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INTH-454

Development stage: Preclinical
Lead developer: Inthera Bioscience
Modality: Small Molecules
Administration: Oral

Overview

INTH-454 is a first-in-class small molecule inhibitor developed by Inthera Bioscience that targets the Negative Elongation Factor (NELF) complex. NELF is a critical regulator of RNA polymerase II pausing, a key checkpoint in the transcription cycle that controls the expression of genes involved in cell growth and stress responses. By disrupting the NELF complex, INTH-454 aims to modulate transcriptional programs driven by oncogenic transcription factors, such as the androgen receptor and MYC, which are frequently dysregulated in solid tumors. The compound is currently undergoing IND-enabling studies for the treatment of castration-resistant prostate cancer (CRPC) and colorectal cancer (CRC).

Targets

Pol II (RNA polymerase II elongation factors)CREBBP (CREB-binding protein)

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