See the DrugPatentWatch profile for rofecoxib

Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that was previously available on the market under the brand name Vioxx. It is a selective cyclooxygenase-2 (COX-2) inhibitor, which distinguishes it from other NSAIDs and contributes to its ability to reduce stomach irritation [1].

Cyclooxygenase (COX) is an enzyme responsible for the production of prostaglandins, which are hormone-like substances involved in pain, fever, and inflammation. There are two main isoforms of COX: COX-1 and COX-2. COX-1 is constitutively expressed and involved in maintaining the normal functions of the stomach lining, while COX-2 is primarily induced during inflammation [2].

Rofecoxib's selective action on COX-2 inhibition reduces stomach irritation in several ways:

1. Minimized effect on COX-1: By primarily inhibiting COX-2, rofecoxib leaves COX-1 relatively uninhibited, allowing it to continue its role in maintaining the stomach lining and reducing the risk of gastrointestinal (GI) side effects, such as ulcers and bleeding, that are commonly associated with non-selective NSAIDs [1][2].

2. Reduced prostaglandin production: Rofecoxib's selective COX-2 inhibition decreases the production of prostaglandins involved in inflammation, thus alleviating pain and inflammation while minimizing the impact on the stomach lining [1].

3. Fewer GI adverse events: Due to its selective COX-2 inhibition, rofecoxib has been associated with a lower incidence of GI adverse events compared to non-selective NSAIDs [1].

It is important to note that, despite its gastrointestinal benefits, rofecoxib was withdrawn from the market in 2004 due to an increased risk of cardiovascular events, such as heart attacks and strokes, associated with long-term use [1].

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