BGC 945
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ONX-0801 (BGC 945) is an experimental drug that has been developed to target ovarian cancer. It is a folate receptor alpha mediated
thymidylate synthase inhibitor Thymidylate synthase inhibitors are chemical agents which inhibit the enzyme thymidylate synthase and have potential as an anticancer chemotherapy. This inhibition prevents the methylation of C5 of deoxyuridine monophosphate (dUMP) thereby inhibiti ...
. ONX-0801 was originally developed by BTG and the
Institute of Cancer Research The Institute of Cancer Research (the ICR) is a public research institute and a member institution of the University of London in London, United Kingdom, specialising in oncology. It was founded in 1909 as a research department of the Royal Mar ...
in the UK, and subsequently licensed to Onyx Pharmaceuticals for clinical development. It is designed to selectively target tumour tissues of certain kinds of cancer. It is poorly absorbed into most cells, but is actively transported by folate receptor alpha (FRĪ±), which is usually only expressed at low levels in the
apical membrane The cell membrane (also known as the plasma membrane (PM) or cytoplasmic membrane, and historically referred to as the plasmalemma) is a biological membrane that separates and protects the interior of all cells from the outside environment (t ...
of some specialised tissues, but is expressed at much higher levels in some subtypes of ovarian cancer. This causes the drug to accumulate selectively in tumour tissues, while healthy tissues are only exposed to a much lower concentration. In 2017, it received press coverage following the successful completion of a Phase I clinical trial.


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