Drug intelligence / Profile preview

SRX3177

Development stage
Preclinical
Lead developer
SignalRX Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

SRX3177 is a rationally designed, first-in-class small molecule that acts as a triple inhibitor targeting cyclin-dependent kinases 4 and 6 (CDK4/6), phosphoinositide 3-kinase (PI3K), and bromodomain-containing protein 4 (BRD4). It was developed to exploit synthetic lethality in cancer cells by simultaneously disrupting three critical oncogenic pathways. SRX3177 demonstrates potent cytotoxic activity across various tumor types, including breast cancer, mantle cell lymphoma, neuroblastoma, and hepatocellular carcinoma. The compound exhibits nanomolar inhibitory potency against its targets and shows marked selectivity for BRD4-BD1 over BRD4-BD2. Preclinical studies indicate that SRX3177 is efficacious in tumor models while being non-toxic to normal epithelial cells. Additionally, it has shown antiviral activity against the SARS-CoV-2 Omicron variant when used alone or in combination with other antivirals[1][2][3][4][5][6].

02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)BRD4 (Bromodomain-containing protein 4)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)

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