tesevatinib
Small moleculeexperimental
Tesevatinib is an experimental drug proposed for use in kidney cancer and polycystic kidney disease. The drug was first developed by Exelixis, Inc. and was later acquired by Kadmon Corporation. Tesevatinib binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including epidermal growth factor receptor, epidermal growth factor receptor 2, vascular endothelial growth factor receptor (VEGFR), and ephrin B4 (EphB4). — Wikipedia
Clinical trial activity
14 trials · 3 clinical orgs · 0 marketing orgs
Phase 1
7
Phase 2
9
Phase 3
1
Phase 4
0
Earliest trial started Jun 1, 2004 (NCT00086528)
Timeline
Indications
Studied for
- Brain Neoplasms · Phase 2
- Breast Neoplasms · Phase 1/Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 3
- Esophageal Neoplasms · Phase 1
- Glioblastoma · Phase 2
- Neoplasm Metastasis · Phase 2
- Neoplasms · Phase 1
- Polycystic Kidney, Autosomal Dominant · Phase 2
- Polycystic Kidney, Autosomal Recessive · Phase 1
- Stomach Neoplasms · Phase 1
Mechanism of action
EGFR inhibitor
- Ephrin type-B receptor 4INHIBITOR
EPHB4 inhibitor
ERBB2 inhibitor
Chemistry & pharmacology
Loading structure…
SMILES
COc1cc2c(Nc3ccc(Cl)c(Cl)c3F)ncnc2cc1OC[C@@H]1C[C@@H]2CN(C)C[C@@H]2C1- Mol. weight
- 491.39 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaTesevatinib ↗
- ChEMBLCHEMBL3544983 ↗
Also known as
- kd019
- kd019
- kd-019
- kd-019
- kd-020
- kd-020
- tesevatinib
- tesevatinib
- tesevatinib
- tesevatinib
- xl647
- xl647
- xl-647
- xl-647
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03203642 | Phase 2 | Jul 29, 2017 | Kadmon |
| NCT03096080 | Phase 1 | Jun 14, 2017 | Kadmon |
| NCT02844439 | Phase 2 | Jun 1, 2016 | Kadmon |
| NCT02616055 | Phase 2 | Dec 1, 2015 | Kadmon |
| NCT02616393 | Phase 2 | Nov 1, 2015 | Kadmon |
| NCT02205463 | Phase 1 | Dec 1, 2014 | New York University |
| NCT02154529 | Phase 1/Phase 2 (Phase 2) | May 1, 2014 | Kadmon |
| NCT01559363 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2012 | Kadmon |
| NCT01487174 | Phase 3 | Nov 1, 2011 | Kadmon |
| NCT00704392 | Phase 1 | Jun 1, 2008 | Exelixis |
| NCT00522145 | Phase 2 | May 1, 2007 | Kadmon |
| NCT00364780 | Phase 2 | Jul 1, 2006 | Kadmon |
| NCT00336765 | Phase 1 | Jul 1, 2006 | Kadmon |
| NCT00086528 | Phase 1 | Jun 1, 2004 | Exelixis, Kadmon |
Showing 14 of 14 trials
Page 1 / 1
Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Kadmon | For profit | 12 | 12 | 3 | 2004 |
| Exelixis | For profit | 2 | 1 | 1 | 2004 |
| New York University | Academic/Hospital | 1 | 1 | 1 | 2014 |
3 organizations
Page 1 / 1