Drug intelligence / Profile preview

H182

Development stage
Preclinical
Lead developer
Cedars-Sinai
Modality
Small Molecules
01

Overview

H182 is a small molecule inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3) currently in preclinical development for the treatment of pancreatic adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC). Developed by researchers at Cedars-Sinai Medical Center, H182 targets the STAT3-proinflammatory axis by suppressing the tyrosine phosphorylation of STAT3 (pYSTAT3). In experimental models, treatment with H182 has been shown to shift the tumor secretome, reduce the expression of genes associated with immune evasion and angiogenesis, and induce apoptosis and cell cycle arrest in cancer cells. Furthermore, H182 has demonstrated efficacy in preventing the progression of pancreatic intraepithelial neoplasia (PanIN) lesions and inhibiting the growth of PDAC xenografts in vivo.

02

Targets

STAT3 (Signal Transducer and Activator of Transcription 3)STAT5A (STAT5)STAT1 (Signal transducer and activator of transcription 1-alpha/beta)

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