Optivia Technology


The Optivia Advantage

Optivia transporter assays are designed with human biology in mind.We strive to provide in vitro assays most likely to predict results in humans. Our assays are used to discover drugs with improved bioavailability, tissue selectivity and fewer drug-drug interactions.

Human Transporters Optivia assays use human transporters. Significant interspecies differences in transporter affinities have been shown. [1]
Mammalian Cells Optivia assays are always performed in polarized mammalian cell monolayers.
Assays using human transporters expressed in mammalian cells can better represent human biology, structure, topology and function than those in artificial environments such as insect vesicles and membranes. Non-mammalian systems have been shown to produce low molecular weight, under-glycosylated versions of human transporter proteins.
Functional Efflux and Uptake Assays Optivia assays always measure actual bi-directional cellular efflux or influx.
Functional flux assays have been shown to have fewer false negatives, fewer false positives and better correlation with human clinical results than receptor binding, ATP-ase and calcein inhibition assays. [2]
Improved Bioavailability and Improved PK Optivia assays enable you to optimize human bioavailability and PK.
Uptake and efflux transporters affecting absorption are expressed differentially throughout the GI tract allowing for increased bioavailability and desirable pharmacokinetic profiles.
Tissue Selectivity and Targeted Tissue Delivery Optivia assays enable you discover drugs with tissue selectivity.
Drugs must reach target tissues needed for efficacy and avoid those where they may cause undesirable or unsafe effects. Many transporters are expressed only in specific tissues [3] allowing for strategies to discover tissue selective drugs.
Drug-Drug Interaction Assessment Optivia assays enable you to avoid transporter mediated drug-drug interactions (DDI).
The FDA has identified 25 important human transporters in the draft DDI guidance. [4]
Continuing Innovation More than 300 unique human transporters are currently known. The body of evidence is growing rapidly for their role in drug absorption, distribution, metabolism, elimination.
At Optivia, we are committed to develop assays for all therapeutically relevant transporters. We introduce new transporter assays every month.

[1] Suzuyama, et al. "Species differences of inhibitory effects on P-glycoprotein-mediated drug transport," J Pharm Sci. 2007 Jun;96(6):1609-18.

[2] Polli, et al. "Rational Use of in Vitro P-glycoprotein Assays in Drug Discovery," J Pharmacol Exp Ther. 2001 Nov;299(2):620-8.

[3] Sugiyama, et al. "Apical/basolateral surface expression of drug transporters and its role in vectorial drug transport," Pharm Res. 2005 Oct;22(10):1559-77.

[4] US FDA, "Guidance for Industry Drug Interaction Studies Study Design, Data Analysisand Implications for Dosing and Labeling (Draft)," Sept. 2006.