Drug Transporters

2009 ◽  
pp. 45-84 ◽  
Author(s):  
Richard H. Ho ◽  
Richard B. Kim
Keyword(s):  
Drug Transporters

Pharmacokinetics, Placental and Breast Milk Transfer of Antiretroviral Drugs in Pregnant and Lactating Women Living with HIV

2019 ◽  
Vol 25 (5) ◽  
pp. 556-576 ◽  
Author(s):  
E.M. Hodel ◽  
C. Marzolini ◽  
C. Waitt ◽  
N. Rakhmanina
Keyword(s):  
Breast Milk ◽  
Protease Inhibitors ◽  
Drug Class ◽  
Drug Transporters ◽  
Maternal Plasma ◽  
Antiretroviral Drugs ◽  
Physiological Changes ◽  
Women Living With Hiv ◽  
Living With Hiv ◽  
In Pregnancy

Background:Remarkable progress has been achieved in the identification of HIV infection in pregnant women and in the prevention of vertical HIV transmission through maternal antiretroviral treatment (ART) and neonatal antiretroviral drug (ARV) prophylaxis in the last two decades. Millions of women globally are receiving combination ART throughout pregnancy and breastfeeding, periods associated with significant biological and physiological changes affecting the pharmacokinetics (PK) and pharmacodynamics (PD) of ARVs. The objective of this review was to summarize currently available knowledge on the PK of ARVs during pregnancy and transport of maternal ARVs through the placenta and into the breast milk. We also summarized main safety considerations for in utero and breast milk ARVs exposures in infants.Methods:We conducted a review of the pharmacological profiles of ARVs in pregnancy and during breastfeeding obtained from published clinical studies. Selected maternal PK studies used a relatively rich sampling approach at each ante- and postnatal sampling time point. For placental and breast milk transport of ARVs, we selected the studies that provided ratios of maternal to the cord (M:C) plasma and breast milk to maternal plasma (M:P) concentrations, respectively.Results:We provide an overview of the physiological changes during pregnancy and their effect on the PK parameters of ARVs by drug class in pregnancy, which were gathered from 45 published studies. The PK changes during pregnancy affect the dosing of several protease inhibitors during pregnancy and limit the use of several ARVs, including three single tablet regimens with integrase inhibitors or protease inhibitors co-formulated with cobicistat due to suboptimal exposures. We further analysed the currently available data on the mechanism of the transport of ARVs from maternal plasma across the placenta and into the breast milk and summarized the effect of pregnancy on placental and of breastfeeding on mammal gland drug transporters, as well as physicochemical properties, C:M and M:P ratios of individual ARVs by drug class. Finally, we discussed the major safety issues of fetal and infant exposure to maternal ARVs.Conclusions:Available pharmacological data provide evidence that physiological changes during pregnancy affect maternal, and consequently, fetal ARV exposure. Limited available data suggest that the expression of drug transporters may vary throughout pregnancy and breastfeeding thereby possibly impacting the amount of ARV crossing the placenta and secreted into the breast milk. The drug transporter’s role in the fetal/child exposure to maternal ARVs needs to be better understood. Our analysis underscores the need for more pharmacological studies with innovative study design, sparse PK sampling, improved study data reporting and PK modelling in pregnant and breastfeeding women living with HIV to optimize their treatment choices and maternal and child health outcomes.

scholarly journals Differential in vitro interactions of the Janus kinase inhibitor ruxolitinib with human SLC drug transporters

Xenobiotica ◽  
2021 ◽  
pp. 1-12
Author(s):  
Arnaud Bruyère ◽  
Marc Le Vée ◽  
Elodie Jouan ◽  
Stephanie Molez ◽  
Anne T. Nies ◽  
...  
Keyword(s):  
Kinase Inhibitor ◽  
Drug Transporters ◽  
Janus Kinase ◽  
Janus Kinase Inhibitor ◽  
In Vitro Interactions

Regulation of drug transporters by microRNA and implications in disease treatment

2021 ◽  
Author(s):  
Yoon-Jee Chae ◽  
Ji-Eun Chang ◽  
Mi-Kyung Lee ◽  
Juhee Lim ◽  
Kwang-Hee Shin ◽  
...  
Keyword(s):  
Drug Transporters ◽  
Disease Treatment

scholarly journals Endotoxin-Mediated Downregulation of Hepatic Drug Transporters in HIV-1 Transgenic Rats

2016 ◽  
Vol 44 (5) ◽  
pp. 709-719 ◽  
Author(s):  
R. H. Ghoneim ◽  
M. Piquette-Miller
Keyword(s):  
Drug Transporters ◽  
Transgenic Rats ◽  
Hepatic Drug ◽  
Hiv 1

Involvement of Drug Transporters in Organ Toxicity: The Fundamental Basis of Drug Discovery and Development

2016 ◽  
Vol 29 (4) ◽  
pp. 545-563 ◽  
Author(s):  
Yaofeng Cheng ◽  
Ayman El-Kattan ◽  
Yan Zhang ◽  
Adrian S. Ray ◽  
Yurong Lai
Keyword(s):  
Drug Discovery ◽  
Drug Transporters ◽  
Drug Discovery And Development ◽  
Organ Toxicity

In Vitro and In Vivo Assessment of Renal Drug Transporters in the Disposition of Mesna and Dimesna

2012 ◽  
Vol 52 (4) ◽  
pp. 530-542 ◽  
Author(s):  
M. J. Cutler ◽  
B. L. Urquhart ◽  
T. J. Velenosi ◽  
H. E. Meyer zu Schwabedissen ◽  
G. K. Dresser ◽  
...  
Keyword(s):  
Drug Transporters ◽  
In Vivo Assessment
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