Therapy Areas: Inflammatory Diseases
Nimbus Therapeutics Identifies Potent, Selective HPK1 Inhibitor with Robust In Vivo Activity
15 May 2020 - - US-based biotechnology company Nimbus Therapeutics has identified an HPK1 inhibitor with highly potent and selective anti-tumor activity in preclinical models, the company said.

The company will present data at the AACR Virtual annual meeting II, June 22-24, 2020.

HPK1 (hematopoietic progenitor kinase 1) is a highly valued target in immuno-oncology due to its role as a regulator of both T cell and dendritic cell activity.

However, a key challenge for development of small molecules acting on HPK1 has been to achieve selectivity against other T cell kinases and MAP4K family members.

Nimbus utilised its unique structure-based drug discovery engine to identify multiple potent and selective small molecule inhibitors of HPK1.

One of these molecules, advanced to in vivo testing, has high selectivity against T cell-specific kinases and kinases in the MAP4K family and exhibits promising activation of human T cells and B cells.

In a mouse syngeneic tumor model, oral administration of the HPK1 inhibitor completely eliminated HPK1's phosphorylation of the T cell receptor, enhanced inflammatory cytokine production, and demonstrated robust tumor growth inhibition.

Nimbus Therapeutics designs medicines.

Utilising its powerful structure-based drug discovery engine, Nimbus designs potent and selective small molecule compounds targeting proteins that are known to be fundamental drivers of pathology in highly prevalent human diseases and which have proven difficult for other drug makers to tackle.

The company's LLC/subsidiary architecture enables diverse and synergistic partnerships to deliver breakthrough medicines. Nimbus is headquartered in Cambridge, Mass. 
Login
Username:

Password: