tariquidar
Small moleculeexperimental
Tariquidar (INN/USAN) is a potent P-glycoprotein inhibitor and a substrate of breast cancer protein (BCRP/ABCG2) undergoing research as an adjuvant against multi-drug resistance in cancer. — Wikipedia
Clinical trial activity
9 trials · 4 clinical orgs · 0 marketing orgs
Phase 1
4
Phase 2
6
Phase 3
2
Phase 4
0
Earliest trial started Dec 1, 1999 (NCT00001944)
Timeline
Indications
Studied for
- Adrenal Cortex Neoplasms · Phase 2
- Adrenal Gland Neoplasms · Phase 1
- Breast Neoplasms · Phase 1
- Carcinoma, Non-Small-Cell Lung · Phase 3
- Kidney Neoplasms · Phase 2
- Lung Neoplasms · Phase 2
- Neoplasms · Phase 2
- Neuralgia · Phase 1/Phase 2
- Ovarian Neoplasms · Phase 2
- Sarcoma · Phase 1
- Uterine Cervical Neoplasms · Phase 2
- Wilms Tumor · Phase 1
Mechanism of action
- P-glycoprotein 1INHIBITOR
ABCB1 inhibitor
Specifically inhibitS ABCB1 among ABC transporters (KD = 5.1 nM).
Chemistry & pharmacology
Loading structure…
SMILES
COc1cc2c(cc1OC)CN(CCc1ccc(NC(=O)c3cc(OC)c(OC)cc3NC(=O)c3cnc4ccccc4c3)cc1)CC2- Mol. weight
- 646.74 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaTariquidar ↗
- ChEMBLCHEMBL348475 ↗
Also known as
- tariquidar
- tariquidar
- tariquidar
- tariquidar
- tariquidarth
- xr9576
- xr9576
- xr9576
- xr 9576
- xr-9576
- xr-9576
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04603066 | Phase 1/Phase 2 (Phase 2) | Jan 31, 2021 | Washington University in St. Louis |
| NCT03809234 | Phase 1 | May 20, 2019 | Washington University in St. Louis |
| NCT00082368 | Phase 2 | May 1, 2004 | National Cancer Institute (NCI), National Institutes of Health (NIH) |
| NCT00071058 | Phase 2 | Oct 1, 2003 | National Cancer Institute (NCI), National Institutes of Health (NIH) |
| NCT00069160 | Phase 2 | Sep 1, 2003 | National Cancer Institute (NCI), National Institutes of Health (NIH) |
| NCT00042315 | Phase 3 | Jun 1, 2002 | Novelion Therapeutics |
| NCT00042302 | Phase 3 | Jun 1, 2002 | Novelion Therapeutics |
| NCT00011414 | Phase 1 | Feb 15, 2001 | National Cancer Institute (NCI) |
| NCT00001944 | Phase 1 | Dec 1, 1999 | National Cancer Institute (NCI) |
Showing 9 of 9 trials
Page 1 / 1
Organizations
Research & Development (4)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| National Cancer Institute (NCI) | Government | 5 | 5 | 2 | 1999 |
| National Institutes of Health (NIH) | Government | 3 | 0 | 1 | 2003 |
| Novelion Therapeutics | For profit | 2 | 2 | 1 | 2002 |
| Washington University in St. Louis | Academic/Hospital | 2 | 2 | 2 | 2019 |
4 organizations
Page 1 / 1