apaziquone
Small moleculeexperimental
Apaziquone is an indolequinone that is a bioreductive prodrug similar to the older chemotherapeutic agent mitomycin C. In hypoxic cells, such as those on the inner surface of the urinary bladder, apaziquone is converted to active metabolites by intracellular reductases. The active metabolites alkylate DNA and lead to apoptosis. This activity is preferentially expressed in neoplastic cells. — Wikipedia
Clinical trial activity
9 trials · 5 clinical orgs · 0 marketing orgs
Phase 1
1
Phase 2
7
Phase 3
7
Phase 4
0
Earliest trial started Jul 1, 2005 (NCT00141531)
Timeline
Indications
Studied for
Mechanism of action
- DNAINHIBITOR
DNA inhibitor
Chemistry & pharmacology
Loading structure…
SMILES
Cn1c(/C=C/CO)c(CO)c2c1C(=O)C=C(N1CC1)C2=O- Mol. weight
- 288.3 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaApaziquone ↗
- ChEMBLCHEMBL73822 ↗
Also known as
- 1h-indole-4,7-dione, 5-(1-aziridinyl)-3-(hydroxymethyl)-2- ((1e)-3-hydroxy-1-propenyl)-1-methyl-
- 3-hydroxymethyl-5-aziridinyl-1-methyl-2-(1h-indole-4,7-dione)prop-beta-en-alpha-ol
- 5-(azridin-1-yl)-3-(hydroxymethyl)-2-((1e)-3-hydroxyprop-1-enyl)-methyl-1h-indole-4,7-dione
- apaziquone
- apaziquone
- apaziquone
- apaziquone
- apaziquone
- e 09
- e-09
- eo9
- eo9
- eo9
- eo 9
- eo-9
- eoquin
- eoquin
- nor-701
- nor-701
- nsc 382459
- nsc 382,459
- nsc-382459
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03224182 | Phase 3 | Jun 28, 2017 | Spectrum Pharmaceuticals |
| NCT02563561 | Phase 3 | Sep 1, 2015 | Spectrum Pharmaceuticals |
| NCT01475266 | Phase 2/Phase 3 (Phase 3) | Nov 1, 2011 | Handok Pharmaceuticals Co., Ltd., Nippon Kayaku Co.,Ltd. |
| NCT01410565 | Phase 3 | Jul 1, 2011 | Allergan, Spectrum Pharmaceuticals |
| NCT01469221 | Phase 3 | Jul 1, 2011 | Allergan, Spectrum Pharmaceuticals |
| NCT01373398 | Phase 1 | May 1, 2011 | Handok Pharmaceuticals Co., Ltd. |
| NCT00598806 | Phase 3 | Sep 1, 2007 | Spectrum Pharmaceuticals |
| NCT00461591 | Phase 3 | Apr 1, 2007 | Spectrum Pharmaceuticals |
| NCT00141531 | Phase 2 | Jul 1, 2005 | Radboud University, Spectrum Pharmaceuticals |
Showing 9 of 9 trials
Page 1 / 1
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Spectrum Pharmaceuticals | For profit | 7 | 7 | 2 | 2005 |
| Allergan | For profit | 2 | 0 | 1 | 2011 |
| Handok Pharmaceuticals Co., Ltd. | For profit | 2 | 1 | 2 | 2011 |
| Nippon Kayaku Co.,Ltd. | For profit | 1 | 1 | 1 | 2011 |
| Radboud University | Academic/Hospital | 1 | 0 | 1 | 2005 |
5 organizations
Page 1 / 1