Pipeline
At 858 Therapeutics, we are advancing a portfolio of small molecule drugs that act on novel therapeutic targets in oncology. Our programs are focused on important nodes in cancer biology, including DNA damage repair, innate immunity, and RNA epigenetics. We leverage our deep expertise in structure-based drug discovery and translational research to develop differentiated drug candidates.
| Target | Indication | Discovery | Preclinical | IND-enabling | Clinical | Rights | ||||
|---|---|---|---|---|---|---|---|---|---|---|
| PARG | Solid tumors | Complete | Complete | In Progress | Incomplete |  | ||||
PARG is a glycohydrolase that removes poly-ADP-ribose (PAR) from proteins to release free ADP-ribose or PAR chains. PARG plays a pivotal role in the regulation of DNA repair mechanisms and cooperates with PARP to carry out the single-strand break (SSB) repair cycle. Pharmacological inhibition of PARG results in hyperPARylation, which leads to cell death in the context of cancer cells undergoing replication stress. We have discovered novel and potent small molecule inhibitors of PARG that demonstrate significant tumor growth inhibition in multiple solid tumor models, including enhanced efficacy in biomarker-defined settings. We expect to initiate a phase 1 trial for our PARG program in 2024. | ||||||||||
| QPCT/L | Neurodegeneration Atherosclerosis | Complete | Complete | In Progress | Incomplete | | ||||
| METTL3 | Solid tumors | Complete | Complete | In Progress | Incomplete | | ||||
| ADAR1 | Solid tumors | Complete | In Progress | Incomplete | Incomplete | | ||||
To learn more about partnering or licensing opportunities, please contact bd@8five8tx.com