Uses
ABBV 075-d5 is a deuterium labelled ABBV 075 (A215280), which is used for selective inhibition of the BD2 bromodomain of bromodomain and extra-??terminal proteins in prostate cancer.
Biological Activity
Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. Binds to the bromodomain of BRD2/4/T with similar affinity (Ki values between 1-2.2 nM) with high selectivity. Low potency against BRD3 (Ki=12.2 nM) and moderate activity against CREBBP (Ki=87 μM). It can effectively trigger apoptosis in a variety of tumor cells.
in vitro
ABBV-075 has potent and potent single-agent activity in a variety of cancer cell lines (from solid tumors, leukemias and lymphomas) in cell viability assays. It is capable of disrupting cell cycle control, leading to G1 arrest, further senescence, inhibition of tumor formation, induction of apoptosis, and possibly targeting the tumor microenvironment to further provide better efficacy.
in vivo
In mouse models laterally xenografted with non-small cell and small cell lung cancer, pancreatic cancer, breast cancer, prostate cancer, head and neck cancer, multiple lymphomas, diffuse giant B-cell lymphoma, and leukemia, ABBV -075 has equal or better efficacy than other standard care agents.
target
| Target | Value |
| BRD2 |
| BRD4 |
| BRD-T |
