Pioneers of the Category

Updated: August 12, 2007

Lpath, Inc. is clearly the category leader in lipidomic-based therapeutics, an emerging field of medical science whereby bioactive signaling lipids are targeted for treating important human diseases (see description of lipidomics below). Through the pioneering efforts of Roger Sabbadini, Ph.D., the company's founder, Lpath was one of the first companies to recognize that bioactive lipid signaling molecules, like S1P and LPA can themselves be targets for rational drug design, and then Lpath unlocked the code to creating antibodies that inhibit the activity of bioactive lipids.

This unique ability is based on our ImmuneY2™ drug-discovery engine (patents pending) that has provided us a pipeline capability: We have already developed two functionally therapeutic monoclonal antibodies against bioactive lipids, Sphingomab™ (it binds to and inhibits S1P) and Lpathomab (it binds to and inhibits LPA), and have started working on three additional bioactive-lipid targets.

The Value of Lipidomics


The drug-development industry is decidedly protein-centric: Most all the drugs on the market (and most all the drug candidates in clinical trials) target a protein, with the next largest category being nucleic acids, which comprise only 2% of drug targets.

As recently stated in the article "Targeting sphingosine-1-phosphate for cancer therapy" [Sabbadini, et al, British Journal of Cancer, October 3, 2006]:

"The focus on proteins was a natural consequence of the science community's evolving understanding of biochemistry, which allowed researchers to identify potential protein targets involved in key metabolic and signaling pathways. Some of the first drugs developed by the rational-drug-design approach to the scientific method came after the discovery of key enzymes, receptors, and ion channels [all proteins] as they emerged in the basic science literature. One can argue that target identification now is driven by the technological developments of proteomics and genomics, both of which reflect the persistent 'protein-centric' view of drug discovery.

"Now, the field of lipidomics (a subset of 'metabolomics') has emerged...and provides new opportunities for drug discovery. As was the case for proteomics and genomics, tools of measurement led the way. For lipidomics, the development of electrospray tandem mass spectrometry and other tools has facilitated our understanding of the cellular lipidome, and we now believe that there are over 1,000 members of the lipidome, opening up an entire array of new potential targets for therapeutic interventions.

"It has been recognized that alterations in lipid metabolism can lead to cancer, cardiovascular disease, diabetes, neurodegenerative disorders, immune function, pain, mental disorders, and inflammation....

"Of late, the attractiveness of the sphingolipid group of bioactive lipids as targets has been fueled by the recent discovery, beginning largely in the mid-1990s, that many small-molecule lipid mediators are ligands for GPCRs (e.g., S1P and LPA), ion channels (e.g., SPC action on SCaMPER) and/or modulators of key kinases (e.g., SPH action on PKC) and transcription factors (e.g., LPA action on PPARγ)."

Lpath as Category Leader


Lpath has emerged as the category leader in lipidomic-based therapeutics because of its technological advantages in the two areas of expertise, (described below) that are key to this area of medical science:

  1. the study of lipidomics (i.e., understanding the role of bioactive lipids in their respective signaling systems) so that the right targets can be selected. The study of lipidomics is complex, as bioactive lipids are considerably smaller than proteins and, unlike proteins, they are not water-soluble. As such, many of the measurement and analytical tools that exist in our protein-centric world do not work when dealing with bioactive lipids. Because of its long-standing focus on bioactive lipids as targets for human disease, the company has developed an expertise and various tools and technologies (many of which are proprietary) to deal with these challenges.

  2. the ability to inhibit the chosen bioactive-lipid target. In this area, we are truly unique, as we believe we are the only company to have developed therapeutically functional monoclonal antibodies against bioactive lipids—and we have now done it twice. As described above, this unique ability is based on our ImmuneY2™ platform technology.

The table below illustrates the evolution of drug targets over time and the enviable positioning Lpath has attained:

Evolution of Targets for Drug Discovery
Wave I Wave IIa Wave IIb Wave III (emerging)
Target Foreign invaders Proteins [DNA, RNA to lesser] Proteins [DNA, RNA to lesser] Bioactive Lipids
Target I.D. Driven By What? Biology Physiology & Cell Biology Genomics & Proteomics Lipidomics [Lpath & a few others have this expertise]
Primary Drug Type(s) Vaccines & Antibodies Small molecules [mAbs later on] Small molecules & mAbs mAbs [Lpath has the expertise & patent; no one else does]