| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H20N6O |
| Molecular Weight | 396.4445 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=CC=CC=C1NC(=O)C2=CC=C(CNC3=NC(=CC=N3)C4=CC=CN=C4)C=C2
InChI
InChIKey=HRNLUBSXIHFDHP-UHFFFAOYSA-N
InChI=1S/C23H20N6O/c24-19-5-1-2-6-21(19)28-22(30)17-9-7-16(8-10-17)14-27-23-26-13-11-20(29-23)18-4-3-12-25-15-18/h1-13,15H,14,24H2,(H,28,30)(H,26,27,29)
Mocetinostat is an rationally designed, orally available, Class 1-selective, small molecule, 2-aminobenzamide HDAC inhibitor with potential antineoplastic activity. Mocetinostat binds to and inhibits Class 1 isoforms of HDAC, specifically HDAC 1, 2 and 3, which may result in epigenetic changes in tumor cells and so tumor cell death; although the exact mechanism has yet to be defined, tumor cell death may occur through the induction of apoptosis, differentiation, cell cycle arrest, inhibition of DNA repair, upregulation of tumor suppressors, down regulation of growth factors, oxidative stress, and autophagy, among others. It is undergoing clinical trials for treatment of various cancers including bladder cancer, diffuse large B cell lymphoma, follicular lymphoma, myelodysplastic syndromes, non-small cell lung cancer. Fatigue, weight loss or anorexia were most common treatment-related adverse events.
Originator
Approval Year
Doses
AEs
Sourcing
PubMed
Sample Use Guides
Starting dose of 85 mg three times per week for four weeks. Dose escalation to 110 mg three times per week was permitted beginning with cycle 2 in patients who failed to achieve a complete response.
Route of Administration:
Oral
ACTIVE MOIETY
SALT/SOLVATE (PARENT)
