Pharmacokinetics and Cyclooxygenase Inhibition of Itazigrel in Normal Volunteers after Single Oral Doses

Structural diversity of selective COX-2 inhibitors

“…Likewise, the 2,3-diarylindole indoxole was disclosed in the early 1960s as a potent anti-inflammatory agent; however, the drug was suspended from clinical development since it caused photosensitivity in humans [27][28][29]. Throughout the period from late 1960s to the early 1980s, a plethora of diarylheterocycles with variations on the central heterocyclic ring were evaluated as anti-inflammatory agents [30] and several were advanced into clinical trials based on their superior pharmacological and gastrointestinal profile in preclinical species compared with traditional NSAIDs [31,32]. An example of such a compound is the 4,5-diarylthiazole derivative itazigrel that was shown to be less ulcerogenic than aspirin in subsequent clinical trials [33].…”