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Discovery in vitro ADMET

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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 provide critical insight into a drug’s absorption, distribution, metabolism and excretion attributes.

Capabilities

Discovery in vivo PK
Discovery in vitro ADMET
Close-up of a blue mass spectrometer in a laboratory setting focused on bioanalytical development. The device features various connectors, wires, and a metallic cylindrical component attached to its front. The background shows partially visible lab equipment, indicating a scientific environment.

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
Watch our webinar: What is the role of physico-chemistry in DMPK
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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
Download our poster about our permeability assay platform
A robotic laboratory instrument, labeled "Biomek", is shown pipetting blue liquid into an array of wells in a plastic plate. The instrument, with "60 µL" written on it, operates in a scientific lab where radiolabelled ADME studies are conducted.

Metabolic Stability and Identification

  • Metabolic stability in 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)
Download our metabolism flyer
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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)
Watch our webinar: The Nasty Surprise of a Complex Drug-Drug Interaction
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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.

View on demand
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.

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