Tricor (fenofibrate)
The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
Primary hypercholesterolemia, mixed lipidemia and hypertriglyceridemia
General Information
TriCor (fenofibrate), previously available as capsules, is now
approved in a tablet formulation. TriCor tablets have been
developed to assist patients in managing their cholesterol levels.
The drug is indicated for use in reducing elevated LDL-C, Total-C,
triglycerides and Apo-B and increasing HDL-C in patients with
primary hypercholesterolemia or mixed lipidemia. The drug has also
been approved as adjunctive therapy for the treatment of
hypertriglyceridemia, a disorder characterized by elevated levels
of very low density lipoprotein (VLDL) in the plasma.
Clinical Results
TriCor (160 mg per day) was evaluated in four randomized,
placebo-controlled, double-blind, parallel-group trials as a
therapy for hypercholesterolemia and mixed dyslipidemia. Treatment
with TriCor was shown to lower LDL-C, Total-C, the LDL-C/HDL-C
ratio and triglycerides, in addition to raising HDL-C. Apo-B levels
were also measured in a subset of subjects. Compared to placebo,
treatment with TriCor significantly reduced Apo-B from baseline to
endpoint.
The effect of TriCor on serum triglycerides was evaluated in two
randomized, double-blind, placebo-controlled trials that included
147 hypertriglyceridemic subjects. Treatment was administered for
eight weeks in both trials. The trials differed in terms of initial
subject triglyceride (TG) levels; one entered subjects with
baseline TG levels of 500 to 1500 mg/dL, and the other entered
subjects with TG levels of 350 to 500 mg/dL. In subjects with
hypertriglyceridemia and normal cholesterolemia with or without
hyperchylomicronemia, treatment with TriCor decreased very low
density lipoprotein (VLDL) triglycerides and VLDL cholesterol.
Side Effects
Adverse events reported by subjects treated with TriCor in
clinical trials include (but are not limited to) the following:
- Respiratory symptoms
- Back pain
- Abdominal pain
- Abnormal liver function tests
- Headache
Individuals with serious liver, kidney or gallbladder disease
should not take TriCor.
Mechanism of Action
Fenofibric acid, the active metabolite of fenofibrate, produces
reductions in total cholesterol, LDL cholesterol, apolipoprotein B,
total triglycerides and triglyceride rich lipoprotein (VLDL) in
treated patients. In addition, treatment with fenofibrate results
in increases in high density lipoprotein (HDL) and apoproteins
apoAI and apoAII.
The effects of fenofibric acid seen in clinical practice have
been explained in vivo in transgenic mice and in vitro in human
hepatocyte cultures by the activation of peroxisome proliferator
activated receptor alpha (PPAR alpha). Through this mechanism,
fenofibrate increases lipolysis and elimination of
triglyceride-rich particles from plasma by activating lipoprotein
lipase and reducing production of apoprotein C-III (an inhibitor of
lipoprotein lipase activity). The resulting fall in triglycerides
produces an alteration in the size and composition of LDL from
small, dense particles (which are thought to be atherogenic due to
their susceptibility to oxidation), to large buoyant particles.
These larger particles have a greater affinity for cholesterol
receptors and are catabolized rapidly. Activation of PPAR alpha
also induces an increase in the synthesis of apoproteins A-I, A-II
and HDL-cholesterol.
Fenofibrate also reduces serum uric acid levels in hyperuricemic
and normal individuals by increasing the urinary excretion of uric
acid. (from TriCor tablets Prescribing Information)
Additional Information
