Transporter Screening Services for Lead Discovery and Optimization

Transporter Screening plays an important role in multiple areas of the drug development pipeline, from the identification of therapeutically active lead compounds to ensuring the clinical safety of development-stage drugs, transporter screening enables you to develop drugs with novel therapeutic actions, better clinical responses, and less risk of adverse effects.

Optivia offers transporter screening services and specialized transporter panels to help you identify new classes of transporter-targeted therapeutics and optimized lead compounds for better ADME properties and decreased safety and drug-drug interaction (DDI) liabilities.

Opti-DDI™ Panel Select and optimize lead compounds with less DDI liability
Opti-Target™ Panel Screen against transporters as therapeutic targets for hit confirmation
Opti-Safety ™ Panel Identify safety liabilities of lead compounds by screening against toxicity related transporters early in the discovery process
Opti-ADME™ Panel Augment the rational design of compounds or pro-drugs that target specific transporters for improved bioavailability and tissue targeting

Key Features of Optivia’s Transporter Screening Services

  • Turn-key solution with fast turnaround time
  • Both inhibitor and substrate tests are provided
  • Available for a large panel of clinically-relevant DDI, ADME, Toxicity and therapeutic target transporters
  • Affordable screening services
  • Reliable and biologically relevant data from robust functional assays designed to meet stringent regulatory standards
  • All assay models overexpress recombinant transporters, providing clean and definitive data
  • Flexible screening project design in 96-well HTS footprint
  • Free technical consultation from experienced, customer-oriented scientists

Please contact us to discuss your specific transporter screening project.

Transporter Screening Applications

In vitro transporter assays are an integral part of the drug discovery and development process. Many transporters are validated or emerging as therapeutic targets for a variety of diseases, including depression, schizophrenia, cancer, and diabetes. Therefore, compound screening against transporter targets (e.g. SERT, DAT, NET, and SGLT2) is essential for the discovery of potent and selective therapeutic candidates. Transporter studies are also routinely conducted for development-stage compounds for assessing drug-drug interaction (DDI), clinical safety, and commercial viability. For transporters such as P-gp, OATP1B1, and BSEP that are associated with life-threatening DDIs and adverse effects, such tests are often performed at discovery stage for earlier identification of compounds with issues in clinical safety and commercial viability. In addition, many organizations are employing transporter-conscious drug design, which utilizes transporters such as PEPT1, OATP1B1, and xCT to improve drug bioavailability, tissue selectivity and disease targeting. Taken together, transporter screening is an invaluable tool in drug discovery that enables researchers to design and optimize lead compounds with novel therapeutic actions, and more desirable pharmacokinetic and clinical safety profiles.

Considerations on Implementing Transporter Screening Projects

A key requirement of transporter screening campaigns is robust functional assays with good signal-to-background ratios and Z’ scores. All of Optivia’s assays employ direct measurement of transporter functional activity, which provides more biologically-relevant results in comparison to indirect binding assays. These robust, validated assays have been extensively in regulatory-compliant transporter studies for clinical- stage compounds, they are also suitable for early-stage screening due to their strong Z’ scores. Our robust assays and extensive experience enable rapid delivery of high-quality screening data, making it easier for clients to identify true modulators of a variety of transporters.

Related Transporter Screening Resources

US FDA, Guidance for Industry Drug Interaction Studies —Study Design, Data Analysis, Implications for Dosing, and Labeling Recommendations (draft guidance), Feb. 2012

European Medicines Agency (EMA), Guideline on the investigation of drug interactions, June 2012

Membrane transporters in drug development

SLC transporters as therapeutic targets: emerging opportunities

Intriguing possibilities and beneficial aspects of transporter-conscious drug design

Possibilities of Cancer Chemotherapy Based on Transporter-Conscious Drug Design

Reducing safety-related drug attrition: the use of in vitro pharmacological profiling

Beyond the ITC White Paper: emerging sciences in drug transporters and opportunities for drug development

A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays