Muraglitazar
Encyclopedia
Muraglitazar is a peroxisome proliferator-activated receptor
agonist with affinity to PPARα and PPARγ.
The drug had completed phase III clinical trials, however in May, 2006 Bristol-Myers Squibb
announced that it had discontinued further development.
Data on muraglitazar is relatively less due to the recent introduction of this agent. One double-blind randomized clinical trial comparing muraglitazar and pioglitazone
found that the effects of the former were favourable in terms of HDL-C increase, decrease in total cholesterol
, apolipoprotein B
, triglyceride
s and a greater reduction in HbA1c
(P<0.0001 for all comparisons). However, the muraglitazar group had a higher all-cause mortality, greater incidence of edema
and heart failure and more weight gain compared to the pioglitazone group. A meta-analysis
of the phase 2 and 3 clinical trials of muraglitazar revealed that it was associated with a greater incidence of myocardial infarction
, stroke, transient ischemic attack
s and CHF
when compared to placebo or pioglitazone.
Peroxisome proliferator-activated receptor
In the field of molecular biology, the peroxisome proliferator-activated receptors are a group of nuclear receptor proteins that function as transcription factors regulating the expression of genes...
agonist with affinity to PPARα and PPARγ.
The drug had completed phase III clinical trials, however in May, 2006 Bristol-Myers Squibb
Bristol-Myers Squibb
Bristol-Myers Squibb , often referred to as BMS, is a pharmaceutical company, headquartered in New York City. The company was formed in 1989, following the merger of its predecessors Bristol-Myers and the Squibb Corporation...
announced that it had discontinued further development.
Data on muraglitazar is relatively less due to the recent introduction of this agent. One double-blind randomized clinical trial comparing muraglitazar and pioglitazone
Pioglitazone
Pioglitazone is a prescription drug of the class thiazolidinedione with hypoglycemic action.Pioglitazone is marketed as trademarks Actos in the USA, Canada, the UK and Germany, Glustin in Europe,"Glizone" and "Pioz" in India by Zydus CND and USV respectively and Zactos in Mexico by Takeda...
found that the effects of the former were favourable in terms of HDL-C increase, decrease in total cholesterol
Cholesterol
Cholesterol is a complex isoprenoid. Specifically, it is a waxy steroid of fat that is produced in the liver or intestines. It is used to produce hormones and cell membranes and is transported in the blood plasma of all mammals. It is an essential structural component of mammalian cell membranes...
, apolipoprotein B
Apolipoprotein B
Apolipoprotein B is the primary apolipoprotein of low-density lipoproteins , which is responsible for carrying cholesterol to tissues. While it is unclear exactly what functional role APOB plays in LDL, it is the primary apolipoprotein component and is absolutely required for its formation...
, triglyceride
Triglyceride
A triglyceride is an ester derived from glycerol and three fatty acids. There are many triglycerides, depending on the oil source, some are highly unsaturated, some less so....
s and a greater reduction in HbA1c
Glycosylated hemoglobin
Glycated hemoglobin is a form of hemoglobin that is measured primarily to identify the average plasma glucose concentration over prolonged periods of time. It is formed in a non-enzymatic glycation pathway by hemoglobin's exposure to plasma glucose...
(P<0.0001 for all comparisons). However, the muraglitazar group had a higher all-cause mortality, greater incidence of edema
Edema
Edema or oedema ; both words from the Greek , oídēma "swelling"), formerly known as dropsy or hydropsy, is an abnormal accumulation of fluid beneath the skin or in one or more cavities of the body that produces swelling...
and heart failure and more weight gain compared to the pioglitazone group. A meta-analysis
Meta-analysis
In statistics, a meta-analysis combines the results of several studies that address a set of related research hypotheses. In its simplest form, this is normally by identification of a common measure of effect size, for which a weighted average might be the output of a meta-analyses. Here the...
of the phase 2 and 3 clinical trials of muraglitazar revealed that it was associated with a greater incidence of myocardial infarction
Myocardial infarction
Myocardial infarction or acute myocardial infarction , commonly known as a heart attack, results from the interruption of blood supply to a part of the heart, causing heart cells to die...
, stroke, transient ischemic attack
Transient ischemic attack
A transient ischemic attack is a transient episode of neurologic dysfunction caused by ischemia – either focal brain, spinal cord or retinal – without acute infarction...
s and CHF
Congestive heart failure
Heart failure often called congestive heart failure is generally defined as the inability of the heart to supply sufficient blood flow to meet the needs of the body. Heart failure can cause a number of symptoms including shortness of breath, leg swelling, and exercise intolerance. The condition...
when compared to placebo or pioglitazone.