Drug-drug interactions of P-gp substrates unrelated to CYP metabolism

Y Akamine, N Yasui-Furukori, T Uno - Current drug metabolism, 2019 - ingentaconnect.com
Background: Recent US Food and Drug Administration (FDA) draft guidance on
pharmacokinetic drugdrug interactions (DDIs) has highlighted the clinical importance of ABC …

Drug–Drug Interactions Mediated Through P‐Glycoprotein: Clinical Relevance and In VitroIn Vivo Correlation Using Digoxin as a Probe Drug

KS Fenner, MD Troutman, S Kempshall… - Clinical …, 2009 - Wiley Online Library
The clinical pharmacokinetics and in vitro inhibition of digoxin were examined to predict the
P‐glycoprotein (P‐gp) component of drug–drug interactions. Coadministered drugs (co …

Suitability of digoxin as a P‐glycoprotein probe: implications of other transporters on sensitivity and specificity

AM Nader, DR Foster - The Journal of Clinical Pharmacology, 2014 - Wiley Online Library
The study of transporter‐mediated drug–drug interactions (DDI) requires use of appropriate
probes to reflect transporter function. Digoxin is often used as a probe in DDI studies …

In vitro predictability of drug-drug interaction likelihood of P-glycoprotein-mediated efflux of dabigatran etexilate based on [I] 2/IC50 threshold

W Kishimoto, N Ishiguro, E Ludwig-Schwellinger… - Drug Metabolism and …, 2014 - ASPET
Dabigatran etexilate, an oral, reversible, competitive, and direct thrombin inhibitor, is an in
vitro and in vivo substrate of P-glycoprotein (P-gp). Dabigatran etexilate was proposed as an …

The utility of in vitro data in making accurate predictions of human P-glycoprotein-mediated drug-drug interactions: a case study for AZD5672

R Elsby, M Gillen, C Butters, G Imisson… - Drug metabolism and …, 2011 - ASPET
To support drug development and registration, Caco-2 cell monolayer assays have
previously been set up and validated to determine whether candidate drugs are substrates …

Development, validation and utility of an in vitro technique for assessment of potential clinical drug–drug interactions involving P-glycoprotein

JP Keogh, JR Kunta - European journal of pharmaceutical sciences, 2006 - Elsevier
Regulatory interest is increasing for drug transporters generally and P-glycoprotein (Pgp) in
particular, primarily in the area of drug–drug interactions. To aid in both identifying and …

Association between the number of coadministered P-glycoprotein inhibitors and serum digoxin levels in patients on therapeutic drug monitoring

G Englund, P Hallberg, P Artursson, K Michaëlsson… - BMC medicine, 2004 - Springer
Abstract Background The ABC transporter P-glycoprotein (P-gp) is recognized as a site for
drug-drug interactions and provides a mechanistic explanation for clinically relevant …

Establishment of in vitro P-glycoprotein inhibition assay and its exclusion criteria to assess the risk of drug–drug interaction at the drug discovery stage

H Sugimoto, SI Matsumoto, M Tachibana… - Journal of …, 2011 - Elsevier
The decision tree to determine whether the P-glycoprotein (P-gp)/multidrug resistance
protein 1 (MDR1)-mediated drug–drug interaction (DDI) study is recommended has been …

Pharmacokinetic Drug–Drug Interactions and Herb–Drug Interactions

MK Choi, IS Song - Pharmaceutics, 2021 - mdpi.com
Due to the growing use of herbal supplementation—ease of taking herbal supplements with
therapeutics drugs (ie, does not require a prescription) and a trend of polypills with different …

Intestinal P‐gp and putative hepatic OATP1B induction: international transporter consortium perspective on drug development implications

MJ Zamek‐Gliszczynski, M Patel… - Clinical …, 2021 - Wiley Online Library
There is an increasing interest in transporter induction (ie, decreased systemic drug
exposure due to increased efflux‐limited absorption or transporter‐mediated clearance) as a …