Biotranex LLC Granted Patent for Bile Salt Export Protein BSEPcyte™ Assay

Methodology Measures Inhibition of BSEP to Help Reduce Drug-Induced Liver Injury.

Biotranex LLC

Biotranex LLC, an innovative contract research laboratory and a leader in developing and offering drug transporter assays, today announced that the United States Patent and Trademark Office (USPTO) has granted the Company United States patent number 9,772,325, covering its novel bile salt export protein (BSEP) inhibition assay that is marketed as BSEPcyteTM.

Drugs that inhibit BSEP are implicated in cholestasis and drug-induced liver injuries (DILI), which has led to the costly withdrawal of several marketed drugs. A unique aspect of the BSEPcyteTM assay platform is that it utilizes hepatocytes in suspension to measure BSEP inhibition. This platform is accurate, reproducible, and flexible as well as cost competitive.

“BSEPcyte™ offers significant advantages over other currently available methodologies”

We are pleased to introduce this validated BSEPcyte"TM" assay methodology to provide significant physiological and technical advantages over other assays, while being cost competitive.

Dr. Kan He

President of Biotranex LLC

A physiologically relevant hepatocyte-based system, BSEPcyteTM allows for the measurement of drug candidate inhibition of human BSEP, provides for cross-species studies, and offers the ability to investigate the effect of drug metabolism on inhibition. Notably, this assay is also run without radioactive reagents. The BSEPcyteTM assay is a better, safer, faster option to other assays currently on the market.

Another distinguishing advantage is that the BSEPcyteTM assay can be used as part of an early screening strategy in drug discovery, or later in drug development to provide more detailed investigations, including metabolism and cross-species studies.

This novel patent is critical in the development phase of new drugs because when bile salt export protein (BSEP) liver transporter is inhibited, drug-induced liver injury (DILI) can result. Drug-induced liver injury encompasses a spectrum of toxicities ranging from mild biochemical abnormalities to acute liver failure, and in some cases, the need for a liver transplant. DILI is responsible not only for the withdrawal of several marketed drugs but also for the necessity of FDA black box warning labels.

“The role that inhibition of liver transporters, including BSEP, plays in cholestasis and drug-induced liver injury is only recently being appreciated by drug developers in the pharmaceutical and biotech industries,” states Dr. Kan He. “Preclinical animal models are poor predictors of DILI in human subjects. A major cause of DILI and cholestasis is the inhibition of human bile salt export protein. Therefore, it is critical to accurately determine the inhibition potential of this human hepatic transport protein for new drug candidates.”

The BSEPcyteTM assay employs a platform using suspensions of human or animal hepatocytes in a 96-well plate format with liquid chromatography-mass spectrometry quantification. The assay is reproducible, sensitive, flexible, robust, and possesses a wide dynamic concentration range. The assay shows excellent correlation with drugs found to inhibit BSEP and that may cause human cholestasis and DILI.

Dr. He further states, “We are pleased to introduce this validated BSEPcyteTM assay methodology to provide significant physiological and technical advantages over other assays, while being cost competitive.”

About Biotranex LLC
Dr. Kan He, President of Biotranex LLC and inventor of the BSEPcyteTM assay, has specialized in research focused on drug metabolism, transporters, and liver toxicity in support of drug discovery and development during an extensive career. His work has evolved at Warner-Lambert Co., Dupont Pharmaceuticals, and Bristol Myers Squibb (BMS), where he played a key role in the discovery of the oral anticoagulant apixaban. Dr. He co-founded two biotech drug discovery companies prior to establishing Biotranex LLC in the United States. Dr. He’s work has been published extensively in the fields of drug metabolism and transporters.

Biotranex LLC is an innovative contract service company that commercializes novel and proprietary assays for research in hepatic transport, cholestasis, drug-induced liver injury, drug interactions, and drug metabolism. Biotranex also offers an extensive array of drug metabolism, transport, pharmacokinetic, and analytic services to the biotech and pharmaceutical industries. The extensive collective experience in the successful discovery and development of marketed drugs allows Biotranex to apply innovative solutions to the ADME/PK needs of other companies. The company’s offices are located near Princeton, New Jersey, in Monmouth Junction.

Kan He, Ph.D. - President
(732) 230-3062

Thomas F. Woolf, Ph.D. - Senior Vice President

Source: Biotranex LLC

Categories: Pharmaceuticals and Biotech, Pharmaceuticals and Biotech

Tags: bile salt export protein, biotech, BSEP, drug development, drug transporter assays, drug-induced liver injury, liver transporters, pharmaceuticals, research laboratory