new cholesterol-lowering drug in development 
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 new cholesterol-lowering drug in development


> ISIS 301012 - ISIS 301012 reduces the production of apolipoprotein
> B-100, or apoB-100, which is the protein that carries certain forms of
> cholesterol and triglyceride particles in the {*filter*}stream.
> Cholesterol can be carried in the {*filter*}stream in a variety of forms,
> with high-density lipoprotein, or HDL, being the good form, and low-
> density lipoproteins or LDL, and very low-density lipoproteins, or
> VLDL, being the bad or atherogenic forms, which are directly involved
> in heart disease.  ApoB-100 is a target that the pharmaceutical
> industry has long recognized as attractive for intervention but that
> has proved to be undruggable using traditional small molecule
> approaches.

> We are developing ISIS 301012 as a new treatment for high cholesterol.
> We plan to develop ISIS 301012 for patients who are unable to achieve
> target cholesterol levels with statins alone, as well as for patients
> who are intolerant of statins. This is a large market opportunity. In
> the U.S. alone, over 16 million patients in the High Risk category are
> not meeting target LDL-cholesterol of less than 100 mg/dL and are in
> need of additional therapies to complement current lipid lowering
> {*filter*} including statins.

> We are also developing ISIS 301012 for patients with familial
> hypercholesterolemia, or FH, a genetic disorder that causes extremely
> high cholesterol levels-often exceeding 500 mg/dL-and results in the
> early onset of heart disease. The FDA granted ISIS 301012 Orphan Drug
> Designation for treatment of patients with homozygous FH, providing a
> potentially accelerated pathway to commercialization because of the
> unmet need in this very high risk patient population.

> We are conducting Phase 2 trials in patients with FH in preparation
> for initiating later this year pivotal studies to support filing with
> the FDA for approval of ISIS 301012 for these patients. In parallel,
> we are conducting Phase 2 trials to address the large commercial
> market represented by the traditional population of patients with high
> cholesterol who are not reaching their target cholesterol levels.

> In March 2007, we reported positive results from three Phase 2 studies
> of ISIS 301012. In a Phase 2 study of ISIS 301012 as a single agent in
> patients with high cholesterol, ISIS 301012 produced rapid, prolonged
> dose-dependent reductions in apoB-100, LDL-cholesterol, and other
> atherogenic lipids. At a dose of 300 mg/week for three months, ISIS
> 301012 reduced LDL-cholesterol and triglycerides by 62% and 43%,
> respectively, and at a dose of 400 mg/week for ten weeks, ISIS 301012
> lowered apoB-100 to at or below the lower limit of normal in 8 of 8
> patients and to undetectable levels in 4 of 8 patients, with a median
> LDL-cholesterol reduction of 70%. In another Phase 2 clinical trial,
> patients with high cholesterol on stable doses of statins who received
> up to 400 mg/week of ISIS 301012 for five weeks achieved median
> reductions of up to 52% in LDL-cholesterol and up to 41% in
> triglycerides beyond the levels achieved with statins alone. In a
> small study that included three homozygous FH patients treated for
> three months with 300 mg/week of ISIS 301012 added to their ongoing
> maximally-tolerated lipid-lowering therapies, including high-dose
> statins, the patients achieved 45%, 50% and 51% additional reductions
> in LDL-cholesterol, with similar reductions in apoB of 45%, 43% and
> 54%. ISIS 301012 has been well tolerated, both as a single agent and
> when coadministered with statins, in both routine high cholesterol
> patients and patients with familial hypercholesterolemia.

> We are continuing the development of ISIS 301012 in the studies
> described above; later in 2007 we plan to announce results of the
> heterozygous FH study and results of the three-month dosing of routine
> high cholesterol patients; ISIS 301012 is being coadministered with
> statins in each of these studies.  We also expect to update results of
> the homozygous FH study, and initiate both a longer term Phase 2 study
> for the general high cholesterol patient populations, and a pivotal
> study to support registration for FH.  We intend to license ISIS
> 301012 to a partner for Phase 3 development, registration and
> marketing for the general high cholesterol population.

> In April 2006, we entered into a collaboration with Symphony Capital
> Partners, L.P. and a group of co-investors to form Symphony GenIsis,
> Inc., which was capitalized with $75 million to be used exclusively
> for the development of ISIS 301012 and two diabetes {*filter*}, ISIS
> 325568, targeting GCGR, and ISIS 377131, targeting GCCR. This
> collaboration has allowed us to advance ISIS 301012 through key Phase
> 2 milestones prior to licensing, adding value to the drug. (return to
> top)

> *  *  *
> The above is from the web site of ISIS Pharmaceuticals.  As you might
> expect, the studies they are doing are only measuring the drug's
> effect on lipids.

> Marilyn

Wiser to eat less, down to the optimal amount, to become healthier
(hungrier) thereby losing the VAT and curing the hypercholesterolemia.

Be hungry... be healthy... be hungrier... be blessed:


Prayerfully in Jesus' awesome love,

Andrew <><
Andrew B. Chung, MD/PhD

Sun, 21 Feb 2010 21:16:06 GMT
 [ 1 post ] 

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