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Drug–drug interactions (DDIs) cause a drug to affect other drugs, leading to reduced drug efficacy or increased toxicity of the affected drug. Some well-known interactions are known to be the cause of adverse drug reactions (ADRs) that are life threatening to the patient. Traditionally, DDI have been evaluated around the selective action of drugs on specific CYP enzymes. The interaction of drugs with CYP remains very important in drug interactions but, recently, other important mechanisms have also been studied as contributing to drug interaction including transport- or UDP-glucuronyltransferase as a Phase II reaction-mediated DDI. In addition, novel mechanisms of regulating DDIs can also be suggested. In the case of the substance targeted for interaction, not only the DDIs but also the herb–drug or food–drug interactions have been reported to be clinically relevant in terms of adverse side effects. Reporting examples of drug interactions on a marketed drug or studies on new mechanisms will be very helpful for preventing the side effects of the patient taking these drugs. This Special Issue aims to highlight current progress in understanding both the clinical and nonclinical interactions of commercial drugs and the elucidation of the mechanisms of drug interactions.

Research & information: general --- Biology, life sciences --- tadalafil --- ticagrelor --- drug-drug interaction --- pharmacokinetics --- plasma concentration --- CYP3A4 --- Loxoprofen --- CYP3A --- Dexamethasone --- Ketoconazole --- CYP2D6 --- O-desmethyltramadol --- physiologically-based pharmacokinetics --- tramadol --- (‒)-sophoranone --- CYP2C9 --- potent inhibition --- in vitro --- in vivo --- drug interaction --- low permeability --- high plasma protein binding --- biflavonoid --- cytochrome P450 --- drug interactions --- selamariscina A --- uridine 5′-diphosphoglucuronosyl transferase --- tissue-specific --- systemic exposure --- P-glycoprotein (P-gp) --- organic anion transporting polypeptide 1A2 (OATP1A2) --- Rumex acetosa --- fexofenadine --- chronic kidney disease --- drug–drug interactions --- polypharmacy --- adverse drug reactions --- Lexicomp --- subset analysis --- signal detection algorithms --- spontaneous reporting systems --- mechanism-based inhibition --- competitive inhibition --- non-competitive inhibition --- substrate --- inhibitor --- cytochromes P450 --- OATP1B1 --- OATP1B3 --- tyrosine kinase inhibitors --- drug-drug interactions --- migraine --- lasmiditan --- gepants --- monoclonal antibodies --- CYP1A1 --- CYP1A2 --- drug–drug interaction --- expression --- metabolism --- regulation --- drug transporter --- ubiquitination --- ixazomib --- DDI --- computational prediction --- in silico --- QSAR --- drug metabolism --- ADME --- CYP --- metabolic DDI --- P450 --- 1A2 --- 2B6 --- 2C19 --- 2C8 --- 2C9 --- 2D6 --- 3A4 --- tadalafil --- ticagrelor --- drug-drug interaction --- pharmacokinetics --- plasma concentration --- CYP3A4 --- Loxoprofen --- CYP3A --- Dexamethasone --- Ketoconazole --- CYP2D6 --- O-desmethyltramadol --- physiologically-based pharmacokinetics --- tramadol --- (‒)-sophoranone --- CYP2C9 --- potent inhibition --- in vitro --- in vivo --- drug interaction --- low permeability --- high plasma protein binding --- biflavonoid --- cytochrome P450 --- drug interactions --- selamariscina A --- uridine 5′-diphosphoglucuronosyl transferase --- tissue-specific --- systemic exposure --- P-glycoprotein (P-gp) --- organic anion transporting polypeptide 1A2 (OATP1A2) --- Rumex acetosa --- fexofenadine --- chronic kidney disease --- drug–drug interactions --- polypharmacy --- adverse drug reactions --- Lexicomp --- subset analysis --- signal detection algorithms --- spontaneous reporting systems --- mechanism-based inhibition --- competitive inhibition --- non-competitive inhibition --- substrate --- inhibitor --- cytochromes P450 --- OATP1B1 --- OATP1B3 --- tyrosine kinase inhibitors --- drug-drug interactions --- migraine --- lasmiditan --- gepants --- monoclonal antibodies --- CYP1A1 --- CYP1A2 --- drug–drug interaction --- expression --- metabolism --- regulation --- drug transporter --- ubiquitination --- ixazomib --- DDI --- computational prediction --- in silico --- QSAR --- drug metabolism --- ADME --- CYP --- metabolic DDI --- P450 --- 1A2 --- 2B6 --- 2C19 --- 2C8 --- 2C9 --- 2D6 --- 3A4

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Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis and still represents one of the global health threats to mankind. The World Health Organization estimated more than 10 million new cases and reported more than 1.5 million deaths in 2019, thus ranking TB among the main causes of death due to a single pathogen. Standard anti-TB therapy includes four first-line antibiotics that should be administered for at least six months. However, in the case of multi- and extensively drug-resistant TB, second-line medications must be used and these frequently cause severe side effects resulting in poor compliance. Developing new anti-TB drug candidates is therefore of outmost importance. In this Special Issue dedicated to Tuberculosis Drug Discovery and Development, we present the main and latest achievements in the fields of drug and target discovery, host-directed therapy, anti-virulence drugs, and describe the development of two advanced compounds: macozinone and delpazolid. In addition, this Special Issue provides an historical perspective focused on Carlo Forlanini, the inventor of pneumothorax for TB treatment, and includes an overview of the state-of-the-art technologies which are being exploited nowadays in TB drug development. Finally, a summary of TB vaccines that are either approved or undergoing clinical trials concludes the Special Issue.

mycobacteria --- tuberculosis --- multi-drug resistance --- drug discovery --- promiscuous targets --- Mycobacterium tuberculosis --- rifampin --- isoniazid --- mechanisms of resistance --- mutations --- granulomas --- caseum --- cell envelope --- dormancy --- delpazolid --- macozinone --- DprE1 inhibitor --- clinical studies --- discovery --- mode of action --- drug resistance --- toxicity --- target --- energy metabolism --- electron transport chain --- oxidative phosphorylation --- bedaquiline --- Q203 --- MID3 --- pharmacokinetics --- pharmacodynamics --- drug-drug interactions --- in vitro --- in vivo --- drug development --- tuberculosis treatment --- biomarkers --- drug combination --- clinical trial --- BCG --- tuberculosis vaccines --- TBVI --- EDCTP --- IAVI --- CTVD --- host-directed therapy --- anti-virulence compounds --- TB --- post-treatment sequelae --- surgery --- pulmonary rehabilitation --- Carlo Forlanini --- artificial pneumothorax --- n/a --- structure-based drug design --- target-based drug design --- PknB --- PknG --- DNA gyrase --- antibiotic --- mycobacterium --- genomics --- transcriptomics --- proteomics --- metabolomics --- lipidomics --- target identification --- mechanism of action --- antimicrobial drug resistance (AMR) --- target-based screening --- phenotypic screening --- antituberculosis agents --- antimycobacterial --- anti-TB drug pipeline --- privileged targets --- lead generation

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Polypharmacy is a necessary and important aspect of drug treatment; however, it becomes a challenge when the medication risks outweigh the benefits for an individual patient. Drug–drug interactions and the introduction of prescribing cascades are common features of polypharmacy, which can lead to ineffectiveness and increased risk of adverse drug reactions (ADR). Genes encoding CYP450 isozymes and other drug-related biomarkers have attracted considerable attention as targets for pharmacogenetic (PGx) testing due to their impact on drug metabolism and response. This Special Issue is devoted to explore the status and initiatives taken to circumvent ineffectiveness and to improve medication safety for polypharmacy patients. Specific areas include drug–drug interactions and consequences thereof in therapeutic management, including PK- and PD-profiling; the application of PGx-based guidance and/or decision tools for drug–gene and drug–drug gene interactions; medication reviews; development and application of deprescribing tools; and drivers and barriers to overcome for successful implementation in the healthcare system.

Medicine --- Pharmaceutical industries --- acute kidney injury --- early biomarker --- plasma neutrophil gelatinase-associated lipocalin --- soluble urokinase plasminogen activator receptor --- medication optimization --- older patients --- emergency department --- multimorbidity --- polypharmacy --- potentially inappropriate medication use --- older adults --- prevalence --- determinants --- chronic --- outpatient --- 2019 Beers criteria --- Ethiopia --- pharmacogenomics --- persons with diabetes --- drug–drug interactions --- drug–gene interactions --- cytochrome P450 --- SLCO1B1 --- drug interaction checkers --- adverse drug reactions --- pharmacogenetics --- personalized medicine --- phenprocoumon --- DOACs --- bleeding --- thromboembolism --- HLA --- drug hypersensitivity --- abacavir --- allopurinol --- flucloxacillin --- antiepileptic drugs --- cost-effectiveness --- shared medication record --- medication reconciliation --- drug information service --- hospital pharmacy service --- electronic prescribing --- electronic medical record --- clinical pharmacist --- CYP2D6 --- CYP2D7P --- CYP2D8P --- copy number variation --- CNV --- genotyping --- 5’nuclease assay --- HRM --- high resolution melting --- drug metabolization --- extracellular vesicles --- exosomes --- microvesicles --- pharmacogene expression --- medication review --- deprescriptions --- quality of life --- aged --- aged, 80 and over --- nursing homes --- deprescribing --- medication-based risk score --- health outcomes --- cytochromes --- CYP1A2 --- adverse drug reaction --- antipsychotics --- olanzapine --- clozapine --- loxapine --- children --- youth --- digital decision-support --- health services research --- general practice --- process evaluation --- antidepressants --- utility --- population-based --- appropriateness --- medication adherence --- digital health --- acute kidney injury --- early biomarker --- plasma neutrophil gelatinase-associated lipocalin --- soluble urokinase plasminogen activator receptor --- medication optimization --- older patients --- emergency department --- multimorbidity --- polypharmacy --- potentially inappropriate medication use --- older adults --- prevalence --- determinants --- chronic --- outpatient --- 2019 Beers criteria --- Ethiopia --- pharmacogenomics --- persons with diabetes --- drug–drug interactions --- drug–gene interactions --- cytochrome P450 --- SLCO1B1 --- drug interaction checkers --- adverse drug reactions --- pharmacogenetics --- personalized medicine --- phenprocoumon --- DOACs --- bleeding --- thromboembolism --- HLA --- drug hypersensitivity --- abacavir --- allopurinol --- flucloxacillin --- antiepileptic drugs --- cost-effectiveness --- shared medication record --- medication reconciliation --- drug information service --- hospital pharmacy service --- electronic prescribing --- electronic medical record --- clinical pharmacist --- CYP2D6 --- CYP2D7P --- CYP2D8P --- copy number variation --- CNV --- genotyping --- 5’nuclease assay --- HRM --- high resolution melting --- drug metabolization --- extracellular vesicles --- exosomes --- microvesicles --- pharmacogene expression --- medication review --- deprescriptions --- quality of life --- aged --- aged, 80 and over --- nursing homes --- deprescribing --- medication-based risk score --- health outcomes --- cytochromes --- CYP1A2 --- adverse drug reaction --- antipsychotics --- olanzapine --- clozapine --- loxapine --- children --- youth --- digital decision-support --- health services research --- general practice --- process evaluation --- antidepressants --- utility --- population-based --- appropriateness --- medication adherence --- digital health

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The gastrointestinal tract (GIT) can be broadly divided into several regions: the stomach, the small intestine (which is subdivided to duodenum, jejunum, and ileum), and the colon. The conditions and environment in each of these segments, and even within the segment, are dependent on many factors, e.g., the surrounding pH, fluid composition, transporters expression, metabolic enzymes activity, tight junction resistance, different morphology along the GIT, variable intestinal mucosal cell differentiation, changes in drug concentration (in cases of carrier-mediated transport), thickness and types of mucus, and resident microflora. Each of these variables, alone or in combination with others, can fundamentally alter the solubility/dissolution, the intestinal permeability, and the overall absorption of various drugs. This is the underlying mechanistic basis of regional-dependent intestinal drug absorption, which has led to many attempts to deliver drugs to specific regions throughout the GIT, aiming to optimize drug absorption, bioavailability, pharmacokinetics, and/or pharmacodynamics. In the book "Regional Intestinal Drug Absorption: Biopharmaceutics and Drug Formulation" we aim to highlight the current progress and to provide an overview of the latest developments in the field of regional-dependent intestinal drug absorption and delivery, as well as pointing out the unmet needs of the field.

Medicine --- Pharmaceutical industries --- bioequivalence --- Biopharmaceutics Classification System --- in vitro --- dissolution test --- pravastatin --- oral absorption --- in silico modeling --- GastroPlus --- Phoenix WinNonlin --- pharmacokinetics --- clinical studies --- ibuprofen --- manometry --- gastrointestinal --- mechanistic modeling --- PBPK --- PBBM --- disintegration --- dissolution --- enteric-coated --- ICH --- quality control --- regional intestinal permeability --- permeation enhancers --- absorption-modifying excipients --- oral peptide delivery --- intestinal perfusion --- pharmaceutical development --- controlled release drug product --- biopharmaceutics classification system --- drug solubility --- drug permeability --- location-dependent absorption --- segregated flow intestinal model (SFM) --- traditional model (TM) --- route-dependent intestinal metabolism --- first-pass effect --- drug-drug interactions --- DDI --- in vitro in vivo extrapolations --- IVIVE --- zero-order absorption --- first-order absorption --- combined zero- and first-order absorption --- transit compartment absorption model --- in situ perfusion --- microdevices --- shape --- mucoadhesion --- colon absorption --- nutrient digestion --- nutrient absorption --- gastrointestinal hormone --- postprandial glycaemia --- energy intake --- region of the gut --- obesity --- type 2 diabetes --- Franz–PAMPA --- BCS drugs --- biomimetic membrane --- Franz cell --- passive drug transport --- BCS class IV drugs --- segmental-dependent intestinal permeability --- intestinal absorption --- oral drug delivery --- biopharmaceutics --- physiologically-based pharmacokinetic (PBPK) modeling --- furosemide --- intestinal permeability --- human colon carcinoma cell layer (Caco-2) --- hierarchical support vector regression (HSVR) --- drug absorption --- drug solubility/dissolution --- regional/segmental-dependent permeability and absorption

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The gastrointestinal tract (GIT) can be broadly divided into several regions: the stomach, the small intestine (which is subdivided to duodenum, jejunum, and ileum), and the colon. The conditions and environment in each of these segments, and even within the segment, are dependent on many factors, e.g., the surrounding pH, fluid composition, transporters expression, metabolic enzymes activity, tight junction resistance, different morphology along the GIT, variable intestinal mucosal cell differentiation, changes in drug concentration (in cases of carrier-mediated transport), thickness and types of mucus, and resident microflora. Each of these variables, alone or in combination with others, can fundamentally alter the solubility/dissolution, the intestinal permeability, and the overall absorption of various drugs. This is the underlying mechanistic basis of regional-dependent intestinal drug absorption, which has led to many attempts to deliver drugs to specific regions throughout the GIT, aiming to optimize drug absorption, bioavailability, pharmacokinetics, and/or pharmacodynamics. In the book "Regional Intestinal Drug Absorption: Biopharmaceutics and Drug Formulation" we aim to highlight the current progress and to provide an overview of the latest developments in the field of regional-dependent intestinal drug absorption and delivery, as well as pointing out the unmet needs of the field.

bioequivalence --- Biopharmaceutics Classification System --- in vitro --- dissolution test --- pravastatin --- oral absorption --- in silico modeling --- GastroPlus --- Phoenix WinNonlin --- pharmacokinetics --- clinical studies --- ibuprofen --- manometry --- gastrointestinal --- mechanistic modeling --- PBPK --- PBBM --- disintegration --- dissolution --- enteric-coated --- ICH --- quality control --- regional intestinal permeability --- permeation enhancers --- absorption-modifying excipients --- oral peptide delivery --- intestinal perfusion --- pharmaceutical development --- controlled release drug product --- biopharmaceutics classification system --- drug solubility --- drug permeability --- location-dependent absorption --- segregated flow intestinal model (SFM) --- traditional model (TM) --- route-dependent intestinal metabolism --- first-pass effect --- drug-drug interactions --- DDI --- in vitro in vivo extrapolations --- IVIVE --- zero-order absorption --- first-order absorption --- combined zero- and first-order absorption --- transit compartment absorption model --- in situ perfusion --- microdevices --- shape --- mucoadhesion --- colon absorption --- nutrient digestion --- nutrient absorption --- gastrointestinal hormone --- postprandial glycaemia --- energy intake --- region of the gut --- obesity --- type 2 diabetes --- Franz–PAMPA --- BCS drugs --- biomimetic membrane --- Franz cell --- passive drug transport --- BCS class IV drugs --- segmental-dependent intestinal permeability --- intestinal absorption --- oral drug delivery --- biopharmaceutics --- physiologically-based pharmacokinetic (PBPK) modeling --- furosemide --- intestinal permeability --- human colon carcinoma cell layer (Caco-2) --- hierarchical support vector regression (HSVR) --- drug absorption --- drug solubility/dissolution --- regional/segmental-dependent permeability and absorption