Regulatory in vitro ADMET Studies
Regulatory in vitro ADMET Studies
Characterizing a drug candidate’s ADME properties and potential drug interactions is essential in drug discovery and is best done early. Pharmaron offers a broad spectrum of in vitro ADMET services to help you gain critical insight into your drug’s absorption, distribution, metabolism, and excretion attributes.
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 a bio-relevant membrane.
- Evaluate excipient effects and compare formulations, food effects, and 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, and 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