Bromodomain inhibitor against cancer
Acute leukemia, breast cancer, glioblastoma, lung cancer, lymphoma, melanoma, mesothelioma, neuroblastoma, ovarian cancer, pancreatic cancer, prostate cancer
Dual inhibitor of BET and CBP/P300
Bromodomains (BRDs) are key modulators of epigenetic control – this control is abnormal in some cancers. BRD4 inhibitors can treat cancer by restoring epigenetic control.
Much support has been accumulating for BRDs as cancer targets. NEO2734 demonstrates a broad spectrum of in-vitro activity against a variety of cancer types and will be explored in priority indications which will be chosen based on data from our extensive pre-clinical collaborations.
Synergistically inhibiting both BRD4 and CBP/P300 may explain the observed enhanced efficacy as compared to other compounds in development.
Safety has been demonstrated in rodents, dogs and non-human primates in several non-GLP studies. In vitro and in vivo studies have shown at least 10-fold better cell membrane penetration and anti-tumor potency than other inhibitors in development while maintaining a good safety profile.
Compounds were identified from 4 different chemical series with distinct scaffolds. Due to its superior in-vivo efficacy NEO2734 was the selected lead candidate.