DYSLIPIDEMIA
Cardiovascular diseases remain the leading cause of death and
kills approximately 17 million people per year.
Dyslipidemia currently affects approximately 10% of
the global population. There is an increasing
prevalence and medical need for lipid-modifying
drugs in obese and type 2 diabetic patients. A high
proportion of type 2 diabetic patients have abnormal
concentrations of lipoproteins. In the US, Japan and
Europe there are more than 240 million people with
abnormal lipoprotein levels. Of these, more than 55
million have low high density lipoprotein (HDL)
and/or high triglyceride levels.
Around 5-8% of the population are intolerant
(contraindicated, non-responsive, or develop serious
side effects) towards statins. Significantly higher
percentages of patients on statins have an inadequate
overall response and do not obtain the desired lipid
profile. These factors are driving the market towards
combination therapies that provide additive or
synergistic benefits.
SLx-4090
is a novel Microsomal Triglyceride
Transfer Protein (MTP) inhibitor that is in development for the treatment of mixed dyslipidemia.
Designed to act selectively in the enterocytes lining the gastrointestinal
tract, SLx-4090 prevents the formation of chylomicrons which are used to transport triglyceride (TG)
and cholesterol into the systemic circulation. The novelty of SLx-4090 is that it is selective for
enterocytes and is not absorbed into the systemic circulation. Previous MTP inhibitors have acted
both in the intestine and in the liver, causing fat build up in the liver, an unacceptable toxicity.
SLx-4090 has completed Phase 1 studies which have confirmed that it is active in the gut significantly
blocking fat absorption, but the drug is not present in the systemic circulation. A Phase 2a study is
in progress. |