RO-6870810

RO-6870810 is a novel small molecule inhibitor of the bromodomain and extra-terminal motif (BET) family of proteins. It is a thienodiazepine derivative structurally related to (+)-JQ1 and was optimized for improved chemical and biological properties. The drug binds non-covalently to the acetylated lysine recognition motifs in BET proteins (including Bromodomain-containing protein 2, Bromodomain-containing protein 3, Bromodomain-containing protein 4, and Bromodomain testis-specific protein), preventing their interaction with acetylated histones and transcription factors. This disrupts chromatin remodeling and gene expression—particularly inhibiting oncogenic drivers such as MYC—and slows proliferation in susceptible tumors[1][3][6]. RO-6870810 has been investigated primarily for hematologic malignancies such as acute myeloid leukemia (AML), myelodysplastic syndrome (MDS), diffuse large B-cell lymphoma (DLBCL), multiple myeloma, as well as solid tumors including NUT carcinoma, ovarian cancer, and triple-negative breast cancer[2][4][7]. Clinical trials have evaluated its use both as monotherapy and in combination with agents like daratumumab or checkpoint inhibitors[4][7]. Development originated at Tensha Therapeutics before acquisition by Roche.

Other names

(S)-JQ-35(S)-JQ35