Carotegrast methyl (trade name Carogra) is a drug used for the treatment of ulcerative colitis. Carotegrast methyl is a

prodrug A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug ...

that has little pharmacological activity itself. The

methyl In organic chemistry, a methyl group is an alkyl derived from methane, containing one carbon atom bonded to three hydrogen atoms, having chemical formula . In formulas, the group is often abbreviated as Me. This hydrocarbon group occurs in many ...

ester, which is designed to enhance oral bioavailability, is hydrolyzed to a

carboxylic acid In organic chemistry, a carboxylic acid is an organic acid that contains a carboxyl group () attached to an R-group. The general formula of a carboxylic acid is or , with R referring to the alkyl, alkenyl, aryl, or other group. Carboxylic ...

, carotegrast, by the enzyme

carboxylesterase 1 Liver carboxylesterase 1 also known as carboxylesterase 1 (CES1, hCE-1 or CES1A1) is an enzyme that in humans is encoded by the ''CES1'' gene. The protein is also historically known as serine esterase 1 (SES1), monocyte esterase and cholesterol e ...

in the liver. Carotegrast is an α4-integrin antagonist which prevents the chronic inflammation affecting the

gastrointestinal tract The gastrointestinal tract (GI tract, digestive tract, alimentary canal) is the tract or passageway of the digestive system that leads from the mouth to the anus. The GI tract contains all the major organ (biology), organs of the digestive syste ...

in individuals with ulcerative colitis. :

Carotegrast methyl received approval in Japan in March 2022 for the treatment of moderate ulcerative colitis in patients who had inadequate response to mesalazine.

References

{{gastrointestinal-drug-stub Prodrugs Methyl esters Chlorobenzenes Benzamides Dimethylamino compounds Quinazolinones