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Tapotoclax
- Development stage
- Discontinued
- Lead developer
- Amgen
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Tapotoclax (AMG-176) is a first-in-class, potent, selective, and orally bioavailable small molecule inhibitor of the Myeloid Cell Leukemia-1 (MCL-1) protein. MCL-1 is an anti-apoptotic protein belonging to the Bcl-2 family, frequently overexpressed in various hematologic malignancies, contributing to tumor cell survival and resistance to therapies. Tapotoclax binds to and inhibits MCL-1, disrupting its interaction with pro-apoptotic proteins like BIM (BCL2L11) and BAK, thereby inducing apoptosis in MCL-1-dependent cancer cells. It has shown potential pro-apoptotic and antineoplastic activities.
- Other names
- TapotoclaxumMCL-1 inhibitor AMG 176MCL1 inhibitor AMG 176MCL 1 inhibitor AMG 176
02
Targets
MCL1 (Myeloid cell leukemia sequence 1)
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