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Tapotoclax

Development stage: Unknown
Lead developer: Amgen
Modality: Small Molecules
Administration: Intravenous, Oral

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

Targets

MCL1 (Myeloid cell leukemia sequence 1)

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