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. There is an ongoing study that is also looking at the effectiveness of the drug in lowering LDL levels in patients that are currently being treated with statins.  The study is expected to be completed in 2010.

eprotirome (KB2115) Being developed by Karo Bio.  Eprotirome is a thyroid receptor beta activator.  This drug is being developed as a second-line treatment to reduce LDL cholesterol levels in patients in whom more conventional therapy is not effective in reaching treatment goals.  The drug was recently shown to lower triglyceride, LDL and Lp(a) levels on top of what was achieved with statin or ezetimibe treatment alone.  The company plans to search for a partner for phase III development of the drug.

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.  According to the company phase II studies using a dose of 80 mg are currently underway.  A recent short-term study showed that the drug was safe and effective when used in combination with simvastatin. 

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 are underway to detemine the effect of the drug on plasma lipids in subjects with dyslipidemia.

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.

R1439 (aleglitezar) Being developed by Roche.  R1439 is a dual PPAR alpha/gamma activator designed to lower triglyceride levels and increase HDL levels.  The drug would also be expected to improve insulin sensitivity in insulin-resistant patients and it appears that it is being developed primiarily as an anti-diabetes drug .  A study testing the abilty of the drug to improve diabetes has recently been completed and showed that aleglitazar is effective in lowering LDL and triglcyrides and can also increase HDL levels.  The drug does casue a significant increase in creatinine which could be casue for concern.  A phase III study testing the benefit of treatment with aleglitazar in patients with acute coronary syndrome and type 2 diabetes is scheduled to begin in March 2010.

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 is expected to be completed in April 2010.

RVX000222 (RVX-208)  Being developed by Resverlogix.  The mechanism of action of RVX-208 has not been disclosed.  The compound is being developed as a treatment to enhance apoA-I production and increase HDL levels.  This is consistent with activation of one of several potential nuclear receptors.

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.  A study testing the benefit of adding the drug to statin treatment was completed in September 2009.

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 choelsterol levels.  A study testing the effectiveness of the drug on lowering plasma triglyceride levels was completed in December 2008 but no news has been released since then.

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.