Drug intelligence / Profile preview

ranolazine + glimepiride

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

Ranolazine + glimepiride is a fixed-dose combination regimen comprising ranolazine, a first-in-class antianginal agent that inhibits cardiac late sodium current, and glimepiride, a sulfonylurea antidiabetic oral agent that stimulates insulin release from pancreatic beta cells. This specific combination is not available as a single co-formulated pharmaceutical product but is studied and used as a co-administration regimen for the treatment of **type 2 diabetes mellitus** in patients who require additional glycemic control beyond glimepiride monotherapy. Ranolazine has shown HbA1c-lowering properties via inhibition of sodium channels (notably Na_v_1.3 isoform) in pancreatic alpha cells, leading to reduced glucagon secretion and improved glycemic parameters. Glimepiride acts primarily by stimulating insulin release. The combination has demonstrated superiority over glimepiride monotherapy by reducing HbA1c by approximately 0.5% at 24 weeks and doubling the rate of patients achieving HbA1c < 7% without a significant increase in hypoglycemia[1][2][3][4]. Ranolazine is not currently approved for diabetes but studied for antihyperglycemic effects in combination with glimepiride.

02

Targets

KCNJ11 (Atp-sensitive inward rectifier potassium channel 11)SCN5A (Sodium channel protein type 5 subunit alpha)

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