Drug intelligence / Profile preview

mevociclib

Development stage
Discontinued
Lead developer
Syros Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous
01

Overview

Mevociclib (SY-1365) is a selective, covalent inhibitor of cyclin-dependent kinase 7 (CDK7), developed as an antineoplastic agent. CDK7 is a serine/threonine kinase that plays a critical role in cell cycle regulation and transcriptional control by activating other cyclin-dependent kinases and regulating gene expression. Inhibition of CDK7 by mevociclib disrupts these processes, leading to decreased proliferation and increased apoptosis in cancer cells—particularly those dependent on high transcriptional activity for survival. Preclinical studies demonstrated potent anti-tumor effects across multiple solid tumor types and hematologic malignancies at nanomolar concentrations. Mevociclib entered clinical trials for advanced solid tumors, including ovarian and breast cancers; it was also studied in combination with carboplatin or fulvestrant. Despite initial signs of activity and tolerability in early-phase trials, development has been discontinued[2][3][6][7][8].

Other names
mevociclib
02

Targets

CDK7

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