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Leflunomide, sold under the brand name Arava among others, is an immunosuppressive disease-modifying antirheumatic drug , [8] used in active moderate-to-severe rheumatoid arthritis and psoriatic arthritis. It is a pyrimidine synthesis inhibitor that works by inhibiting dihydroorotate dehydrogenase. [9] Bottle of Leflunomide (Arava) and tablet
csDMARDs are the traditional drugs (such as methotrexate, sulfasalazine, leflunomide, hydroxychloroquine, gold salts) tsDMARDs are drugs that were developed to target a particular molecular structure; biological (bDMARD) can be further separated into original and biosimilar DMARDs (boDMARDs and bsDMARDs)
This is considered a simple structural modification and a technically simple one-step synthetic transformation. Upon oral administration of leflunomide in vivo, the isoxazole ring of leflunomide is opened and teriflunomide is formed. [15] Teriflunomide is the only active metabolite of leflunomide, completely responsible for its therapeutic actions.
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The thalidomide molecule is a synthetic derivative of glutamic acid and consists of a glutarimide ring and a phthaloyl ring (Figure 5). [15] [16] Its IUPAC name is 2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione and it has one chiral center [15] After thalidomide's selective inhibition of TNF-α had been reported, a renewed effort was put in thalidomide's clinical development.
Arava, a brand name for the antirheumatic drug leflunomide Arava Shahaf (born 1990), Israeli female footballer Aravah (Sukkot) , a willow branch, one of the four species used on the Jewish holiday of Sukkot
English: The process of in vivo activation of leflunomide (an immunosuppressive antirheumatic drug Arava) to its one and only active metabolite teriflunomide (an immunosuppressant to treat multiple sclerosis, sold under the brand name Aubagio). Created with ChemDoodle 7.0.2 and Adobe Illustrator CC.
A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. [1] [2] Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted ().