Quick Definition
What is ADME?: ADME stands for Absorption, Distribution, Metabolism, and Excretion — the four pharmacokinetic processes that determine a drug's journey through the body from administration to elimination. ADME profiling is a central part of preclinical drug development that predicts in vivo pharmacokinetic behaviour from in vitro assay data and guides drug candidate selection.
Why ADME profiling matters
A drug with excellent target potency will fail in clinical development if it is rapidly metabolised (short half-life), poorly absorbed (low oral bioavailability), or toxic due to reactive metabolite formation. ADME profiling identifies these liabilities in early discovery and allows medicinal chemistry to address them before expensive clinical investment.
ADME and regulatory submissions
FDA, EMA and ICH M12 require a complete in vitro ADME package in IND-enabling studies: metabolic stability, reaction phenotyping, CYP inhibition/induction, plasma protein binding, and transporter DDI assessment. SeamlessBio provides the biological tools: ABC transporter vesicle kits and human AB serum/plasma for protein binding assays.
Key Facts
- A: Absorption — how the drug enters systemic circulation; determined by solubility, permeability, and efflux transporter activity (P-gp, BCRP) at the gut wall
- D: Distribution — how the drug distributes into tissues; determined by plasma protein binding (fu,plasma), lipophilicity (logP), and tissue transporter expression
- M: Metabolism — chemical transformation by hepatic CYP450 enzymes (CYP3A4, 2D6, 2C9, 2C19, 1A2) and Phase II enzymes (UGTs, SULTs)
- E: Excretion — elimination via renal (OCT2, OAT1/3, MATE1/2-K) and biliary routes (BSEP, MRP2, P-gp)
- ADME profiling reduces late-stage attrition — ~40% of clinical drug failures in the 1990s were due to poor ADME
- Key in vitro assays: Caco-2/PAMPA (permeability), plasma protein binding (fu), microsomal stability, hepatocyte clearance, transporter DDI
Further Reading
- What is DDI?
- In Vitro Drug Metabolism Guide
- FDA & EMA Mandatory Transporters
- What is ABC Transporter?
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