MyFatDog        

apoA-I Milano (ETC-216) (The Medicines Company under licencse from Pfizer).  Commonly referred to as "Drano for the heart" since it was shown to rapidly reduced atheroclerotic plaque in earlier clinical studies, this is a synthetic HDL containing recombinant apoA-I (Milano). This drug was initially developed by Esperion which was subsequently purchased by Pfizer.  Esperion re-emerged as a private company while Pfizer retained the rights to ETC-216.

BI-204 (anti oxLDL)   Being co-developed by Genentech and BioInvent.  This compound is an antibody to oxidized LDL.  This drug is being developed to reduce levels of oxidized LDL in plasma and has completed a successful phase I trial.  The company recently (January 2010) announced that they plan to raise money to move their pipeline drugs forward. 

DB959  Being developed by Dara Biosciences.  DB959 is a dual PPAR gamma/delta activator.  The drug is being developed as a way to improve insulin sensitivity in diabetics as well as a way of improving the plasma lipoprotein profile in these patients.

DRL-17822  Being developed by Dr. Reddy's Labs.  DRL-17822 is a cholesteryl ester transfer protein inhibitor (CETP inhibitor) that is being developed as a treatment to increase HDL levels. 

ETC-1002  Being developed by Esperion Therapeutics. The mechanism by which ECT-1002 works hasn't been publicized but it sounds like it is some type of nuclear receptor activator that reduces fat and cholesterol synthesis and increased fat breakdown.

MB07811 Being developed by Metabasis (acquired by Ligand).  MB07811 is a thyroid receptor beta activator.  This drug is being developed as a treatment to reduce LDL cholesterol and triglyceride levels alone and in combination with a statin.  Data from phase I studies showed that the drug could lower LDL and triglyceride levels.  Higher doses of the drug were associated with mild increases in liver enzymes and shifts in thyroid hormone levels.   A subsequent study was discontinued and it is likely that the drug has been discontinued also.  Ligand has reported that they are working on developing second generation thyroid receptor beta activators.

REGN727 Being developed by Regeneron.  REGN727 is an antibody that binds to PCSK9.  When adminstered this will interfere with PCSK9 and allow more LDL to be cleared fromthe blood resulting in LDL lowering.  A phase I study is underway with results expected in late 2010.

Sobetirome (QRX-431) Being developed by QuatRx.   Sobetirome is a thyroid receptor beta activator.  This drug is being developed as a treatment to reduce LDL cholesterol levels.  Initial studies indicate that the drug is safe and well-tolerated and significantly lowers LDL and Lp(a) levels.  The drug also significantly reduced body weight by 3-4% in 7 days.  No new news on this drug has been reported since January 2008 so it appears to be stalled in development.

Phase I – Once a new drug has demonstrated that it is safe and effective in animals the company can file an Investigational New Drug (IND) application with the FDA.  This allows for limited testing in humans.  Initial testing is usually done in a small number (about 20) of normal volunteers.  The drug is first tested at a very low dose and then the dose is increased to a dose that is thought to be effective for treating disease.   The duration of treatment in phase I is fairly short at 1-2 weeks.