tosedostat
Small moleculeexperimental
Clinical trial activity
11 trials · 31 clinical orgs · 0 marketing orgs
Phase 1
7
Phase 2
8
Phase 3
0
Phase 4
0
Earliest trial started Oct 1, 2004 (NCT00692354)
Timeline
Indications
Mechanism of action
- AminopeptidaseINHIBITOR
Aminopeptidase inhibitor
Inhibition of the aminopeptidases disrupts normal protein turnover leading to peptide accumulation and decrease in free amino acids which leads to a stress response, amino acid depravation response, including activation of stress-related pathways such NF-¿B and pro-apoptotic regulators.
- Aminopeptidase N (ANPEP) ↗
- Puromycin-sensitive aminopeptidase (NPEPPS) ↗
- Aminopeptidase B (RNPEP) ↗
- Methionine aminopeptidase 1 (METAP1) ↗
- Leucyl-cystinyl aminopeptidase (LNPEP) ↗
- Aspartyl aminopeptidase (DNPEP) ↗
- Glutamyl aminopeptidase (ENPEP) ↗
- Xaa-Pro aminopeptidase 1 (XPNPEP1) ↗
- Cytosol aminopeptidase (LAP3) ↗
- Methionine aminopeptidase 2 (METAP2) ↗
- Xaa-Pro aminopeptidase 2 (XPNPEP2) ↗
- Endoplasmic reticulum aminopeptidase 2 (ERAP2) ↗
- Endoplasmic reticulum aminopeptidase 1 (ERAP1) ↗
- Aminopeptidase Q (LVRN) ↗
- Aminopeptidase O (AOPEP) ↗
- Methionine aminopeptidase 1D, mitochondrial (METAP1D) ↗
- Probable aminopeptidase NPEPL1 (NPEPL1) ↗
- Aminopeptidase RNPEPL1 (RNPEPL1) ↗
- Xaa-Pro aminopeptidase 3 (XPNPEP3) ↗
- Aminopeptidase N
- Xaa-Pro aminopeptidase 1
- Methionine aminopeptidase 1
- Methionine aminopeptidase 2
- Aminopeptidase B
- Cystinyl aminopeptidase
- Xaa-Pro aminopeptidase 2
- Aspartyl aminopeptidase
- Puromycin-sensitive aminopeptidase
- Aminopeptidase A
- Leucine aminopeptidase
- Endoplasmic reticulum aminopeptidase 2
- Endoplasmic reticulum aminopeptidase 1
Chemistry & pharmacology
Loading structure…
SMILES
CC(C)C[C@@H](C(=O)N[C@H](C(=O)OC1CCCC1)c1ccccc1)[C@H](O)C(=O)NO- Mol. weight
- 406.48 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL2103847 ↗
Also known as
- 2-(2-(hydroxy(hydroxycarbamoyl)methyl)-4-methylpentanoylamino)-2-phenylethanoic acid cyclopentyl ester
- chr2797
- chr 2797
- chr-2797
- chr-2797
- chr-2797
- chr-2797
- tosedostat
- tosedostat
- tosedostat
- tosedostat
- tosedostat
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02352831 | Phase 1/Phase 2 (Phase 2) | Aug 31, 2015 | Washington University in St. Louis |
| NCT02452346 | Phase 2 | Mar 20, 2015 | Cornell University, CTI BioPharma |
| NCT01636609 | Phase 1/Phase 2 (Phase 2) | Nov 1, 2012 | CTI BioPharma, University of Texas at Houston |
| NCT01638442 | Phase 1 | Jun 1, 2012 | Chroma Therapeutics, Covance, CTI BioPharma |
| NCT01567059 | Phase 2 | May 1, 2012 | National Cancer Institute (NCI), University of Washington |
| NCT01180426 | Phase 2 | Jun 1, 2010 | Chroma Therapeutics |
| NCT00780598 | Phase 2 | Oct 1, 2009 | Ben Gurion University, Chroma Therapeutics, Cornell University, Duke University, Emory University, Erasmus University Rotterdam, Froedtert Memorial Lutheran Hospital, Georgetown University, IQVIA, Monter Cancer Center, Rutgers University, University of California, Los Angeles, University of Chicago, University of Melbourne, University of Michigan, University of Rochester, University of Texas at Houston, University of Toronto, Washington University in St. Louis, Yeshiva University |
| NCT00522938 | Phase 1/Phase 2 (Phase 2) | Dec 1, 2007 | Chroma Therapeutics |
| NCT00737555 | Phase 1 | Aug 1, 2006 | Chroma Therapeutics, Erasmus University Rotterdam, Radboud University |
| NCT00689000 | Phase 1/Phase 2 (Phase 2) | May 1, 2006 | Cardiff University, Chroma Therapeutics, Erasmus University Rotterdam, Free University of Amsterdam, Katholieke Universiteit Leuven, Royal Marsden Hospital NHS Trust, ZNA Antwerpen |
| NCT00692354 | Phase 1 | Oct 1, 2004 | Chroma Therapeutics, University of London |
Showing 11 of 11 trials
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Organizations
Research & Development (31)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Chroma Therapeutics | For profit | 7 | 6 | 2 | 2004 |
| CTI BioPharma | For profit | 3 | 1 | 2 | 2012 |
| Erasmus University Rotterdam | Academic/Hospital | 3 | 0 | 2 | 2006 |
| Cornell University | Academic/Hospital | 2 | 1 | 1 | 2009 |
| University of Texas at Houston | Academic/Hospital | 2 | 1 | 1 | 2009 |
| Washington University in St. Louis | Academic/Hospital | 2 | 1 | 1 | 2009 |
| Ben Gurion University | Academic/Hospital | 1 | 0 | 1 | 2009 |
| Cardiff University | Academic/Hospital | 1 | 0 | 1 | 2006 |
| Covance | For profit | 1 | 0 | 1 | 2012 |
| Duke University | Academic/Hospital | 1 | 0 | 1 | 2009 |
| Emory University | Academic/Hospital | 1 | 0 | 1 | 2009 |
| Free University of Amsterdam | Academic/Hospital | 1 | 0 | 1 | 2006 |
| Froedtert Memorial Lutheran Hospital | Academic/Hospital | 1 | 0 | 1 | 2009 |
| Georgetown University | Academic/Hospital | 1 | 0 | 1 | 2009 |
| IQVIA | For profit | 1 | 0 | 1 | 2009 |
| Katholieke Universiteit Leuven | Academic/Hospital | 1 | 0 | 1 | 2006 |
| Monter Cancer Center | Academic/Hospital | 1 | 0 | 1 | 2009 |
| National Cancer Institute (NCI) | Government | 1 | 0 | 1 | 2012 |
| Radboud University | Academic/Hospital | 1 | 0 | 1 | 2006 |
| Royal Marsden Hospital NHS Trust | Academic/Hospital | 1 | 0 | 1 | 2006 |
31 organizations
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