Current Drug Metabolism - Volume 17, Issue 5, 2016

Introduction: The kynurenine pathway includes several neuroactive compounds, including kynurenic acid, picolinic acid, 3-hydroxykynurenine and quinolinic acid. The enzymatic cascade of the kynurenine pathway is tightly connected with the immune system, and may provide a link between the immune system and neurotransmission. Main Areas Covered: Alterations in this cascade are associated with neurodegenerative, ne Read More

Background: ABCB1 is a key ABC efflux transporter modulating the pharmacokinetics of a large percentage of drugs. ABCB1 is also a site of transporter mediated drug-drug interactions (tDDI). It is the transporter most frequently tested for tDDIs both in vitro and in the clinic. Objective: Understanding the limitations of various in vitro and in vivo models, therefore, is crucial. In this review we cover regulatory aspects of A Read More

Background: Hepatic transporters, including efflux transporters and uptake transporters, have been recognized to play an important role in the disposition of various drugs. These membrane transporters show extensive substrate specificity with an abundance of overlap, implying the probability of transporter involved in the drugdrug interactions with other drugs. Thus reliable techniques are taken into consideration to Read More

Background: Over the decade, miRNAs are the most important molecules for the biopharmaceutical industry due to their relation with several human diseases. Presently, the phase-II clinical trial has been initiated for the first miRNA-based therapeutics (“Miravirsen”) to treat HCV infection. It has been expected that many more miRNA-based therapeutics will enter the clinical trials. Therefore, it is important to develop differe Read More

Background: Nanoparticles have shown great potential in biomedical applications such as imaging probes and drug delivery. However, the increasing use of nanoparticles has raised concerns about their adverse effects on human health and environment. Reproductive tissues and gametes represent highly delicate biological systems with the essential function of transmitting genetic information to the offspring, whi Read More

Background: Diabetic nephropathy (DN) is currently the most common cause of end-stage renal disease (ESRD). Although nowadays much is known about its classification, pathogenesis, clinical manifestations and evolution, to date we are not yet able to stop the natural progression of nephropathy in diabetic patients. Methods: Treatment options are: lifestyle change with close blood pressure monitoring and tight glyce Read More

Background: Circadian clocks are endogenous timing systems that regulate various aspects of mammalian metabolism, physiology and behavior. Traditional chronotherapy refers to the administration of drugs in a defined circadian time window to achieve optimal pharmacokinetic and therapeutic efficacies. In recent years, substantial efforts have been dedicated to developing novel small-molecule modulators of circadi Read More

Backround: Parkinson’s disease is a pathology involving the progressive degeneration of dopaminergic neurons in the substantia nigra of the brain. L-DOPA combined with an inhibitor of DOPA decarboxylase, a pyridoxal 5’-phosphate-dependent enzyme, is still the most effective treatment for symptoms of Parkinson's disease. LDOPA increases synaptic dopamine, while the inhibitor of peripheral DOPA decarboxylase reduces th Read More