zosuquidar
Zosuquidar is an experimental antineoplastic drug. Zosquidir inhibits P-glycoproteins. Other drugs with this mechanism include tariquidar and laniquidar. P-glycoproteins are trans-membrane proteins that pump foreign substances out of cells in an ATP dependent fashion. Cancers overexpressing P-glycoproteins are able to pump out therapeutic molecules before they are able to reach their target, effectively making the cancer multi-drug resistant. Zosuquidar inhibits P-glycoproteins, inhibiting the efflux pump and restoring sensitivity to chemotherapeutic agents. — Wikipedia
Clinical trial activity
3 trials · 5 clinical orgs · 0 marketing orgs
Earliest trial started Jul 1, 2002 (NCT00046930)
Timeline
Indications
Mechanism of action
- Multidrug resistance protein 3INHIBITOR
ABCB4 inhibitor
- P-glycoprotein 1INHIBITOR
P-glycoprotein 1 inhibitor
To reduce drug resistance.
Chemistry & pharmacology
SMILES
O[C@@H](COc1cccc2ncccc12)CN1CCN([C@@H]2c3ccccc3[C@@H]3[C@H](c4ccccc42)C3(F)F)CC1- Mol. weight
- 527.62 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaZosuquidar ↗
- ChEMBLCHEMBL444172 ↗
Also known as
- zosuquidar
- zosuquidar
- zosuquidar
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00233909 | Phase 1/Phase 2 (Phase 2) | Oct 1, 2005 | Kanisa Pharmaceuticals |
| NCT00129168 | Phase 1/Phase 2 (Phase 2) | Aug 1, 2005 | Kanisa Pharmaceuticals |
| NCT00046930 | Phase 3 | Jul 1, 2002 | Eastern Cooperative Oncology Group, Eli Lilly, Indiana University, Kanisa Pharmaceuticals, National Cancer Institute (NCI) |
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Kanisa Pharmaceuticals | For profit | 3 | 2 | 2 | 2002 |
| Eastern Cooperative Oncology Group | Academic/Hospital | 1 | 1 | 1 | 2002 |
| Eli Lilly | For profit | 1 | 0 | 1 | 2002 |
| Indiana University | Academic/Hospital | 1 | 0 | 1 | 2002 |
| National Cancer Institute (NCI) | Government | 1 | 0 | 1 | 2002 |