Pharmaceuticals

29 pages, 1680 KiB

Open AccessFeature PaperEditor’s ChoiceReview

Current Prospects for Treatment of Solid Tumors via Photodynamic, Photothermal, or Ionizing Radiation Therapies Combined with Immune Checkpoint Inhibition (A Review)

by Sanjay Anand, Timothy A. Chan, Tayyaba Hasan and Edward V. Maytin

Pharmaceuticals 2021, 14(5), 447; https://doi.org/10.3390/ph14050447 - 10 May 2021

Cited by 36 | Viewed by 4390

Abstract

Photodynamic therapy (PDT) causes selective damage to tumor cells and vasculature and also triggers an anti-tumor immune response. The latter fact has prompted the exploration of PDT as an immune-stimulatory adjuvant. PDT is not the only cancer treatment that relies on electromagnetic energy [...] Read more.

Photodynamic therapy (PDT) causes selective damage to tumor cells and vasculature and also triggers an anti-tumor immune response. The latter fact has prompted the exploration of PDT as an immune-stimulatory adjuvant. PDT is not the only cancer treatment that relies on electromagnetic energy to destroy cancer tissue. Ionizing radiation therapy (RT) and photothermal therapy (PTT) are two other treatment modalities that employ photons (with wavelengths either shorter or longer than PDT, respectively) and also cause tissue damage and immunomodulation. Research on the three modalities has occurred in different “silos”, with minimal interaction between the three topics. This is happening at a time when immune checkpoint inhibition (ICI), another focus of intense research and clinical development, has opened exciting possibilities for combining PDT, PTT, or RT with ICI to achieve improved therapeutic benefits. In this review, we surveyed the literature for studies that describe changes in anti-tumor immunity following the administration of PDT, PTT, and RT, including efforts to combine each modality with ICI. This information, collected all in one place, may make it easier to recognize similarities and differences and help to identify new mechanistic hypotheses toward the goal of achieving optimized combinations and tumor cures. Full article

(This article belongs to the Special Issue Photodynamic Therapy 2021)

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28 pages, 693 KiB

Open AccessEditor’s ChoiceReview

COVID-19 Vaccines: A Review of the Safety and Efficacy of Current Clinical Trials

by Zhi-Peng Yan, Ming Yang and Ching-Lung Lai

Pharmaceuticals 2021, 14(5), 406; https://doi.org/10.3390/ph14050406 - 25 Apr 2021

Cited by 104 | Viewed by 19609

Abstract

Various strategies have been designed to contain the COVID-19 pandemic. Among them, vaccine development is high on the agenda in spite of the unknown duration of the protection time. Various vaccines have been under clinical trials with promising results in different countries. The [...] Read more.

Various strategies have been designed to contain the COVID-19 pandemic. Among them, vaccine development is high on the agenda in spite of the unknown duration of the protection time. Various vaccines have been under clinical trials with promising results in different countries. The protective efficacy and the short-term and long-term side effects of the vaccines are of major concern. Therefore, comparing the protective efficacy and risks of vaccination is essential for the global control of COVID-19 through herd immunity. This study reviews the most recent data of 12 vaccines to evaluate their efficacy, safety profile and usage in various populations. Full article

(This article belongs to the Special Issue Current Trends in RNA Virus Vaccines)

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25 pages, 4268 KiB

Open AccessEditor’s ChoiceArticle

A Novel Combination Therapy Using Rosuvastatin and Lactobacillus Combats Dextran Sodium Sulfate-Induced Colitis in High-Fat Diet-Fed Rats by Targeting the TXNIP/NLRP3 Interaction and Influencing Gut Microbiome Composition

by Sameh Saber, Eslam E. Abd El-Fattah, Galal Yahya, Naglaa A. Gobba, Abdalkareem Omar Maghmomeh, Ahmed E. Khodir, Ahmed A. E. Mourad, Ahmed S. Saad, Hager G. Mohammed, Nehal A. Nouh, Ahmed Shata, Noha A. Amin, Magdy Abou El-Rous, Samuel Girgis, Eman El-Ahwany, Eman M. Khalaf, Attalla F. El-Kott and Ahmed M. El-Baz

Pharmaceuticals 2021, 14(4), 341; https://doi.org/10.3390/ph14040341 - 8 Apr 2021

Cited by 47 | Viewed by 5663

Abstract

Inflammasome targeting and controlling dysbiosis are promising therapeutic approaches to control ulcerative colitis. This report is the first to investigate the mechanisms underlying the coloprotective effects of rosuvastatin and Lactobacillus and their combined therapy on dextran sodium sulfate (DSS)-induced colitis in high-fat diet [...] Read more.

Inflammasome targeting and controlling dysbiosis are promising therapeutic approaches to control ulcerative colitis. This report is the first to investigate the mechanisms underlying the coloprotective effects of rosuvastatin and Lactobacillus and their combined therapy on dextran sodium sulfate (DSS)-induced colitis in high-fat diet (HFD)-fed rats. Our results demonstrate the aggravation of intestinal inflammation as a consequence of an HFD following DSS administration. An association between dyslipidemia, LDL oxidation, CD36 expression, ROS generation, thioredoxin-interacting protein (TXNIP) upregulation, and NLRP3 inflammasome activation was demonstrated by DSS exposure in HFD-fed rats. We demonstrated that rosuvastatin/Lactobacillus significantly suppressed the DSS/HFD-induced increase in colon weight/length ratio, DAI, MDI, and myeloperoxidase, as well as corrected dysbiosis and improved histological characteristics. Additionally, caspase-1 activity and IL-1β-driven pyroptotic activity was significantly reduced. Rosuvastatin/Lactobacillus showed prominent anti-inflammatory effects as revealed by the IL-10/IL-12 ratio and the levels of TNF-α and IL-6. These latter effects may be attributed to the inhibition of phosphorylation-induced activation of NF-κB and a concomitant reduction in the expression of NLRP3, pro-IL-1β, and pro-IL-18. Furthermore, rosuvastatin/Lactobacillus reduced Ox-LDL-induced TXNIP and attenuated the inflammatory response by inhibiting NLRP3 inflammasome assembly. To conclude, rosuvastatin/Lactobacillus offers a safe and effective strategy for the management of ulcerative colitis. Full article

(This article belongs to the Special Issue Gut Microbiota, Inflammatory Bowel Diseases, and Therapeutic Targets)

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21 pages, 1746 KiB

Open AccessEditor’s ChoiceReview

Ultramicronized Palmitoylethanolamide (um-PEA): A New Possible Adjuvant Treatment in COVID-19 patients

by Annalisa Noce, Maria Albanese, Giulia Marrone, Manuela Di Lauro, Anna Pietroboni Zaitseva, Daniela Palazzetti, Cristina Guerriero, Agostino Paolino, Giuseppa Pizzenti, Francesca Di Daniele, Annalisa Romani, Cartesio D’Agostini, Andrea Magrini, Nicola Biagio Mercuri and Nicola Di Daniele

Pharmaceuticals 2021, 14(4), 336; https://doi.org/10.3390/ph14040336 - 6 Apr 2021

Cited by 23 | Viewed by 9739

Abstract

The Coronavirus Disease-19 (COVID-19) pandemic has caused more than 100,000,000 cases of coronavirus infection in the world in just a year, of which there were 2 million deaths. Its clinical picture is characterized by pulmonary involvement that culminates, in the most severe cases, [...] Read more.

The Coronavirus Disease-19 (COVID-19) pandemic has caused more than 100,000,000 cases of coronavirus infection in the world in just a year, of which there were 2 million deaths. Its clinical picture is characterized by pulmonary involvement that culminates, in the most severe cases, in acute respiratory distress syndrome (ARDS). However, COVID-19 affects other organs and systems, including cardiovascular, urinary, gastrointestinal, and nervous systems. Currently, unique-drug therapy is not supported by international guidelines. In this context, it is important to resort to adjuvant therapies in combination with traditional pharmacological treatments. Among natural bioactive compounds, palmitoylethanolamide (PEA) seems to have potentially beneficial effects. In fact, the Food and Drug Administration (FDA) authorized an ongoing clinical trial with ultramicronized (um)-PEA as an add-on therapy in the treatment of Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) infection. In support of this hypothesis, in vitro and in vivo studies have highlighted the immunomodulatory, anti-inflammatory, neuroprotective and pain-relieving effects of PEA, especially in its um form. The purpose of this review is to highlight the potential use of um-PEA as an adjuvant treatment in SARS-CoV-2 infection. Full article

(This article belongs to the Special Issue COVID-19 in Pharmaceuticals)

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18 pages, 2669 KiB

Open AccessEditor’s ChoiceArticle

Covalently Functionalized Carbon Nano-Onions Integrated Gelatin Methacryloyl Nanocomposite Hydrogel Containing γ-Cyclodextrin as Drug Carrier for High-Performance pH-Triggered Drug Release

by Narsimha Mamidi, Ramiro Manuel Velasco Delgadillo and Enrique V. Barrera

Pharmaceuticals 2021, 14(4), 291; https://doi.org/10.3390/ph14040291 - 25 Mar 2021

Cited by 68 | Viewed by 6058

Abstract

Herein, poly (n-(4-aminophenyl) methacrylamide)) carbon nano-onions (PAPMA-CNOs = f-CNOs) and γ-cyclodextrin/DOX-complex (CD) reinforced gelatin methacryloyl (GelMA)/f-CNOs/CD supramolecular hydrogel interfaces were fabricated using the photo-crosslinking technique. The physicochemical properties, morphology, biodegradation, and swelling properties of hydrogels were investigated. The composite hydrogels demonstrated [...] Read more.

Herein, poly (n-(4-aminophenyl) methacrylamide)) carbon nano-onions (PAPMA-CNOs = f-CNOs) and γ-cyclodextrin/DOX-complex (CD) reinforced gelatin methacryloyl (GelMA)/f-CNOs/CD supramolecular hydrogel interfaces were fabricated using the photo-crosslinking technique. The physicochemical properties, morphology, biodegradation, and swelling properties of hydrogels were investigated. The composite hydrogels demonstrated enriched drug release under the acidic conditions (pH 4.5 = 99%, and pH 6.0 = 82%) over 18 days. Owing to the f-CNOs inclusion, GelMA/f-CNOs/CD supramolecular hydrogels presented augmented tensile strength (σ_ult = 356.1 ± 3.4 MPa), toughness (K = 51.5 ± 0.24 Jg⁻¹), and Young’s modulus (E = 41.8 ± 1.4 GPa). The strengthening of GelMA/f-CNOs/CD hydrogel systems indicates its good dispersion and the degree of polymer enveloping of f-CNOs within GelMA matrixes. Furthermore, the obtained hydrogels showed improved cell viability with human fibroblast cells. Nevertheless, the primed supramolecular hydrogels would pave the way for the controlled delivery systems for future drug delivery. Full article

(This article belongs to the Special Issue New Frontiers in Cyclodextrin Technologies)

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26 pages, 953 KiB

Open AccessEditor’s ChoiceReview

Atypical Antipsychotics and Metabolic Syndrome: From Molecular Mechanisms to Clinical Differences

by Marco Carli, Shivakumar Kolachalam, Biancamaria Longoni, Anna Pintaudi, Marco Baldini, Stefano Aringhieri, Irene Fasciani, Paolo Annibale, Roberto Maggio and Marco Scarselli

Pharmaceuticals 2021, 14(3), 238; https://doi.org/10.3390/ph14030238 - 8 Mar 2021

Cited by 113 | Viewed by 17615

Abstract

Atypical antipsychotics (AAPs) are commonly prescribed medications to treat schizophrenia, bipolar disorders and other psychotic disorders. However, they might cause metabolic syndrome (MetS) in terms of weight gain, dyslipidemia, type 2 diabetes (T2D), and high blood pressure, which are responsible for reduced life [...] Read more.

Atypical antipsychotics (AAPs) are commonly prescribed medications to treat schizophrenia, bipolar disorders and other psychotic disorders. However, they might cause metabolic syndrome (MetS) in terms of weight gain, dyslipidemia, type 2 diabetes (T2D), and high blood pressure, which are responsible for reduced life expectancy and poor adherence. Importantly, there is clear evidence that early metabolic disturbances can precede weight gain, even if the latter still remains the hallmark of AAPs use. In fact, AAPs interfere profoundly with glucose and lipid homeostasis acting mostly on hypothalamus, liver, pancreatic β-cells, adipose tissue, and skeletal muscle. Their actions on hypothalamic centers via dopamine, serotonin, acetylcholine, and histamine receptors affect neuropeptides and 5′AMP-activated protein kinase (AMPK) activity, thus producing a supraphysiological sympathetic outflow augmenting levels of glucagon and hepatic glucose production. In addition, altered insulin secretion, dyslipidemia, fat deposition in the liver and adipose tissues, and insulin resistance become aggravating factors for MetS. In clinical practice, among AAPs, olanzapine and clozapine are associated with the highest risk of MetS, whereas quetiapine, risperidone, asenapine and amisulpride cause moderate alterations. The new AAPs such as ziprasidone, lurasidone and the partial agonist aripiprazole seem more tolerable on the metabolic profile. However, these aspects must be considered together with the differences among AAPs in terms of their efficacy, where clozapine still remains the most effective. Intriguingly, there seems to be a correlation between AAP’s higher clinical efficacy and increase risk of metabolic alterations. Finally, a multidisciplinary approach combining psychoeducation and therapeutic drug monitoring (TDM) is proposed as a first-line strategy to avoid the MetS. In addition, pharmacological treatments are discussed as well. Full article

(This article belongs to the Special Issue Molecular and Cellular Targets of Old and New Atypical Antipsychotics)

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18 pages, 10479 KiB

Open AccessEditor’s ChoiceArticle

Repurposing of Some Natural Product Isolates as SARS-COV-2 Main Protease Inhibitors via In Vitro Cell Free and Cell-Based Antiviral Assessments and Molecular Modeling Approaches

by Hossam M. Abdallah, Ali M. El-Halawany, Alaa Sirwi, Amr M. El-Araby, Gamal A. Mohamed, Sabrin R. M. Ibrahim, Abdulrahman E. Koshak, Hani Z. Asfour, Zuhier A. Awan and Mahmoud A. Elfaky

Pharmaceuticals 2021, 14(3), 213; https://doi.org/10.3390/ph14030213 - 4 Mar 2021

Cited by 50 | Viewed by 5253

Abstract

The emergence of the SARS-CoV-2 pandemic has prompted scientists to search for an efficient antiviral medicine to overcome the rapid spread and the marked increase in the number of patients worldwide. In this regard natural products could be a potential source of substances [...] Read more.

The emergence of the SARS-CoV-2 pandemic has prompted scientists to search for an efficient antiviral medicine to overcome the rapid spread and the marked increase in the number of patients worldwide. In this regard natural products could be a potential source of substances active against coronavirus infections. A systematic computer-aided virtual screening approach was carried out using commercially available natural products found on the Zinc Database in addition to an in-house compound library to identify potential natural product inhibitors of SARS-CoV-2 main protease (M^PRO). The top eighteen hits from the screening were selected for in vitro evaluation on the viral protease (SARS-CoV-2 M^PRO). Five compounds (naringenin, 2,3′,4,5′,6-pentahydroxybenzophenone, apigenin-7-O-glucoside, sennoside B, and acetoside) displayed high activity against the viral protein. Acteoside showed similar activity to the positive control GC376. The most potent compounds were tested in vitro on SARS-CoV-2 Egyptian strain where only naringenin showed moderate anti-SARS-CoV-2 activity at non-cytotoxic micromolar concentrations in vitro with a significant selectivity index (CC₅₀/IC₅₀ = 178.748/28.347 = 6.3). Moreover; a common feature pharmacophore model was generated to explain the requirements for enzyme inhibition by this diverse group of active ligands. These results pave a path for future repurposing and development of natural products to aid in the battle against COVID-19. Full article

(This article belongs to the Special Issue Identification of Phytochemicals and Derivatives against Infectious Diseases)

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14 pages, 1726 KiB

Open AccessFeature PaperEditor’s ChoiceReview

2020 FDA TIDES (Peptides and Oligonucleotides) Harvest

by Othman Al Musaimi, Danah Al Shaer, Fernando Albericio and Beatriz G. de la Torre

Pharmaceuticals 2021, 14(2), 145; https://doi.org/10.3390/ph14020145 - 11 Feb 2021

Cited by 57 | Viewed by 6183

Abstract

2020 has been an extremely difficult and challenging year as a result of the coronavirus disease 2019 (COVID-19) pandemic and one in which most efforts have been channeled into tackling the global health crisis. The US Food and Drug Administration (FDA) has approved [...] Read more.

2020 has been an extremely difficult and challenging year as a result of the coronavirus disease 2019 (COVID-19) pandemic and one in which most efforts have been channeled into tackling the global health crisis. The US Food and Drug Administration (FDA) has approved 53 new drug entities, six of which fall in the peptides and oligonucleotides (TIDES) category. The number of authorizations for these kinds of drugs has been similar to that of previous years, thereby reflecting the consolidation of the TIDES market. Here, the TIDES approved in 2020 are analyzed in terms of chemical structure, medical target, mode of action, and adverse effects. Full article

(This article belongs to the Special Issue The Story of Successful Drugs and Recent FDA-Approved Molecules)

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21 pages, 4303 KiB

Open AccessEditor’s ChoiceArticle

Photophysical Properties of Protoporphyrin IX, Pyropheophorbide-a, and Photofrin^® in Different Conditions

by Bauyrzhan Myrzakhmetov, Philippe Arnoux, Serge Mordon, Samir Acherar, Irina Tsoy and Céline Frochot

Pharmaceuticals 2021, 14(2), 138; https://doi.org/10.3390/ph14020138 - 9 Feb 2021

Cited by 51 | Viewed by 5827

Abstract

Photodynamic therapy (PDT) is an innovative treatment of malignant or diseased tissues. The effectiveness of PDT depends on light dosimetry, oxygen availability, and properties of the photosensitizer (PS). Depending on the medium, photophysical properties of the PS can change leading to increase or [...] Read more.

Photodynamic therapy (PDT) is an innovative treatment of malignant or diseased tissues. The effectiveness of PDT depends on light dosimetry, oxygen availability, and properties of the photosensitizer (PS). Depending on the medium, photophysical properties of the PS can change leading to increase or decrease in fluorescence emission and formation of reactive oxygen species (ROS) especially singlet oxygen (¹O₂). In this study, the influence of solvent polarity, viscosity, concentration, temperature, and pH medium on the photophysical properties of protoporphyrin IX, pyropheophorbide-a, and Photofrin^® were investigated by UV-visible absorption, fluorescence emission, singlet oxygen emission, and time-resolved fluorescence spectroscopies. Full article

(This article belongs to the Special Issue Photodynamic Therapy 2021)

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23 pages, 7117 KiB

Open AccessEditor’s ChoiceReview

Monofunctional Platinum(II) Anticancer Agents

by Suxing Jin, Yan Guo, Zijian Guo and Xiaoyong Wang

Pharmaceuticals 2021, 14(2), 133; https://doi.org/10.3390/ph14020133 - 7 Feb 2021

Cited by 53 | Viewed by 5791

Abstract

Platinum-based anticancer drugs represented by cisplatin play important roles in the treatment of various solid tumors. However, their applications are largely compromised by drug resistance and side effects. Much effort has been made to circumvent the drug resistance and general toxicity of these [...] Read more.

Platinum-based anticancer drugs represented by cisplatin play important roles in the treatment of various solid tumors. However, their applications are largely compromised by drug resistance and side effects. Much effort has been made to circumvent the drug resistance and general toxicity of these drugs. Among multifarious designs, monofunctional platinum(II) complexes with a general formula of [Pt(3A)Cl]⁺ (A: Ammonia or amine) stand out as a class of “non-traditional” anticancer agents hopeful to overcome the defects of current platinum drugs. This review aims to summarize the development of monofunctional platinum(II) complexes in recent years. They are classified into four categories: fluorescent complexes, photoactive complexes, targeted complexes, and miscellaneous complexes. The intention behind the designs is either to visualize the cellular distribution, or to reduce the side effects, or to improve the tumor selectivity, or inhibit the cancer cells through non-DNA targets. The information provided by this review may inspire researchers to conceive more innovative complexes with potent efficacy to shake off the drawbacks of platinum anticancer drugs. Full article

(This article belongs to the Special Issue Applications of Medicinal Bioinorganic Chemistry)

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33 pages, 1094 KiB

Open AccessEditor’s ChoiceReview

The Current and Potential Therapeutic Use of Metformin—The Good Old Drug

by Józef Drzewoski and Markolf Hanefeld

Pharmaceuticals 2021, 14(2), 122; https://doi.org/10.3390/ph14020122 - 5 Feb 2021

Cited by 77 | Viewed by 16265

Abstract

Metformin, one of the oldest oral antidiabetic agents and still recommended by almost all current guidelines as the first-line treatment for type 2 diabetes mellitus (T2DM), has become the medication with steadily increasing potential therapeutic indications. A broad spectrum of experimental and clinical [...] Read more.

Metformin, one of the oldest oral antidiabetic agents and still recommended by almost all current guidelines as the first-line treatment for type 2 diabetes mellitus (T2DM), has become the medication with steadily increasing potential therapeutic indications. A broad spectrum of experimental and clinical studies showed that metformin has a pleiotropic activity and favorable effect in different pathological conditions, including prediabetes, type 1 diabetes mellitus (T1DM) and gestational diabetes mellitus (GDM). Moreover, there are numerous studies, meta-analyses and population studies indicating that metformin is safe and well tolerated and may be associated with cardioprotective and nephroprotective effect. Recently, it has also been reported in some studies, but not all, that metformin, besides improvement of glucose homeostasis, may possibly reduce the risk of cancer development, inhibit the incidence of neurodegenerative disease and prolong the lifespan. This paper presents some arguments supporting the initiation of metformin in patients with newly diagnosed T2DM, especially those without cardiovascular risk factors or without established cardiovascular disease or advanced kidney insufficiency at the time of new guidelines favoring new drugs with pleotropic effects complimentary to glucose control. Moreover, it focuses on the potential beneficial effects of metformin in patients with T2DM and coexisting chronic diseases. Full article

(This article belongs to the Special Issue Metformin: Mechanism and Application 2022)

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21 pages, 719 KiB

Open AccessEditor’s ChoiceReview

Informing Patients about Biosimilar Medicines: The Role of European Patient Associations

by Yannick Vandenplas, Steven Simoens, Philippe Van Wilder, Arnold G. Vulto and Isabelle Huys

Pharmaceuticals 2021, 14(2), 117; https://doi.org/10.3390/ph14020117 - 4 Feb 2021

Cited by 37 | Viewed by 5675

Abstract

Biosimilar medicines support the sustainability of national healthcare systems, by reducing costs of biological therapies through increased competition. However, their adoption into clinical practice largely depends on the acceptance of healthcare providers and patients. Patients are different from health care professionals (HCPs), who [...] Read more.

Biosimilar medicines support the sustainability of national healthcare systems, by reducing costs of biological therapies through increased competition. However, their adoption into clinical practice largely depends on the acceptance of healthcare providers and patients. Patients are different from health care professionals (HCPs), who are informing themselves professionally. For patients, the biosimilar debate only becomes actual when they are confronted with disease and drug choices. This paper provides a literature review on how patients are and should be informed about biosimilars, searching in scientific databases (i.e., Medline, Embase). Several large surveys have shown a lack of knowledge and trust in biosimilars among European patients in recent years. This review identified five main strategies to inform patients about biosimilars: (1) provide understandable information, (2) in a positive and transparent way, (3) tailored to the individual’s needs, (4) with one voice, and (5) supported by audiovisual material. Moreover, the importance of a multistakeholder approach was underlined by describing the role of each stakeholder. Patients are a large and diffuse target group to be reached by educational programs. Therefore, patient associations have become increasingly important in correctly informing patients about biosimilar medicines. This has led to widespread biosimilar information for patients among European patient associations. Therefore, a web-based screening of European Patients’ Forum (EPF) and International Alliance of Patients’ Organizations (IAPO) member organizations on publicly available information about biosimilars was performed. We found that the level of detail, correctness, and the tone of the provided information varied. In conclusion, it is paramount to set up a close collaboration between all stakeholders to communicate, develop, and disseminate factual information about biosimilars for patients. Full article

(This article belongs to the Special Issue Biosimilars in Europe)

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12 pages, 1330 KiB

Open AccessFeature PaperEditor’s ChoiceReview

Tauvid™: The First FDA-Approved PET Tracer for Imaging Tau Pathology in Alzheimer’s Disease

by Caitlin V. M. L. Jie, Valerie Treyer, Roger Schibli and Linjing Mu

Pharmaceuticals 2021, 14(2), 110; https://doi.org/10.3390/ph14020110 - 30 Jan 2021

Cited by 64 | Viewed by 10712

Abstract

Tauvid has been approved by the U.S. Food and Drug Administration (FDA) in 2020 for positron emission tomography (PET) imaging of adult patients with cognitive impairments undergoing evaluation for Alzheimer’s disease (AD) based on tau pathology. Abnormal aggregation of tau proteins is one [...] Read more.

Tauvid has been approved by the U.S. Food and Drug Administration (FDA) in 2020 for positron emission tomography (PET) imaging of adult patients with cognitive impairments undergoing evaluation for Alzheimer’s disease (AD) based on tau pathology. Abnormal aggregation of tau proteins is one of the main pathologies present in AD and is receiving increasing attention as a diagnostic and therapeutic target. In this review, we summarised the production and quality control of Tauvid, its clinical application, pharmacology and pharmacokinetics, as well as its limitation due to off-target binding. Moreover, a brief overview on the second-generation of Tau PET tracers is provided. The approval of Tauvid marks a step forward in the field of AD research and opens up opportunities for second-generation tau tracers to advance tau PET imaging in the clinic. Full article

(This article belongs to the Special Issue Targets, Tracers and Translation, Part 2 - New Horizons in Radiopharmaceutical Development)

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23 pages, 4177 KiB

Open AccessFeature PaperEditor’s ChoiceReview

Repurposing Clinical Agents for Chemical Exchange Saturation Transfer Magnetic Resonance Imaging: Current Status and Future Perspectives

by Zelong Chen, Zheng Han and Guanshu Liu

Pharmaceuticals 2021, 14(1), 11; https://doi.org/10.3390/ph14010011 - 24 Dec 2020

Cited by 17 | Viewed by 4727

Abstract

Molecular imaging is becoming an indispensable tool to pursue precision medicine. However, quickly translating newly developed magnetic resonance imaging (MRI) agents into clinical use remains a formidable challenge. Recently, Chemical Exchange Saturation Transfer (CEST) MRI is emerging as an attractive approach with the [...] Read more.

Molecular imaging is becoming an indispensable tool to pursue precision medicine. However, quickly translating newly developed magnetic resonance imaging (MRI) agents into clinical use remains a formidable challenge. Recently, Chemical Exchange Saturation Transfer (CEST) MRI is emerging as an attractive approach with the capability of directly using low concentration, exchangeable protons-containing agents for generating quantitative MRI contrast. The ability to utilize diamagnetic compounds has been extensively exploited to detect many clinical compounds, such as FDA approved drugs, X-ray/CT contrast agents, nutrients, supplements, and biopolymers. The ability to directly off-label use clinical compounds permits CEST MRI to be rapidly translated to clinical settings. In this review, the current status of CEST MRI based on clinically available compounds will be briefly introduced. The advancements and limitations of these studies are reviewed in the context of their pre-clinical or clinical applications. Finally, future directions will be briefly discussed. Full article

(This article belongs to the Special Issue Next Generation of MRI Agents)

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