MyFatDog        

AMG-145 Being developed by Amgen.  AMG-145 is an antibody to the protein PCSK9 that is being developed as a treatment for elevated LDl levels.  A phase I study that is underway is expected to be completed in October 2011.

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 announced that expect to begin a phase II trial that examines the change in atherosclerotic plaque inflammation in early 2011.

BMS-844421(BMS-PCSK9Rx)  Being co-developed by Bristol-Myers Squibb and Isis Pharmaceuticals. PCSK9 antisense is a drug that reduces plasma levels of PCSK9, a protein that targets the LDL receptor for degradation.  This drug is being developed as a treatment to lower LDL levels.  A phase I study was terminated so the status of this drug is currently unknown.

Cerenis-001  Being developed by Cerenis Therapeutics.  This drug is a apoA-I mimetic peptide that is designed to increase reverse cholesterol transport. A phase I study showed that the drug was well tolerated.  Phase II studies are expected towarsd the end of 2010.

CSL112 Being developed by CSL Limited.  CSL112 is a reconstituted HDL that is being developed as a treatment to increase HDL levels and stimulate cholesterol removal from tissues (reverse cholesterol transport). The percursor to CSL112 was a similar compound, CSL111 that had progressed to phase II studies. CSL111 appears to have been discontinued following  a study that showed that the drug was no better than placebo in reducing atherosclerosis.  CSL112 is reported to be more potent than CSL111.  A phase I study is currently underway and is expected to be completed in May 2011.

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.  Results from phase I indicate that the drug is able to increase HDL from 51-111% and reduce LDL from 25-56%.

IMO-3100  Being developed by Idera Pharmaceuticals.   IMO-3100 is a compound that blocks the action of two receptors, Toll-like receptors (TLR) 7 and 9, that turn on inflammatory pathways in cells.  Although intially developed to treat inflammation, IMO-3100 has been shown to effectively reduce LDL in preclinical studies in mice and may prove to be of benefit in improving diseases with generalized inflammation such as the metabolic syndrome.

MDCO-216 (formerly 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 an earlier clinical study, this is a synthetic HDL containing recombinant apoA-I (Milano).   Clinical studies with MDCO-216 are expected to begin in 2011.

MP-136 Being developed by Mitsubishi Tanabe Pharma.  MP-136 is a PPAR alpha activator being developed as a treatment for dyslipidemia.

NCX6560 Being developed by NicOx.  NCX6560 is a new statin drug that also has vasodilatory properties.  This drug is being developed to lower LDL levels and to enhance vasodilation.  A phase Ib study showed that the highest dose was able to lower LDl levels by 57% which was similar to what was acieved with atorvastatin.

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 showed that LDL could be lowered by up to 60% for more than 1 month in patients taking statins after a single dose of the drug.  Phase II studies are expected to begin in 2011.

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.

TA-8995 Being developed by Mitsubishi Tanabe Pharma.  TA-8995 is a cholesteryl ester transfer protein inhibitor (CETP inhibitor) that is being developed as a treatment to increase HDL and reduce LDL levels. 

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.