Indobufen

Abstract

Indobufen is an inhibitor of platelet aggregation which acts by reversibly inhibiting the platelet cyclo-oxygenase enzyme. Improvements in walking distances and microcirculatory parameters have been achieved during therapy with indobufen in patients with peripheral vascular disease and intermittent claudication. Indobufen has been shown to be as effective as aspirin plus dipyridamole in preventing the reocclusion of coronary and femoro-popliteal artery bypass grafts and has been shown to significantly reduce platelet deposition on haemodialysis membranes. Initial studies have also indicated that indobufen may have a prophylactic effect on the incidence of secondary thrombotic events following transient ischaemic attack or mild stroke and may be effective in the prophylaxis of migraine. Indobufen is well tolerated following oral administration and has been associated with a low incidence of adverse effects rarely requiring withdrawal of treatment. Thus, available evidence indicates that indobufen may be an effective alternative to aspirin for the treatment of cerebral, peripheral and coronary vascular diseases with the advantage of a lower incidence of gastrointestinal effects compared to high dose aspirin, rendering indobufen more suitable for longer term therapy.

Anticoagulant Activities of Indobufen, an Antiplatelet Drug

“…Indobufen (laboratory code K 3920, Figure 1 )—chemically 2-[ p -(1-oxo-2-isoindolinyl) phenyl] butyric acid—is a new generation of anti-platelet aggregation drug that reversibly inhibits the platelet cyclooxygenase and decreases thromboxane A2 (TXA2) production [ 7 ]. It also inhibits platelet aggregation induced by adenosine diphosphate (ADP) [ 8 ], epinephrine, platelet activating factor [ 1 ], collagen, arachidonic acid [ 9 ]. Clinical uses include ischemic stroke [ 4 , 10 ], myocardial infarction [ 8 ], non-rheumatic atrial fibrillation [ 11 , 12 ], peripheral vascular disease, and thrombosis formation in patients with venous thrombosis [ 13 ], especially in the prevention and treatment of atherothrombosis [ 14 ].…”

Real-world performance of indobufen versus aspirin after percutaneous coronary intervention: insights from the ASPIRATION registry

“…Indobufen, a phenylbutyrate derivative, is a relatively new generation of antiplatelet drugs, which can reversibly inhibit cyclooxygenase-1 and reduce the formation of thromboxane A2. It can also prevent the platelet aggregation induced by arachidonic acid or adenosine diphosphate, thus inhibiting the formation of thrombus [ 18 ]. Studies on healthy volunteers [ 19 ] and patients [ 20 ] showed that indobufen effectively inhibited thromboxane A2 formation, but had little effect on prostacycline, which was different from aspirin.…”

Reversible and Non-Competitive Inhibition of Cyclooxygenase by Indobufen for Efficient Antiplatelet Action and Relief of Gastrointestinal Irritation

“…In broad terms, arterial thrombosis is treated with drugs targeting platelets, and venous thrombosis is treated with drugs targeting coagulation cascade proteins [ 2 ]. As a reversible inhibitor of cyclooxygenase-1 (COX-1), indobufen can suppress the production of thromboxane A 2 (TXA 2 ), which plays a vital role during the formation of the platelet thrombus [ 3 ]. After the platelets adhere to the exposed collagen of the damaged vascular endothelium, the signal transduction mechanism is activated in the platelets.…”