Comparison of Bromhexine and its Active Metabolite - Ambroxol as Potential Analgesics Reducing Oxaliplatin-Induced Neuropathic Pain - Pharmacodynamic and Molecular Docking Studies.
CONCLUSION: The conversion of bromhexine to other than ambroxol active metabolites should be considered when interpreting some of its in vivo effects. Nav-blocking properties of bromhexine (and previously also predicted for ambroxol) might underlie their ability to attenuate pain caused by oxaliplatin. PMID: 32651960 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 11, 2020 Category: Drugs & Pharmacology Authors: Furgała-Wojas A, Kowalska M, Nowaczyk A, Fijałkowski Ł, Sałat K Tags: Curr Drug Metab Source Type: research

Updates on the Pharmacology of Chloroquine against Coronavirus Disease 2019 (COVID-19): A Perspective on its Use in the General and Geriatric Population.
CONCLUSION: According to literature reports, chloroquine has been proved to have anti-SARS-CoV-2 effect in vitro and the potential mechanism of chloroquine in vivo. Pharmacokinetic characteristics and DDIs study are helpful to guide rational drug use in general and geriatric patients. Although there have been reports of successful clinical application of chloroquine in treatment COVID-19,more clinical test data are still needed to prove its effectiveness and safety. PMID: 32651961 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 11, 2020 Category: Drugs & Pharmacology Authors: Yao X, Hou Z, Cui C, Zhang M, Tu S, Li H, Liu D Tags: Curr Drug Metab Source Type: research

Chemistry and antioxidant potential of phytoconstituents from Aegle marmelos fruit-shell.
CONCLUSION: Results showed that the hard shell of the Aegle marmelos fruit was a potent source for antioxidant compounds, which can be developed for therapeutic applications in control and management of metabolic diseases. PMID: 32651962 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 11, 2020 Category: Drugs & Pharmacology Authors: Chaubey A, Dubey AK Tags: Curr Drug Metab Source Type: research

Challenges in the Discovery of Novel Therapeutic Agents for Cancer Treatment (Part IV).
PMID: 32608350 [PubMed - in process] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 3, 2020 Category: Drugs & Pharmacology Authors: Nagaraju GP, Kamal MA Tags: Curr Drug Metab Source Type: research

New Therapeutic Molecules and their Metabolism in Gastroenterology.
PMID: 32613914 [PubMed - in process] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 3, 2020 Category: Drugs & Pharmacology Authors: Nakov R, Maida M, Ianiro G Tags: Curr Drug Metab Source Type: research

Annonaceae family alkaloids as agents against leishmaniasis: review and molecular docking evaluation.
This study presents an overview of the potential use of Annonaceae alkaloids to treat leishmaniasis and describes a molecular docking study examining 215 isoquinoline alkaloids. All selected compounds contain a bisbenzyltetrahydroisoquinoline, suggesting the affinity of this skeleton for the target. PMID: 32614742 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 2, 2020 Category: Drugs & Pharmacology Authors: Lorenzo VP, Scotti L, da Silva Almeida JRG, Scotti MT Tags: Curr Drug Metab Source Type: research

Exosomes as Targeted Drug Delivery Vehicles: Perspectives and Challenges.
PMID: 32614741 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 1, 2020 Category: Drugs & Pharmacology Authors: Liu D, Li X Tags: Curr Drug Metab Source Type: research

Hepatoprotective Role of Berberine on Doxorubicin Induced Hepatotoxici-ty - Involvement of Cyp.
CONCLUSION: It could be concluded that berberine may be an efficient anti-oxidant and immune modulator. It possesses low to moderate cytochrome modulatory potentials. PMID: 32586251 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - June 20, 2020 Category: Drugs & Pharmacology Authors: Sun B, Yang Y, He M, Jin Y, Cao X, Du X, Yang R Tags: Curr Drug Metab Source Type: research

Strong Association between Serotonin Transporter 5-HTTVNTR Variant and Psychoactive Substance (Nicotine) Use in the Turkish Cypriot Population.
Abstract BACKGROUND: The use of psychoactive substances is one of the most dangerous social problems worldwide. Nicotine dependence results from the interaction between neurobiological, environmental and genetic factors. Serotonin is a neurotransmitter that has a wide range of central nervous system activities. The serotonin transporter gene has been previously linked to psychological traits. OBJECTIVE: A variable number of tandem repeats within the serotonin transporter-linked polymorphic gene region is believed to alter the transcriptional efficiency of the 5-HTT gene. Therefore, we aimed to investigate the...
Source: Current Drug Metabolism - June 20, 2020 Category: Drugs & Pharmacology Authors: Kandemis E, Tuncel G, Asut O, Temel SG, Ergoren MC Tags: Curr Drug Metab Source Type: research

Preclinical Evidence for the Pharmacological Actions of Glycyrrhizic Acid: A Comprehensive Review.
Abstract BACKGROUND: Glycyrrhiza glabra L. (Family: Fabaceae) is one of the important traditional medicinal plant used extensively in folk medicine. INTRODUCTION: It is known for its ethanopharmacological value in curing a wide variety of ailments. Glycyrrhizin, an active compound of G. glabra, possesses anti-inflammatory activity due to which it is mostly used in traditional herbal medicine for the treatment and management of chronic diseases. METHODOLOGY: The present review is focused extensively on the pharmacology, pharmacokinetics, toxicology and potential effects of Glycyrrhizic Acid (GA). A thorou...
Source: Current Drug Metabolism - June 20, 2020 Category: Drugs & Pharmacology Authors: Rehman MU, Farooq A, Ali R, Bashir S, Bashir N, Majeed S, Taifa S, Ahmad SB, Arafah A, Sameer AS, Khan R, Qamar W, Rasool S, Ahmad A Tags: Curr Drug Metab Source Type: research

2020 FDA Drug-Drug Interaction Guidance -Comparison Analysis and Action Plan by Pharmaceutical Industrial Scientists.
CONCLUSION: The new 2020 clinical DDI guidance from the FDA now has even higher harmonization with the guidances (or guidelines) from the EMA and PMDA. A comparison of DDI guidances from the FDA 2017, 2020, EMA, and PMDA on CYP and transporter based DDI, mathematical models, PBPK and clinical evaluation of DDI is presented in this review. PMID: 32562522 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - June 20, 2020 Category: Drugs & Pharmacology Authors: Sudsakorn S, Bahadduri P, Fretland J, Lu C Tags: Curr Drug Metab Source Type: research

Salidroside - Can it be a multifunctional drug?
CONCLUSION: Salidroside is produced by a three-step pathway in the plants with tyrosol as an intermediate molecule. The molecule is biotransformed into many metabolites through phase I and II pathways. These metabolites, together with a certain amount of salidroside may be responsible for various pharmacological functions. The salidroside based inhibition of PI3k/AKT, JAK/ STAT, and MEK/ERK pathways and activation of apoptosis and autophagy are the major reasons for its anti-cancer activity. AMPK pathway modulation plays a significant role in its anti-diabetic activity. The neuroprotective activity was linked with decrease...
Source: Current Drug Metabolism - June 10, 2020 Category: Drugs & Pharmacology Authors: Magani SKJ, Mupparthi SD, Gollapalli BP, Shukla D, Tiwari AK, Gorantala J, Yarla NS, Tantravahi S Tags: Curr Drug Metab Source Type: research

Review on the clinical pharmacology of hydroxychloroquine sulfate for the treatment of COVID-19.
CONCLUSION: It has been proved that HCQ, which has an established safety profile, is effective against SARS-CoV-2 with sufficient pre-clinical rationale and evidence. Data from high-quality clinical trials are urgently needed worldwide. PMID: 32520683 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - June 10, 2020 Category: Drugs & Pharmacology Authors: Cui C, Tu S, En VSJ, Li X, Yao X, Li H, Liu D Tags: Curr Drug Metab Source Type: research

Gold nanoparticles; potential nanotheranostic agent in breast cancer: a comprehensive review with systematic search strategy.
CONCLUSION: Divergent strategies have shown the theranostic potential of surface tuned GNPs against breast cancer even in the metastatic stage with minimum cytotoxic effect both in vitro and in vivo. PMID: 32520684 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - June 10, 2020 Category: Drugs & Pharmacology Authors: Khandker SS, Shakil MS, Hossen MS Tags: Curr Drug Metab Source Type: research

The Potential Role of Serum Exosomes in Preeclampsia.
Abstract Preeclampsia is a serious pregnancy-specific disease that affects about 5%-8% of pregnant women and is the main reason for the increase in maternal and perinatal mortality. Due to unknown etiology, preeclampsia is still the main cause of increased mortality in maternal and perinatal infants, which is mainly manifested by new hypertension after 20 weeks of pregnancy. As the pathogenesis has not been fully elucidated, early diagnosis and full treatment are lacking. Exosomes secreted from the placenta to the peripheral circulation may be involved in the pathogenesis of preeclampsia, and can be detected from ...
Source: Current Drug Metabolism - May 25, 2020 Category: Drugs & Pharmacology Authors: Gao X, Shao L, Ge X, Zhang L, Chen D, He R Tags: Curr Drug Metab Source Type: research

Modulation of the drug resistance by Platonia insignis Mart. extract, ethyl acetate fraction and Morelloflavone/Volkensiflavone (biflavonoids) in Staphylococcus aureus strains overexpressing efflux pump genes.
CONCLUSION: P. inignisis a source of efflux pump inhibitors, including volkensiflavone and morelloflavone which were able to potentiate the Norfloxacin activity by NorA inhibition, being also able to inhibit QacA/B, TetK and MsrA. Volkensiflavone and morelloflavone could be used as adjuvant in the antibiotic therapy of multidrug resistant S. aureus strains overexpressing efflux pumps. PMID: 32445452 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 23, 2020 Category: Drugs & Pharmacology Authors: Ferreira E Silva AK, Dos Reis AC, Pinheiroc EEA, de Sousa JN, de Alcântara Oliveira FA, Moura AKS, de Souza Lima Neto J, das Graças Lopes Citó AM, de Siqueira-Júnior JP, Kaatz GW, Barreto HM Tags: Curr Drug Metab Source Type: research

Nano phytomedicine based delivery system for CNS disease.
This article reviews herbal medicines which have prominent activity in Central Nervous System (CNS) disorder and reported nano-phytomedicines based delivery systems. Keywords: Nano formulation, phytomedicine, central nervous system, neurodegenerative disorder, nano-phytomedicines, herbal medicine. PMID: 32445453 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 23, 2020 Category: Drugs & Pharmacology Authors: Jahangir MA, Anand C, Muheem A, Gilani SJ, Taleuzzaman M, Zafar A, Jaffer M, Verma S, Barkat MA Tags: Curr Drug Metab Source Type: research

Challenges in the Discovery of Novel Therapeutic Agents in Cancer (Part III).
PMID: 32423370 [PubMed - in process] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 21, 2020 Category: Drugs & Pharmacology Authors: Kamal MA, Nagaraju GP Tags: Curr Drug Metab Source Type: research

Kolliphor ® HS 15-Cyclodextrin Complex for the Delivery of Voriconazole: Preparation, Characterization, and Antifungal Activity.
This study aimed to reduce the amount of sulfobutylether-β-cyclodextrin (SBECD) used in the marketed voriconazole injections to meet the clinical needs of patients with moderateto-severe renal impairment (creatinine clearance rate
Source: Current Drug Metabolism - May 19, 2020 Category: Drugs & Pharmacology Authors: Li Y, Zhu C, Wu H, Pan H, Liu H Tags: Curr Drug Metab Source Type: research

Using reduced amino acid alphabet and biological properties to analyze and predict animal neurotoxin protein.
In this study, the differences between the animal neurotoxin proteins and nontoxin proteins were analyzed. Significant differences were found between them. In addition, the support vector machine was proposed to predict the animal neurotoxin proteins. The predictive results of our classifier achieved the overall accuracy of 96.46%. Furthermore, the random forest and k-nearest neighbors were applied to predict the animal neurotoxin proteins. The compared results indicated that the predictive performances of our classifier were better than other two algorithms. PMID: 32433000 [PubMed - as supplied by publisher] (Source:...
Source: Current Drug Metabolism - May 19, 2020 Category: Drugs & Pharmacology Authors: Yu Y, Wang S, Wang Y, Cao Y, Yu C, Pan Y, Su D, Lu Q, Zuo Y, Yang L Tags: Curr Drug Metab Source Type: research

Role of exosomes in the exchange of spermatozoa after leaving the seminiferous tubule. A review.
CONCLUSION: This review thoroughly discussed the role that exosomes play in the exchange of spermatozoa after leaving the seminiferous tubule and its potential as a drug delivery tool and biomarkers for diseases as well. PMID: 32433001 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 19, 2020 Category: Drugs & Pharmacology Authors: Wu L, Ding Y, Han S, Wang Y Tags: Curr Drug Metab Source Type: research

Tumor-targeted drug delivery by nanocomposites.
CONCLUSION: In our review, we illustrate different types of triggered moods and stimuli of tumor environment which help in smart multistage drug delivery systems by nanoparticles, basically a multi-stimuli sensitive delivery system, and elaborate their function, effects, and diagnosis. PMID: 32433002 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 19, 2020 Category: Drugs & Pharmacology Authors: Baker A, Khan MS, Iqbal MZ, Khan MS Tags: Curr Drug Metab Source Type: research

Exosome-based Tumor Therapy: Opportunities and Challenges.
CONCLUSION: Exosomes are involved in multiple processes during tumor development and should be further studied as novel targets for cancer therapy. PMID: 32410558 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 14, 2020 Category: Drugs & Pharmacology Authors: Li C, Hou X, Zhang P, Li J, Liu X, Wang Y, Guan Q, Zhou Y Tags: Curr Drug Metab Source Type: research

Evaluating Lean Liver Volume as a Potential Scaler for in vitro-in vivo Extrapolation of Drug Clearance in Obesity using the model drug antipyrine.
Conclusion The analysis indicates that LLV is potentially a more appropriate descriptor of functional liver size than LV, particularly in overweight individuals. Therefore, LLV has potential application in IVIVE of CL in obesity. PMID: 32410559 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 14, 2020 Category: Drugs & Pharmacology Authors: Sinha J, Duffull SB, Green B, Al-Sallami HS Tags: Curr Drug Metab Source Type: research

Effect of Green Tea and (-)-epigallocatechin Gallate on the Pharmacokinetics of Rosuvastatin.
This study aimed to investigate the effects of green tea on the pharmacokinetics of rosuvastatin and its mechanism. METHODS: Male Sprague-Dawley rats received different doses of green tea extract (GTE) and (-)- epigallocatechin-3-gallate (EGCG). Caco-2 cells and OATP1B1-HEK293T cells were used in drug uptake and transport assay. The matrix concentrations of rosuvastatin and catechins were determined by ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). RESULTS: GTE and EGCG were both found to increase the area under the plasma concentration-time curve (AUC0-∞) of rosuvastatin ((p
Source: Current Drug Metabolism - May 14, 2020 Category: Drugs & Pharmacology Authors: Huang S, Xu Q, Liu L, Bian Y, Zhang S, Huang C, Miao L Tags: Curr Drug Metab Source Type: research

Effect of Nigella sativa and Fenugreek on the pharmacokinetics and pharmacodynamics of amlodipine, in hypertensive rats.
CONCLUSION: Results of pharmacodynamics and pharmacokinetics studies suggested that simultaneous administration of fenugreek or N. sativa with amlodipine improves the pharmacological response of amlodipine in hypertensive rats, though there was no remarkable change in pharmacokinetic parameters (Cmax, Kel, elimination t1/2, and AUC0-t,). PMID: 32407268 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 14, 2020 Category: Drugs & Pharmacology Authors: Alam MA, Bin Jardan YA, Raish M, Al-Mohizea AM, Ahad A, Al-Jenoobi FI Tags: Curr Drug Metab Source Type: research

Pharmacogenetic evaluation of metformin and sulphonylurea response in Mexican Mestizos with type 2 diabetes.
CONCLUSION: The interaction between rs72552763 and rs622342 in OCT1, and rs12943590 in MATE2 suggested an important role of these polymorphisms in metformin response in T2D Mexican Mestizo population. PMID: 32407269 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 14, 2020 Category: Drugs & Pharmacology Authors: Marta M, Katy SP, Joel JS, Jazmin ME, Carolina RS, de Los Ángeles GM, Guadalupe OM Tags: Curr Drug Metab Source Type: research

Model-based Meta-analysis to Compare Primary Efficacy-endpoint, Efficacy-time Course, safety, and Tolerability of Opioids Used in the Management of Osteoarthritic Pain in Humans.
CONCLUSIONS: This MBMA provides clinically meaningful insights into the efficacy and safety profiles of oxycodone, oxymorphone, and tramadol. Resultantly, the presented framework analysis can have an impact in the clinic on drug development where it can guide: the optimization of doses of opioids required to manage osteoarthritic pain; the making of precise key decisions for the positioning of new drugs, and; the design more efficient trials. PMID: 32407270 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 14, 2020 Category: Drugs & Pharmacology Authors: Suliman SO, Milavetz G, Salem AK Tags: Curr Drug Metab Source Type: research

Absorption, metabolism and excretion of surufatinib in rats and humans.
CONCLUSION: Fecal excretion was the predominant way for the elimination of surufatinib and its metabolites in rats and humans. No disproportionate circulating metabolite was observed in humans. PMID: 32407271 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 14, 2020 Category: Drugs & Pharmacology Authors: Li K, Ma S, Miao L, Fan S, Pan B, Zhang W, Su W, Xiong Y, Gu Z, Guo L, Sai Y Tags: Curr Drug Metab Source Type: research

Influence of Rifampicin Pre-treatment on the In Vivo Pharmacokinetics of Metoclopramide in Pakistani Healthy Volunteers Following Concurrent Oral Administration.
This study was aimed at the evaluation of rifampicin's enzyme induction effect on the pharmacokinetic parameters of orally administered metoclopramide. METHOD: This randomized, single-blind, two-phase cross-over pharmacokinetic study separated by a 4-week wash-out period was conducted at a single center in Pakistan. It involved twelve Pakistani healthy male volunteers (non-smokers) divided into two groups. In the reference phase, each volunteer received a single oral dose of 20 mg metoclopramide (Maxolon 10 mg, GlaxoSmithKline, Pakistan), while in the rifampicin-treated phase, each volunteer received 600 mg rifampicin...
Source: Current Drug Metabolism - May 14, 2020 Category: Drugs & Pharmacology Authors: Kaukab I, Shah SNH, Abrar MA, Anwer N, Murtaza G Tags: Curr Drug Metab Source Type: research

Role of Genetic Polymorphisms of Cytochrome P450 2C19 in Pantoprazole Metabolism and Pantoprazole-based Helicobacter pylori Eradication Regimens.
CONCLUSION: The data on cytochrome P450 gene polymorphisms and their role in pantoprazole metabolism and pantoprazole based Helicobacter pylori eradication remain conflicting. Individual differences in pantoprazole metabolism might be partly related to genetic polymorphisms of CYP450 enzymes. Most of the studies support the observation that cytochrome 2C19 polymorphisms have an impact on the pharmacokinetics of pantoprazole and its therapeutic effects: poor metabolizers of PPIs are more likely to have a better response to pantoprazole therapy and achieve better H. pylori eradication rates compared to rapid metabolizers. Th...
Source: Current Drug Metabolism - May 13, 2020 Category: Drugs & Pharmacology Authors: Jonaitis P, Jonaitis L, Kupcinskas J Tags: Curr Drug Metab Source Type: research

Secondary Metabolites in the Treatment of Diabetes Mellitus: A Paradigm Shift.
Abstract Diabetes mellitus (DM) is a chronic, polygenic and non-infectious group of diseases that occurs due to insulin resistance or its low production by pancreas and is also associated with lifelong damage, dysfunction and collapse of various organs. Management of diabetes is quite complex having many bodily and emotional complications and warrants efficient measures for prevention and control of the same. As per the estimates of current and future diabetes prevalence around 425 million people were diabetic in 2017 which is anticipated to rise upto 629 million by 2045. Various studies have vaguely proven the fa...
Source: Current Drug Metabolism - May 13, 2020 Category: Drugs & Pharmacology Authors: Chauhan DS, Gupta P, Pottoo FH, Amir M Tags: Curr Drug Metab Source Type: research

Dose optimization of gentamicin in critically ill neonates.
CONCLUSION: Currently used dose of 4 mg/kg/day is adequate to maintain Cmax in large majority of the study population, with onefourth population reporting the recommended AUC0-24. Increasing the dose to 5-6 mg/kg/day more likely will help to achieve both the recommended Cmax and AUC0-24 values. PMID: 32394828 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 12, 2020 Category: Drugs & Pharmacology Authors: Sridharan K, Al Jufairi M, Qader AM, Elsegai OA Tags: Curr Drug Metab Source Type: research

Evaluation of the effects of Maytenus ilicifolia on the activities of cytochrome P450 3A and P-glycoprotein.
CONCLUSION: The results suggest that M. ilicifolia can inhibit the intestinal metabolism and transport of drugs mediated by CYP3A and P-gp, respectively, however, involvement of other transporters and the clinical relevance of such interaction still need to be clarified. PMID: 32394829 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 12, 2020 Category: Drugs & Pharmacology Authors: de Castro WV, do Nascimento SB, de Lima Nascimento M, de Araújo LL, de Oliveira FM, do Carmo Vieira M, Duarte-Almeida JM, Siqueira JM, da Costa César I, Derendorf H Tags: Curr Drug Metab Source Type: research

Changes of Transporters and Drug-metabolizing Enzymes in Nephrotic Syndrome.
CONCLUSION: The changes of drug-metabolizing enzymes and transporters expression in AN rats were clarified, which may be beneficial for understanding the altered pharmacokinetics and pharmacodynamics of clinical drugs and reduce unexpected clinical findings for nephropathy patients. PMID: 32394830 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 12, 2020 Category: Drugs & Pharmacology Authors: Dong Y, Gong L, Lu X, Ye M, Lin Y, Xie S, Zhang J, Zhou F, Tang L, Zou W, Liu M Tags: Curr Drug Metab Source Type: research

Polymeric Nanoparticles For Brain Drug Delivery - A Review.
CONCLUSION: More standardized methods for the preparation of nanoparticles and to assess the relationship of surface modification on drug delivery. While the preparation and its output like drug loading, particle size and charge, permeation is always conflicted, so it requires more attention for the acceptance of nanoparticles for brain delivery. PMID: 32384025 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 7, 2020 Category: Drugs & Pharmacology Authors: Raman S, Mahmood S, Hilles AR, Javed MN, Azmana M, Al-Japairai KAS Tags: Curr Drug Metab Source Type: research

Genetic analysis of pharmacogenomic VIP variants of ABCB1, VDR and TPMT genes in an ethnically isolated population from the North Caucasus living in Jordan.
CONCLUSION: Significant differences in allelic frequencies of eleven ABCB1, VDR and TPMT VIP variants were found between Jordanian Chechens and other populations. In our study, the most populations that are similar to Chechens are those from South Asian, European (Finnish) and European, including: Utah residents with Northern and Western European ancestry, Toscani in Italia, Mexican ancestry in Los Angeles and Circassian from Jordan. The level of similarity between Chechens and those populations means that they might have shared high levels of gene flow in the past. The results obtained in this study will contribute to the...
Source: Current Drug Metabolism - May 4, 2020 Category: Drugs & Pharmacology Authors: Al-Eitan LN, Al-Maqableh HW, Mohammad NN, Hakooz NM, Dajani RB Tags: Curr Drug Metab Source Type: research

Lead optimization from natural ligands by in-silico approach for discovering potential monoamine oxidasesinhibitors(MAOIs).
CONCLUSIONS: These natural potential ligands have been found comparable to the standard drugs against MAO-A and MAO-B, which may be treated as alead compound for the exploration of new drug compounds. The results of in silico screening were in good correlation with in vitro hMAO inhibitory activity. PMID: 32357811 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 1, 2020 Category: Drugs & Pharmacology Authors: Dhiman P, Malik N, Khatkar A Tags: Curr Drug Metab Source Type: research

Preclinical Study of the Pharmacokinetics of p75ECD-Fc, a Novel Human Recombinant Protein for Treatment of Alzheimer's Disease, in Sprague Dawley rats.
CONCLUSION: these acceptable pharmacokinetic properties of p75ECD-Fc present it as a potential candidate for clinical development for the treatment of Alzheimer's disease. PMID: 32357812 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 1, 2020 Category: Drugs & Pharmacology Authors: Kelliny S, Lam HY, Parikh A, Wang Y, Bobrovskaya L, Upton R, Zhou XF Tags: Curr Drug Metab Source Type: research

Effect of curcumin nanoemulsions stabilized with modified phosphatidylcholine on skin carcinogenesis in transgenic mice K14E6.
;a HS Abstract BACKGROUND: Cancer is one of the main causes of death by disease; several alternative treatments have been developed to counteract this condition. Curcumin (diferuloylmethane), extracted from the rhizome of Curcuma longa, has antioxidant, antiinflammatory, and anti-cancer properties; however, it has low water solubility and poor intestinal absorption. Carrier systems, such as nanoemulsions, can increase the bioavailability of lipophilic bioactive compounds. OBJECTIVE: To evaluate the effect of curcumin nanoemulsions prepared with lecithin modified with medium-chain fatty acids as an emulsifier,...
Source: Current Drug Metabolism - April 29, 2020 Category: Drugs & Pharmacology Authors: Agame-Lagunes B, Alegria-Rivadeneyra M, Quintana-Castro R, Torres-Palacios C, Grube-Pagola P, Cano-Sarmiento C, Garcia-Varela R, Alexander-Aguilera A, García HS Tags: Curr Drug Metab Source Type: research

Potential of mirabegron and its extended-release formulations for the treatment of overactive bladder syndrome.
Conclusion: Mirabegron shows a distinct mode of action, i.e., targeting β3-adrenoreceptors and improve bladder storage without altering void contractions. The limited side effects, high safety, efficacy and tolerability of mirabegron present an adequate substitute to antimuscarinics. However, long-term analysis and clinical studies are prerequisites for assessing the safety , tolerebility and efficacy profile of mirabegron. PMID: 32334500 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - April 25, 2020 Category: Drugs & Pharmacology Authors: Mandpe P, Prabhakar B, Shende P Tags: Curr Drug Metab Source Type: research

Human papillomavirus induced Cervical and Oropharyngeal Cancers: From Mechanisms to Potential Immuno-Therapeutic Strategies.
Abstract The human papillomavirus (HPV) associated infections are the hallmark of cervical and neck cancer. Almost all the cases of cervical cancer (CC) and 70% of oropharyngeal cancer (OC) are more or less caused by the persistent infection of HPV. CC is fourth most common cancer globally and is commenced by the persistent infection with human papillomaviruses (HPVs), predominantly HPV types; 16 and 18. In the light of above facts, there is an immediate requirement to develop novel preventive and innovative therapeutic strategies that may help in lower occurrences of HPV mediated cancers. Currently, only radiatio...
Source: Current Drug Metabolism - April 21, 2020 Category: Drugs & Pharmacology Authors: Saeed M, Faisal SM, Akhtar F, Ahmad S, Alreshidi MM, Kausar MA, Kazmi S, Saeed A, Adnan M, Ashraf GM Tags: Curr Drug Metab Source Type: research

Insights of potent therapeutical anti leukemic agent L-Glutaminase enzyme under solid state fermentation: A review.
Conclusion: In the current review, study was focussed on the production of L-glutaminase by SSF. The production of L-glutaminase by SSF has reported from both bacteria and fungi. It was understood from the reported literature that optimization studies enhanced the production of L-glutaminase. Researchers has also confirmed the anti-leukemic, anti-tumour properties of the purified L-glutaminase on various cell lines. PMID: 32316889 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - April 21, 2020 Category: Drugs & Pharmacology Authors: Durthi CP, Pola M, Rajulapati SB, Kola AK Tags: Curr Drug Metab Source Type: research

Drug-induced bile duct injury - a short review.
Abstract The liver represents the major site of drug metabolism, i.e. the key organ in the processes of detoxification and elimination of drugs from the organism. It is therefore often affected by toxic metabolites and suffers sometimes fatal consequences. The spectrum of pathologies differs by the cell type primarily damaged and the group of the cholangiopathies includes those conditions affecting the bile duct epithelium or the cholangiocytes. They can range from transient cholestasis to vanishing bile duct syndrome and sclerosing cholangitis, both leading eventually to the development of biliary fibrosis and ci...
Source: Current Drug Metabolism - April 19, 2020 Category: Drugs & Pharmacology Authors: Dobreva I, Karagyozov P Tags: Curr Drug Metab Source Type: research

Clinical Pharmacokinetics of Propranolol Hydrochloride: A Review.
CONCLUSION: Physiochemical and pooled pharmacokinetic parameters of propranolol are beneficial in order to establish physiologically based pharmacokinetic modeling among the diseased population. PMID: 32286940 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - April 13, 2020 Category: Drugs & Pharmacology Authors: Kalam MN, Rasool MF, Asim Ur Rehman, Ahmed N Tags: Curr Drug Metab Source Type: research

Aox1 And Xdh Enzymes Genotyping And Its Effect On Clinical Response To Azathioprine In Inflammatory Bowel Disease Patients Among Jordanian Population.
CONCLUSIONS: this study revealed that 16% of our patients were Non-responders to AZA; they needed an alternative therapy (biological agent) or steroids along with AZA. There were no statistically significant association (p-value>0.05) between the AOX1 3404G, XDH 1936C and XDH 2107C polymorphisms and the response to AZA among Jordanian IBD patients. Finally, the study showed an association between the age of the patient and the response to AZA (p-value=0.013). PMID: 32282298 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - April 13, 2020 Category: Drugs & Pharmacology Authors: Mahasneh S, Sharab A, Al Shhab M, Rashid M, Zihlif M Tags: Curr Drug Metab Source Type: research

Glioblastoma under siege of Therapeutics and Research: "Advancements and Future Targets".
Glioblastoma under siege of Therapeutics and Research: "Advancements and Future Targets". Curr Drug Metab. 2020 Apr 07;: Authors: Chavda V, Patel V, Yadav D, Shah J, Patel S, Jin JO Abstract Glioblastoma, most common primary brain tumor has been recognized as a one of the most lethal and fatal human tumors, which has a dismal prognosis with an average life duration not more than 15 months and end up with surgery and radiotherapy which ideally suggest a hope to escape an underprivileged diagnosis. As aimed at, numerous strategies were currently believed to upgrade in-vivo and in-vitro models ...
Source: Current Drug Metabolism - April 7, 2020 Category: Drugs & Pharmacology Authors: Chavda V, Patel V, Yadav D, Shah J, Patel S, Jin JO Tags: Curr Drug Metab Source Type: research

Has the time come to employ population and individual bioequivalence for the evaluation of generics?
CONCLUSION: The outcome of the evaluation clearly states that the bioequivalence outcome of all these approaches are the same. Obviously, it does not mean that these three approaches provide the same outcome though the consideration of variances vary. Certainly, population bioequivalence and individual bioequivalence approach will be more accurate for the assessment of drug interchangeability. PMID: 32234000 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - March 31, 2020 Category: Drugs & Pharmacology Authors: Micheal F, Sayana M, Prasad R, Motial BM Tags: Curr Drug Metab Source Type: research

Further considerations towards an effective and efficient oncology drug discovery DMPK strategy.
CONCLUSION: Application of our updated drug-drug interaction and central nervous system drug exposure strategies are exemplified, as is the impact of physiologically based pharmacokinetic and pharmacokinetic-pharmacodynamic modelling, for human predictions. PMID: 32164508 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - March 11, 2020 Category: Drugs & Pharmacology Authors: Williamson B, Colclough N, Fretland A, Jones B, Owen R, McGinnity D Tags: Curr Drug Metab Source Type: research

Meta-analysis of NFKB1 -94 ATTG ins/del polymorphism and risk of breast cancer.
CONCLUSION: To summarize, our meta-analysis demonstrates that the NFKB1 -94 ATTG I/D polymorphism is not a major risk factor for BC. PMID: 32156231 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - March 10, 2020 Category: Drugs & Pharmacology Authors: Kancharla J, Devi VPI, Lakkakula BV, Veera BP, Afroz A Tags: Curr Drug Metab Source Type: research