Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium
Molecular Weight(MW): 440.29
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM in a cell-free assay. Fosbretabulin Disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature. Phase 3.
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|Description||Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM in a cell-free assay. Fosbretabulin Disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature. Phase 3.|
|Features||A microtubule associated inhibitor with higher affinity to β-tubulin vs. Colchicine. Best for advanced solid tumors, anaplastic thyroid cancer, & choroidal neovascularization.|
Fosbretabulin disodium (Combretastatin A-4 phosphate disodium, CA4P disodium) is the water-soluble prodrug of combretastatin A4 (CA4), which is originally isolated from African tree Combretum caffrum. CA4 is a tubulin-binding agent that binds at or near the colchicine binding site of β-tubulin (Kd = 0.40 μM), inhibits tubulin assembly with IC50 of 2.4 μM.  CA4 is cytotoxic towards proliferating but not quiescent endothelial cells, has potent and selective toxicity towards tumor vasculature.  CA4P (1 mM, 30 minutes) disrupts the endothelial microtubule cytoskeleton and mediates changes in endothelial cell morphology. CA4P stimulates actin stress fiber formation and membrane blebbing and increases monolayer permeability via Rho/Rho-kinase.  CA4P increases endothelial cell permeability, while inhibiting endothelial cell migration and capillary tube formation predominantly through disruption of VE-cadherin/β-catenin/Akt signaling pathway, thereby leading to rapid vascular collapse and tumor necrosis. 
|In vivo||CA4P causes rapid, extensive and irreversible vascular shutdown in experimental tumor models following the administration of a single dose at 10% of the maximum tolerated dose (MTD). CA4P causes a 93% reduction in vascular volume 6 h following drug administration.  CA4P(100 mg/kg, 6 h following administration) reduces tumor blood by approximately 100-fold, compared with approximately 7-fold in the spleen. |
Tubulin assembly-disassembly:The assembly of microtubules from isolated tubulin is carried out spectrophotometrically at 350 nm and utilises the increase in turbidity which is associated with microtubule formation. Assembly is initiated by temperature increase from 10 to 35 °C. The effect of drugs on the increase in light absorption is carried. Drugs are dissolved in DMSO (<4%), which does not affect control assembly
|In vitro||Water||28 mg/mL (63.59 mM)|
|In vivo||Saline with a few drops of 5% Na2CO3||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02641639||Recruiting||Platinum Resistant Ovarian Cancer||Mateon Therapeutics||June 2016||Phase 2|Phase 3|
|NCT01701349||Withdrawn||Anaplastic Thyroid Cancer||Mateon Therapeutics||March 2015||Phase 3|
|NCT02279602||Enrolling by invitation||Neuroendocrine Tumors||Mateon Therapeutics||December 2014||Phase 2|
|NCT02055690||Recruiting||Ovarian Neoplasms|Neoplasms, Ovarian|Ovarian Cancer||Heather Driscoll|Novartis|Mateon Therapeutics|East and North Hertfordshire NHS Trust|The Christie NHS Foundation Trust||September 2014||Phase 1|Phase 2|
|NCT02132468||Active, not recruiting||Neuroendocrine Tumors||Mateon Therapeutics||September 2014||Phase 2|
|NCT01305213||Active, not recruiting||Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma||National Cancer Institute (NCI)||March 2011||Phase 2|
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