.21 μM)...Antibacterial assays revealed enhanced activity against Gram-positive (51.3 ± 3.5 mm) compared to cefixime (27 ± 0.31 mm) by aminodichlorophenyl derivative and Gram-negative (15.0 ± 0.12 mm) bacterial strains compared to cefixime (29 ± 0.17 mm) by thiophene-based compounds...The incorporation of sulfur and halogen along with amino..."

Journal • Infectious Disease • Oncology • Tyrosinase

Comparative cardiovascular outcomes and safety of hypoglycemic drug classes in patients with type 2 diabetes and hypertension: a multicenter cohort analysis. (PubMed, Cardiovasc Diabetol) - "This study highlights the differential cardiovascular effectiveness and safety profiles of hypoglycemic therapies in real-world settings, providing valuable insights for optimizing T2D management, particularly in patients with comorbid hypertension."

Clinical • Journal • Retrospective data • Atherosclerosis • Cardiovascular • Chronic Kidney Disease • CNS Disorders • Diabetes • Heart Failure • Hypertension • Immunology • Inflammatory Arthritis • Insomnia • Metabolic Disorders • Nephrology • Renal Disease • Sleep Disorder • Type 2 Diabetes Mellitus

Canagliflozin or acarbose vs placebo to ameliorate post-bariatric hypoglycaemia: mechanistic insights from the HypoBar I randomised clinical trial (EASD 2025) - P2 | "While both pharmacological approaches failed to raise postprandial glycaemic nadir during the meal test, they altered postprandial glycaemic excursions and associated entero-pancreatic hormone dynamics and could, thus, prove relevant for PBH treatment through modulation of its pathophysiology."

Clinical • Diabetes • Hypoglycemia • Metabolic Disorders

Introduction of new quinolone-2-thio-acetamide-propane hydrazide-benzimidazole derivatives as new α-glucosidase and α-amylase inhibitors. (PubMed, Sci Rep) - "This compound was 5 and 23.8 folds more potent than acarbose against α-glucosidase and α-amylase, respectively, and with excellent binding energies in comparison to acarbose attached to active sites of these enzymes. Molecular dynamics and pharmacokinetic studies of compound 12n was also performed."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

DES-Promoted Synthesis of 3,4-Dihydropyrimidinones and Their Antidiabetic and Antioxidant Evaluation Supported With Computational Studies. (PubMed, Chem Biodivers) - "Among the series, compound 3f exhibited superior inhibitory activity against α-glucosidase (IC50 = 35.25 µM) and α-amylase (IC50 = 38.61 µM), being ∼2.3- and ∼2.6-fold more potent, respectively, than the standard drug acarbose...Furthermore, density functional theory (DFT) studies revealed favorable electronic and reactivity profiles, whereas ADME/T predictions indicated good drug-likeness. Overall, compound 3f shows strong potential as a lead antidiabetic agent for managing postprandial hyperglycemia."

Journal • Diabetes

Piperonal-derived Schiff base molecules as potential multi-target therapeutic agents against Alzheimer's and diabetes. (PubMed, Future Med Chem) - "Compounds 7 (IC50 = 5.73 ± 0.01; 3.52 ± 0.02 µM) and 17 (IC50 = 10.91 ± 0.02; 7.38 ± 0.02 µM) showed potent inhibitory effects against AG and AA enzymes, in comparison to acarbose (IC50 = 14.98 ± 0.02 µM; 14.64 ± 0.02 µM). However, analogs 7, 9, 10, 14, and 15, compounds 7 (IC50 = 2.92 ± 0.02; 3.34 ± 0.02 µM) and 9 (IC50 = 8.16 ± 0.03; 7.19 ± 0.03 µM) showed remarkable inhibitory results against AChE and BChE, respectively, compared to standard donepezil chloride (IC50 = 37.89 ± 0.02 µM; 41.56 ± 0.03 µM)...Synthesized derivatives were also checked for their antioxidant potential and demonstrated significant activity. These complementary studies highlight several hit candidates for further development as therapeutic agents against DM and AD."

Journal • Alzheimer's Disease • CNS Disorders • Diabetes • Metabolic Disorders • Pain

Synthesis, crystal structure, and in vitro evaluation of newer 2,4-thiazolidinedione hybrids as α-glucosidase inhibitors. (PubMed, Future Med Chem) - "Compared to Acarbose, VD-TZD hybrids displayed good AGI activity...The in silico ADMET profile of compound 6f indicates satisfactory oral drug-likeness and the absence of toxic effects. In conclusion, compound 6f could be considered a promising lead compound for further optimization in AGI development for the treatment of T2DM."

Journal • Preclinical • Type 2 Diabetes Mellitus

Pan-cancer analysis and oncogenic implications of MGAM and MGAM2: Toward precision oncology and drug repurposing in colorectal cancer. (PubMed, J Cell Commun Signal) - "In CRC patients, MGAM downregulation was confirmed in 64 samples, and WES revealed a novel MGAM mutation (rs2960746). These findings underscore MGAM and MGAM2 as promising biomarkers and therapeutic targets, supporting their relevance in advancing personalized oncology."

Journal • Pan tumor • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • MGAM

Bioactive Potential of Nepenthes miranda Flower Extracts: Antidiabetic, Anti-Skin Aging, Cytotoxic, and Dihydroorotase-Inhibitory Activities. (PubMed, Plants (Basel)) - "For antidiabetic evaluation, the ethanol extract demonstrated potent α-glucosidase inhibition (IC50 = 24.53 μg/mL), outperforming standard inhibitors such as acarbose and quercetin...Furthermore, the ethanol extract strongly inhibited the activity of purified human dihydroorotase (IC50 = 25.11 μg/mL), indicating that disruption of pyrimidine biosynthesis may underlie its anticancer activity. Overall, this study provides the first characterization of N. miranda flower extracts, particularly the ethanol fraction, as a promising source of multifunctional bioactive compounds with possible applications in cosmetics, antidiabetic therapy, and cancer treatment."

Journal • Oncology • Squamous Cell Carcinoma • ELANE • Tyrosinase

Integrating data augmentation and BERT-based deep learning for predicting alpha-glucosidase inhibitors derived from Black Cohosh. (PubMed, Sci Rep) - "Further molecular docking and MD simulations presented this compound to interact stably with the enzyme and possess a high inhibition probability when compared to acarbose. The results of insilico drug discovery displayed that actaeaepoxide 3-O-xyloside is pointed out to be a potential candidate for diabetes therapy. In conclusion, the role of augmentation techniques and pre-trained models was also emphasized in the presented investigation to accelerate drug discovery toward more effective therapeutic solutions."

Journal • Cognitive Disorders • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity

New 1E,1'E-hydrazine-bis(phenoxy-1,2,3-triazol-acetamide) derivatives as potent inhibitors against acetylcholinesterase, butyrylcholinesterase, and α-glucosidase. (PubMed, RSC Adv) - "In this regard, all the synthesized compounds were more potent than the standard inhibitors tacrine and donepezil against BChE, and most of these compounds were more potent than tacrine against AChE. Moreover, most of the target synthesized compounds were more potent than the standard inhibitor acarbose against α-glucosidase...Furthermore, docking studies demonstrated that compound 10k interacted with both the catalytic and peripheral anionic sites of AChE and BChE. This property led to the better efficacy of the compound in the treatment of AD."

Journal • Alzheimer's Disease • CNS Disorders • Diabetes • Metabolic Disorders • Neuroblastoma • Oncology • Pain • Solid Tumor

Synthesis and radiolabelled evaluation of novel pyrimidine derivatives as dual α-amylase inhibitors and GIT-targeted molecular imaging probe. (PubMed, RSC Adv) - "Compound 1 showed the strongest inhibitory in vitro amylase effect, in comparison to the reference drug acarbose...A gradual increase in muscle uptake was observed, raising possible insights into side effects reported with similar drugs. These results suggest that compound 1 not only possesses potent amylase-blocking and related effective antidiabetic activity but also holds promise as a molecular probe for molecular dynamic imaging for the GIT system."

Journal • Gastrointestinal Disorder

Molecular insights of acarbose metabolization catalyzed by acarbose-preferred glucosidase. (PubMed, Nat Commun) - "Additionally, further investigation of the acarbose analogs acarstatins A and B that are resistant to Apg is conducted by computational analysis. Overall, our studies provide perspectives into the intricacies of Apg's catalytic mechanism, contributing to the design of next-generation hypoglycemic pharmaceuticals."

Journal

Proximate Composition, Phytochemicals, Phenolic Compounds, and Bioactive Characterization of Mauritia flexuosa L.f. Seeds. (PubMed, Plants (Basel)) - "Notably, MFS ethanolic extracts exhibited significant in vitro antihyperglycemic activity via inhibiting α-amylase and α-glucosidase enzymes, demonstrating comparable inhibition to acarbose at higher concentrations. High-performance liquid chromatography-mass spectrometry (UHPLC-ESI-HRMS) analysis of the seed extract identified phenolic compounds including ellagic, p-coumaric, and chlorogenic acids, as well as flavonoids such as quercetin, myricetin, and epicatechin. This study provides the first evidence of the hypoglycemic activity of MFSs, offering valuable insights into their phytochemistry and potential therapeutic applications."

Journal • Diabetes • Metabolic Disorders

Design and Synthesis of Sulfonium and Selenonium Derivatives Bearing 3',5'-O-Benzylidene Acetal Side Chains as Potent α-Glucosidase Inhibitors. (PubMed, ChemMedChem) - "In vivo, 20b (15.0 mg kg-1) reduced postprandial blood glucose levels in sucrose-loaded mice by 40.6% (15 min), 49.5% (30 min), and 43.6% (60 min), surpassing acarbose (20.0 mg kg- 1)...Cytotoxicity assessments confirmed the favorable safety profile of selected compounds in normal cell lines. Enzyme kinetic studies demonstrated fully competitive inhibition of α-glucosidase by these sulfonium salts."

Journal • MGAM

Novel Biphenyls From Garcinia multiflora: Isolation and α-Amylase Inhibitory Properties. (PubMed, Chem Biodivers) - "The results showed that all seven compounds exhibited strong binding to α-amylase. Additionally, further enzyme inhibition assays using a multifunctional microplate reader revealed that, compared with the positive control acarbose (half-maximal inhibitory concentration [IC50] = 17.23 ± 2.43 µM), only compounds 5 (IC50 = 2190 ± 180 µM) and 6 (IC50 = 4420 ± 1480 µM) exhibited relatively weak α-amylase inhibitory activity."

Journal

Molecular Docking and In Vitro Assessment of Gymnema sylvestre R. Br. and Trigonella foenum-graecum L. Phytochemicals as Dual α-Amylase and α-Glucosidase Inhibitors. (PubMed, Chem Biodivers) - "The α-amylase and α-glucosidase inhibitory potentials were screened in vitro using 50% EtOH extracts of G. sylvestre leaves and T. foenum-graecum seeds with acarbose as the reference compound...In vitro assays further revealed that T. foenum-graecum seed extract showed the highest α-amylase inhibition (IC50 = 12.09 ± 2.13 mg/mL) and α-glucosidase inhibition (IC50 = 5.23 ± 0.33 mg/mL). Trigoneoside XIIa, trigofoenoside G, and gymnemasaponin V were identified as promising drug candidates for the development of antidiabetic drug leads, further validating the in vitro α-amylase and α-glucosidase inhibitory potentials."

Journal • Preclinical

Utility of Continuous Glucose Monitoring in the Management of Severe Post-Bariatric Hypoglycemia (ENDO 2025) - "Management can be challenging with limited options including dietary modification and medications such as acarbose, diazoxide and octreotide...However, CGM use is currently not part of official guidelines for hypoglycemia management in non-diabetic patients, which hinders access to CGM for many patients. Wide use of CGM in patients with post-bariatric hypoglycemia may improve clinical outcomes and should be advocated."

CNS Disorders • Epilepsy • Genetic Disorders • Hypoglycemia • Metabolic Disorders • Obesity • Severe Hypoglycemia • Solid Tumor

Synthesis and In vitro Biological Evaluation of Quinolone-Based Hydrazones as Potential Antidiabetic Agents Targeting Key Metabolic Enzymes. (PubMed, ACS Omega) - "Notably, compound 5o (5-nitrofuran) demonstrated the most potent inhibition against both enzymes (α-glucosidase IC50 = 7.44 ± 0.07 μg/mL; α-amylase IC50 = 21.05 ± 0.17 μg/mL), surpassing the standard drug acarbose...Density functional theory (DFT) analysis of 5o revealed a small HOMO-LUMO energy gap (0.112566 eV) and a soft nature, suggesting good chemical reactivity. These findings showcase the potential of quinolone-based hydrazones, particularly compound 5o, as promising candidates aiming at the development of multitarget therapies for antidiabetic agents."

Journal • Preclinical • Diabetes • Metabolic Disorders • AKR1B1

CARAT: Safety and Efficacy Evaluation of Cofrogliptin (HSK7653) and Acarbose Research Among T2DMs (clinicaltrials.gov) - P=N/A | N=200 | Not yet recruiting | Sponsor: Haisco Pharmaceutical Group Co., Ltd.

New trial • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Crosstalk-free dual-mode biosensing in a single MOF for α-glucosidase activity monitoring and inhibitor screening. (PubMed, Talanta) - "Upon α-glucosidase-mediated generation of hydroquinone, simultaneous signal transduction occurs through independent pathways: colorimetric attenuation via suppression of the oxidase-like catalytic process, and fluorescence recovery due to ligand-to-metal charge transfer modulation. Furthermore, the system facilitates precise inhibitor screening with IC50 values of 8.13 μM for fluorescence-based detection and 10.06 μM for colorimetric detection of acarbose. By integrating self-validating detection and drug evaluation within a single-material architecture, this work establishes a paradigm for designing robust MOF-based biosensors equipped with built-in cross-validation capabilities."

Journal

The Effects of Acarbose on the Postprandial Hypotensive Response in Older Adults. (PubMed, Can J Aging) - P2 | "Although the average decrease in SBP during the meal test was significantly attenuated in the acarbose group (standardized β  = 0.724 ± 0.286, p = 0.017), the acarbose group experienced significantly more PPH events (standardized β  = 0.593 ± 0.279, p = 0.040). Although acarbose attenuated the mean decrease in SBP during the meal test, it did not reduce the actual number of PPH events recorded in a general population of older adults.ClinicalTrials.gov ID NCT01914133."

Journal • Diabetes • Hypotension • Metabolic Disorders

Bioassay-guided evaluation of a potent dual inhibitor of host and gut microbial α-glucosidases from Galla chinensis: mechanism insights and in silico studies. (PubMed, Fitoterapia) - "The binding energies of PGG with α-Glu and SusB were - 7.5 kcal/mol and - 9.3 kcal/mol, while them for acarbose were - 8.2 kcal/mol and - 7.3 kcal/mol, respectively. These findings revealed the potential mechanism of PGG for diabetic therapy through retarding the absorption of carbohydrates."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Seaweed extract as a sustainable resource for Au nanoparticle synthesis and its biological and environmental applications. (PubMed, Artif Cells Nanomed Biotechnol) - "Notably, Hfs-AuNPs exhibited encouraging tyrosinase inhibition (31.74 % inhibition while kojic acid showed 52.40 % inhibition at 100 µg/ml), antidiabetic effect (56.38 % α-amylase activity while acarbose exhibited 61.19 % activity at 100 µg/ml), and antioxidant properties (82.89 % of DPPH scavenging while 60.04 % scavenging by BHT and 63.73 SOD effect while 61.77 % scavenging by BHT at 100 µg/ml). Besides, Hfs-AuNPs also displayed positive photocatalytic degradation of toxic industrial dyes like methylene blue (29.20 % degradation at 5 h) and methyl orange (21.26 % degradation at 3 h). The above eco-friendly, cost-effective, and sustainable synthesis method can be explored further for large-scale production and future substantial applications in therapeutic and industrial needs."

Journal • Tyrosinase