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Similar to last year, 2021 will be remembered for the COVID-19 pandemic. Although five vaccines have been approved by the two most important drug regulatory agencies, namely the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA), the pandemic has still not been brought under control. However, despite the context of a global pandemic, 2021 has been an excellent year with respect to drug approvals by the FDA. In 2021, 50 drugs have been authorized, making it the fourth-best year after 2018 (59 drugs) and 1996 and 2020 (53 each). Regarding biologics, 2021 has been the third-best year to date, with 14 approvals, and it has also witnessed the authorization of 36 small molecules. Of note, nine peptides, eight monoclonal antibodies, two antibody-drug conjugates, and two oligonucleotides have been approved this year. From them, five of the molecules are pegylated and three of them highly pegylated. The presence of nitrogen aromatic heterocycles and/or fluorine atoms are once again predominant among the so-called small molecules. This report analyzes the 50 new drugs approved in 2021 from a chemical perspective, as it did for those authorized in the previous five years. On the basis of chemical structure alone, the drugs that received approval in 2021 are classified as the following: biologics (antibodies, antibody-drug conjugates, enzymes, and pegylated proteins); TIDES (peptide and oligonucleotides); combined drugs; natural products; nitrogen aromatic heterocycles; fluorine-containing molecules; and other small molecules., The work performed by the authors laboratory is funded by the National Research Foundation (NRF) and the University of KwaZulu-Natal.

Although the pharmaceutical industry will remember 2020 as the year of COVID-19, it is important to highlight that this year has been the second-best—together with 1996—in terms of the number of drugs accepted by the US Food and Drug Administration (FDA). Each of these two years witnessed the authorization of 53 drugs—a number surpassed only in 2018 with 59 pharmaceutical agents. The 53 approvals in 2020 are divided between 40 new chemical entities and 13 biologic drugs (biologics). Of note, ten monoclonal antibodies, two antibody–drug conjugates, three peptides, and two oligonucleotides have been approved in 2020. Close inspection of the so-called small molecules reveals the significant presence of fluorine atoms and/or nitrogen aromatic heterocycles. This report analyzes the 53 new drugs of the 2020 harvest from a strictly chemical perspective, as it did for those authorized in the previous four years. On the basis of chemical structure alone, the drugs that received approval in 2020 are classified as the following: biologics (antibodies, antibody-drug conjugates, and proteins); TIDES (peptide and oligonucleotides); natural products; fluorine-containing molecules; nitrogen aromatic heterocycles; and other small molecules, The work performed by the authors is funded by the National Research Foundation (NRF) and the University of KwaZulu-Natal.

peer-reviewed Poor solubility of new chemical entities (NCEs) is a major bottleneck in the pharmaceutical industry which typically leads to poor drug bioavailability and efficacy. Nanotechnologies offer an interesting route to improve the apparent solubility and dissolution rate of pharmaceutical drugs, and processes such as nano-spray drying and supercritical CO2-assisted spray drying (SASD) provide a route to engineer and produce solid drug nanoparticles. However, dried nanoparticles often show poor rheological properties (e.g. flowability, tabletability) and their isolation using these methods is typically inefficient and leads to poor collection yields. The work presented herein demonstrates a novel production and isolation method for drug nanoparticles using a ‘top spray dynamic bed coating’ process, which uses CO2 spray as the fluidizing gas. Nanoparticles of three BCS class II Active Pharmaceutical Ingredients (APIs), namely carbamazepine (CBZ), ketoprofen (KET) and risperidone (RIS), were produced and successfully coated onto micron-sized microcrystalline cellulose (MCC) particles. The size distribution of the API nanoparticles was in the range of 90–490 nm. The stable forms of CBZ (form III), KET (form I), and the metastable form of RIS (form B) were produced and coated onto MCC carrier microparticles. All the isolated solids presented optimal rheological properties along with a 2–6 fold improvement in the dissolution rate of the corresponding APIs. Hence, the ‘top spray dynamic bed coater’ developed in this work demonstrates to be an efficient approach to produce and coat API nanoparticles onto carrier particles with optimal rheological properties and improved dissolution.

During 2019, the US Food and Drug Administration (FDA) approved 48 new drugs (38 New Chemical Entities and 10 Biologics). Although this figure is slightly lower than that registered in 2018 (59 divided between 42 New Chemical Entities and 17 Biologics), a year that broke a record with respect to new drugs approved by this agency, it builds on the trend initiated in 2017, when 46 drugs were approved. Of note, three antibody drug conjugates, three peptides, and two oligonucleotides were approved in 2019. This report analyzes the 48 new drugs of the class of 2019 from a strictly chemical perspective. The classification, which was carried out on the basis of chemical structure, includes the following: Biologics (antibody drug conjugates, antibodies, and proteins); TIDES (peptide and oligonucleotides); drug combinations; natural products; and small molecules.

The Food and Drug Administration approved 59 new drugs (42 New Chemical Entities and 17 Biologics) during 2018. This number breaks the previous record of 53 approved by the same organization in 1996. The 17 new biologics approved in 2018 also represent an important milestone for this kind of drug and they clearly exceed the 12 approved in 2015 and 2017. Herein, the 59 new drugs of the class of 2018 are analyzed from a strictly chemical perspective. The classification has been carried out on the basis of the chemical structure and includes the following: Biologics (antibodies and enzymes); TIDES (peptides and oligonucleotides) and natural products; drug combinations; and small molecules.

This is an analysis from a chemical point of view of the 46 drugs (34 New Chemical Entities and 12 Biologics) approved by the FDA during 2017. The drugs included in the 2017 "harvest" have been classified on the basis of their chemical structure: biologics (antibodies and proteins); peptides; amino acids and natural products; drug combinations; and small molecules.

This is an analysis from a chemical point of view of the 22 drugs accepted by the FDA during 2016. The different drugs from the 2016 "harvest" have been classified according to their chemical structure: antibodies; TIDES (oligonucleotides and peptides); amino acids and natural products; drug combination; and small molecules.

Integration of open access, curated, high-quality information from multiple disciplines in the Life and Biomedical Sciences provides a holistic understanding of the domain. Additionally, the effective linking of diverse data sources can unearth hidden relationships and guide potential research strategies. However, given the lack of consistency between descriptors and identifiers used in different resources and the absence of a simple mechanism to link them, gathering and combining relevant, comprehensive information from diverse databases remains a challenge. The Open Pharmacological Concepts Triple Store (Open PHACTS) is an Innovative Medicines Initiative project that uses semantic web technology approaches to enable scientists to easily access and process data from multiple sources to solve real-world drug discovery problems. The project draws together sources of publicly-available pharmacological, physicochemical and biomolecular data, represents it in a stable infrastructure and provides well-defined information exploration and retrieval methods. Here, we highlight the utility of this platform in conjunction with workflow tools to solve pharmacological research questions that require interoperability between target, compound, and pathway data. Use cases presented herein cover 1) the comprehensive identification of chemical matter for a dopamine receptor drug discovery program 2) the identification of compounds active against all targets in the Epidermal growth factor receptor (ErbB) signaling pathway that have a relevance to disease and 3) the evaluation of established targets in the Vitamin D metabolism pathway to aid novel Vitamin D analogue design. The example workflows presented illustrate how the Open PHACTS Discovery Platform can be used to exploit existing knowledge and generate new hypotheses in the process of drug discovery.

International audience; Considerable information on the chemistry and biological properties of dietary phytochemicals has accumulated over the past three decades. The scattering of the data in tens of thousands publications and the diversity of experimental approaches and reporting formats all make the exploitation of this information very difficult. Some of the data have been collected and stored in electronic databases so that they can be automatically updated and retrieved. These databases will be particularly important in the evaluation of the effects on health of phytochemicals and in facilitating the exploitation of nutrigenomic data. The content of over 50 databases on chemical structures, spectra, metabolic pathways in plants, occurrence and concentrations in foods, metabolism in humans and animals, biological properties, and effects on health or surrogate markers of health is reviewed. Limits of these databases are emphasized, and needs and recommendations for future developments are underscored. More investments in the construction of databases on phytochemicals and their effects on health are clearly needed. They should greatly contribute to the success of future research in this field.

The rapid increase in the flow rate of published digital information in all disciplines has resulted in a pressing need for techniques that can simplify the use of this information. The chemistry literature is very rich with information about chemical entities. Extracting molecules and their related properties and activities from the scientific literature to “text mine” these extracted data and determine contextual relationships helps research scientists, particularly those in drug development. One of the most important challenges in chemical text mining is the recognition of chemical entities mentioned in the texts. In this review, the authors briefly introduce the fundamental concepts of chemical literature mining, the textual contents of chemical documents, and the methods of naming chemicals in documents. We sketch out dictionary-based, rule-based and machine learning, as well as hybrid chemical named entity recognition approaches with their applied solutions. We end with an outlook on the pros and cons of these approaches and the types of chemical entities extracted.