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"Albericio, Fernando"
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The Pharmaceutical Industry in 2023: An Analysis of FDA Drug Approvals from the Perspective of Molecules
by
de la Torre, Beatriz G.
,
Albericio, Fernando
in
Amino acids
,
antibodies
,
Antibodies, Monoclonal
2024
With the COVID-19 pandemic behind us, the U.S. Food and Drug Administration (FDA) has approved 55 new drugs in 2023, a figure consistent with the number authorized in the last five years (53 per year on average). Thus, 2023 marks the second-best yearly FDA harvest after 2018 (59 approvals) in all the series. Monoclonal antibodies (mAbs) continue to be the class of drugs with the most approvals, with an exceptional 12, a number that makes it the most outstanding year for this class. As in 2022, five proteins/enzymes have been approved in 2023. However, no antibody–drug conjugates (ADCs) have been released onto the market. With respect to TIDES (peptides and oligonucleotides), 2023 has proved a spectacular year, with a total of nine approvals, corresponding to five peptides and four oligonucleotides. Natural products continue to be the best source of inspiration for drug development, with 10 new products on the market. Three drugs in this year’s harvest are pegylated, which may indicate the return of pegylation as a method to increase the half-lives of drugs after the withdrawal of peginesatide from the market in 2013. Following the trends in recent years, two bispecific drugs have been authorized in 2023. As in the preceding years, fluorine and/or N-aromatic heterocycles are present in most of the drugs. Herein, the 55 new drugs approved by the FDA in 2023 are analyzed exclusively on the basis of their chemical structure. They are classified as the following: biologics (antibodies, proteins/enzymes); TIDES (peptide and oligonucleotides); combined drugs; pegylated drugs; natural products; nitrogen aromatic heterocycles; fluorine-containing molecules; and other small molecules.
Journal Article
Contemporary Developments in Ferrocene Chemistry: Physical, Chemical, Biological and Industrial Aspects
by
Albericio, Fernando
,
Shabir, Ghulam
,
Saeed, Aamer
in
applications
,
asymmetric catalysis
,
bioreceptors
2023
Ferrocenyl-based compounds have many applications in diverse scientific disciplines, including in polymer chemistry as redox dynamic polymers and dendrimers, in materials science as bioreceptors, and in pharmacology, biochemistry, electrochemistry, and nonlinear optics. Considering the horizon of ferrocene chemistry, we attempted to condense the neoteric advancements in the synthesis and applications of ferrocene derivatives reported in the literature from 2016 to date. This paper presents data on the progression of the synthesis of diverse classes of organic compounds having ferrocene scaffolds and recent developments in applications of ferrocene-based organometallic compounds, with a special focus on their biological, medicinal, bio-sensing, chemosensing, asymmetric catalysis, material, and industrial applications.
Journal Article
The Pharmaceutical Industry in 2020. An Analysis of FDA Drug Approvals from the Perspective of Molecules
2021
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.
Journal Article
Antibiotic Resistance: From the Bench to Patients
by
Albericio, Fernando
,
Gajdács, Márió
in
Antibiotic resistance
,
Antibiotics
,
Antimicrobial agents
2019
Direct consequences of antibiotic resistance include delays in the onset of the appropriate (effective) antimicrobial therapy, the need to use older, more toxic antibiotics (e.g., colistin) with a disadvantageous side-effect profile, longer hospital stays, and an increasing burden on the healthcare infrastructure; overall, a decrease in the quality-of-life (QoL) and an increase in the mortality rate of the affected patients [4,5]. To highlight the severity of the issue, several international declarations have been published to call governments around the globe to take action on antimicrobial resistance [6,7,8,9]. Since the 1980s, pharmaceutical companies have slowly turned away from antimicrobial research and towards the drug therapy of chronic non-communicable diseases [10,11]. [...]programs and interventions aiming at optimizing the use of antimicrobial drugs (such as implementation of policies and guidelines, drug utilization reports, point prevalence surveys, both locally and internationally), collectively termed “antimicrobial stewardship”, have received substantial attention [23].
Journal Article
Strategies for Improving Peptide Stability and Delivery
by
Albericio, Fernando
,
Al Musaimi, Othman
,
Williams, Daryl R.
in
Amino acids
,
Biological activity
,
cell-penetrating peptides
2022
Peptides play an important role in many fields, including immunology, medical diagnostics, and drug discovery, due to their high specificity and positive safety profile. However, for their delivery as active pharmaceutical ingredients, delivery vectors, or diagnostic imaging molecules, they suffer from two serious shortcomings: their poor metabolic stability and short half-life. Major research efforts are being invested to tackle those drawbacks, where structural modifications and novel delivery tactics have been developed to boost their ability to reach their targets as fully functional species. The benefit of selected technologies for enhancing the resistance of peptides against enzymatic degradation pathways and maximizing their therapeutic impact are also reviewed. Special note of cell-penetrating peptides as delivery vectors, as well as stapled modified peptides, which have demonstrated superior stability from their parent peptides, are reported.
Journal Article
The Pharmaceutical Industry in 2021. An Analysis of FDA Drug Approvals from the Perspective of Molecules
by
de la Torre, Beatriz G.
,
Albericio, Fernando
in
Alzheimer's disease
,
antibodies
,
antibody-drug conjugate
2022
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.
Journal Article
The Pharmaceutical Industry in 2019. An Analysis of FDA Drug Approvals from the Perspective of Molecules
by
de la Torre, Beatriz G.
,
Albericio, Fernando
in
Antibodies
,
antibody drug conjugate
,
Biological products
2020
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.
Journal Article
Linkers: An Assurance for Controlled Delivery of Antibody-Drug Conjugate
by
de la Torre, Beatriz G.
,
Sheyi, Rotimi
,
Albericio, Fernando
in
Acids
,
antibody-drug conjugates (ADCs)
,
Antigens
2022
As one of the major therapeutic options for cancer treatment, chemotherapy has limited selectivity against cancer cells. Consequently, this therapeutic strategy offers a small therapeutic window with potentially high toxicity and thus limited efficacy of doses that can be tolerated by patients. Antibody-drug conjugates (ADCs) are an emerging class of anti-cancer therapeutic drugs that can deliver highly cytotoxic molecules directly to cancer cells. To date, twelve ADCs have received market approval, with several others in clinical stages. ADCs have become a powerful class of therapeutic agents in oncology and hematology. ADCs consist of recombinant monoclonal antibodies that are covalently bound to cytotoxic chemicals via synthetic linkers. The linker has a key role in ADC outcomes because its characteristics substantially impact the therapeutic index efficacy and pharmacokinetics of these drugs. Stable linkers and ADCs can maintain antibody concentration in blood circulation, and they do not release the cytotoxic drug before it reaches its target, thus resulting in minimum off-target effects. The linkers used in ADC development can be classified as cleavable and non-cleavable. The former, in turn, can be grouped into three types: hydrazone, disulfide, or peptide linkers. In this review, we highlight the various linkers used in ADC development and their design strategy, release mechanisms, and future perspectives.
Journal Article
The Pharmaceutical Industry in 2025: An Analysis of FDA Drug Approvals from the Perspective of Molecules
by
de la Torre, Beatriz G.
,
Albericio, Fernando
in
Antibodies
,
Antibodies, Monoclonal - chemistry
,
Antibodies, Monoclonal - therapeutic use
2026
In 2025, the U.S. Food and Drug Administration (FDA) approved 44 new drugs, reflecting a slight decrease compared to previous years but maintaining the overall trends in pharmaceutical innovation. Biologics accounted for 25% of approvals, including nine monoclonal antibodies (mAbs), two antibody–drug conjugates (ADCs), and one fusion protein, with cancer remaining the primary therapeutic focus. TIDES, comprising three oligonucleotides and one peptide, continued to consolidate their presence in the market, with the three oligonucleotides featuring N-acetylgalactosamine (GalNAc) for liver-targeted delivery. Small molecules dominate the remainder, with a high prevalence of N-aromatic moieties and fluorine atoms present in most of the molecules. Peptide manufacturing and sustainability concerns, including PFAS usage, remain key challenges. Despite these advances, the high cost of innovative therapies limits access, particularly in low- and middle-income countries. This report provides a structural and chemical analysis of the newly approved drugs, highlighting trends in molecular design, therapeutic areas, and technological innovations shaping modern drug discovery.
Journal Article
Peptide Therapeutics 2.0
2020
In recent years, the peptide drug discovery field has shown a high level of dynamism, with hundreds of academic groups working on this topic, the creation of new peptide-focused companies, and the consolidation of peptide business by so-called big pharma [...]
Journal Article