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Membrane transporters in drug development
TLDR
Overall, it is advised that the timing of transporter investigations should be driven by efficacy, safety and clinical trial enrolment questions, as well as a need for further understanding of the absorption, distribution, metabolism and excretion properties of the drug molecule, and information required for drug labelling. Expand
The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors.
TLDR
It is demonstrated that P-glycoprotein limits the oral bioavailability and penetration of these agents into the brain and raises the possibility that higher HIV-1 protease inhibitor concentrations may be obtained by targeted pharmacologic inhibition of P- glycoprotein transport activity. Expand
Polymorphisms in Human MDR1 (P‐glycoprotein): Recent Advances and Clinical Relevance
TLDR
SNPs in MDR1 in relation to population frequencies, drug levels, and phenotypes are outlined and issues relating to M DR1 haplotypes, environmental factors, and study design, as potential confounding factors of the observed MDR 1 polymorphism effect in vivo, are discussed. Expand
Identification of functionally variant MDR1 alleles among European Americans and African Americans
TLDR
Allelic variation in MDR1 is more common than previously recognized and involves multiple SNPs whose allelic frequencies vary between populations, and some of these SNPs are associated with altered P‐glycoprotein function. Expand
OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine.
TLDR
OATP transporters and P-gp colocalize in organs of importance to drug disposition such as the liver, their activity provides an explanation for the heretofore unknown mechanism(s) responsible for fexofenadine's disposition and suggests potentially similar roles in the disposition of other xenobiotics. Expand
Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics.
TLDR
Multiple transporters mediate the overall hepatic uptake of rosuvastatin, and NTCP may be a heretofore unrecognized transporter important to the disposition of roviastatin and possibly other drugs/statins in clinical use. Expand
The orphan nuclear receptor HNF4α determines PXR- and CAR-mediated xenobiotic induction of CYP3A4
TLDR
It is shown that the orphan nuclear receptor hepatocyte nuclear factor-4α (HNF4α; HNF4A) is critically involved in the PXR- and CAR-mediated transcriptional activation of CYP3A4, an important regulator of coordinate nuclear-receptor–mediated response to xenobiotics. Expand
Polymorphisms in OATP-C
TLDR
The presence of multiple functionally relevant single-nucleotide polymorphisms (SNPs) in OATP-C in a population of African- and European-Americans is demonstrated and may represent a heretofore unrecognized factor influencing drug disposition. Expand
Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group study
TLDR
A CYP2B6 allelic variant that is more common in African-Americans than in Europeans-Americans was associated with significantly greater efavirenz plasma exposure during HIV therapy, and inter-individual differences in metabolism may, in part, explain susceptibility to efvirenz central nervous system side effects. Expand
Polymorphisms in Human Organic Anion-transporting Polypeptide 1A2 (OATP1A2)
TLDR
In vitro functional assessment revealed that the A516C and A404T variants had markedly reduced capacity for mediating the cellular uptake of OATP1A2 substrates and two δ-opioid receptor agonists, deltorphin II, and [d-penicillamine2,5]-enkephalin, while the G559A and C2003G variants appeared to have substrate-dependent changes in transport activity. Expand
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