David Orchard-WebbMarch 18, 2025
Tag: AGIs , Type 2 diabetes , inhibitors
Alpha-glucosidase inhibitors (AGIs) are oral medicines used to manage type 2 diabetes. These medicines block the small intestine's alpha-glucosidase enzyme, slowing carbohydrate breakdown and glucose absorption. This process helps control postprandial blood glucose levels can be an effective diabetes care technique. Acarbose, miglitol, and voglibose are three commonly used AGIs.
The three primary AGIs (acarbose, miglitol, and voglibose) share a similar mode of action but differ in specificity, absorption, and potency.
The three medications block alpha-glucosidase enzymes in the small intestine's brush border, slowing the breakdown of complex carbs into absorbable monosaccharides such as glucose. They improve glycemic control in people with type 2 diabetes by delaying carbohydrate digestion and lowering postprandial glucose spikes.
Despite their shared main activity against alpha-glucosidase, there are some notable distinctions. Acarbose, a pseudo-tetrasaccharide, inhibits alpha-amylase and alpha-glucosidase enzymes, making it efficient against starch and disaccharides (Figueiredo-González, 2016). Acarbose, unlike miglitol, has limited systemic absorption and mostly affects the gastrointestinal tract. Miglitol, a monosaccharide-like molecule derived from 1-deoxynojirimycin, effectively inhibits alpha-glucosidase enzymes in the small intestine and throughout the body (NIDDK, 2012). Voglibose, a synthetic N-substituted valiolamine derivative, has the lowest systemic absorption and targets alpha-glucosidase enzymes in the small intestine. It inhibits sucrase and maltase more than alpha-amylase (Yasuda, 2003).
Acarbose inhibits both starch and disaccharides, while miglitol and voglibose target disaccharides more specifically. Acarbose and voglibose are poorly absorbed and operate mostly in the stomach, reducing systemic effects but raising the risk of gastrointestinal side effects such flatulence and bloating. Miglitol's systemic absorption may result in metabolic consequences beyond the gut. Clinical options include acarbose for broad-spectrum inhibition, voglibose for strong sucrase and maltase inhibition, and miglitol for further systemic action.
The global market for alpha-glucosidase inhibitors is constantly developing due to the rising prevalence of type 2 diabetes. The market was worth around USD 3.3 billion in 2023 and is predicted to increase at a Compound Annual Growth Rate (CAGR) of 3.2% from 2024 to 2032, reaching a value of USD 4.0 billion by 2030 (Faizullabhoy, 2024). Rising diabetes rates, increased understanding of diabetes treatment, and increased use of oral antidiabetic medicines have all contributed to this trend.
a. Increasing Prevalence of Type 2 Diabetes
The global increase in type 2 diabetes incidence is a major driver of the AGI market. Sedentary lifestyles, bad diets, and an aging population all contribute to this increase. The International Diabetes Federation (IDF) predicts that the number of individuals with diabetes will rise from 537 million in 2021 to 783 million by 2045 (IDF, 2025). As the prevalence of diabetes rises, effective treatments such as AGIs are necessary to regulate blood glucose levels.
b. Preference for Oral Antidiabetic Medications
Patients and healthcare professionals prefer oral drugs over injectable therapy for convenience of administration and increased compliance. Because AGIs are oral, they are more easily included into diabetes control plans.
c. Advancements in Diabetes Treatment Strategies
Diabetes treatment regimens have been optimized by ongoing research and development efforts. AGIs are increasingly used in combination therapy with other antidiabetic medications to provide complete glycemic control while lowering the risk of hypoglycemia.
a. By Drug Type
Acarbose
Acarbose is the most popular AGI, accounting for a sizable market share. In 2023, the global acarbose active pharmaceutical ingredient sales market size was valued at roughly USD 1.2 billion (Sharma, 2024). Its effectiveness in managing postprandial hyperglycemia makes it a top option among doctors.
Miglitol and Voglibose
Miglitol and voglibose are two more important AGIs with specialized therapeutic uses. Although they have a lesser market share, they provide options for individuals who cannot take acarbose or need individualized treatment.
b. By Distribution Channel
Hospital Pharmacies
Hospital pharmacies had a substantial market share in 2023. Their crucial role in inpatient diabetes management leads to their importance in the market.
Retail Pharmacies and Online Pharmacies
Retail pharmacies remain a significant distribution method due to their accessibility. However, internet pharmacies are gaining popularity by providing convenience and low price, hence increasing their market position.
a. North America
North America dominates the AGI market, owing to its high prevalence of type 2 diabetes and obesity. This position is further bolstered by advanced healthcare infrastructure and increased understanding of diabetes management. In 2023, the United States market alone accounted for a considerable portion of regional revenue.
b. Asia-Pacific
The Asia-Pacific region is expected to witness substantial growth in the AGI market. Factors such as increasing urbanization, changing dietary patterns, and a rising diabetic population drive this trend. Moreover, growing healthcare investments and initiatives aimed at managing chronic diseases effectively contribute to market expansion.
c. Europe
Europe holds a significant share of the AGI market, supported by well-established healthcare systems and a focus on preventive care. The region’s proactive approach to diabetes management and patient education enhances the adoption of AGIs.
a. Gastrointestinal Side Effects
AGIs are associated with gastrointestinal side effects such as flatulence, diarrhea, and abdominal discomfort (Arun, 2024). These adverse effects can lead to poor patient compliance and limit the widespread use of these medications.
b. Availability of Alternative Therapies
Alternative antidiabetic treatments, particularly newer types such as DPP-4 inhibitors, GLP-1 receptor agonists, and SGLT2 inhibitors, pose a challenge to AGIs (ADA, n.d.). These alternatives frequently have equivalent or higher effectiveness with a better side effect profile, altering prescription habits.
Despite limitations, alpha-glucosidase inhibitors (AGIs) are nevertheless used for controlling type 2 diabetes due to their significant advantages.
Reduction of postprandial hyperglycemia: AGIs like acarbose and miglitol inhibit carbohydrate digestion in the small intestine, resulting in a slower and lower increase in blood glucose levels following meals. This technique substantially lowers postprandial hyperglycemia, which aids overall glycemic management.
Low Risk of Hypoglycemia: Unlike other diabetic drugs, AGIs seldom produce low blood sugar levels (hypoglycemia) when administered alone. This safety profile makes them an excellent choice, especially for those at risk of hypoglycemia.
Weight Neutrality: AGIs have a neutral effect on body weight, which means they don't encourage weight growth or decrease. This feature is useful for people who are concerned about weight fluctuations caused by diabetes therapy.
Combination Therapy: AGIs can be efficiently coupled with other antidiabetic medications to improve overall blood glucose control without considerably raising the risk of side effects.
While AGIs can induce gastrointestinal adverse effects such as flatulence and diarrhea, they are frequently manageable by beginning with a low dosage and gradually increasing it. The advantages of AGIs, notably in terms of controlling postprandial blood glucose levels without inducing hypoglycemia or weight gain, justify their ongoing use in specific therapeutic circumstances (Editorial, 2017).
c. Regulatory Challenges
Stringent regulatory procedures for medication approval and post-marketing surveillance can hinder market entrance expansion. Compliance with different rules across geographies needs a significant investment in regulatory affairs.
Despite these limitations, the AGI market is expected to develop steadily. Current research attempts to increase the safety and efficacy of AGIs, potentially broadening their medicinal uses. For example, producing formulations with less gastrointestinal side effects may improve patient adherence and increase the patient population.
Integrating AGIs into personalized medicine can improve treatment results by taking into account patient genetic and phenotypic variability. Collaborations between pharmaceutical corporations and academic institutes are expected to spur innovation in this industry.
ADA. (n.d.). Oral & Injectable medications for type 2 diabetes. What Are My Options for Type 2 Diabetes Medications? https://diabetes.org/health-wellness/medication/oral-other-injectable-diabetes-medications
Arun, N., & Vettath, R. E. (2024). Adverse events due to oral hypoglycemic drugs. In G. Abraham, J. Kesavadev, P. Govindan, N. Arun, & S. Teckchandani (Eds.), Management of diabetic complications: Calling for a team approach (pp. 285–300). Springer Nature Singapore. https://doi.org/10.1007/978-981-97-6406-8_21
Editorial Team. (2017, April). Alpha-glucosidase inhibitors for type 2 diabetes. Type2Diabetes.com. https://type2diabetes.com/treatment/medications/alpha-glucosidase
Faizullabhoy, M., & Wani, G. (2024, August). Alpha-glucosidase inhibitors market size report, 2032. Gminsights.com. https://www.gminsights.com/industry-analysis/alpha-glucosidase-inhibitors-market
Figueiredo-González, M., Grosso, C., Valentão, P., & Andrade, P. B. (2016). α-Glucosidase and α-amylase inhibitors from Myrcia spp.: A stronger alternative to hiacarbose? Journal of Pharmaceutical and Biomedical Analysis, 118, 322–327. https://doi.org/10.1016/j.jpba.2015.10.042
IDF. (2025, February 14). Facts & figures. Idf.org. https://idf.org/about-diabetes/diabetes-facts-figures/
NIDDK - National Institute of Diabetes and Digestive and Kidney Diseases. (2012). Alpha glucosidase inhibitors. In LiverTox: Clinical and research information on drug-induced liver injury. Bethesda, MD: National Institute of Diabetes and Digestive and Kidney Diseases. https://www.ncbi.nlm.nih.gov/books/NBK548416
Sharma, R. (2024, September 22). Acarbose API sales market research report 2032. Dataintelo.com. https://dataintelo.com/report/global-acarbose-api-sales-market
Yasuda, K., Shimowada, K., Uno, M., Odaka, H., Adachi, T., Shihara, N., Suzuki, N., Tamon, A., Nagashima, K., Hosokawa, M., Tsuda, K., & Seino, Y. (2003). Long-term therapeutic effects of voglibose, a potent intestinal alpha-glucosidase inhibitor, in spontaneous diabetic GK rats. Diabetes Research and Clinical Practice, 59(2), 113–122.
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