Sigma(R) Life Science Begins Licensing Efflux Transporter Knockout Human Cell-Based Assays to CROs and Pharmaceutical Companies Performing ADME Studies

Published: Oct 15, 2012

ST. LOUIS, Oct. 15, 2012 /PRNewswire/ -- Sigma-Aldrich® Corporation (Nasdaq: SIAL) today announced that Sigma Life Science, its innovative biological products and services business, initiated a licensing program aimed at contract research organizations (CROs) and pharmaceutical companies for its novel CompoZr® Transporter Knockout Cell Lines for preclinical ADME screening and safety studies. Complete functional knockouts of transporters in the intestinal cell line (Caco-2) enables identification of critical safety and efficacy characteristics compared to current chemical inhibitor-based assays and more precise determination of a drug candidate's potential drugdrug interactions. Cyprotex, a leading ADME-Tox service company with sites in both the UK and USA, is the first non-exclusive licensee in the program. For more information, visit

The U.S. Food and Drug Administration and the European Medicines Agency recently recommended defining a drug candidate's interactions with efflux transporters, which act as doorways for drugs to exit or be expelled from human cells, to ascertain a drug candidate's probable safety profile and potential for adverse drugdrug interactions. Current efflux transporter assays use standard chemical inhibitors that can interact with multiple transporters simultaneously. This may produce an ambiguous representation of a drug candidates true ADME properties in the human body or potential contradictions with other medications.

"Complete transporter knockout human cell lines identify efflux transporter interactions unambigously to produce a clearly defined safety profile for a drug candidate. Sigma's CRO and pharma licensing program will facilitate rapid adoption of this superior approach to identifying potential safety issues and meeting the new regulatory guidelines," explains Paul Brooks, Ph.D., Market Segment Manager at Sigma Life Science.

The MDR1 (P-gp), BCRP and MRP2 Caco-2 single and double knockout cell lines were confirmed by genomic analysis and functional transporter activity assays. Sigma Life Science generated the cell lines using its CompoZr Zinc Finger Nuclease technology.

At the International Society for the Study of Xenobiotics' (ISSX) 18th North American Regional Meeting, new functional data on the gene knockout cell lines will be presented by Kathleen E. Sampson, Ph.D., Senior Scientist at Sigma Life Science, during an industry sponsored symposia on October 16 and a poster session on October 17, 2012.

For continuing ADME studies in animals, Sprague-Dawley rats containing identical homozygous efflux transporter gene knockouts are also available for purchase from Sigma Advanced Genetic Engineering (SAGE®) Labs.

For more information on the ISSX symposium, poster presentation or SAGE animal models, visit

Cautionary Statement: The foregoing release contains forward-looking statements that can be identified by terminology such as "more precise," "unambiguously," "will facilitate" or similar expressions, or by expressed or implied discussions regarding potential future revenues from products derived there from. You should not place undue reliance on these statements. Such forward-looking statements reflect the current views of management regarding future events, and involve known and unknown risks, uncertainties and other factors that may cause actual results to be materially different from any future results, performance or achievements expressed or implied by such statements. There can be no guarantee that transporter gene knockout rat and human cell lines or related services will assist the Company to achieve any particular levels of revenue in the future. In particular, management's expectations regarding products associated with transporter gene knockout rat and human cell lines or related services could be affected by, among other things, unexpected regulatory actions or delays or government regulation generally; the Company's ability to obtain or maintain patent or other proprietary intellectual property protection; competition in general; government, industry and general public pricing pressures; the impact that the foregoing factors could have on the values attributed to the Company's assets and liabilities as recorded in its consolidated balance sheet, and other risks and factors referred to in Sigma-Aldrich's current Form 10-K on file with the US Securities and Exchange Commission. Should one or more of these risks or uncertainties materialize, or should underlying assumptions prove incorrect, actual results may vary materially from those anticipated, believed, estimated or expected. Sigma-Aldrich is providing the information in this press release as of this date and does not undertake any obligation to update any forward-looking statements contained in this press release as a result of new information, future events or otherwise.

About Sigma Life Science: Sigma Life Science is a Sigma-Aldrich business that represents the Company's leadership in innovative biological products and services for the global life science market and offers an array of biologically-rich products and reagents that researchers use in scientific investigation. Product areas include biomolecules, genomics and functional genomics, cells and cell-based assays, transgenics, protein assays, stem cell research, epigenetics and custom services/oligonucleotides. Sigma Life Science also provides an extensive range critical bioessentials like biochemicals, antibiotics, buffers, carbohydrates, enzymes, forensic tools, hematology and histology, nucleotides, amino acids and their derivatives, and cell culture media.

About Sigma-Aldrich: Sigma-Aldrich is a leading Life Science and High Technology company whose biochemical, organic chemical products, kits and services are used in scientific research, including genomic and proteomic research, biotechnology, pharmaceutical development, the diagnosis of disease and as key components in pharmaceutical, diagnostics and high technology manufacturing. Sigma-Aldrich customers include more than 1.3 million scientists and technologists in life science companies, university and government institutions, hospitals and industry. The Company operates in 38 countries and has nearly 9,100 employees whose objective is to provide excellent service worldwide. Sigma-Aldrich is committed to accelerating customer success through innovation and leadership in Life Science and High Technology. For more information about Sigma-Aldrich, please visit its website at

Sigma-Aldrich and Sigma are trademarks of Sigma-Aldrich Co. LLC registered in the US and other countries. CompoZr and SAGE are registered trademarks of Sigma-Aldrich Co. LLC.

SOURCE Sigma-Aldrich Corporation

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