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ZEN-3694 is a BET inhibitor from Zenith Epigenetics being tested in NUT carcinoma, where the cancer's driving fusion is itself a BET protein, and in prostate and breast cancers.
BET inhibitors block the bromodomain proteins that switch on growth genes such as MYC. NUT carcinoma is the clearest use: its BRD4-NUT fusion is a BET protein, and inhibitors make the cells differentiate in the laboratory, with objective but short-lived responses in early trials of molibresib and birabresib. ZEN-3694 is the BET inhibitor now carrying that idea forward in National Cancer Institute trials with platinum chemotherapy and with abemaciclib in NUT carcinoma, and it has been studied with enzalutamide in castration-resistant prostate cancer and with talazoparib in triple-negative breast cancer. Thrombocytopenia and fatigue are the class side effects.
Binds the bromodomains of BRD2, BRD3 and BRD4 so they cannot read acetylated histones; in NUT carcinoma this displaces the BRD4-NUT fusion from chromatin and lets the cells differentiate, and in other cancers it lowers MYC and androgen receptor signalling. Connects to BRD4.
1.ZEN-3694 slips into a pocket on BRD4.
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
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Query for this drug: (TITLE:"ZEN-3694" OR ABSTRACT:"ZEN-3694" OR TITLE:"ZEN003694" OR ABSTRACT:"ZEN003694" OR TITLE:"Zenith BET inhibitor" OR ABSTRACT:"Zenith BET inhibitor") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about ZEN-3694, not a curated reading list.
Shares NUT carcinoma (midline carcinoma with NUTM1 rearrangement) and the tag owner-request.
Shares Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET) and the tag owner-request.
Shares Prostate cancer and the tag owner-request.
Shares Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET), Prostate cancer.
Shares Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET), Prostate cancer.
Shares Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET), Prostate cancer.
Shares Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET), Prostate cancer.
Shares Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET), Prostate cancer.