Mechanisms of action<unk>  is an enzyme inhibitor. It combines with the enzyme thromboxane A2 synthase to prevent the normal substrate-enzyme combination and the catalytic reaction. Thromboxane A2, the compound synthesized by this enzyme, promotes the aggregation of platelets and is a vasoconstrictor. The compound plays a role in several diseases involving thrombosis, the occurrence of blood clots that block veins or arteries. Thromboxane is synthesized from a fatty acid called arachidonic acid. In platelets this fatty acid is metabolized to an endoperoxide called prostaglandin H2 by the enzyme cyclooxygenase 1. This endoperoxide is in turn metabolized to thromboxane A2 by thromboxane A2 synthase, a cytochrome P450 enzyme that occurs in the endoplasmic reticulum membrane. Multiple cyclooxygenase inhibitors are already used as drugs against thrombotic diseases. These drugs inhibit both the production of thromboxane and prostacyclin.<unk>  however, specifically inhibits thromboxane A2 synthase. Metabolism The route of administration of<unk>  is oral. The absorption and disposition of the parent drug in male volunteers have been studied after single- and multiple-dose oral administration. The results from the single-dose study indicate that<unk>  is rapidly absorbed in the blood, within maximally 1.0 to 1.7 hr. Distribution, metabolism and elimination happened with a rate constant of 0.12 to 0.17 hr-1.<unk>  is primarily eliminated by the kidney, with 62 to 78% of the dose excreted as parent drug. Dog experiments indicated that<unk>  is rapidly distributed. The half‐life of the compound was 132 min after an intravenous dose. Oral exposure to the drug had similar absorption and elimination kinetics as the intravenous results. The bioavailability of<unk>  dosed orally was either around 80% based on measurements of the blood concentration or more than 90% based on urinary excretion of the parent compound. Oral absorption of the drug in dogs occurred rapidly. The plasma levels reached a peak in one to two hours after ingestion. The drug was measurable in blood within 30 minutes. Thromboxane A2 is hydrated within about 30 seconds to the biologically inactive thromboxane B2. For this reason thromboxane B2 can be used as an indicator for the inhibition of thromboxane A2 synthase, and thus the presence of<unk> .
Furegrelate
Lemborexant
Fosaprepitant
Tezacaftor
Eteplirsen
Protokylol
Prasugrel
Bocasan