Antibody drug to treat LDL cholesterol REGN727 promising: Regeneron

REGN727, an antibody drug to control bad cholesterol being developed by sanofi-aventis and Regeneron, has been found promising.

REGN727 is a fully human antibody that targets Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9), a naturally-occurring molecule involved in regulating cholesterol levels by modulating low-density lipoprotein (LDL) cholesterol receptors.

In an interim efficacy analysis of a dose-escalating, randomized, double-blind, placebo-controlled, phase-1 trial in healthy volunteers, REGN727 achieved substantial, dose dependent decreases of LDL (bad) cholesterol.

LDL cholesterol levels in the blood have been shown to correlate with coronary artery disease risk, and lowering LDL has been proven to reduce the risk of cardiac events, such as death and heart attacks, in patients with coronary artery disease (CAD).

However, despite the relatively wide use of LDL cholesterol-lowering therapies, including the statin class of agents, coronary artery disease remains a leading cause of morbidity and mortality.

REGN727 is a fully human monoclonal antibody intended to robustly lower LDL cholesterol through a novel mechanism of action.

REGN727 is targeted at inhibiting PCSK9, which results in prevention of the degradation of LDL receptors in the liver and facilitates LDL clearance from the systemic circulation, thereby lowering LDL levels in the blood.

The trial is ongoing with both intravenous and subcutaneous routes of administration being studied.

At the highest dose tested to date, there was a highly significant lowering of mean LDL cholesterol that lasted for more than one month following a single dose, with a maximum mean reduction of more than 60 per cent.

There have been no serious adverse events and no dose limiting toxicities observed. Dose escalation is ongoing.

Regeneron Pharmaceuticals Inc has also provided an update on REGN475 (SAR164877) are being developed with sanofi-aventis under a global, strategic collaboration to discover, develop and commercialize fully human antibodies.

REGN475 is a fully human antibody that selectively targets nerve growth factor (NGF), a naturally-occurring molecule demonstrated to modulate pain.

In an interim efficacy analysis of a randomized, double-blind, four-arm, placebo-controlled phase-2 trial, in 217 patients with osteoarthritis of the knee, REGN475 demonstrated significant improvements at the two highest doses tested as compared to placebo in average walking pain scores over 8 weeks following a single intravenous infusion.

“We are extremely pleased by the productivity of our antibody collaboration with sanofi-aventis, and the progress of the NGF and PCSK9 antibodies, in particular,” stated Leonard S Schleifer, president and chief executive officer.

Regeneron will provide additional corporate and clinical updates at its first Investor Day in New York City on July 15.

Despite the availability of several classes of pain relievers, millions of Americans continue to suffer from moderate to severe pain due to a variety of medical disorders (e.g., osteoarthritis, cancer, inflammation, neuropathic diseases, etc.).

Regeneron is a biopharmaceutical company that discovers, develops, and commercializes medicines for the treatment of serious medical conditions.

In addition to Arcalyst (rilonacept) injection for subcutaneous use, its first commercialized product, Regeneron has therapeutic candidates in Phase 3 clinical trials for the potential treatment of gout, diseases of the eye (wet age-related macular degeneration and central retinal vein occlusion), and certain cancers.

Additional therapeutic candidates are in earlier stage development programs in rheumatoid arthritis and other inflammatory conditions, pain, cholesterol reduction, allergic and immune conditions, and cancer.