Combretastatin A1 diphosphate
A chemotherapy agent derived from the African bush willow tree
| Combretastatin A1 diphosphate | |
|---|---|
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| CAS Number | 117048-59-6 |
| PubChem | 6440177 |
| DrugBank | |
| ChemSpider | 4944950 |
| KEGG | D08895 |
Combretastatin A1 diphosphate (CA1P) is a chemotherapy agent that is derived from the African bush willow tree, Combretum caffrum. It is a member of the combretastatin family of compounds, which are known for their ability to disrupt the formation of blood vessels in tumors, a process known as angiogenesis.
Mechanism of Action[edit | edit source]
Combretastatin A1 diphosphate functions primarily as a vascular disrupting agent (VDA). It targets the endothelial cells of the tumor vasculature, leading to rapid and selective shutdown of blood flow to the tumor. This results in tumor necrosis due to the lack of oxygen and nutrients. The compound binds to the colchicine binding site on tubulin, inhibiting its polymerization and thus disrupting the cytoskeleton of endothelial cells.
Clinical Applications[edit | edit source]
Combretastatin A1 diphosphate is currently under investigation in clinical trials for its potential use in treating various types of cancer, including leukemia, ovarian cancer, and lung cancer. Its ability to selectively target tumor vasculature makes it a promising candidate for combination therapies with other chemotherapeutic agents or radiation therapy.
Pharmacokinetics[edit | edit source]
The pharmacokinetics of CA1P involve its rapid conversion to the active form, combretastatin A1 (CA1), in the bloodstream. CA1 is the active moiety that exerts the anti-vascular effects. The diphosphate form is more water-soluble, allowing for easier administration and better bioavailability.
Side Effects[edit | edit source]
As with many chemotherapy agents, CA1P can cause a range of side effects. Common side effects include fatigue, nausea, and hypertension. More severe side effects can include cardiotoxicity and neutropenia.
Research and Development[edit | edit source]
Research into combretastatin A1 diphosphate is ongoing, with several clinical trials exploring its efficacy and safety in combination with other treatments. The unique mechanism of action of CA1P makes it a valuable subject of study in the field of oncology.
Also see[edit | edit source]
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