mocetinostat
Mocetinostat (MGCD0103) is a benzamide histone deacetylase inhibitor undergoing clinical trials for treatment of various cancers including follicular lymphoma, Hodgkin's lymphoma and acute myelogenous leukemia. — Wikipedia
Clinical trial activity
23 trials · 14 clinical orgs · 0 marketing orgs
Earliest trial started Apr 1, 2004 (NCT00323934)
Timeline
Indications
Studied for
- Breast Neoplasms · Phase 1
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Carcinoma, Squamous Cell · Phase 1
- Carcinoma, Transitional Cell · Phase 2
- Hodgkin Disease · Phase 2
- Leiomyosarcoma · Phase 2
- Leukemia · Phase 1
- Leukemia, Lymphocytic, Chronic, B-Cell · Phase 2
- Leukemia, Myeloid, Acute · Phase 2
- Lung Neoplasms · Phase 1
- Lymphoma · Phase 2
- Lymphoma, Follicular · Phase 1/Phase 2
- Lymphoma, Non-Hodgkin · Phase 2
- Melanoma · Phase 1
- Myelodysplastic Syndromes · Phase 2
- Neoplasms · Phase 1/Phase 2
- Prostatic Neoplasms · Phase 1
- Rhabdomyosarcoma · Phase 1
- Squamous Cell Carcinoma of Head and Neck · Phase 1
- Stomach Neoplasms · Phase 1
Mechanism of action
- Histone deacetylase 2INHIBITOR
HDAC2 inhibitor
Isotype-selective Class I (HDAC1, -2, -3, and -8) and IV (HDAC11) HDAC inhibitor.
- Histone deacetylase 3INHIBITOR
HDAC3 inhibitor
Isotype-selective Class I (HDAC1, -2, -3, and -8) and IV (HDAC11) HDAC inhibitor.
- Histone deacetylase 8INHIBITOR
HDAC8 inhibitor
Isotype-selective Class I (HDAC1, -2, -3, and -8) and IV (HDAC11) HDAC inhibitor.
- Histone deacetylase 11INHIBITOR
HDAC11 inhibitor
Isotype-selective Class I (HDAC1, -2, -3, and -8) and IV (HDAC11) HDAC inhibitor.
- Histone deacetylase 1INHIBITOR
HDAC1 inhibitor
Isotype-selective Class I (HDAC1, -2, -3, and -8) and IV (HDAC11) HDAC inhibitor.
Chemistry & pharmacology
SMILES
Nc1ccccc1NC(=O)c1ccc(CNc2nccc(-c3cccnc3)n2)cc1- Mol. weight
- 396.45 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaMocetinostat ↗
- ChEMBLCHEMBL272980 ↗
Also known as
- mg0103
- mg 0103
- mg-0103
- mg4230
- mg 4230
- mg-4230
- mg4915
- mg 4915
- mg-4915
- mg 5026
- mg-5026
- mg5206
- mgcd0103
- mgcd0103
- mgcd0103
- mgcd0103
- mgcd 0103
- mgcd-0103
- mgcd-0103
- mgcd-0103
- mocetinostat
- mocetinostat
- mocetinostat
- mocetinostat
- mocetinostat
- n-(2-aminophenyl)-4-((4-pyridin-3-ylpyrimidin-2-ylamino)methyl)benzamide
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04299113 | Phase 1 | Mar 29, 2020 | Mirati Therapeutics Inc., Phase One Foundation, University of California, Los Angeles |
| NCT03565406 | Phase 1 | Apr 25, 2018 | New York University |
| NCT03220477 | Phase 1 | Aug 4, 2017 | Astex Pharmaceuticals, Inc., Memorial Sloan-Kettering Cancer Center, Merck, Mirati Therapeutics Inc., Stand Up To Cancer, Van Andel Research Institute |
| NCT02993991 | Phase 1 | Jan 1, 2017 | AstraZeneca, Mirati Therapeutics Inc., University of Toronto |
| NCT02954991 | Phase 2 | Nov 1, 2016 | Mirati Therapeutics Inc. |
| NCT02805660 | Phase 1/Phase 2 (Phase 2) | May 1, 2016 | Mirati Therapeutics Inc. |
| NCT02303262 | Phase 2 | Sep 1, 2015 | Sarcoma Alliance for Research through Collaboration |
| NCT02429375 | Phase 1/Phase 2 (Phase 2) | Apr 1, 2015 | Cornell University, MethylGene Inc. |
| NCT02236195 | Phase 2 | Oct 1, 2014 | Mirati Therapeutics Inc. |
| NCT02282358 | Phase 1/Phase 2 (Phase 2) | Oct 1, 2014 | Cornell University, MethylGene Inc. |
| NCT02018926 | Phase 1/Phase 2 (Phase 2) | Dec 1, 2013 | Mirati Therapeutics Inc. |
| NCT00666497 | Phase 2 | Jun 1, 2008 | MethylGene Inc., Mirati Therapeutics Inc. |
| NCT00543582 | Phase 2 | Oct 1, 2007 | MethylGene Inc., Mirati Therapeutics Inc. |
| NCT00511576 | Phase 1 | Aug 1, 2007 | MethylGene Inc., Mirati Therapeutics Inc. |
| NCT00431873 | Phase 2 | Jan 1, 2007 | MethylGene Inc., Mirati Therapeutics Inc. |
| NCT00372437 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2006 | MethylGene Inc., Mirati Therapeutics Inc. |
| NCT00374296 | Phase 2 | Sep 1, 2006 | MethylGene Inc., Mirati Therapeutics Inc. |
| NCT00358982 | Phase 2 | Aug 1, 2006 | MethylGene Inc., Mirati Therapeutics Inc. |
| NCT00359086 | Phase 2 | Aug 1, 2006 | MethylGene Inc., Mirati Therapeutics Inc. |
| NCT00324220 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2006 | MethylGene Inc., Mirati Therapeutics Inc. |
Organizations
Research & Development (14)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Mirati Therapeutics Inc. | For profit | 19 | 16 | 2 | 2004 |
| MethylGene Inc. | For profit | 14 | 0 | 2 | 2004 |
| Cornell University | Academic/Hospital | 2 | 2 | 1 | 2014 |
| Astex Pharmaceuticals, Inc. | For profit | 1 | 0 | 1 | 2017 |
| AstraZeneca | For profit | 1 | 0 | 1 | 2017 |
| Memorial Sloan-Kettering Cancer Center | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Merck | For profit | 1 | 0 | 1 | 2017 |
| New York University | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Phase One Foundation | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Sarcoma Alliance for Research through Collaboration | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Stand Up To Cancer | Academic/Hospital | 1 | 0 | 1 | 2017 |
| University of California, Los Angeles | Academic/Hospital | 1 | 1 | 1 | 2020 |
| University of Toronto | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Van Andel Research Institute | Academic/Hospital | 1 | 0 | 1 | 2017 |