Drug intelligence / Profile preview

HE3286 + metformin

Development stage
Unknown
Lead developer
BioVie
Modality
Small Molecules
Administration
Oral
01

Overview

HE3286 + metformin is a combination of two small molecule drugs. HE3286 (also known as NE3107 or bezisterim) is a synthetic derivative of androstenetriol and an orally active anti-inflammatory agent with insulin-sensitizing properties. It acts primarily by modulating inflammatory pathways through regulation of nuclear factor NF-kappa-B (NF-κB), increasing regulatory T cell production, and binding to ERK1/2, low-density lipoprotein receptor-related protein 1 (LRP1), and sirtuin 2 (SIRT2). Unlike glucocorticoids or sex steroids, it does not act via steroid hormone receptors and is not immunosuppressive[1][3][4][5]. Metformin is a well-established oral antihyperglycemic agent in the biguanide class that decreases hepatic glucose production and improves insulin sensitivity. The combination may be investigated for synergistic effects in metabolic diseases such as type 2 diabetes due to their complementary mechanisms—metformin targeting glucose metabolism and HE3286 targeting inflammation-mediated insulin resistance[1][5].

Other names
17α-Ethynyl-5-androstene-3β,7β,17β-triolbezisterim
02

Targets

NF-κBAMPK (Adenosine monophosphate–activated protein kinase)GSEC (Gamma-Secretase Complex)SIRT2 (NAD-dependent protein deacetylase sirtuin-2)LRP1 (Prolow-density lipoprotein receptor-related protein 1)MAPK3 (Mitogen-activated protein kinase 1)

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