fosbretabulin
Small moleculeexperimental
Fosbretabulin is a microtubule destabilizing experimental drug, a type of vascular-targeting agent, a drug designed to damage the vasculature of cancer tumours causing central necrosis. It is a derivative of combretastatin. It is formulated as the salts fosbretabulin disodium and fosbretabulin tromethamine. — Wikipedia
Clinical trial activity
18 trials · 15 clinical orgs · 0 marketing orgs
Phase 1
8
Phase 2
12
Phase 3
2
Phase 4
0
Earliest trial started Jul 1, 1998 (NCT00003698)
Timeline
Indications
Studied for
- Central Nervous System Neoplasms · Phase 1
- Choroidal Neovascularization · Phase 2
- Drugs, Investigational · Phase 1/Phase 2
- Everolimus · Phase 1
- Fallopian Tube Neoplasms · Phase 2
- Hamartoma · Phase 2
- Head and Neck Neoplasms · Phase 2
- Livedoid Vasculopathy · Phase 2
- Macular Degeneration · Phase 1/Phase 2
- Myopia, Degenerative · Phase 2
- Neoplasms · Phase 2
- Neuroendocrine Tumors · Phase 2
- Ovarian Neoplasms · Phase 2/Phase 3
- Thyroid Carcinoma, Anaplastic · Phase 3
- Wet Macular Degeneration · Phase 1/Phase 2
Mechanism of action
- TubulinDISRUPTING AGENT
Tubulin disrupting agent
Reversible tubulin depolymerizing agent.
- Tubulin beta-4B chain (TUBB4B) ↗
- Tubulin beta-1 chain (TUBB1) ↗
- Tubulin alpha-3C chain (TUBA3C) ↗
- Tubulin alpha-4A chain (TUBA4A) ↗
- Tubulin beta-3 chain (TUBB3) ↗
- Tubulin alpha-1A chain (TUBA1A) ↗
- Tubulin beta-4A chain (TUBB4A) ↗
- Tubulin beta-8 chain (TUBB8) ↗
- Tubulin beta chain (TUBB) ↗
- Tubulin alpha-1B chain (TUBA1B) ↗
- Tubulin alpha-1C chain (TUBA1C) ↗
- Tubulin alpha-3E chain (TUBA3E) ↗
- Tubulin beta-2A chain (TUBB2A) ↗
- Tubulin beta-2B chain (TUBB2B) ↗
- Tubulin beta-6 chain (TUBB6) ↗
- TubulinINHIBITOR
Tubulin inhibitor
- Tubulin beta-4B chain (TUBB4B) ↗
- Tubulin beta-1 chain (TUBB1) ↗
- Tubulin alpha-3C chain (TUBA3C) ↗
- Tubulin alpha-4A chain (TUBA4A) ↗
- Tubulin beta-3 chain (TUBB3) ↗
- Tubulin alpha-1A chain (TUBA1A) ↗
- Tubulin beta-4A chain (TUBB4A) ↗
- Tubulin beta-8 chain (TUBB8) ↗
- Tubulin beta chain (TUBB) ↗
- Tubulin alpha-1B chain (TUBA1B) ↗
- Tubulin alpha-1C chain (TUBA1C) ↗
- Tubulin alpha-3E chain (TUBA3E) ↗
- Tubulin beta-2A chain (TUBB2A) ↗
- Tubulin beta-2B chain (TUBB2B) ↗
- Tubulin beta-6 chain (TUBB6) ↗
Chemistry & pharmacology
Loading structure…
SMILES
COc1ccc(/C=C\c2cc(OC)c(OC)c(OC)c2)cc1OP(=O)(O)O- Mol. weight
- 396.33 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Prodrug
Sources
- WikipediaFosbretabulin ↗
- ChEMBLCHEMBL289351 ↗
- ChEMBLCHEMBL2105643 ↗
- ChEMBLCHEMBL1206232 ↗
- WikipediaCombretastatin A-4 phosphate ↗
Also known as
- 1-(3,4,5-trimethoxyphenyl)-2-(3'-hydroxy-4'-methoxyphenyl)ethene
- 2-methoxy-5-((z)-2-(3,4,5-trimethoxyphenyl)vinyl)phenyl dihydrogen phosphate
- 3,4,5-trimethoxy-3'-hydroxy-4'-methoxystilbene
- ca4dp
- ca4dp
- ca4dp
- combretastatin a4
- combretastatin a-4
- combretastatin a-4 disodium phosphate
- combretastatin a-4 phosphate
- combretastatin a-4 phosphate
- combretastatin a4 phosphate
- combretastatin a4 phosphate
- combretastatin a4 phosphate
- crc 87-09
- crc-98-09
- deoxycombretastatin a-4
- fosbretabulin
- fosbretabulin
- fosbretabulin
- fosbretabulin
- fosbretabulin
- fosbretabulin disodium
- fosbretabulin disodium
- fosbretabulin disodium
- fosbretabulin tromethamine
- fosbretabulin tromethamine
- isocombretastatin a-4
- nsc 817373
- nsc-817373
- phenol, 2-methoxy-5-((1z)-2-(3,4,5-trimethoxyphenyl)ethenyl)-,1-(dihydrogen phosphate)
- phenol, 2-methoxy-5-((z)-2-(3,4,5-trimethoxyphenyl)ethenyl)-, dihydrogen phosphate
- zybrestat
- zybrestat
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03014297 | Phase 1 | Mar 6, 2017 | University of Kentucky |
| NCT02641639 | Phase 2/Phase 3 (Phase 3) | Jun 1, 2016 | Mateon Therapeutics |
| NCT01701349 | Phase 3 | Mar 1, 2015 | Mateon Therapeutics, University of Milan, University of Pennsylvania, Yale University |
| NCT02279602 | Phase 2 | Dec 1, 2014 | Mateon Therapeutics |
| NCT02132468 | Phase 2 | Sep 1, 2014 | Mateon Therapeutics |
| NCT02055690 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2014 | East and North Hertfordshire NHS Trust, Mateon Therapeutics, Novartis, The Christie NHS Foundation Trust |
| NCT01305213 | Phase 2 | Mar 1, 2011 | National Cancer Institute (NCI), NRG Oncology |
| NCT01052363 | Phase 1 | Jan 1, 2010 | West Virginia University |
| NCT01023295 | Phase 2 | Jul 1, 2009 | Mateon Therapeutics |
| NCT00653939 | Phase 2 | Mar 1, 2008 | Mateon Therapeutics |
| NCT00395434 | Phase 1 | Sep 1, 2006 | Inova Health System, Mateon Therapeutics |
| NCT01423149 | Phase 2 | Mar 1, 2005 | Mateon Therapeutics |
| NCT00113438 | Phase 2 | Mar 1, 2005 | Mateon Therapeutics |
| NCT00077103 | Phase 1/Phase 2 (Phase 2) | Nov 1, 2003 | Case Western Reserve University, National Cancer Institute (NCI) |
| NCT01570790 | Phase 1/Phase 2 (Phase 2) | May 1, 2003 | Johns Hopkins University |
| NCT00060242 | Phase 2 | Feb 1, 2003 | Case Western Reserve University, National Cancer Institute (NCI) |
| NCT00003768 | Phase 1 | Sep 1, 1998 | Case Western Reserve University, National Cancer Institute (NCI) |
| NCT00003698 | Phase 1 | Jul 1, 1998 | Inova Health System, University of Glasgow |
Showing 18 of 18 trials
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Organizations
Research & Development (15)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Mateon Therapeutics | For profit | 10 | 9 | 3 | 2005 |
| National Cancer Institute (NCI) | Government | 4 | 1 | 2 | 1998 |
| Case Western Reserve University | Academic/Hospital | 3 | 3 | 2 | 1998 |
| Inova Health System | Academic/Hospital | 2 | 0 | 1 | 1998 |
| East and North Hertfordshire NHS Trust | Academic/Hospital | 1 | 0 | 1 | 2014 |
| Johns Hopkins University | Academic/Hospital | 1 | 1 | 1 | 2003 |
| Novartis | For profit | 1 | 0 | 1 | 2014 |
| NRG Oncology | Academic/Hospital | 1 | 0 | 1 | 2011 |
| The Christie NHS Foundation Trust | Academic/Hospital | 1 | 1 | 1 | 2014 |
| University of Glasgow | Academic/Hospital | 1 | 1 | 1 | 1998 |
| University of Kentucky | Academic/Hospital | 1 | 1 | 1 | 2017 |
| University of Milan | Academic/Hospital | 1 | 0 | 1 | 2015 |
| University of Pennsylvania | Academic/Hospital | 1 | 0 | 1 | 2015 |
| West Virginia University | Academic/Hospital | 1 | 1 | 1 | 2010 |
| Yale University | Academic/Hospital | 1 | 0 | 1 | 2015 |
15 organizations
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