acarbose / Generic mfg. - LARVOL DELTA

New Pyrazole-Based Tetrazole Derivatives: Synthesis, Characterization, and Their Vasorelaxant and α-Amylase Inhibition Activities. (PubMed, Chem Biol Drug Des) - "Notably, compounds 2 and 6 demonstrated a comparable activity to the positive control acarbose. These experimental findings were further supported by molecular docking studies."

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Orthostatic Hypotension (OH), Postural Orthostatic Tachycardia Syndrome (POTS), and Reactive Hypoglycemia: Are they connected? (ENDO 2025) - "Although the HYPO episodes decreased with starting acarbose 25 mg with meals, she was unable to tolerate this due to gastrointestinal symptoms and HYPO episodes increased with lightheadedness on changes in position.Case 2:A 61-year-old male with complaints of syncopal episodes and low systolic blood pressure readings was referred to Endocrinology for evaluation and management of nOH...While therapy of non-neurogenic OH is mostly straight-forward, nOH is often difficult to treat. A structured approach is important in the management of patients with nOH. Our cases highlight that there is an interaction between the autonomic nervous system and glucose homeostasis."

Cardiovascular • Endocrine Disorders • Hypoglycemia • Hypotension • Metabolic Disorders • Mood Disorders • Movement Disorders • Psychiatry

Post Bariatric Hypoglycemia Successfully Treated With GLP-1 Receptor Agonist (ENDO 2025) - "After unsuccessful trials or contraindications to acarbose, octreotide, nifedipine, and diazoxide, the patient was started on liraglutide (0.6 mg subcutaneously daily). Although the exact mechanism is unclear, it is hypothesized that exogenous GLP-1 at consistent concentrations may attenuate the exaggerated GLP-1 release following rapid nutrient delivery after bariatric surgery. However, given the limited data available, further high-quality studies are needed to validate this theory and evaluate the overall efficacy of GLP-1 receptor agonists in managing PBH."

CNS Disorders • Endocrine Disorders • Epilepsy • Hypoglycemia • Nephrology • Renal Disease • Solid Tumor

Hyperproinsulinemia due to a rare variant in the INS gene complicating the diagnosis of post gastric bypass hypoglycemia (ENDO 2025) - "Medications: acarbose, vitamins and famotidine. We report a case of gastric bypass associated hypoglycemia where initial concerns included a proinsulin secreting tumor, yet meal testing dissociated hypoglycemia from proinsulin values, leading us to pursue bypass reversal and find a rare variant in the INS gene associated with hyperproinsulinemia likely due to impaired proinsulin cleavage."

Bariatric surgery • Asthma • Diabetes • Genetic Disorders • Hypoglycemia • Immunology • Metabolic Disorders • Obesity • Oncology • Polycystic Ovary Syndrome • Respiratory Diseases

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

Navigating the Uncertainty: Atypical Diabetes Mellitus with Negative Biomarkers and Complex Management (ENDO 2025) - "He was discharged with insulin (Lantus 8 units and Novolog 2 units TID) and metformin (METF) 1000 mg BID.Two weeks later when he was evaluated in clinic he was only taking METF with small doses of short-acting insulin, as needed...Patient was trialed with acarbose with no effect on BG, then a dipeptidyl peptidase-4 (DDP-4) inhibitor... This case highlights the complexity involved in diagnosing and managing atypical forms of DM, including LADA, monogenic, and ketosis-prone DM. It is a spectrum, which may present with features of both type 1 and type 2 DM but lacks definitive biomarkers. Clinicians should consider the atypical forms in adult patients with new-onset diabetes and atypical presentations, especially when there is an absence of typical autoimmune markers."

Biomarker • Diabetes • Diabetic Retinopathy • Fatigue • Hypoglycemia • Immunology • Metabolic Disorders • Renal Disease • Retinal Disorders • Type 1 Diabetes Mellitus

Insulin Autoimmune Syndrome - The Underdog of Hypoglycemia. A Case Report and Comparative Analysis (ENDO 2025) - "This report highlights an uncommon case of IAS among a 54-year-old African American male who, after being misdiagnosed for many years, presented with remitting and relapsing symptoms despite being on appropriate treatment of IAS and eventually started on acarbose for hypoglycemia management. We also briefly review the current literature to discuss similar cases, their associated factors and treatment methods."

Case report • Clinical • Hypoglycemia • Immunology

Non-Insulin Mediated Postprandial Hypoglycemia following Roux-en-Y Gastric Bypass in a Patient with Panhypopituitarism (ENDO 2025) - "She was also prescribed acarbose with meals and snacks. glucose 60 (RR 70-90 mg/dL), insulin 2.2 (RR 3-25 mIU/L), proinsulin <4.0 (RR <18.8 pmol/L), C-peptide 0.75 (RR 0.81-3.85 ng/mL), beta-hydroxybutyrate 2.20 (RR 0.02-0.27 mmol/L) consistent with a non-insulin mediated process. IGF-1, insulin autoantibodies, celiac screen, and hypoglycemia panel were unremarkable. The total dosage of hydrocortisone was increased to 25 mg/day with doses divided into 4 times per day."

Bariatric surgery • Clinical • Cardiovascular • Diabetes • Endocrine Disorders • Genetic Disorders • Hypoglycemia • Metabolic Disorders • Nephrology • Obesity • Renal Disease • IGF1

Glucagon Like Peptide 1 Receptor Agonists as a Potential Treatment of Post Bariatric Hypoglycemia (ENDO 2025) - "Management typically includes dietary modifications and pharmacotherapy with acarbose, octreotide, nicardipine, or diazoxide; however, effective treatment remains challenging... GLP1-RAs may be an effective treatment for PBH, particularly in patients refractory to dietary changes or other medications. Further studies are needed to confirm long-term efficacy and safety."

Hypoglycemia • Infectious Disease • Novel Coronavirus Disease

Benzimidazole derivatives as potent α-amylase inhibitors: synthesis, characterization and in vitro α-amylase inhibition. (PubMed, Future Med Chem) - "The synthesized benzimidazole derivatives, notably compounds 7b, 7c, and 7i, demonstrated potent α-amylase inhibitory activity, surpassing the standard drug acarbose. These findings highlight their potential as lead compounds for developing novel antidiabetic agents."

Journal • Preclinical

Design and synthesis of novel quinoline-piperazines fused to a phenylhydrazinecarbothioamide scaffold as promising α-glucosidase inhibitors with anti-diabetic potential. (PubMed, Future Med Chem) - "Among them, 7j was the most active, with an IC50 value of 1.0 µM, approximately 750-fold more potent than acarbose...MD simulations further indicated that the complex formed between 7j and the enzyme was stable, with limited conformational fluctuations. The results confirm that quinoline-piperazine derivatives bearing phenylhydrazinecarbothioamide moieties are promising scaffolds for α-glucosidase inhibition."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Bioactive Isobenzofuranone and Isochromenones From a Marine-Derived Fungus Penicillium sp.: Isolation, Characterization, and Inhibitory Activity Against α-Glucosidase. (PubMed, Chem Biodivers) - "Compounds 1 (IC₅₀ = 76.4 µM), 3 (IC₅₀ = 95.4 µM), and 4 (IC₅₀ = 88.3 µM) exhibited inhibitory effects against α-glucosidase, showing comparable activity to the positive control acarbose (IC₅₀ = 67.7 µM). Molecular docking revealed that these structurally analogous compounds exhibited similar binding modes within the active site."

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Expediting multiple biological properties of main bioactive compounds of Mentha pulegium L. (PubMed, AMB Express) - "In antidiabetic assays, all tested compounds outperformed acarbose...In silico analysis confirmed strong binding affinities of pulegone and menthone to target enzymes involved in glucose regulation. These findings highlight MPEO as a promising natural source of bioactive compounds with antibacterial, antidiabetic, and dermatoprotective properties, supporting its potential use in pharmaceutical and therapeutic applications."

Journal • Diabetes • Infectious Disease • Metabolic Disorders • ELANE • Tyrosinase

Evaluation of modified benzaldehyde derivatives as dual α-glucosidase and α-amylase inhibitors: a viable alternative to acarbose. (PubMed, Food Sci Biotechnol) - "The combination of benzaldehyde with hydroxyl, methyl, or methoxy groups suggests the potential for benzaldehyde to serve as a parent compound for the development of selective inhibitors. The results indicate that 3,4-dihydroxybenzaldehyde, 3,5-dihydroxybenzaldehyde, 2,5-dihydroxybenzaldehyde, 2,4,5-trihydroxybenzaldehyde, and 2,3,4-trihydroxybenzaldehyde may prove beneficial in alleviating diabetic pathological conditions."

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Antidiabetic Activity of Compounds Isolated From Zanthoxylum mildbraedii: An In Vitro α-Amylase Inhibition and In Silico Analysis. (PubMed, Chem Biodivers) - "All four compounds exhibited moderate α-amylase inhibition (IC50 = 16.38-27.73 mM) compared to the standard drug acarbose (IC50 = 11.98 ± 1.07 mM)...These findings suggest that the isolated compounds from Z. mildbraedii possess promising α-amylase inhibitory potential and drug-like properties, indicating their potential as lead candidates for further development of natural antidiabetic therapeutics. Their favorable pharmacokinetic attributes and multimodal inhibition mechanisms highlight the significance of this study in contributing to the discovery of safer, plant-derived agents for diabetes management."

Journal • Preclinical • Diabetes • Metabolic Disorders

Azolo[5',1',2,3]pyrimido[5,4-e]tetrazolo[1,5-c]pyrimidines as dual-action antiglycators and α-glucosidase inhibitors. (PubMed, Bioorg Med Chem Lett) - "The obtained azolo[5',1':2,3]pyrimido[5,4-e]tetrazolo[1,5-c]pyrimidines 12 inhibited the glycation reaction in the BSA-glucose assay more strongly than pyridoxamine as a reference compound, which is promising in terms of preventing AGEs assosiated pathologies such as long-term complication of diabetes and cancer. Furthermore, some heterocycles 12 inhibited α-glucosidase in the mid-micromolar range - more effectively than acarbose, with an IC50 17.52 μM for the lead compound 12k."

Journal • Diabetes • Metabolic Disorders • Oncology

One-Pot Synthesis of Novel Pyrimidine Derivatives with Potential Antidiabetic Activity Through Dual α-Glucosidase and α-Amylase Inhibitors. (PubMed, Molecules) - "Compound 4 expressed the highest level of activity against α-glucosidase and α-amylase, with a greater inhibitory concentration (IC50 of 12.16 ± 0.12 µM and IC50 11.13 ± 0.12 µM) compared to that of acarbose (IC50 = 10.60 ± 0.17 µM and IC50 = 11.30 ± 0.12 µM), which is widely used as a standard antidiabetic drug. The primary structure activity relationship analysis identified the impact of an electron- withdrawing group, especially with respect to fluorine on inhibitory activity. This was further confirmed in molecular docking studies, which demonstrated that both compounds exhibited similar inhibition patterns and emphasized the significance of incorporating a lipophilic electron-withdrawing substituent on the phenyl ring, along with the 2,4-diaminopyrimidine scaffold."

Journal • Diabetes • Metabolic Disorders

Design and Synthesis of Sulfonium and Selenonium Derivatives Bearing 3',5'-O-Benzylidene Acetal Side Chain Structure as Potent α-Glucosidase Inhibitors. (PubMed, Molecules) - "The most potent inhibitor 20c (10.0 mg/kg) reduced postprandial blood glucose by 48.6% (15 min), 52.8% (30 min), and 48.1% (60 min) in sucrose-loaded mice, outperforming acarbose (20.0 mg/kg)...The selected compounds exhibited a high degree of safety in cytotoxicity tests against normal cells. Kinetic characterization of α-glucosidase inhibition confirmed a fully competitive inhibitory mode of action for these sulfonium salts."

Journal • Diabetes

Phytochemical Composition and Biological Activities of the Lichen Usnea aciculifera in the Southern Vietnam. (PubMed, Chem Biodivers) - "As a result, 1-10 exhibited similar or superior α-glucosidase inhibition activity (IC50 values ranging from 18.60 to 93.19 µM) than the positive standard, acarbose (IC50 = 100.02 µM). Furthermore, molecular docking evaluation suggested that effective α-glucosidase inhibition can be achieved by firmly blocking Site 1 while extending the structure toward Site 2 enhances the bioactivity if done correctly. As for the cytotoxicity of compounds 1 and 2, they both exhibited moderate activity against the three cancer cell lines (IC50 values ranging from 18.11 to 30.28 µM)."

Journal • Oncology

The lifespan-extending MEK1 inhibitor trametinib promotes regulation of de novo lipogenesis enzymes by chaperone-mediated autophagy. (PubMed, Front Aging) - "Here we show that decreased protein abundance of enzymes involved in hepatic de novo lipogenesis (DNL) is characteristic of mice exposed to two anti-aging drugs that modulate glucose homeostasis (acarbose and canagliflozin), as well as in calorically restricted mice and in two long-lived mutant models. The trametinib effect on DNL enzymes is, unexpectedly, not related to transcriptional changes, but depends on selective protein degradation through chaperone-mediated autophagy. Our data support models in which chaperone-mediated proteomic alterations, triggered through the MEK1-ERK-MNK kinase pathway, may collaborate with mTORC1 changes to slow aging and extend mouse lifespan."

Journal • Targeted Protein Degradation • EIF4E • MAP2K1

Design, synthesis, and comprehensive evaluation of novel imidazole-chromone hybrids as potent cholinesterase and α-glucosidase inhibitors. (PubMed, Eur J Med Chem) - "Among the tested compounds, derivative 4c exhibited the most promising inhibitory activity against both AChE (3.93 μM) and α-glucosidase (9.61 μM), with an efficacy comparable to or even exceeding that of the standard inhibitors tacrine and acarbose. In silico studies, including molecular docking and DFT calculations, were conducted to better understand the interaction modes between the synthesized molecules and their target enzymes, as well as the reaction mechanism underlying their synthesis. Overall, the results of this study highlight the therapeutic potential of the synthesized compounds, particularly the cyclized derivatives."

Journal • Pain

Recognition of bioactive saponins from Polygonatum based on UPLC-QTOF/MS and molecular docking. (PubMed, Talanta) - "Molecular docking analyses revealed that Sibiricoside B (-8.051 kcal/mol) and Kingianoside H (-7.757 kcal/mol) exhibited significantly lower binding energies and shorter hydrogen bond distances compared to acarbose (-7.641 kcal/mol). These findings suggest that Sibiricoside B and Kingianoside H may serve as promising candidates for the development of natural inhibitors targeting type 2 diabetes mellitus, as well as potential active components in functional foods. Furthermore, all these findings also provide a basis for the valorization of Polygonatum species as natural resources, highlighting their potential to develop novel natural antioxidants and functional food ingredients."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Colon cancer cells evade drug action by enhancing drug metabolism. (PubMed, Oncogene) - "Finally, we identify two clinically accessible approaches to inhibiting drug glucuronidation: (i) blocking an initial HDAC1-mediated deacetylation step of trametinib with the FDA-approved drug vorinostat; (ii) reducing blood glucose by the alpha-glucosidase inhibitor acarbose. Overall, our observations demonstrate a key mechanism by which oncogenic RAS/WNT activity promotes increased drug clearance in CRC and provides a practical path towards abrogating drug resistance in CRC tumours."

Journal • Colon Cancer • Colorectal Cancer • Oncology • Solid Tumor • HDAC1 • KRAS • TP53

Facile indazole-endowed thiadiazole hybrid derivatives as antibacterial, anti-diabetic and thymidine phosphorylase inhibitors: An insight to experimental, in-vitro biological potential and computational approaches. (PubMed, Saudi Pharm J) - "Moreover, the inhibitory potential of the derivatives were compared with standard 7-Deazaxanthine (7DX) and acarbose...As a result of this study, indazole based thiadiazole hybrid derivatives have been designed, synthesized, and biologically evaluated as potent dual inhibitors of thymidine phosphorylase and α-glucosidase. These scaffolds display significant inhibitory potential, which were further analysed by docking and ADMET studies, emphasizing their potential as potent compounds for the development of new therapeutic agents that target these enzymes."

Journal • Preclinical

Adamantane Appended 1,2,3-Triazole Hybrids: Synthesis and α-Glucosidase Inhibition Studies Through Experimental and In Silico Approach. (PubMed, ChemMedChem) - "Compounds 6c (IC50 = 8.30 ± 0.33 μM) and 6b (IC50 = 14.0 ± 0.16 μM) demonstrated promising inhibition of α-glucosidase in comparison to reference used (Acarbose, IC50 = 13.50 ± 0.32 μM)...All compounds fit in the Lipinski rules of five, when ADME studies was carried out. This study paves the way for developing small molecule based α-glucosidase inhibitors as potential lead molecules using these frameworks."

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