Fosbretabulin

Fosbretabulin (also known as combretastatin A-4 phosphate or CA4P) is a microtubule destabilizing experimental drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumours causing central necrosis. It is a derivative of combretastatin. It is formulated as the salts fosbretabulin disodium and fosbretabulin tromethamine.[1]

Fosbretabulin
Clinical data
Other namesCombretastatin A-4 phosphate; CA4P; CA4PD; fosbretabulin disodium; fosbretabulin tromethamine
Legal status
Legal status
  • Investigational
Identifiers
  • Phosphoric acid mono-{2-methoxy-5-[(Z)-2-(3,4,5-trimethoxy-phenyl)-vinyl]-phenyl} ester
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC18H21O8P
Molar mass396.332 g·mol−1
3D model (JSmol)
  • O=P(O)(O)Oc1c(OC)ccc(c1)\C=C/c2cc(OC)c(OC)c(OC)c2
  • InChI=1S/C18H21O8P/c1-22-14-8-7-12(9-15(14)26-27(19,20)21)5-6-13-10-16(23-2)18(25-4)17(11-13)24-3/h5-11H,1-4H3,(H2,19,20,21)/b6-5-
  • Key:WDOGQTQEKVLZIJ-WAYWQWQTSA-N
  (verify)

Fosbretabulin is a prodrug. In vivo, it is dephosphorylated to its active metabolite, combretastatin A-4.[2]

In July 2007, the pharmaceutical company OXiGENE initiated a 180-patient phase III clinical trial of fosbretabulin in combination with carboplatin for the treatment of anaplastic thyroid cancer.[3] There is currently no fully FDA approved treatment for this form of cancer. By 2017, it had completed multiple clinical trials (e.g. for solid tumours,[4] non-small cell lung cancer[5]) with more in progress.[6]

See also

References
  1. Clinical trial number NCT02132468 for "A Ph 2 Study to Investigate the Safety and Activity of Fosbretabulin Tromethamine (CA4P) in the Treatment of Well-Differentiated, Low-to-Intermediate-Grade Unresectable, Recurrent or Metastatic PNET or GI-NET Neuroendocrine Tumors/Carcinoid With Elevated Biomarkers" at ClinicalTrials.gov
  2. "Fosbretabulin disodium". National Cancer Institute. U.S. Department of Health and Human Services.
  3. Clinical trial number NCT00507429 for "A Phase II/III Study to Evaluate the Safety and Efficacy of Combretastatin A-4 Phosphate in Combination With Paclitaxel and Carboplatin in Comparison With Paclitaxel and Carboplatin Against Anaplastic Thyroid Carcinoma [FACT]" at ClinicalTrials.gov
  4. Clinical trial number NCT00113438 for "A Randomized Open-Labeled Phase II Study of Combretastatin A-4 Phosphate in Combination With Paclitaxel and Carboplatin to Evaluate the Safety and Efficacy in Subjects With Advanced Imageable Malignancies" at ClinicalTrials.gov
  5. Clinical trial number NCT00653939 for "A Phase II Study to Assess the Safety and Efficacy of the Combination of Carboplatin, Paclitaxel, and Bevacizumab ± Combretastatin A4 Phosphate (CA4P) Followed by Bevacizumab ± CA4P in Subjects With Chemotherapy Naïve Stage IIIB/IV Non-Squamous Cell Histology Non-Small Cell Lung Cancer (NSCLC)" at ClinicalTrials.gov
  6. "Search of: CA4P - List Results - ClinicalTrials.gov". clinicaltrials.gov.


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