oral JNK2 kinase inhibitor
Ph. II candidate for pulmonary fibrosis
from HTS and SBDD
Journal of Medicinal Chemistry
Celgene (Bristol Myers Squibb), San Diego, CA
CC-90001 was nominated by reviewer Christian Kuttruff. CC-90001 is a JNK (c-Jun N-Terminal Kinase) inhibitor and a Phase II clinical candidate for idiopathic pulmonary fibrosis (NCT03142191). Christian says, “Preclinical evidence suggests that c-Jun N-terminal kinase (JNK) enzyme function is required for key steps in the pulmonary fibrotic process. Celgene had previously progressed tanzisertib (CC-930) into Phase 2 clinical trials for IPF but eventually stopped the compound because of the benefit/risk profile.” “With CC-930 displaying a strong JNK2 potency (5 nM over 133 nM for JNK1) and with increasing evidence that JNK1 is the more important isoform to target for fibrotic diseases, the backup program aimed to identify JNK inhibitors with an increased JNK1 bias relative to CC-930. A high throughput…