Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes. Indobufen prevents TF expression and activity both in isolated and in whole blood monocytes. Reduction of TxA2 synthesis, coupled with a lack of effect on PGE2 levels and prevention of ERK1/2 phosphorylation are highlighted as the mechanisms through which indobufen negatively affects TF[1]. Intragastric-administrated indobufen can significantly reduce the APTT (activated partial thromboplastin time), PT (prothrombin time), TT (thrombin time), PF3 (platelet factor 3,4), FI, II, V, VIII, and X (the coagulation factor 1, 2, 5, 8, 10) plasma contents. Its inhibitory effect on plasma FII was better than thrombin inhibitor dabigatran with effect on FX better than FXa inhibitor rivaroxaban[2]. 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[3].
Indobufen/吲哚布芬 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Rabbit platelets
0.1, 0.2, 0.4, 0.6, 0.8 mmol/L
5 minutes
Evaluate the inhibitory effect of Indobufen on ADP-induced platelet aggregation. Results showed that Indobufen significantly inhibited platelet aggregation, and the effect was stronger than Ticlopidine.
Pharmaceutics. 2023 Aug 14;15(8):2135
Rabbit platelets
2, 4, 6, 8 μmol/L
5 minutes
Evaluate the inhibitory effect of Indobufen on AA-induced platelet aggregation. Results showed that Indobufen significantly inhibited platelet aggregation, and the effect was stronger than aspirin.
Pharmaceutics. 2023 Aug 14;15(8):2135
Rabbit plasma
20 mg/kg
5 days
Evaluate the effect of Indobufen on APTT, PT, and TT in rabbit plasma, results showed that Indobufen significantly prolonged APTT, PT, and TT.
Molecules. 2018 Jun 15;23(6):1452
platelets
0–128 mg/L
10 minutes
To evaluate the inhibitory effect of S- and R-indobufen on platelet aggregation. The S-form was more potent, whereas the R-form showed less inter-individual variation.
Transl Clin Pharmacol. 2018 Dec;26(4):160-165
Indobufen/吲哚布芬 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
SD rats
Gastric ulcer model
Oral gavage
20, 30, 40 mg/kg
Once daily for 8 consecutive days
Evaluate the effect of Indobufen on gastric ulcers. Results showed that the incidence of gastric ulcers in the low and medium dose Indobufen groups was significantly lower than that in the aspirin group, while the high dose group was higher than the aspirin group.
Pharmaceutics. 2023 Aug 14;15(8):2135
Mice
Bleeding time and clotting time model
Intragastric administration
160, 80, 40 mg/kg
Once daily for 5 days
Evaluate the effect of Indobufen on bleeding time and clotting time in mice, results showed that Indobufen significantly prolonged bleeding time and clotting time.
Molecules. 2018 Jun 15;23(6):1452
Wistar rats
Adenine-induced chronic kidney disease model
Oral
20 mg/kg/day
Once daily for 4 weeks and 8 weeks
To compare the effects of indobufen with warfarin in a rat model of adenine-induced CKD. Results showed that the degree of kidney fibrosis in the indobufen group was significantly lower than that in the DMSO and warfarin groups.
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