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Drug intelligence / Profile preview
murizatoclax
- Development stage
- Discontinued
- Lead developer
- Amgen
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Murizatoclax (AMG 397) is a potent, selective, and orally active small molecule inhibitor of myeloid cell leukemia-1 (MCL-1), an anti-apoptotic protein in the B-cell lymphoma 2 (Bcl-2) family. By binding to the BH3-binding groove of MCL-1 with high affinity (\(K_i\) = 15 pM), murizatoclax prevents MCL-1 from inactivating pro-apoptotic proteins, thereby promoting apoptosis in cancer cells that overexpress MCL-1. This mechanism targets tumor cell survival and has shown antineoplastic activity in preclinical models. Murizatoclax was developed primarily for hematological malignancies such as acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma (MM). The drug reached phase I clinical trials but development was placed on hold by regulatory authorities[1][2][4][5][6][8].
- Other names
- murizatoclax2245848-05-7
02
Targets
MCL1 (Myeloid cell leukemia sequence 1)
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