Drug intelligence / Profile preview

repaglinide + isophane human insulin

Development stage
Unknown
Lead developer
Novo Nordisk
Modality
Recombinant Proteins and Enzymes, Small Molecules
Administration
Oral, Subcutaneous
01

Overview

Repaglinide + isophane human insulin is a combination therapy used for the management of type 2 diabetes mellitus, aiming to improve glycemic control in patients inadequately controlled by oral agents alone. **Repaglinide** is an oral antihyperglycemic small molecule that acts as a rapid-acting insulin secretagogue by stimulating endogenous insulin release from pancreatic β-cells via inhibition of ATP-sensitive potassium channels, leading to depolarization and subsequent calcium influx and insulin secretion. Its action is glucose-dependent and primarily targets postprandial glucose elevations[2]. **Isophane human insulin**, also known as Neutral Protamine Hagedorn (NPH) insulin, is an intermediate-acting recombinant human insulin formulation that lowers blood glucose by facilitating cellular glucose uptake and inhibiting hepatic glucose production. When used in combination, repaglinide handles meal-time glucose spikes while NPH insulin maintains basal glycemic control, offering better postprandial and overall blood glucose management than conventional basal insulin regimens in clinical studies[3][1]. This combination is typically indicated in adults with type 2 diabetes after inadequate response to oral antidiabetic drugs. The combination should not be confused with fixed mixtures (e.g., biphasic insulin); repaglinide is given orally before meals and NPH insulin is administered subcutaneously, often at bedtime. Repaglinide is developed and manufactured by Novo Nordisk, while various pharmaceutical companies manufacture isophane human insulin. Note: Repaglinide is not specifically indicated by regulatory agencies for concomitant use with NPH insulin due to increased risk of myocardial ischemia seen in trials, and combinations should be prescribed carefully[2].

02

Targets

INSR (Insulin receptor)KATP channel (ATP-sensitive potassium channel)

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