Regulatory in vitro ADMET Studies
Regulatory in vitro ADMET Studies
Characterizing a drug candidate’s ADME properties and potential drug interactions is an important step in the drug discovery process and is best done early. To help you gain critical insight into your drug’s absorption, distribution, metabolism, and excretion attributes, Pharmaron has a broad spectrum of in vitro ADMET services.
Capabilities
Filing in vitro ADMET Studies
- Regulatory PPB and blood partition
- Metabolism and metabolite identification
- Permeability and transportation
- Drug-drug interactions
Drug Absorption and Transport
- Permeability evaluation (PAMPA, Caco-2, MDCK and transfected MDCK cell lines)
- Transporter investigation on substrate and inhibitor evaluation (P-gp, BCRP, BSEP, MRP2, MRP3, MRP4, OATP1B1, OATP1B3, OTAP2B1, OAT1, OAT3, OCT1, OCT2, MATE1, MATE2K, PEPT1, NTCP)
- Hepatic uptake using media-loss method
in vitro Dissolution Absorption System (IDAS)
- Combine traditional dissolution testing with a means to determine and quantify with a bio-relevant membrane
- Evaluate excipient effects and compare formulations, food effects, locally acting GI products
BCS-based Biowaiver Studies
- Regulatory acceptance of in vitro BCS classification data as a reliable surrogate for in vivo BE studies
- Accelerated and de-risked alternative to clinical PK, BA/BE, DDI studies
- Applicable to high-variability drugs, drugs with serious adverse event profiles and drugs requiring special patient populations
- Eligibility extended to include Class I and Class III drug substances
Enzyme Drug-Drug Interactions (DDI)
- CYP phenotyping: 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A
- CYP inhibition: 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A
- CYP induction: 1A2, 2B6, 3A4, 2C (if positive for 3A4)
- Non-CYP DDI:
- Phase I (CYP2A6, 2J2, 4F2, 2E1, AO, CES, MAO, FMO, XO, ADH/ALDH)
- Phase II (UGTs, SULTs)
Transporter Drug-Drug Interactions (DDI)
- Phenotyping: efflux transporters: P-gp, BCRP; hepatic transporters: OATP1B1, OATP1B3; renal transporters: OAT1, OAT3, OCT2, MATE1 & MATE2K
- Inhibition
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