3,985 results match your criteria Expert Opinion on Drug Metabolism & Toxicology[Journal]


Enhancement of lung levels of antibiotics by ambroxol and bromhexine.

Expert Opin Drug Metab Toxicol 2019 Mar 7;15(3):213-218. Epub 2019 Feb 7.

b Department of Pharmaceutical Sciences, College of Pharmacy , University of New Mexico Health Sciences Center , Albuquerque , NM , USA.

Introduction: Major unmet needs remain for improved antibiotic treatment in lung infections. While development of new antibiotics is needed to overcome resistance, other approaches to optimize therapy using existing agents are also attractive. Ambroxol induces lung autophagy at human-relevant doses and improves lung levels of several approved antibiotics. Read More

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http://dx.doi.org/10.1080/17425255.2019.1578748DOI Listing
March 2019
4 Reads

Rational and clinical development of the anti-MAdCAM monoclonal antibody for the treatment of IBD.

Expert Opin Biol Ther 2019 Jan 29:1-6. Epub 2019 Jan 29.

a Inflammatory Bowel Disease Center and Amsterdam Gastroenterology and Metabolism , Amsterdam UMC, University of Amsterdam , Amsterdam , The Netherlands.

Introduction: Mucosal addressin cell adhesion molecule-1 (MAdCAM-1) expression in gut-associated lymphoid tissue is upregulated in patients with inflammatory bowel disease (IBD). Blocking adhesion molecules and thereby inhibiting migration of lymphocytes into sites of inflammation in the gut is an attractive new treatment target in drug development for IBD. Areas covered: This review discusses the preclinical and clinical experience on SHP647 (previously called PF-00547659 and PF-00547,659), a fully human IgG2K monoclonal antibody that binds to MAdCAM-1 to selectively reduce lymphocyte homing to the intestinal tract. Read More

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http://dx.doi.org/10.1080/14712598.2019.1576631DOI Listing
January 2019
1 Read

Pharmacokinetic considerations for anti-epileptic drugs in children.

Expert Opin Drug Metab Toxicol 2019 Mar 7;15(3):199-211. Epub 2019 Feb 7.

a Department of Pediatrics , University of L'Aquila , L'Aquila , Italy.

Introduction: Epilepsy is a chronic and debilitating neurological disease, with a peak of incidence in the first years of life. Today, the vast armamentarium of antiepileptic drugs (AEDs) available make even more challenging to select the most appropriate AED and establish the most effective dosing regimen. In fact, AEDs pharmacokinetics is under the influence of important age-related factors which cannot be ignored. Read More

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http://dx.doi.org/10.1080/17425255.2019.1575361DOI Listing
March 2019
7 Reads

Strategies to optimize drug half-life in lead candidate identification.

Expert Opin Drug Discov 2019 Mar 24;14(3):221-230. Epub 2019 Jan 24.

a Department of Drug Metabolism and Pharmacokinetics , Genentech , South San Francisco , CA , USA.

Introduction: The PK optimization of drug candidates is one of the most resource-intensive tasks in pharmaceutical research and development. With the increasing availability of in silico, in vitro and mechanistic in vivo ADME models, drug discovery scientists have progressively learned to recognize common SAR patterns and engineer data-driven strategies to accelerate the resolution of ADME issues in lead optimization. Many of these strategies gravitate toward the concept of drug-likeness, which defines a number of optimal holistic physicochemical parameters (such as lipophilicity) that idealized oral drugs possess. Read More

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http://dx.doi.org/10.1080/17460441.2019.1569625DOI Listing

Chemical activation of estrogen and aryl hydrocarbon receptor signaling pathways and their interaction in toxicology and metabolism.

Expert Opin Drug Metab Toxicol 2019 Mar 27;15(3):219-229. Epub 2019 Jan 27.

a Department of Chemical & Product Safety , German Federal Institute for Risk Assessment (BfR) , Berlin , Germany.

Introduction: Estrogen receptors (ERs) and the arylhydrocarbon receptor (AHR) are ligand-activated transcription factors that regulate the expression of genes involved in many physiological processes. With both receptors binding a broad range of natural and anthropogenic ligands, they are molecular targets for many substances, raising concerns for possible health effects. Areas covered: This review shall give a brief overview on the physiological functions of both receptors including their underlying molecular mechanisms. Read More

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http://dx.doi.org/10.1080/17425255.2019.1569627DOI Listing
March 2019
4 Reads

GPR17 receptor modulators and their therapeutic implications: review of recent patents.

Expert Opin Ther Pat 2019 Feb 24;29(2):85-95. Epub 2019 Jan 24.

a School of Pharmacy, Medicinal Chemistry Unit , University of Camerino , Camerino , Italy.

Introduction: The GPR17 receptor, phylogenetically related to both purinergic P2Y and CysLT receptors, is mainly expressed in the CNS and, in general, in organs that can typically undergo ischemic damage. This receptor is involved in various pathologies including stroke, brain and spinal cord trauma, multiple sclerosis and in all diseases characterized by neuronal and myelin dysfunction. Therefore, there is a strong needed to identify molecules capable of binding specifically to GPR17 receptors. Read More

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http://dx.doi.org/10.1080/13543776.2019.1568990DOI Listing
February 2019
2 Reads

A patent review of arginine methyltransferase inhibitors (2010-2018).

Expert Opin Ther Pat 2019 Feb;29(2):97-114

a CAS Key Laboratory of Receptor Research, State Key Laboratory of Drug Research, Drug Discovery and Design Center , Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai , China.

Introduction: Protein arginine methyltransferases (PRMTs) are fundamental enzymes that specifically modify the arginine residues of versatile substrates in cells. The aberrant expression and abnormal enzymatic activity of PRMTs are associated with many human diseases, especially cancer. PRMTs are emerging as promising drug targets in both academia and industry. Read More

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http://dx.doi.org/10.1080/13543776.2019.1567711DOI Listing
February 2019
1 Read
4.297 Impact Factor

Pharmacokinetics and pharmacodynamics of monoclonal antibodies for asthma treatment.

Expert Opin Drug Metab Toxicol 2019 Feb 24;15(2):113-120. Epub 2019 Jan 24.

b Department of Internal Medicine, Respiratory Disease Clinic , IRCCS Humanitas Clinical and Research Center, Humanitas University , Milan , Italy.

Introduction: Asthma is a chronic inflammatory airway disease. It occurs in a 'severe' form in about 8-10% of asthmatic patients. In the last decade, the development of biological drugs (e. Read More

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http://dx.doi.org/10.1080/17425255.2019.1568409DOI Listing
February 2019
4 Reads

Novel β-lactam-β-lactamase inhibitor combinations: expectations for the treatment of carbapenem-resistant Gram-negative pathogens.

Expert Opin Drug Metab Toxicol 2019 Feb 10;15(2):133-149. Epub 2019 Jan 10.

a 1st Department of Internal Medicine-Infectious Diseases , Hygeia General Hospital , Athens , Greece.

Introduction: The burden of antimicrobial resistance among Gram-negative bacteria is increasing and growing into a major threat of public health. Treatment options for carbapenem-resistant Enterobacteriaceae are limited and resistance rates to existing compounds are mounting. The pipeline includes only a small number of novel anti-infective agents in development or in the market with promising results against multidrug-resistant (MDR) Gram-negative. Read More

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http://dx.doi.org/10.1080/17425255.2019.1563071DOI Listing
February 2019
3 Reads

Selective Tyk2 inhibitors as potential therapeutic agents: a patent review (2015-2018).

Expert Opin Ther Pat 2019 Feb 22;29(2):137-149. Epub 2019 Jan 22.

a Key Laboratory of Elemene Class Anti-Cancer Chinese Medicine of Zhejiang Province, Hangzhou Normal University , Hangzhou , Zhejiang Province , China.

Introduction: Tyrosine kinase 2 (Tyk2) is a non-receptor tyrosine-protein kinase, an enzyme that in humans is encoded by the TYK2 gene. Tyk2, together with three other family subtypes, namely, Jak1, Jak2, and Jak3, belong to the JAK family. Before 2014, far more publications and patents appeared in public domain attributing to the development of selective Jak2 and Jak3 inhibitors than those for selective Tyk2 and Jak1 inhibitors. Read More

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http://dx.doi.org/10.1080/13543776.2019.1567713DOI Listing
February 2019
22 Reads

Pharmacotherapeutic strategies for treating pancreatic cancer: advances and challenges.

Expert Opin Pharmacother 2018 Dec 28:1-12. Epub 2018 Dec 28.

a Department of Oncology, Karmanos Cancer institute , Wayne State University , Detroit , MI , USA.

Introduction: Despite many efforts to improve the outcome of pancreatic ductal adenocarcinoma (PDAC), its prognosis remains poor, which is mostly related to late diagnosis and drug resistance. Improving systemic therapy is considered the major challenge in improving the outcome of this disease. Areas covered: This review covers novel chemotherapy and targeted agents in the treatment of PDAC, with a focus on advanced stage disease. Read More

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https://www.tandfonline.com/doi/full/10.1080/14656566.2018.1
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http://dx.doi.org/10.1080/14656566.2018.1561869DOI Listing
December 2018
5 Reads

Rapastinel - an investigational NMDA-R modulator for major depressive disorder: evidence to date.

Expert Opin Investig Drugs 2019 Feb 26;28(2):113-119. Epub 2018 Dec 26.

a Mood Disorders Psychopharmacology Unit , University Health Network , Toronto , Canada.

Introduction: Major depressive disorder (MDD) is a debilitating disorder with increasing prevalence globally. Despite the development of novel treatments for MDD, many patients present with treatment resistant depression (TRD), identified by treatment non-response following one or more adequate trials of an antidepressant. Rapastinel may prove to be a viable treatment for TRD; it has the potential to produce a rapid antidepressant response without serious adverse events and improve functional symptoms. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543784.2019.1
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http://dx.doi.org/10.1080/13543784.2019.1559295DOI Listing
February 2019
4 Reads

An update on polyphenol disposition via coupled metabolic pathways.

Expert Opin Drug Metab Toxicol 2019 Feb 24;15(2):151-165. Epub 2018 Dec 24.

a Joint Laboratory for Translational Cancer Research of Chinese Medicine of the Ministry of Education of the People's Republic of China, International Institute for Translational Chinese Medicine , Guangzhou University of Chinese Medicine , Guangzhou, Guangdong , China.

Introduction: Polyphenols, which are widely distributed in plants and the human diets, are known to have numerous biological activities. However, the low bioavailability of polyphenols is mediated by coupled metabolic pathways. Areas covered: The key role of the interplay between drug metabolic enzymes (DMEs) and efflux transporters (ETs), nuclear receptors (NRs), and intestinal microflora in the disposition of polyphenols is summarized. Read More

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http://dx.doi.org/10.1080/17425255.2019.1559815DOI Listing
February 2019

Overcoming barriers to optimal drug dosing during ECMO in critically ill adult patients.

Expert Opin Drug Metab Toxicol 2019 Feb 3;15(2):103-112. Epub 2019 Jan 3.

f Adult Intensive Care Services , The Prince Charles Hospital , Chermside , Australia.

Introduction: One major challenge to achieving optimal patient outcome in extracorporeal membrane oxygenation (ECMO) is the development of effective dosing strategies in this critically ill patient population. Suboptimal drug dosing impacts on patient outcome as patients on ECMO often require reversal of the underlying pathology with effective pharmacotherapy in order to be liberated of the life-support device. Areas covered: This article provides a concise review of the effective use of antibiotics, analgesics, and sedative by characterizing the specific changes in PK secondary to the introduction of the ECMO support. Read More

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http://dx.doi.org/10.1080/17425255.2019.1563596DOI Listing
February 2019

Factors influencing hepatic metabolism of antihypertensive drugs: impact on clinical response.

Expert Opin Drug Metab Toxicol 2019 Jan 24;15(1):1-13. Epub 2018 Dec 24.

a Departamento de Farmacología , Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica , Buenos Aires , Argentina.

Introduction: Although main antihypertensive drugs are able to efficiently reduce blood pressure, only a third of treated hypertensive patients achieve optimal blood pressure control. Extensive interpatient variability on drug metabolism and oral disposition of blood pressure lowering drugs can contribute to this failure in hypertension management. Areas covered: The aim of the present review is to update the knowledge on the features of hepatic metabolism of the main antihypertensive agents, including β-blockers, calcium channel blockers, angiotensin receptor blockers, and angiotensin converting enzyme inhibitors. Read More

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https://www.tandfonline.com/doi/full/10.1080/17425255.2019.1
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http://dx.doi.org/10.1080/17425255.2019.1558204DOI Listing
January 2019
4 Reads

Pharmacokinetic mechanisms underlying the detoxification effect of Glycyrrhizae Radix et Rhizoma (Gancao): drug metabolizing enzymes, transporters, and beyond.

Expert Opin Drug Metab Toxicol 2019 Feb 7;15(2):167-177. Epub 2019 Jan 7.

b Department of Pharmacology, School of Pharmacy , Shanghai University of Traditional Chinese Medicine , Shanghai , China.

Introduction: Glycyrrhizae Radix et Rhizoma (Gancao in Chinese) is the most frequently used traditional Chinese medicine (TCM) owing to its various pharmacological effects and, more importantly, the synergistic effects that enhance the efficacy and reduce the toxicity of other TCMs. Areas covered: We reviewed publications, predominantly between 1990 and 2018, that examined pharmacokinetic interactions between Gancao and other TCMs, or the bioactive constituents of these TCMs. This review focuses on the underlying mechanisms and the components responsible for the pharmacokinetic modulation by Gancao. Read More

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http://dx.doi.org/10.1080/17425255.2019.1563595DOI Listing
February 2019

Pharmacodynamics of the agents used for the treatment of erectile dysfunction.

Expert Opin Drug Metab Toxicol 2019 Feb 22;15(2):121-131. Epub 2018 Dec 22.

a Department of Urology , Tulane University School of Medicine , New Orleans , LA , USA.

Introduction: Erectile dysfunction (ED) is one of the most common complaints encountered by the practicing urologist, particularly when treating older men. The last 20 years have represented a pivotal time in the treatment of ED. Areas covered: Several pharmacologic agents have been approved by regulatory agencies, including phosphodiesterase type 5 (PDE5) inhibitors, intraurethral suppositories, and vasoactive injectable agents. Read More

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http://dx.doi.org/10.1080/17425255.2019.1560421DOI Listing
February 2019
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Pharmacokinetic drug evaluation of abemaciclib for advanced breast cancer.

Expert Opin Drug Metab Toxicol 2019 Feb 5;15(2):85-91. Epub 2019 Jan 5.

a Medical Oncology , Institut de Cancérologie de l'Ouest, René Gauducheau , St Herblain , France.

Introduction: The combination of cyclin-dependent kinases 4 and 6 (CDK 4 and 6) inhibitors with endocrine therapy represents a new standard of care for endocrine-receptor positive metastatic breast cancer. Currently, three compounds are approved. Abemaciclib is the latest CDK4/6 inhibitor approved by the US Food and Drug Administration in view of the results of the MONARCH1 and 2 trials. Read More

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https://www.tandfonline.com/doi/full/10.1080/17425255.2019.1
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http://dx.doi.org/10.1080/17425255.2019.1559816DOI Listing
February 2019
5 Reads

Pharmacokinetic and pharmacodynamic considerations for the clinical efficacy of perampanel in focal onset seizures.

Expert Opin Drug Metab Toxicol 2019 Feb 26;15(2):93-102. Epub 2018 Dec 26.

a Neurology Unit, Department of Neurosciences , University Hospital of Udine , Udine , Italy.

Introduction: Medical therapy is the mainstay of management of epilepsy. Despite the increasing number of available antiepileptic drugs (AEDs), approximately one-third of epileptic patients do not have adequate control of seizures. There is still a need for the development of new AEDs with enhanced effectiveness and tolerability. Read More

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http://dx.doi.org/10.1080/17425255.2019.1560420DOI Listing
February 2019
5 Reads

Emerging oral VEGF inhibitors for the treatment of renal cell carcinoma.

Expert Opin Investig Drugs 2019 Feb 21;28(2):121-130. Epub 2018 Dec 21.

a Department of Pharmaceutical Sciences, College of Pharmacy , The University of Findlay , Findlay , OH , USA.

Introduction: The incidence of renal cell carcinoma (RCC) has increased in recent years and, unfortunately, many patients initially present with metastatic disease. When surgery is not an option, treatment involves administration of targeted therapies. The vascular endothelial growth factor (VEGF) pathway has been identified as an important mediator for the development of RCC. Read More

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http://dx.doi.org/10.1080/13543784.2019.1559296DOI Listing
February 2019

Targeted treatment of anaerobic cancer. Patent evaluation of US2016279084 and US2017056350.

Expert Opin Ther Pat 2019 Jan 17;29(1):1-6. Epub 2018 Dec 17.

a Istituto di Biostrutture e Bioimmagini-CNR , Naples , Italy.

Introduction: Based on the initial studies of J. Folkman in 1970s, which led to the proposal of the antiangiogenic therapy, many drugs targeting VEGF or its receptors have been developed with some of them approved for cancer treatment. However, these molecules so far have shown only a limited effect on survival benefits in patients. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2019.1
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http://dx.doi.org/10.1080/13543776.2019.1558210DOI Listing
January 2019
5 Reads

Physiologically based pharmacokinetic (PBPK) modeling and simulation in neonatal drug development: how clinicians can contribute.

Expert Opin Drug Metab Toxicol 2018 Dec 17:1-10. Epub 2018 Dec 17.

b Department of Development and Regeneration , KU Leuven , Leuven , Belgium.

Introduction: Legal initiatives to stimulate neonatal drug development should be accompanied by development of valid research tools. Physiologically based (PB)-pharmacokinetic (PK) modeling and simulation are established tools, accepted by regulatory authorities. Consequently, PBPK holds promise to be a strong research tool to support neonatal drug development. Read More

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http://dx.doi.org/10.1080/17425255.2019.1558205DOI Listing
December 2018
4 Reads

Novel therapeutic approaches in primary hyperoxaluria.

Expert Opin Emerg Drugs 2018 Dec 12:1-9. Epub 2018 Dec 12.

a Division of Pediatric Nephrology , University Childrens Hospital, Universitatsklinikum Bonn , Bonn , Germany.

Introduction: Currently, three types of primary hyperoxaluria (PH I-III) are known, all based on different gene-mutations affecting the glyoxylate metabolism in the liver. Disease hallmark is an increased endogenous oxalate production and thus massively elevated urinary excretion of oxalate and other type-specific metabolites. Hyperoxaluria induces the formation of calcium-oxalate kidney stones and/or nephrocalcinosis. Read More

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http://dx.doi.org/10.1080/14728214.2018.1552940DOI Listing
December 2018
3 Reads

Mipomersen and its use in familial hypercholesterolemia.

Expert Opin Pharmacother 2019 Feb 10;20(2):127-131. Epub 2018 Dec 10.

a Division of Endocrinology, Metabolism, and Lipid Research, Department of Medicine , Washington University School of Medicine , St. Louis , MO , USA.

Introduction: Familial Hypercholesterolemia (FH) is an inherited disorder characterized by a defect in the binding and internalization of low-density lipoprotein (LDL) particles, resulting in markedly elevated LDL levels and premature atherosclerosis. It is one of the most common inherited disorders of lipid metabolism. Many FH patients, especially those with homozygous FH do not reach LDL goals with traditional LDL therapies and may require additional, less often used, therapies. Read More

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http://dx.doi.org/10.1080/14656566.2018.1550071DOI Listing
February 2019
1 Read

Current state on tryptophan 2,3-dioxygenase inhibitors: a patent review.

Expert Opin Ther Pat 2019 Jan 16;29(1):11-23. Epub 2019 Jan 16.

a Medicinal Chemistry Research Group (CMFA), Louvain Drug Research Institute (LDRI) , Université Catholique de Louvain (UCLouvain) , Brussels , Belgium.

Introduction: Tryptophan-2, 3-dioxygenase (TDO2) is a tryptophan-degrading enzyme constitutively expressed in the liver and to a lesser extend in the brain. Before its link to cancer immunotherapy was discovered in 2011, the search for TDO2 inhibitors was initially driven by depression therapy. In the recent years, TDO2 has drawn an increasing attention as a promising target in both cancer and neuropsychiatric diseases. Read More

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http://dx.doi.org/10.1080/13543776.2019.1556638DOI Listing
January 2019
1 Read

New developments in investigational HDAC inhibitors for the potential multimodal treatment of cachexia.

Expert Opin Investig Drugs 2019 Feb 14;28(2):179-189. Epub 2018 Dec 14.

a Department of Clinical and Biological Science , University of Torino , Italy.

Introduction: Cachexia is a frequent feature of chronic diseases. This syndrome includes loss of body weight, depletion of skeletal muscle mass and altered metabolic homeostasis. Acceleration of protein and energy metabolism, impaired myogenesis, and systemic inflammation contribute to cachexia. Read More

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http://dx.doi.org/10.1080/13543784.2019.1557634DOI Listing
February 2019
2 Reads

Pharmacotherapy for metastatic esophageal cancer: where do we need to improve?

Expert Opin Pharmacother 2019 Feb 7;20(3):357-366. Epub 2018 Dec 7.

a Department of Medicine , Perlmutter Cancer Center, NYU Langone Medical Center , New York , NY , USA.

Introduction: Esophageal cancer is a heterogeneous cancer comprised of differing cells of origin, molecular changes, and immune microenvironments. To date, most advances have been made in chemotherapy regimens where a one-size-fits-all approach is used. As a result, there remains a lack of tailored treatment options for such a heterogeneous cancer. Read More

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http://dx.doi.org/10.1080/14656566.2018.1551881DOI Listing
February 2019

An update of cyclooxygenase (COX)-inhibitors in epilepsy disorders.

Authors:
Ashish Dhir

Expert Opin Investig Drugs 2019 Feb 13;28(2):191-205. Epub 2018 Dec 13.

a Department of Neurology, School of Medicine , University of California, Davis , Sacramento , CA , USA.

Introduction: Neuroinflammation has a critical role in brain disorders. Cyclooxygenase (COX) is one of the principal drug targets for the reduction of neuroinflammation; however, studies have yielded mixed results for COX-inhibitors in the treatment of diverse acute and chronic models of epilepsy. Areas covered: The article covers the effects of COX-inhibitors in epilepsy disorders. Read More

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http://dx.doi.org/10.1080/13543784.2019.1557147DOI Listing
February 2019
3 Reads

Prostaglandin D receptor antagonists in allergic disorders: safety, efficacy, and future perspectives.

Expert Opin Investig Drugs 2019 Jan 7;28(1):73-84. Epub 2018 Dec 7.

c Department of Translational Medical Sciences and Center for Basic and Clinical Immunology Research (CISI) , University of Naples Federico II , Naples , Italy.

Introduction: Prostaglandin D (PGD) is a major cyclooxygenase mediator that is synthesized by activated human mast cells and other immune cells. The biological effects of PGD are mediated by D-prostanoid (DP), DP (CRTH2) and thromboxane prostanoid (TP) receptors that are expressed on several immune and non-immune cells involved in allergic inflammation. PGD exerts various proinflammatory effects relevant to the pathophysiology of allergic disorders. Read More

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http://dx.doi.org/10.1080/13543784.2019.1555237DOI Listing
January 2019
8 Reads

HER2-targeted therapy: an emerging strategy in advanced colorectal cancer.

Expert Opin Investig Drugs 2019 Jan 9;28(1):29-38. Epub 2018 Dec 9.

a Oncology Department , Hospital Universitario 12 de Octubre , Madrid , Spain.

Introduction: Colorectal cancer (CRC) is one of the most common malignant tumors; it is a focus of research globally, but the identification of clinically actionable oncogenic drivers remains elusive. Human epidermal growth factor receptor 2 (HER2) activation is present in approximately 5% of CRC and has acquired resistance to epidermal growth factor receptor (EGFR)-targeted therapy. Early clinical trials suggest an emerging role for personalized HER2-targeted therapy in a subset of metastatic CRC. Read More

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http://dx.doi.org/10.1080/13543784.2019.1555583DOI Listing
January 2019
1 Read

An evaluation of pitavastatin for the treatment of hypercholesterolemia.

Expert Opin Pharmacother 2018 Nov 27:1-11. Epub 2018 Nov 27.

e Department of Cardiac Surgery , Shanghai East Hospital, Tongji University , Shanghai , China.

Introduction: Statins are the first line of therapy to reduce low-density lipoprotein cholesterol (LDL-C) in order to decrease cardiovascular events. Pitavastatin is the latest statin to be introduced to the market. Areas covered: In this article, the authors review the efficacy, safety, and tolerability of pitavastatin. Read More

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http://dx.doi.org/10.1080/14656566.2018.1544243DOI Listing
November 2018
1 Read

Drug-drug interactions in patients receiving hematopoietic stem cell transplantation.

Expert Opin Drug Metab Toxicol 2019 Jan 27;15(1):49-59. Epub 2018 Nov 27.

a Faculty of Medical Sciences , University of Kragujevac , Kragujevac , Serbia.

Introduction: Recipients of hematopoietic stem cell transplantation (HSCT) are exposed to numerous drugs in both pre- and post-transplantation period, which creates an opportunity for drug-drug interactions (DDIs); if clinically relevant DDIs happen, the risk of adverse treatment outcomes is increased. Areas covered: This review is focused on DDIs in recipients of HSCT that were observed and published as clinical trials, case series or case reports. Relevant publications were found by the systematic search of the following online databases: MEDLINE, SCOPUS, EBSCO, and SCINDEX. Read More

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http://dx.doi.org/10.1080/17425255.2019.1552256DOI Listing
January 2019
5 Reads

Pharmacokinetic drug evaluation of letermovir prophylaxis for cytomegalovirus in hematopoietic stem cell transplantation.

Expert Opin Drug Metab Toxicol 2018 Dec 4;14(12):1197-1207. Epub 2018 Dec 4.

c Department of Microbiology and Immunology , KU Leuven , Leuven , Belgium.

Introduction: Letermovir is a new antiviral approved to prevent cytomegalovirus infection in hematopoietic stem cell transplant recipients. It has a distinct mechanism of action as it acts as a terminase complex inhibitor, and shows some advantages compared to the current treatment options for cytomegalovirus infection. Areas covered: This review focuses on the efficacy, safety, pharmacokinetics, pharmacodynamics, and drug-drug interactions of letermovir. Read More

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https://www.tandfonline.com/doi/full/10.1080/17425255.2018.1
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http://dx.doi.org/10.1080/17425255.2018.1550485DOI Listing
December 2018
15 Reads

Pharmacokinetic drug evaluation of CVT-301 for the treatment of Parkinson's disease.

Expert Opin Drug Metab Toxicol 2018 Dec 2;14(12):1189-1195. Epub 2018 Dec 2.

a Departement of Neurology , University and Institute for Research and Medical Care, San Raffaele Rome , Roma , Italy.

Introduction: Levodopa (LD), in combination with a decarboxylase inhibitor, is a mainstay and the most effective therapeutic agent in the treatment of Parkinson's disease (PD). Unfortunately, during chronic treatment with this agent, ON-OFF phenomena and dyskinesia appear. Despite the many medical treatment options available, unpredictable OFF episodes can still occur and be severe and disabling. Read More

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http://dx.doi.org/10.1080/17425255.2018.1550483DOI Listing
December 2018
17 Reads

c-Met kinase inhibitors: an update patent review (2014-2017).

Expert Opin Ther Pat 2019 Jan 12;29(1):25-41. Epub 2018 Dec 12.

a Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry , China Pharmaceutical University , Nanjing , P. R. China.

Introduction: The receptor tyrosine kinase c-Met is involved in the formation, metastasis and invasion of various malignant tumors thus it has been an attractive target for anti-tumor drug designing. Many compositions targeting c-Met have been developed in pharmaceutical industry for cancer therapy and some of them are in clinical study now. Among them, Crizotinib was the first small molecular inhibitor approved by FDA in 2011. Read More

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http://dx.doi.org/10.1080/13543776.2019.1552261DOI Listing
January 2019
6 Reads

Dose adjustment in orphan disease populations: the quest to fulfill the requirements of physiologically based pharmacokinetics.

Expert Opin Drug Metab Toxicol 2018 Dec 22;14(12):1315-1330. Epub 2018 Nov 22.

a Centre for Applied Pharmacokinetic Research , University of Manchester , Manchester , UK.

Introduction: While the media is engaged and fascinated by the idea of 'Precision Medicine', the nuances related to 'Precision Dosing' seem to be largely ignored. Assuming the 'right drug' is selected, clinicians still need to decide on the 'right dose' for individuals. Ideally, optimal dosing should be studied in clinical trials; however, many drugs on the market lack evidence-based dosing recommendations, and small groups of patients (orphan disease populations) are dependent on local guidance and clinician experience to determine drug dosage adjustments. Read More

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http://dx.doi.org/10.1080/17425255.2018.1546288DOI Listing
December 2018

The pharmacokinetics and pharmacodynamics of SGLT2 inhibitors for type 2 diabetes mellitus: the latest developments.

Expert Opin Drug Metab Toxicol 2018 Dec 29;14(12):1287-1302. Epub 2018 Nov 29.

a Atherothrombosis Research Unit, Cardiovascular Institute , Icahn School of Medicine at Mount Sinai , New York , NY , USA.

Introduction: Type 2 diabetes mellitus (T2DM) is a complex metabolic disorder associated with high cardiovascular (CV) risk. Some of the therapeutic strategies are contraindicated in patients with concomitant heart disease. However, the newest antidiabetic medications, sodium-glucose cotransporter 2 (SGLT2) inhibitors, have shown to significantly reduce CV mortality and heart failure (HF) hospitalizations. Read More

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http://dx.doi.org/10.1080/17425255.2018.1551877DOI Listing
December 2018
21 Reads

How can we best monitor 5-FU administration to maximize benefit to risk ratio?

Expert Opin Drug Metab Toxicol 2018 Dec 23;14(12):1303-1313. Epub 2018 Nov 23.

g Service Pharmacie , Centre Georges-François Leclerc , Dijon , France.

Introduction: 5-Fluorouracil (5-FU) is currently used as a chemotherapy in several cancers such as head-and-neck (H&N) and colorectal cancers. 5-FU dosing is traditionally based on body surface area (BSA), but this strategy is usually associated with severe toxicities. 5-FU is mainly catabolized by dihydropyrimidine dehydrogenase (DPD), and 5-FU dosage adaptation according to DPD status at the first cycle of treatment is now recommended. Read More

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https://www.tandfonline.com/doi/full/10.1080/17425255.2018.1
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http://dx.doi.org/10.1080/17425255.2018.1550484DOI Listing
December 2018
6 Reads

A patent review of the ubiquitin ligase system: 2015-2018.

Expert Opin Ther Pat 2018 Dec 23;28(12):919-937. Epub 2018 Nov 23.

c Barbara Ann Karmanos Cancer Institute, and Departments of Oncology, Pharmacology and Pathology, School of Medicine , Wayne State University , Detroit , MI , USA.

Introduction: Ubiquitin-proteasome system (UPS) has been validated as a novel anticancer drug target in the past 20 years. The UPS contains two distinct steps: ubiquitination of a substrate protein by ubiquitin activating enzyme (E1), ubiquitin conjugating enzyme (E2), and ubiquitin ligase (E3), and substrate degradation by the 26S proteasome complex. The E3 enzyme is the central player in the ubiquitination step and has a wide range of specific substrates in cancer cells, offering great opportunities for discovery and development of selective drugs. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1549229DOI Listing
December 2018
25 Reads

αβ integrin inhibitors: a patent review.

Expert Opin Ther Pat 2018 Dec 22;28(12):903-917. Epub 2018 Nov 22.

c Research Division of Clinical Pharmacology , Τhe First Affiliated Hospital of Nanjing Medical University , Nanjing , China.

Introduction: The αβ integrin is heterodimeric cell surface receptors expressed on most leukocytes. Mucosal addressing cell adhesion molecule 1(MAdCAM-1) is an exclusive ligand for αβ integrin. Areas covered: This article will highlight the progress that has been made in the discovery and development of αβ integrin inhibitors, and their use in the treatment of inflammatory bowel diseases, multiple sclerosis, asthma, hepatic disorders, human immunodeficiency virus, allergic conjunctivitis and type 1 diabetes. Read More

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http://dx.doi.org/10.1080/13543776.2018.1549227DOI Listing
December 2018
11 Reads
4.300 Impact Factor

Nanoparticle albumin bound-paclitaxel for treatment of advanced non-small cell lung cancer: an evaluation of the clinical evidence.

Expert Opin Pharmacother 2019 Jan 15;20(1):95-102. Epub 2018 Nov 15.

a Department of Medical Oncology , Albert Einstein College of Medicine/Montefiore Medical Center , Bronx , NY , USA.

Introduction: Nanoparticle albumin-bound paclitaxel (nab-paclitaxel), a microtubule inhibitor, has demonstrated clinical efficacy in the treatment of advanced non-small cell lung cancer (NSCLC) either as monotherapy or in combination. Nab-paclitaxel was developed to reduce the toxicities associated with solvent-bound paclitaxel (sb-paclitaxel). Areas covered: This review first focuses on the clinical trials evaluating the efficacy and tolerability of nab-paclitaxel in NSCLC at different settings. Read More

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http://dx.doi.org/10.1080/14656566.2018.1546290DOI Listing
January 2019
3 Reads

Carbonic anhydrase inhibitors as emerging agents for the treatment and imaging of hypoxic tumors.

Expert Opin Investig Drugs 2018 Dec 22;27(12):963-970. Epub 2018 Nov 22.

a NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche , Università degli Studi di Firenze , Sesto Fiorentino (Firenze) , Italy.

Introduction: Hypoxic tumors overexpress two carbonic anhydrases (CA, EC 4.2.1. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543784.2018.1
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http://dx.doi.org/10.1080/13543784.2018.1548608DOI Listing
December 2018
10 Reads

Emerging cell cycle inhibitors for treating metastatic castration-resistant prostate cancer.

Expert Opin Emerg Drugs 2018 12 28;23(4):271-282. Epub 2018 Nov 28.

a Division of Medical Oncology, Department of Oncology, Schulich School of Medicine & Dentistry , Western University and London Health Sciences Centre , London , ON , Canada.

Introduction: Disease progression despite androgen suppression defines lethal castration-resistant prostate cancer (CRPC). Most of these cancers remain androgen receptor (AR)-signaling dependent. Therapy for metastatic CRPC includes abiraterone acetate, enzalutamide, docetaxel, cabazitaxel, sipuleucel-T, and radium-223. Read More

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https://www.tandfonline.com/doi/full/10.1080/14728214.2018.1
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http://dx.doi.org/10.1080/14728214.2018.1547707DOI Listing
December 2018
14 Reads

Disease-modifying drugs in osteoarthritis: current understanding and future therapeutics.

Expert Opin Emerg Drugs 2018 12 3;23(4):331-347. Epub 2018 Dec 3.

a Rheumatology Department, Royal North Shore Hospital, and, Institute of Bone and Joint Research, Kolling Institute , University of Sydney , Sydney , Australia.

Introduction: Osteoarthritis (OA) is a leading cause of pain and disability among adults with a current prevalence of around 15% and a predicted prevalence of 35% in 2030 for symptomatic OA. It is increasingly recognized as a heterogeneous multi-faceted joint disease with multi-tissue involvement of varying severity. Current therapeutic regimens for OA are only partially effective and often have significant associated toxicities. Read More

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https://www.tandfonline.com/doi/full/10.1080/14728214.2018.1
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http://dx.doi.org/10.1080/14728214.2018.1547706DOI Listing
December 2018
289 Reads
3.058 Impact Factor

Chemical management of levodopa-induced dyskinesia in Parkinson's disease patients.

Expert Opin Pharmacother 2019 Feb 9;20(2):219-230. Epub 2018 Nov 9.

a Neurology Clinic, CCS, School of Medicine , Universtiy of Belgrade , Belgrade , Serbia.

Introduction: Levodopa-induced dyskinesias (LID) appears in more than 50% of Parkinson's disease patients after 5 years of treatment and clinicians always have to ensure that there is a balance between the beneficial effect of the treatment and the potential complications. Areas covered: In this review, the authors discuss the treatment of LID. Treatment can be divided into strategies for preventing their occurrence, modification of dopaminergic therapy, and providing more continuous dopaminergic stimulation as well as the use of nondopaminergic drugs. Read More

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http://dx.doi.org/10.1080/14656566.2018.1543407DOI Listing
February 2019
8 Reads

Adaptation of 2016 European Society of Cardiology/European Atherosclerosis Society guideline for lipid management to Indian patients - A consensus document.

Indian Heart J 2018 Sep - Oct;70(5):736-744. Epub 2018 Jul 18.

Woodlands Multi-Speciality Hospital, Kolkata, India. Electronic address:

In the year 2016, European Society of Cardiology/European Atherosclerosis Society (ESC/EAS) guidelines provided recommendations on dyslipidemia management. The recommendation from these guidelines are restricted to European subcontinent. To adapt the updated recommendations for Indian subset of dyslipidemia, a panel of experts in management of dyslipidemia provided their expert opinions. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00194832183013
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http://dx.doi.org/10.1016/j.ihj.2018.03.011DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6204479PMC
January 2019
7 Reads

CSL112, a reconstituted, infusible, plasma-derived apolipoprotein A-I: safety and tolerability profiles and implications for management in patients with myocardial infarction.

Expert Opin Investig Drugs 2018 Dec 3;27(12):997-1005. Epub 2018 Nov 3.

d Division of Cardiology , University of Florida College of Medicine , Jacksonville , FL , USA.

Introduction: The risk of major adverse cardiac events (MACE) remains elevated soon after a coronary event. High-density lipoprotein (HDL) cholesterol has been proposed as a target to reduce cardiovascular endpoints, but there is growing recognition that increasing the function of HDL may be more important than merely increasing its concentration. CSL112 is a reconstituted, infusible human plasma-derived apolipoprotein A-I (apoA-I) that increases cholesterol efflux capacity - an ex vivo measure of the ability of HDL to accept cholesterol from macrophages. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543784.2018.1
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http://dx.doi.org/10.1080/13543784.2018.1543399DOI Listing
December 2018
2 Reads

Metformin transporter pharmacogenomics: insights into drug disposition-where are we now?

Expert Opin Drug Metab Toxicol 2018 Nov 13;14(11):1149-1159. Epub 2018 Nov 13.

e Department of Cardiac Surgery, Shanghai East Hospital , Tongji University , Shanghai , China.

Introduction: Metformin is recommended as first-line treatment for type 2 diabetes (T2D) by all major diabetes guidelines. With appropriate usage it is safe and effective overall, but its efficacy and tolerability show considerable variation between individuals. It is a substrate for several drug transporters and polymorphisms in these transporter genes have shown effects on metformin pharmacokinetics and pharmacodynamics. Read More

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http://dx.doi.org/10.1080/17425255.2018.1541981DOI Listing
November 2018
1 Read

T-type calcium channel blockers: a patent review (2012-2018).

Authors:
Ghilsoo Nam

Expert Opin Ther Pat 2018 Dec 11;28(12):883-901. Epub 2018 Nov 11.

a Center for Neuro-Medicine , Brain Science Institute, Korea Institutes of Science and Technology (KIST) , Seoul , Republic of Korea.

Introduction: T-type calcium channels are attractive targets for potential treatment of epilepsy inflammatory or neuropathic pain, insomnia, Parkinson's disease, and cancer. Three isoforms having different biophysical functions are expressed in peripheral and central nerve. Since the withdrawal of mibefradil, the first compound marketed for selective T-type calcium channel blockade, extensive efforts have been made to identify more selective T-type calcium channel blockers. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1541982DOI Listing
December 2018
11 Reads

CDK4-6 inhibitors in breast cancer: current status and future development.

Expert Opin Drug Metab Toxicol 2018 Nov 3;14(11):1123-1138. Epub 2018 Nov 3.

a Department of Haematology-Oncology , National University Cancer Institute, National University Health System (NUHS) , Singapore , Singapore.

Introduction: Aberrant cellular proliferation due to dysregulation of the cyclin-dependent kinase (CDK) retinoblastoma (Rb)-pathway occurs in several cancers. Selective inhibition of CDK4/6 is an attractive target particularly in hormone-receptor positive (HR+) metastatic breast cancer (MBC), where it has transformed the treatment of these cancers in recent years. Three CDK4/6 inhibitors, palbociclib, ribociclib, and abemaciclib, have been approved for the treatment of HR+, HER2 negative (HER2-) MBC. Read More

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https://www.tandfonline.com/doi/full/10.1080/17425255.2018.1
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http://dx.doi.org/10.1080/17425255.2018.1541347DOI Listing
November 2018
10 Reads