An updated patent review of BRD4 degraders.
Zonghui MaCun ZhangAndrew A BolingerJia ZhouPublished in: Expert opinion on therapeutic patents (2024)
BRD4 degraders exhibit superior efficacy and selectivity to BRD4 inhibitors, given their unique mechanism of protein degradation instead of protein inhibition. Excitingly, RNK05047 is now in phase I/II clinical trials, indicating that selective BRD4 protein degradation may offer a viable therapeutic strategy, particularly for cancer. Targeting BRD4 with small molecule BRD4 degraders provides a promising approach with the potential to overcome therapeutic resistance for treating various BRD4-associated diseases.