Drug intelligence / Profile preview

mocetinostat + docetaxel

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Mocetinostat (MGCD0103) is an orally available, isotype-selective benzamide inhibitor of histone deacetylases (HDACs), primarily targeting HDAC1, HDAC2, HDAC3 (class I), and HDAC11 (class IV). It modulates aberrant gene expression and restores normal growth control in malignancies by increasing histone acetylation, leading to cell cycle arrest and apoptosis. Mocetinostat has been investigated in clinical trials for various cancers including follicular lymphoma, Hodgkin's lymphoma, acute myeloid leukemia, and solid tumors[4][6][8]. Docetaxel is a semisynthetic taxane antineoplastic agent that promotes microtubule assembly while inhibiting their depolymerization. This disrupts mitotic spindle function during cell division, resulting in inhibition of mitosis and induction of apoptosis. Docetaxel is approved for the treatment of several cancers including breast cancer, non-small cell lung cancer, prostate cancer, gastric adenocarcinoma, and head/neck cancer[1][2][3]. The combination of mocetinostat (MGCD0103) with docetaxel has been explored in clinical studies as a potential therapy for advanced solid tumors due to their complementary mechanisms—epigenetic modulation by mocetinostat and cytotoxicity via microtubule stabilization by docetaxel.

Brand names
TaxotereDocefrezDocivyx
Other names
MGCD0103 + docetaxelmocetinostat + docetaxel
02

Targets

HDAC11 (Histone Deacetylase 11)HDAC1 (Histone Deacetylase 1)TUBB (Tubulin (alpha and beta subunits))

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