A new alpha‐glucosidase inhibitor (Bay‐m‐1099) reduces insulin requirements with meals in insulin‐dependent diabetes mellitus

Retardation of meal carbohydrate absorption by inhibition of starch degradation improves glucose tolerance in normal and diabetic humans. To determine the effects of Bay‐m‐1099, a new α‐glucosidase inhibitor, on insulin requirements and prandial glucose tolerance in patients with insulin‐dependent diabetes mellitus (IDDM), plasma glucose, triglyceride, and free insulin concentrations were measured after ingestion of a standard breakfast, lunch, and dinner in nine patients with IDDM in a single‐blind, randomized, crossover design. A 20% reduction in insulin was given 30 minutes before the meals when the subjects received Bay‐m‐1099 (50 mg). This resulted in the AUC for plasma insulin to be significantly less with Bay‐m‐1099 (AUC, 8.2 ± 1.3 vs. 12.8 ± 1.6 µU/ml/min with placebo; P < 0.01). Despite this reduction in plasma insulin levels, postprandial plasma glucose concentrations were reduced for the breakfast (73 ± 15 vs. 112 ± 14 mg/dl/min with placebo; P < 0.01) and dinner (23 ± 8 vs. 4 ± 1 mg/dl/min with placebo; P < 0.05) meal with Bay‐m‐1099. Bay‐m‐1099 did not affect postprandial plasma triglycerides and was well tolerated, the major side effect being flatulence (4/9) and mild diarrhea (4/9). We conclude that inhibition of intestinal a‐glucosidases by Bay‐m‐1099 in IDDM reduces meal insulin requirements by at least 20% and that such an agent could be useful in the management of diabetes mellitus by reducing hyperinsulinemia. Clinical Pharmacology and Therapeutics (1987) 42, 455–458; doi: 10.1038/clpt.1987.177