See the DrugPatentWatch profile for rofecoxib

Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits cyclooxygenase-2 (COX-2) [1]. This selective inhibition of COX-2 is the key factor in reducing gastric side effects associated with NSAIDs.

Non-selective NSAIDs, such as ibuprofen and naproxen, inhibit both COX-1 and COX-2 enzymes. COX-1 is responsible for producing prostaglandins that protect the stomach lining, while COX-2 produces prostaglandins that promote inflammation and pain [2]. The inhibition of COX-1 by non-selective NSAIDs can lead to gastric side effects such as ulcers, bleeding, and perforation [3].

Rofecoxib's selective inhibition of COX-2 means that it does not inhibit COX-1 and therefore does not interfere with the production of prostaglandins that protect the stomach lining [4]. This selective inhibition reduces the risk of gastric side effects compared to non-selective NSAIDs [5].

However, it is important to note that selective COX-2 inhibitors like rofecoxib have been associated with an increased risk of cardiovascular events, such as myocardial infarction and stroke [6]. Therefore, the use of rofecoxib and other selective COX-2 inhibitors should be carefully considered and balanced against the potential risks and benefits for each individual patient [7].

In summary, rofecoxib's selective inhibition of COX-2 reduces the risk of gastric side effects associated with non-selective NSAIDs by not inhibiting COX-1 and therefore not interfering with the production of prostaglandins that protect the stomach lining.

Sources:

[1] DrugPatentWatch.com. (n.d.). Rofecoxib. Retrieved from <https://www.drugpatentwatch.com/drugs/rofecoxib>

[2] University of Washington. (n.d.). Nonsteroidal Anti-inflammatory Drugs (NSAIDs). Retrieved from <https://www.uwmedicine.org/conditions/nonsteroidal-anti-inflammatory-drugs-nsaids>

[3] National Institute of Diabetes and Digestive and Kidney Diseases. (2016). Nonsteroidal Anti-inflammatory Drugs (NSAIDs). Retrieved from <https://www.niddk.nih.gov/health-information/illness-conditions/nonsteroidal-anti-inflammatory-drugs-nsaids>

[4] Mayo Clinic. (2021). Nonsteroidal anti-inflammatory drugs (NSAIDs). Retrieved from <https://www.mayoclinic.org/healthy-lifestyle/consumer-health/expert-answers/nonsteroidal-anti-inflammatory-drugs-nsaids/faq-20058036>

[5] U.S. Food and Drug Administration. (2015). FDA Drug Safety Communication: FDA strengthens warning that non-aspirin nonsteroidal anti-inflammatory drugs (NSAIDs) can cause heart attacks or strokes. Retrieved from <https://www.fda.gov/drugs/drug-safety-and-availability/fda-drug-safety-communication-fda-strengthens-warning-non-aspirin-nonsteroidal-anti-inflammatory-drugs-nsaids-can>

[6] U.S. Food and Drug Administration. (2015). FDA requires label changes to warn of serious mental health risks with non-aspirin nonsteroidal anti-inflammatory drugs (NSAIDs). Retrieved from <https://www.fda.gov/drugs/drug-safety-and-availability/fda-requires-label-changes-warn-serious-mental-health-risks-non-aspirin-nonsteroidal-anti-inflammatory>

[7] American Gastroenterological Association. (2019). Nonsteroidal Anti-inflammatory Drugs (NSAIDs). Retrieved from <https://www.gastro.org/practice-guidance/gi-patient-care/patient-education/nsaids>