oral BCL6 BTB inhibitor
promising in vitro safety + oral mouse/dog PK data
from virtual screen + SBDD
ACS Med. Chem. Lett., January 12, 2023
OICR, Toronto, CA (Janssen)
A protein-protein interaction inhibitor for a challenging-to-drug master transcription factor. OICR12694 is an oral protein-protein interaction inhibitor targeting the challenging-to-drug oncogenic transcription factor, B cell lymphoma 6 (BCL-6). As a master regulator of B cell differentiation in germinal centers and hence a common driver of B-cell malignancies like diffuse large B-cell lymphoma (DLBCL), BCL-6 inhibition could be beneficial for treatment of B-cell cancers and B-cell-mediated diseases. In 2015, JNJ signed a deal with Novera and the Ontario Institute for Cancer Research (OICR) to an exclusive worldwide license option for small molecules to treat blood cancers for up to $348M ($450M Canadian), in which the OICR will identify novel candidates from its drug discovery program and JNJ will be responsible for…