Drug intelligence / Profile preview

BAY 1143269 + docetaxel

Development stage
Discontinued
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

BAY 1143269 + docetaxel is an experimental combination therapy consisting of **BAY 1143269**, an orally administered small molecule inhibitor of mitogen-activated protein kinase interacting serine/threonine-protein kinase 1 (MKNK1), together with **docetaxel**, an intravenous taxane chemotherapy agent. BAY 1143269 binds to and inhibits MKNK1, thereby blocking phosphorylation of the eukaryotic translation initiation factor 4E (eIF4E), which suppresses oncogenic protein synthesis, angiogenesis, and induces apoptosis in tumor cells. Docetaxel, as a taxane, stabilizes microtubules, disrupts mitotic spindle function, causes mitotic arrest, and induces cell death. The combination was investigated in Phase 1 clinical studies for advanced solid tumors refractory to standard therapies, aiming to synergistically enhance anti-tumor activity by targeting both translation regulation (via BAY 1143269) and cell division (via docetaxel)[3][5].

02

Targets

MKNK1 (Mitogen‑activated protein kinase‑interacting serine/threonine-protein kinase 1)TUBB (Tubulin (alpha and beta subunits))

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