Thymidylate synthase inhibitor
Encyclopedia
Thymidylate synthase inhibitors are chemical agents which inhibit
the enzyme thymidylate synthase
and have potential as an anticancer chemotherapy
. Five agents were in clinical trials in 2002: raltitrexed
, pemetrexed
, nolatrexed
, ZD9331, and GS7904L.
Examples include
Enzyme inhibitor
An enzyme inhibitor is a molecule that binds to enzymes and decreases their activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. They are also used as herbicides and pesticides...
the enzyme thymidylate synthase
Thymidylate synthase
Thymidylate synthetase is the enzyme used to generate thymidine monophosphate , which is subsequently phosphorylated to thymidine triphosphate for use in DNA synthesis and repair....
and have potential as an anticancer chemotherapy
Chemotherapy
Chemotherapy is the treatment of cancer with an antineoplastic drug or with a combination of such drugs into a standardized treatment regimen....
. Five agents were in clinical trials in 2002: raltitrexed
Raltitrexed
Raltitrexed is an antimetabolite drug used in cancer chemotherapy. It is an inhibitor of thymidylate synthase, and is manufactured by AstraZeneca.-Mechanism of action:...
, pemetrexed
Pemetrexed
Pemetrexed is a chemotherapy drug manufactured and marketed by Eli Lilly and Company. Its indications are the treatment of Pleural Mesothelioma as well as non-small cell lung cancer.-History:...
, nolatrexed
Nolatrexed
Nolatrexed is a thymidylate synthase inhibitor....
, ZD9331, and GS7904L.
Examples include
- Raltitrexed, used for colorectal cancer since 1998
- FluorouracilFluorouracilFluorouracil is a drug that is a pyrimidine analog which is used in the treatment of cancer. It is a suicide inhibitor and works through irreversible inhibition of thymidylate synthase. It belongs to the family of drugs called antimetabolites...
, used for colorectal cancer - BGC 945