Discovery in vitro ADMET

Close-up of a Biomek automated liquid handler with multiple pipettes dispensing blue liquid into a well plate for DMPK studies.

Discovery in vitro ADMET Services

Pharmaron’s Discovery in vitro ADMET services support the characterization of DMPK properties for molecules discovered and invented, including hits, leads, and potential preclinical candidates. In vitro ADMET assays are designed to meet the specific needs of each drug discovery program. Pharmaron’s broad spectrum of in vitro ADMET services provides critical insight into a drug’s absorption, distribution, metabolism, and excretion attributes.

Close-up of a SCIEX Triple Quad 5500 mass spectrometer used for pharmacokinetic/pharmacodynamic (PK/PD) analysis in a laboratory setting.

Solution Properties

  • Aqueous solubility (kinetic and thermodynamic solubility)
  • pKa using Sirius T3 with solid material or DMSO stock
  • Distribution/partition coefficient (LogD/P)
  • Protein binding/tissue binding (plasma, blood, brain, kidney, skin, lung, liver microsomes and hepatocytes)
  • Blood partitioning
  • Chemical stability
Organized racks of pipette tips in various colors, representing tools used in discovery in vitro ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) studies.

Drug Absorption and Transport

  • Permeability evaluation (PAMPA, Caco-2, MDCK, and MDCKIIko cells transfected with different species of MDR1)
  • Transporter investigation on substrate and inhibitor evaluation (P-gp, BCRP, BSEP, MRP2/3/4, OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2, OATP2B1, OATP1A2, MATE1, MATE2, PEPT1, NTCP, ASBT)
  • Hepatic uptake using media-loss method
Close-up of a Biomek liquid handler dispensing blue solution into a multiwell plate, used for Discovery in vitro ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) assays.

Metabolic Stability and Identification

  • Metabolic stability in the liver, intestine, lung, and colon using subcellular fractions
  • Long-term hepatocyte culture and micro liver systems for low clearance
  • compounds
  • After change
  • Plasma/blood stability
  • Metabolite profiling and identification
  • GSH/CN/Methoxyamine trapping
  • Reactivity and stability of Acyl Glucuronides (Ags)
Scientist wearing protective gear operates laboratory equipment for in vitro ADMET studies, focusing on drug discovery and metabolic profiling.

Drug-drug Interactions

  • Substrate evaluation & isoform ID (CYP, FMO, MAO, AO, XO, CES, ADH, ALDH, UGT, SULT, NAT1, NAT2, GST)
  • Enzyme inhibition (CYP, UGT, and non-CYP enzymes) – direct inhibition and time-dependent inhibition
  • KI/kinact determination
  • CYP induction (human hepatocytes; HepaRG cells; PXR activation using DPX2 cells from PuraCYP)
Scientist analyzing cell images on a computer, with a colleague using a microscope in a nearby room, conducting Discovery DMPK research at Pharmaron.

in vitro Toxicity

  • Liver toxicity package (general and mechanistic toxicity evaluation)
  • Phototoxicity (3T3 NRU)
  • Cardiotoxicity
  • Genotoxicity

Learn more about innovative in vitro ADMET models at Pharmaron.

Banner for the PHARMARON DMPK Webinar Series featuring a panel discussion on the impact of complex cell models in DMPK and preclinical ADME studies. The banner includes headshots and names of five speakers: Yassen Abbas, Jing Lai, Ph.D., Elnaz Gozalpour, Ph.D., Helen Rollison, and Kritika Sadhi, Ph.D.