Drug intelligence / Profile preview

mivebresib + navitoclax

Development stage
Unknown
Lead developer
AbbVie
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination therapy** consisting of two small molecule inhibitors: **mivebresib**, a potent inhibitor of bromodomain and extra-terminal motif (BET) proteins, and **navitoclax**, an inhibitor of the BCL-2 family of anti-apoptotic proteins. **Mivebresib** functions as an epigenetic modulator by inhibiting BET proteins, leading to downregulation of genes such as MCL1 and induction of apoptosis in cancer cells, particularly in hematological malignancies. **Navitoclax** targets and inhibits multiple BCL-2 family proteins (BCL-2, BCL-xL, BCL-w), promoting apoptosis by disrupting cancer cell survival mechanisms. Preclinical and early clinical studies suggest synergy between BET inhibition (mivebresib) and BCL-2 inhibition (navitoclax) in acute myeloid leukemia (AML) and myelofibrosis, providing a rationale for the combination in these indications. The combination is under clinical investigation, primarily for hematologic cancers[1][5].

02

Targets

Bcl-w (B-cell lymphoma 2-like 2)BRD3 (Bromodomain-containing protein 3)BRDT (Bromodomain testis-specific protein)BRD4 (Bromodomain-containing protein 4)BCL2L1 (B-cell lymphoma-extra large protein)BRD2 (Bromodomain-containing protein 2)

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