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Genotyped Human Hepatocytes for Polymorphism Studies

 

Geneknown™ hepatocytes are characterized for pharmacologically relevant polymorphisms affecting the ADME-Tox properties of xenobiotics.

Genetic polymorphisms in the CYP450 family impact Drug-Drug Interaction (DDI) liability. Several examples are well documented in the literature, such as Midazolam & CYP3A4. For Warfarin, CYP2C polymorphisms explain 10% of the dose variation between patients.

It's thus important to better understand CYP polymorphism at a given stage of the drug development of your NCEsFor this purpose, XenoTech have developped the Geneknown™ hepatocytes for performing in vitro ADME-Tox assays using cellular models that reflect genetically-defined subpopulations of patients.

 

Geneknown™ hepatocytes: your fully characterized cellular models for ADME-tox studies

Geneknown™ hepatocytes are evaluated for the presence of significant alleles and SNPs for 30 genes:

  • CYP1A1, 1A2, 2A6, 2B6, 2D6, 2C8, 2C9, 2C19, 2E1, 3A4, 3A5
  • MDR1 (ABCB1), MRP2 (ABCC2), BCRP (ABCG2), PEPT2 (SLC15A2), OCT1 (SLC22A1), OCT2 (SLC22A2), OAT1 (SLC22A6), OATP1B1 (SLCO1B1), OATP1B3 (SLCO1B3), OATP2B1 (SLCO2B1)
  • DPYD (dihydropyrimidine dehydrogenase), GSTP1 (glutathione S-transferase pi 1), NAT1 (N-acetyltransferase 1), NAT2 (N-acetyltransferase 2), TPMT (thiopurine S-methyltransferase), UGT1A1 (UDP glucuonosyltransferase 1 family polypeptide A1), UGT2B15 (UDP glucuronosyltransferase 2 family polypeptide B15), UGT2B7 (UDP glucuronosyltransferase 2 family polypeptide B7), VKORC1 (vitamin K epoxide reductase complex subunit 1)

 

Datasheet 2C19 High Activity Lot 1510234

 

Geneknown™ cryopreserved human hepatocytes are offered as pools of cryopreserved cells from multiple donors assembled to study the effects of individual genetic variants.

Geneknown™ hepatocytes are cryopreserved using the same proprietary single-freeze method that is used with XenoTech's CryostaX® product.

 

 

Geneknown™ hepatocytes highlights

  • CYP2C19*2/*2 no activity homozygotes and CYP2C19*1/*1 wild-type controls
  • Complex genetics of CYP2D gene cluster are characterized with 25 individual SNP assays, as well as, CYP2D6 and CYP2D7 gene copy number variation assays, allowing identification of ultra-rapid, extensive and poor metabolizers
  • CYP3A5*1/*1 high-activity homozygotes, CYP3A5*1/*3 intermediate activity heterozygotes and CYP3A5*3/*3 no-activity control cells
  • UGT1A1 low-activity donors carrying two alleles of reduced activity and wild-type UGT1A1*1/*1 control donors
  • OATP1B1*5/*5 homozygotes and wild-type OATP1B1*1/*1 control cells

 

 

Looking for advices regarding genotyped human hepatocytes? Contact our experts at mycells@tebu-bio.com!