Bezafibrate

361.82

361.82

255-567-9

Y9449Q51XH

758174

DTXSID3029869

C87449

C10AB02|C - Cardiovascular system

29242990

75.6

3.8

solid

1.260±0.06 g/cm3(Predicted)

186 °C

572.1°C at 760 mmHg

299.8ºC

1.583

DMF: soluble

Refrigerator

LD50 oral in rat: 1082mg/kg

177.3 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]|183.8 Ų [M-H]-

1

22

36

UE8755000

Xn

Stable at normal temperatures and pressures.

P201, P202, P264, P270, P281, P301+P312, P308+P313, P330, P405, P501

H302

|Warning|H302 (50.48%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P264, P270, P281, P301+P312, P308+P313, P330, P405, and P501|Aggregated GHS information provided by 105 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

94-96% of bezafibrate is bound to protein in human serum.

For the treatment of primary hyperlipidaemia types IIa, IIb, III, IV and V (Fredrickson classification) corresponding to groups I, II and III of the European Atherosclerosis Society guidelines - when diet alone or improvements in lifestyle such as increased exercise or weight reduction do not lead to an adequate response. Also for the treatment of secondary hyperlipidaemias, e.g. severe hypertriglyceridemias, when sufficient improvement does not occur after correction of the underlying disorder (e.g. diabetes mellitus).

Bezafibrate has known transformation products that include 3-[(4-chlorobenzoyl)amino]propanoic acid.

Bezafibrate is an antilipemic agent that lowers cholesterol and triglycerides. It decreases low density lipoproteins and increases high density lipoproteins. Bezafibrate lowers elevated blood lipids (triglycerides and cholesterol). Elevated VLDL and LDL are reduced by treatment with bezafibrate, whilst HDL-levels are increased. The activity of triglyceride lipases (lipoprotein lipase and hepatic lipoproteinlipase) involved in the catabolism of triglyceride-rich lipoproteins is increased by bezafibrate. In the course of the intensified degradation of triglyceride-rich lipoproteins (chylomicrons, VLDL) precursors for the formation of HDL are formed which explains an increase in HDL. Furthermore, cholesterol biosynthesis is reduced by bezafibrate, which is accompanied by a stimulation of the LDL-receptor-mediated lipoprotein catabolism. Elevated fibrinogen appears to be an important risk-factor, alongside the lipids, smoking and hypertension, in the development of atheroma. Fibrinogen plays an important role in viscosity, and therefore blood flow, and also appears to play an important role in thrombus development and lysability. Bezafibrate exerts an effect on thrombogenic factors. A significant decrease in elevated plasma fibrinogen levels can be achieved. This may lead, amongst other things, to a reduction in both blood and plasma viscosity. Inhibition of platelet aggregation has also been observed. A reduction in blood glucose concentration due to an increase in glucose tolerance has been reported in diabetic patients. In the same patients, the concentration of fasting and postprandial free fatty acids was reduced by bezafibrate.

Substances that lower the levels of certain LIPIDS in the BLOOD. They are used to treat HYPERLIPIDEMIAS. (See all compounds classified as Hypolipidemic Agents.)

Bezafibrate is almost completely absorbed after oral administration. The relative bioavailability of bezafibrate retard compared to the standard form is about 70%.

Hepatic.

1-2 hours

It is generally accepted that bezafibrate is likely an agonist of PPAR-alpha. However, certain other investigations have also suggested that the substance might also elicit some effects on PPAR-gamma and PPAR-delta too.

Azufibrat

Pharmaceuticals -> Cardiovascular system -> Lipid modifying agents -> Lipid modifying agents, plain -> Fibrates -> Antilipemics