Correction: High not "Hit" Throughput Screening

Yesterday, I posted a piece on "hit'  throughput screening (see below).  At the time, I learned about  'hit" throughput screening, I mentioned that  I had never heard of "hit" throughput screening but I did know about high throughput screening.  As it turns out, there was a problem in translation and in fact, there is no such thing as hit throughput screening and it is actually high throughput screening.  Mea Culpa!  I apologize for the error and in the future I will be assiduous in my fact checking before I post (a lesson that the boneheads in the Obama administration learned the hard way in the recent Sherrod brouhaha)

The Growth of High Throughput Screening

No; this isn’t a typo! My colleagues at Meet the Boss sent me a press release today about efforts underway at Pfizer and GlaxoSmithKline to redefine HTS to mean “hit” throughput screening rather than high throughput screening. As many of you may know, high throughput screening which began in the mid 1990s was supposed to revolutionize drug discovery and development—it did not! Nevertheless, after almost 15 years of refinement it appears that the technology may be paying off and can be used as an adjunctive tool to expedite and lower the cost of small molecule and protein-based drug discovery. While I don’t know much about this emerging technology, the press release presented below suggests that a meeting about HTS may be in the works. 

It is understood that huge amounts of money have been invested into drug discovery and the biggest problem faced by the industry is investing in drugs which may not make it onto the market. Europe has always been seen to trail behind the US when discussing drug discovery within the pharmaceutical industry, but with the biotechnology revolution they have begun to catch and becoming a driving force within the global industry.

The NGP EU committee has been celebrating the success of their pioneering roles in genome sequencing and the development of proteomic. Pfizer has recently announced to the NGP Drug Discovery committee that they plan to roll out a hit identification and screening file strategy. The process will offer a new flexible strategy for hit identification while sculpting a more reliable and efficient screening process. 

High throughput screening (HTS) has grown rapidly over the last ten years and Pfizer themselves noted the huge advances in both detection technology and laboratory automation. Pfizer believe that not only big Pharma but also smaller companies can implement HTS as well. By implementing HTS,  it can remove the indecision over which compunds will be profiles, many smaller companies agonize over the costs of conventional profiling sometimes only choosing between 10 and 20 compounds, this already removes other possibilities before true research can really begin. Pfizer among other members of the NGP EU Drug Discovery committee wish to discuss how they wish to implement large scale profiling at a lower cost, while maintaining the incredible biological, technological, and scientific advancements they are already demonstrating globally.

GSK have also joined Pfizer recently in encouraging the implementation of HTS. “We are now at a stage where we can exploit the benefits of cutting edge technology for increased quality, performance and capabilities. We also have the option to supply the same number of compounds, with the same level of quality at an affordable price”. 

Key to discussions will be representatives from AstraZeneca - Goran Wennberg, VP Discovery Information, Bayer Schering Pharma - Andreas Busch, Head of Global Drug Discovery & Member of the Board , Novartis - Olivier Grenet , Group Head of Genome Biology ,GlaxoSmithKline - Tino Rossi, VP of PreClinical Drug Discovery & Enabling Technologies and Pfizer - John Mathias, Head of High Through Put Screening all determined to firmly place Europe as the Drug Discovery capital.

The discovery and implementation of HTS not only offers an opportunity to smaller Pharma companies but also the consumer, if research and quality is increased and cost decreased this in turn will be passed onto the consumer.

Stay tuned for more details.

Until next time...

Good Luck and Good Job Hunting

 

The End of an Era: Ligand Pharmaceuticals to Buy Pharmacopeia for $70 Million in a Stock Deal

New Jersey-based Pharmacopeia, the first-ever combinatorial chemistry company, announced that it had agreed to be purchased by Ligand Pharmaceuticals in a stock deal worth about $70 million. Onetime a leader in combinatorial chemistry and high throughput screening, Pharmacopeia has struggled of late after it jettisoned its profitable molecular modeling division several years ago. While the company was able to advance several of its lead compounds into early phase clinical testing, its  longtime business model, predicated on multiple, small discovery deals with large pharmaceutical companies, was unable to provide enough capital to continue to sustain operations.

Pharmacopeia was established in 1993 after its founders licensed from Columbia University several of the first issued combinatorial chemistry patents. The company was a pioneer in combinatorial chemistry (and subsequently high throughput screening) and was the first to publicly tout the virtues of combinatorial chemistry in drug discovery. By the mid-1990s, many pharmaceutical companies had embraced combinatorial chemistry as the “next big thing” and began eliminating traditional natural product and medicinal chemistry jobs. The industry’s love affair with combinatorial chemistry grew so strong that many companies (most notably Merck), completely eliminated their natural products discovery departments in the late 1990s. Unfortunately, the role of combinatorial chemistry in drug discovery never lived up to its promised potential and was largely abandoned in the early 2000s. Although combinatorial chemistry is now part of the modern day drug discovery paradigm, this onetime “shining star” has largely been relegated to a minor supporting role.

I first became acquainted with Pharmacopeia in 1994 after I took a job with Transcell Technologies, a now-defunct biotechnology company that was co-located with Pharmacopeia in a research facility in Monmouth Junction, NJ. While Transcell and Pharmacopeia shared a cafeteria and some common laboratory equipment, Pharmacopeia employees were strictly forbidden to talk with Transcell employees— lest they inadvertently divulge proprietary combinatorial chemistry concepts that might jeopardize the company’s future. Coincidentally, a guy who lived two doors down from my family and me turned out to be Pharmacopeia’s in-house intellectual property attorney. Although, Ron and I became good friends, he was also extremely tight-lipped about the “goings-on” at Pharmacopeia. Privately-held Pharmacopeia went public in 1995 and at one time, its market capitalization was almost $1.0 billion.

By any reckoning, a 15-year run is outstanding for a biopharmaceutical company. However, as the old adage goes, “All good things must come to an end.” At present, it is not clear, whether or not California-based Ligand will relocate the company or cut jobs. Nevertheless, Pharmacopeia’s impending demise sends a clear signal that the golden age of combinatorial chemistry has ended!

Until next time….

Good Luck and Good Job Hunting!!!