MyFatDog        

anacetrapib (MK-859) Being developed by Merck.  Anacetrapib is a cholesteryl ester transfer protein inhibitor (CETP inhibitor) that is being developed as a treatment to increase HDL levels. The results of the DEFINE trial showed that the drug reduced LDL by 40% in patients with moderate baseline LDL levels that were already undergoing under treatment with statins.  The drug also increased HDL elvels by 138%.  Anacetrapib did not show any effect on blood pressure which was seen in a study with a different drug in the same class.   A new study, REVEAL (Randomized EValuation of the Effects of Anacetrapib through Lipid-modification), will be conducted at mutiple worldwide sites to test if anacetrapib can reduce coronary events and heart attacks.  The study is planned to being in early 2011 and is expected to enroll  30,000 people that will be studied over a 4 year period.

eprotirome (KB2115) Being developed by Karo Bio.  Eprotirome is a thyroid receptor beta activator.  This drug is being developed as an add-on to conventional treatment to reduce LDL in patients with heterozygous familial hypercholesterolemia.  The drug was previously shown to lower triglyceride, LDL and Lp(a) levels on top of what was achieved with statin or ezetimibe treatment alone.  The company was unable to find a partner for phase III development of the drug and has been raising funds to conduct the phase III trial on their own.  The trial is expected to be conducted in Europe and will involve up to 1,150 patients treated over a 12-18 month period.  The trial is anticipated to begin in 2011 and will be conducted in 30-50 medical centers in 8-10 European countries.  The primary outcome will be a clinically relevant reduction in LDL levels when added to existing lipid-lowering treatment (primarily statins).

ETC-1002  (formerly ESP 55016) Being developed by Esperion Therapeutics. The drug inhibits enzymes within fatty acid and cholesterol synthesis pathways.  The drug is currently being tested for for its effect on reducing LDL choleserol levels.

GFT505 Being developed by Genfit.  GFT505 is a pan PPAR alpha/gamma/delta activator.  The drug is being developed as a treatment designed to decrease triglyceride levels and increase HDL levels.  Initial reports suggest beneficial effects on triglyceride and HDL levels at higher (100 mg and 60 mg vs. 30 mg) doses but the most recent study is using a slightly lower dose of 80 mg.  A recent short-term study showed that the drug was safe and effective when used in combination with simvastatin.   A study, GFT505-210-5, is currently underway in Europe to determine if the drug is effective in controlling hemoglobin A1C in patients with type 2 diabetes.  Secondary endpoints include other measures of glucose and lipid contraol as well as measures of inflammation which are thought to contribute to both diabetes and risk of heart disease.  Results are expected in mid-2011

GSK-256073 Being developed by GlaxoSmithKline.  GSK-256073 is a niacin receptor activator that is being developed to reduce plasma triglyceride levels and increase HDL levels.  Phase I clinical trials have been conducted to see if this drug can minimize niacin-induced flushing when given in combination with niacin.  According to the company's website, phase II studies have been conducted to detemine the effect of the drug on plasma lipids in subjects with dyslipidemia.  The drug is also be tested to determine if it is able to reduce glucose levels in patients with type 2 diabetes.

JTT-130  Being developed by Akros Pharma, a subsidiary of Japan Tobacco.  JTT-705 is an intestine-specific MTP inhibitor.  This drug is being developed to reduce the production of chylomicrons, particles that carry dietary fat into blood.  This drug is being developed to reduce chylomicron, VLDL and LDL levels.  A study testing the safety and effectiveness in patients wth diabetes was completed in July 2010.

JTT-302 Being developed by Akros Pharma, a subsidiary of Japan Tobacco. JTT-302 is a cholesteryl ester transfer protein inhibitor that is being developed as a treatment for dyslipidemia. 

LY2484595  Being developed by Eli Lilly and Co.  LY2484595  is a cholesteryl ester transfer protein inhibitor that is being developed as a treatment for dyslipidemia. There is an ongoing study that is looking at the effectiveness of the drug in patients that are currently being treated with statins.  The study is expected to be completed in May 2011.

MBX-8025  Being developed by Metabolex.  MBX-8025 (formerly RWJ-800025) is a PPAR delta activator.  It is being developed as a treatment to reduce LDL choelsterol levels and to increase HDL cholesterol levels.  The drug has been reported to be safe when used alone and in combination with atorvastatin.  Treatment resulted in triglyceride and LDL lowering and an increase in HDL.  It was also reported that the drug was effective in reducing insulin and blood glucose.  There has been no news on this compound since 2008 so its development status is unclear.

Rilapladib Being developed by GlaxoSmithKline.  Rilapladib is an inhibitor of lipoprotein-associated phospholipase A2 (LP-PLA2 inhibitor) which is being developed as a treatment to reduce the formation of pro-atherogenic LDL.  It has also been tested for its effects on platelet aggregation.  A study testing the effect of the drug on the stability of atherosclerotic plaque has been completed although the results have not been announced.

RVX-208 (RVX000222) Being developed by Resverlogix.  The exact structure of RVX-208 has not been disclosed although it is described as being a member of the quinazoline family.  A 13 week phase II study, ASSERT, did not meet the primary and secondary endopoints of increasing apoA-I and HDL.  There was also a significant increase in liver enzymes and a trend towards an increase in creatinine which is used to monitor kidney function.  As a result, a second study ASSURE will proceed in Q1 of 2011 after having its enrollment procedure reassessed.  The primary endoing of the ASSURE study is regression of atherosclerotic plaque volume with secondary endpoints being change in apoA-I, HDL and HDL subclass.  An exploratory endpoint is the change in plaque composition which has been associated with a beneficial change in plaque stability in other studies.  The ASSURE study currently has 43 sites confirmed although Investigational Review Board approval, which is required for the study to begin, has not been obtained as of November 2010. 

SLx4090  Being developed by Surface Logix.  SLx4090 is an intestinal-specific MTP inhibitor.  This drug is being developed to reduce the production of chylomicrons, particles that carry dietary fat into blood.  This drug is being developed to reduce chylomicron, VLDL and LDL levels.  All clinical trials with this compound are listed as being completed as of December 2009 although no results have been announced.

TRIA-662 Being developed by Cortria.  TRIA-662 is a niacin derivative that is reported to be "flush-free" meaning that the drug does not cause the subcutaneous flshing that is associated with niacin or extended release niacin use.  The drug is being developed as a treatment of dyslipidemia (high triglcyeride levels, high LDL cholesterol levels, low HDL cholesterol levels.  A study testing the effectiveness of the drug on lowering plasma triglyceride levels is listed as completed as of March 2010 but no results have been announced.

Phase II – If a drug is found to be safe in phase I studies it can, following approval of the FDA, move to phase II.  Phase II studies involve treatment of patients with the disease or condition that the drug is intended for.  Phase II studies usually involve more patients (about 100) than phase I studies and last for a longer duration at 1-2 months.  The objective of phase II is to demonstrate both safety and clinical benefit.