Publication

Intracellular 'boosting' of darunavir using known transport inhibitors in primary PBMC

Ruben Hartkoorn
2009
Journal Articles

Abstract

center dot Antiretroviral protease inhibitors such as lopinavir and saquinavir have been shown to be substrates of ABCB1. Co-administration with the potent ABCB1 and CYP3A4 inhibitor, ritonavir, has shown improved pharmacokinetics and subsequent therapeutic effects of protease inhibitors. Darunavir is a recently licensed protease inhibitor with potent antiretroviral effects but has yet to be characterized as a potential substrate for drug transporters.

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Ruben Hartkoorn
2009
Journal Articles

Abstract

Official source

Related concepts (32)

Protease inhibitor (biology)

In biology and biochemistry, protease inhibitors, or antiproteases, are molecules that inhibit the function of proteases (enzymes that aid the breakdown of proteins). Many naturally occurring protease inhibitors are proteins. In medicine, protease inhibitor is often used interchangeably with alpha 1-antitrypsin (A1AT, which is abbreviated PI for this reason). A1AT is indeed the protease inhibitor most often involved in disease, namely in alpha-1 antitrypsin deficiency.

Reuptake inhibitor

A reuptake inhibitor (RI) is a type of drug known as a reuptake modulator that inhibits the plasmalemmal transporter-mediated reuptake of a neurotransmitter from the synapse into the pre-synaptic neuron. This leads to an increase in extracellular concentrations of the neurotransmitter and an increase in neurotransmission. Various drugs exert their psychological and physiological effects through reuptake inhibition, including many antidepressants and psychostimulants.

CYP3A4

Cytochrome P450 3A4 (abbreviated CYP3A4) () is an important enzyme in the body, mainly found in the liver and in the intestine. It oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from the body. It is highly homologous to CYP3A5, another important CYP3A enzyme. While many drugs are deactivated by CYP3A4, there are also some drugs which are activated by the enzyme. Some substances, such as some drugs and furanocoumarins present in grapefruit juice, interfere with the action of CYP3A4.

Related publications (12)

Intracellular 'boosting' of darunavir using known transport inhibitors in primary PBMC

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Rapid Progression of Kidney Dysfunction in People Living With HIV: Use of Polygenic and Data Collection on Adverse Events of Anti-HIV Drugs (D:A:D) Risk Scores

Extended Gate Field Effect Transistor Based Sensor for Detection of Trace Amounts of Anti-Depressant Drug