Drug Discovery Today

Papers
(The TQCC of Drug Discovery Today is 19. The table below lists those papers that are above that threshold based on CrossRef citation counts [max. 250 papers]. The publications cover those that have been published in the past four years, i.e., from 2021-12-01 to 2025-12-01.)
ArticleCitations
Dysbiosis versus diabesity: Pathological signaling and promising therapeutic strategies280
Advancing drug repurposing research: Trends, collaborative networks, innovation and knowledge leaders239
Generative AI: driving productivity and scientific breakthroughs in pharmaceutical R&D204
On-body drug delivery systems: State-of-the-art technologies, clinical application, and future perspectives192
The global status of bioequivalence trials: a comprehensive clinical trial landscape analysis based on the Trialtrove database152
Tubulin targeting agents and their implications in non-cancer disease management149
Multiple strategies for the treatment of invasive breast carcinoma: A comprehensive prospective139
Bridging data and drug development: Machine learning approaches for next-generation ADMET prediction130
Achieving end-to-end success in the clinic: Pfizer’s learnings on R&D productivity124
CIPDB: A biological structure databank for studying cation and π interactions122
Opportunities and challenges in drug discovery targeting the orphan receptor GPR12121
Contents page119
Development of JmjC-domain-containing histone demethylase (KDM2-7) inhibitors for cancer therapy100
Repurposing of parenterally administered active substances used to treat pain both systemically and locally99
Demystifying the potential of inhibitors targeting DNA topoisomerases in unicellular protozoan parasites99
The potential value of 5-androstenediol in countering acute radiation syndrome97
General aspects of powder rheology applied to pharmaceutical formulations96
Models and approaches to comprehend and address glial inflammation following spinal cord injury90
Antibody–drug conjugates: What drives their progress?89
The recent progress of deep-learning-based in silico prediction of drug combination88
A global bibliometric and visualized analysis of bacteria-mediated cancer therapy87
Trends in oral small-molecule drug discovery and product development based on product launches before and after the Rule of Five85
Targeted drug delivery to the retinal pigment epithelium: Untapped therapeutic potential for retinal diseases85
Computational modeling approaches and regulatory pathways for drug combinations85
Gastroretentive drug delivery systems: A holy grail in oral delivery85
Redox active or thiol reactive? Optimization of rapid screens to identify less evident nuisance compounds80
Exploration of small-molecule inhibitors targeting Hsp110 as novel therapeutics79
From promise to progress: the dynamic landscape of glioblastoma immunotherapy79
Caught between a ROCK and a hard place: current challenges in structure-based drug design75
Systematic review and QSPR analysis of chemical penetration through the nail to inform onychomycosis candidate selection74
Recent advancements in mass spectrometry for higher order structure characterization of protein therapeutics74
Triple-negative breast cancer brain metastasis: An update on druggable targets, current clinical trials, and future treatment options73
Steps toward nebulization in-use studies to understand the stability of new biological entities73
Recent advances towards overcoming the blood–brain barrier71
MTHFD2: A significant mitochondrial metabolic enzyme and a novel target for anticancer therapy70
ImmunoPET imaging of hematological malignancies: From preclinical promise to clinical reality68
Organoids in modelling infectious diseases66
Master protocols and other innovative trial designs in inflammation and immunology to expedite clinical drug development66
The main aspects of non-clinical studies required for obtaining marketing authorisation for small molecules and biologics/biopharmaceuticals in the European Union and the United States64
MRI assessment of cerebral perfusion in clinical trials63
Regulatory approvals of therapeutic biologics: continuing progress or plateauing out compared with those of small molecules?63
Randomized controlled trials do not always fit the purpose: A science-based response to Venetis and Mol’s editorial on biosimilars of follitropin alfa63
Lipid- and polymer-based formulations containing TNF-α inhibitors for the treatment of inflammatory bowel diseases63
Targeting mutant EGFR in non-small cell lung cancer in the context of cell adaptation and resistance62
Embryonic and larval zebrafish models for the discovery of new bioactive compounds against tuberculosis61
Unlocking therapeutic frontiers: harnessing artificial intelligence in drug discovery for neurodegenerative diseases60
Pathogenic TDP-43 in amyotrophic lateral sclerosis59
The emerging role of fatty acid binding protein 7 (FABP7) in cancers59
Therapeutic strategies targeting ocular vasculopathies: Current advances and emerging challenges58
Bridging informatics and medicinal inorganic chemistry: Toward a database of metallodrugs and metallodrug candidates58
Gaps between medical biology and AI drug discovery58
Role of siRNA-based nanocarriers for the treatment of neurodegenerative diseases58
Mutation informatics: SARS-CoV-2 receptor-binding domain of the spike protein56
Translational PK/PD: a retrospective analysis of performance and impact from a drug portfolio56
Advancing pharmacogenetics research in Africa: the “Project Africa GRADIENT” initiative56
Lactose in tablets: Functionality, critical material attributes, applications, modifications and co-processed excipients55
Investigating miRNA subfamilies: Can they assist in the early diagnosis of acute myocardial infarction?55
Oral delivery of nucleic acid therapeutics: Challenges, strategies, and opportunities55
Towards Pharma 4.0 in clinical trials: A future-orientated perspective54
Global landscape and translational trajectories of flavonoid-based wound-healing research54
Molecular approaches for the treatment and prevention of Friedreich's ataxia53
Metabolic reprogramming: Unveiling the therapeutic potential of targeted therapies against kidney disease53
Targeted protein degradation: current molecular targets, localization, and strategies53
A review on the recent advances of interaction studies of anticancer metal-based drugs with therapeutic targets, DNA and RNAs53
PD-L1 small-molecule modulators: A new hope in epigenetic-based multidrug cancer therapy?52
Medicinal chemistry aspects of uracil containing dUTPase inhibitors targeting colorectal cancer52
Genetic–epigenetic targets for PCOS-associated diabesity52
50 shades of AI in regulatory science51
Overview of new indications for novel drugs approved in China between 2018 and 202451
Sustainability by design for recombinant protein therapeutics50
Advancements and challenges in using AI for biomarker detection in early Alzheimer’s disease50
Back on the scene: Advances and challenges in CD3-related drugs in tumor therapy49
Elevating life science R&D success with AI: a framework49
Regulatory readiness to facilitate the appropriate use of innovation in clinical trials: The case of decentralized clinical trial approaches49
Potential nanocarrier-mediated miRNA-based therapy approaches for multiple sclerosis48
Global or local: The future of biotech48
Contents page48
Opioid epidemic and the urge to discover new treatment options48
Review of the impact of the FDA’s Fast Track Designation on biotechnology companies’ share prices47
Hippo signaling in acute kidney injury to chronic kidney disease transition: Current understandings and future targets47
Development of LRRK2 inhibitors through computational strategies: a promising avenue for Parkinson’s disease46
IRE1α-mediated UPR activation in gastrointestinal cancers: Adaptive mechanisms and therapeutic potential46
Open innovation: A paradigm shift in pharma R&D?46
In silico resources help combat cancer drug resistance mediated by target mutations46
Decentralised, patient-centric, site-less, virtual, and digital clinical trials? From confusion to consensus45
Recent advances in dual-drug co-amorphous systems45
Vaginal drug delivery system: A promising route of drug administration for local and systemic diseases45
Recent advances in multitarget-directed ligands via in silico drug discovery45
Pharmaceutical strategies for the treatment of bacterial biofilms in chronic wounds44
Indole therapeutics: Latest FDA updates, ongoing trials, and future directions43
Renal cell carcinoma therapy: Current and new drug candidates43
Disruptions in bioactivity driven by dose: a challenge for drug discovery43
Self-amplifying mRNA vaccines: Mode of action, design, development and optimization43
UCP1 activation: Hottest target in the thermogenesis pathway to treat obesity using molecules of synthetic and natural origin42
Illuminating function of the understudied druggable kinome42
CPPsite3: An updated large repository of experimentally validated cell-penetrating peptides42
Cubosome-based cosmeceuticals: A breakthrough in skincare41
Recent insights into viral infections as a trigger and accelerator in alzheimer's disease41
An overview of progress in human metapneumovirus (hMPV) research: Structure, function, and therapeutic opportunities41
Impact of HDAC inhibitors on macrophage polarization to enhance innate immunity against infections41
Drugs from drugs: New chemical insights into a mature concept41
The role of gut microbial β-glucuronidase in drug disposition and development41
Corrigendum to “Role of transient receptor potential channels in the regulation of vascular tone” [Drug Discov. Today 29(7) (2024) 104051]40
Does pharma R&D need a strategic reset? Adapting to a changing US landscape40
Metabophore-mediated retro-metabolic (‘MeMeReMe’) approach in drug design40
2023 in review: FDA approvals of new medicines40
Small molecules targeting canonical transient receptor potential channels: an update38
A new era for schizophrenia drug development – Lessons for the future38
Transforming patient engagement in clinical trials: Moving from a transactional relationship to human-centered care38
Corrigendum to “Therapeutic potential of fucosyltransferases in cancer and recent development of targeted inhibitors” [Drug Discov. Today 28(1) (2023) 103394]38
Artificial intelligence methods in kinase target profiling: Advances and challenges38
Real-world data in drug development strategies for orphan drugs: Tafasitamab in B-cell lymphoma, a case study for an approval based on a single-arm combination trial38
Strategizing the human microbiome for small molecules: Approaches and perspectives38
Oncological drug discovery: AI meets structure-based computational research38
Geometric deep learning methods and applications in 3D structure-based drug design38
The Unitary Patent and UPC – Implications for the pharmaceutical sector38
Therapeutic potential of targeting IL-17 and its receptor signaling in neuroinflammation37
Targeting hepatitis B virus cccDNA levels: Recent progress in seeking small molecule drug candidates37
dbDNA™: An advanced platform for genetic medicines37
Science of, and insights into, thermodynamic principles for dermal formulations37
Operational and path dependencies impede the feasibility of hospital-based production of individually engineered drugs37
Innovation testbeds as enabling ecosystems driving nanopharmaceuticals to market37
Artificially engineered bacteria to treat gastrointestinal disease and cancer37
Neurotrophin peptidomimetics for the treatment of neurodegenerative diseases36
Advances in lipid-based nanoformulations for inhaled antibiotic therapy in respiratory infections36
Recent advances in flavonoid-based nanocarriers as an emerging drug delivery approach for cancer chemotherapy36
Breakthrough in RAS targeting with pan-RAS(ON) inhibitors RMC-7977 and RMC-623636
Insight into the pivotal role of signaling pathways in psoriasis pathogenesis, potential therapeutic molecules and drug delivery approaches36
Nanoformulations of chemotherapeutic activators of the cGAS–STING pathway in tumor chemoimmunotherapy36
Therapeutic targeting of the complement system in ocular disease36
Death ligand receptor (DLR) signaling: Its non-apoptotic functions in cancer and the consequences of DLR-directed therapies35
Approaches to advance drug discovery for neglected tropical diseases35
Compound–protein interaction prediction by deep learning: Databases, descriptors and models35
Molecular medicinal insights into scaffold hopping-based drug discovery success35
Harnessing G-quadruplex ligands for lung cancer treatment: A comprehensive overview35
The expanding repertoire of covalent warheads for drug discovery35
PROTAC technology: A new drug design for chemical biology with many challenges in drug discovery35
Peptide-derived ligands for the discovery of safer opioid analgesics34
Harnessing personalized tailored medicines to digital-based data-enriched edible pharmaceuticals34
The importance of a go-to-market strategy in the commercialisation of cellular immunotherapies34
Advancing ocular gene therapy: a machine learning approach to enhance delivery, uptake and gene expression34
Regulatory oversight on the use of experimental therapies during a pandemic: The case of early access to convalescent plasma therapy in three LMICs34
Corrigendum to “Critical path activities in clinical trial setup & conduct – How to avoid bottlenecks and accelerate clinical trials” [Drug Discov. Today 28(10) (2023) 103733]34
Druggable genome special issue: An introduction34
Corrigendum to “Pharmacological modulation of autophagy for epilepsy therapy: Opportunities and obstacles” [Drug Discov. Today 28(6) (2023) 103600]33
Advances in antibody-based strategies for targeting cancer-associated glycopeptide antigens33
Contents page33
A pipeline analysis of advanced therapy medicinal products33
Expanding therapeutic potential of Bdellovibrio bacteriovorus against multidrug-resistant pathogens33
Small molecule inhibitors of the co-receptor neuropilin-133
How health technology assessment can help to address challenges in drug repurposing: a conceptual framework33
Blocking platelet glycoprotein VI (GPVI) as a promising antithrombotic treatment32
IdopNetwork as a genomic predictor of drug response32
Targeting autophagy in colorectal cancer: An update on pharmacological small-molecule compounds32
Social media mining in drug development—Fundamentals and use cases32
Early career researchers’ experiences in drug discovery in Africa32
A retrospective regulatory analysis of FDA recalls carried out by pharmaceutical companies from 2012 to 202332
‘Home inspections’ for life sciences companies going public before clinical proof-of-concept32
Competition of regulatory ecosystems in approving medicines: policy implications in the case of Europe31
Regulating NETosis: An emerging facet of statin pleiotropy31
Nanomedicine approaches to reduce cytokine storms in severe infections31
Surface-enhanced Raman scattering biosensors for detection of oncomiRs in breast cancer31
ADAM10: Function insights, disease implications, and promise of therapeutic targeting31
Drugging the entire human proteome: Are we there yet?31
Nanophotonic waveguide-based sensing of circulating cell-free mitochondrial DNA: implications for personalized medicine31
Publisher’s Note31
Deadly interactions: Synergistic manipulations of concurrent pathogen infections potentially enabling future pandemics31
COVID-19 therapeutics: Small-molecule drug development targeting SARS-CoV-2 main protease30
Translating precision medicine for autism spectrum disorder: A pressing need30
Recent discoveries of the role of histone modifications and related inhibitors in pathological cardiac hypertrophy30
Lysine lactylation: Regulatory mechanisms, role in health and disease, and its therapeutic potential30
Recent progress in covalent organic frameworks for cancer therapy30
Effectiveness of histamine receptor antagonists in the treatment of histamine-driven clinical symptoms: do we have a histamine or, better, an anti-histamine problem?30
Evaluating the performance of drug-repurposing technologies29
Opportunities and challenges of physiologically based pharmacokinetic modeling in drug delivery29
Exosome-mediated PROTAC delivery for treatment of RNA viral infections and zoonosis29
Machine learning and natural language processing in clinical trial eligibility criteria parsing: a scoping review29
Antimicrobial and anti-biofilm activities of bio-inspired nanomaterials for wound healing applications29
Orphan GPR52 as an emerging neurotherapeutic target29
Using computers to ESKAPE the antibiotic resistance crisis29
TDP-43 protein interactome informs about perturbed canonical pathways and may help develop personalized medicine approaches for patients with TDP-43 pathology29
Targeting SIRT1-regulated autophagic cell death as a novel therapeutic avenue for cancer prevention28
Therapies for Inherited Retinal Dystrophies: What is Enough?28
Therapeutic potential of fucosyltransferases in cancer and recent development of targeted inhibitors28
Prospects of halofuginone as an antiprotozoal drug scaffold28
Evaluation of the implementation effectiveness of accelerated drug marketing registration procedures in China: lessons from the 2016–2024 regulatory review28
Can preclinical drug development help to predict adverse events in clinical trials?28
Integrating heterogeneous data to facilitate COVID-19 drug repurposing28
Generic dry powder inhalers bioequivalence: Batch–to-batch variability insights28
A review of the efficacy of prostate cancer therapies against castration-resistant prostate cancer28
Chiral-engineered supraparticles: Emerging tools for drug delivery28
Peptide modulators of cell migration: Overview, applications and future development28
Patents, trade secrets and pricing28
A personalized pharmaco-epistatic network model of precision medicine28
Biopharmaceutical R&D outsourcing: Short-term gain for long-term pain?28
Sustaining pharmaceutical innovation after the Inflation Reduction Act: trends in R&D spending, equity investment, and business development27
Optical tweezers for drug discovery27
Methionine biosynthesis as a key metabolic pathway for antimicrobial drug discovery in Streptococcus mutans27
Which cryptic sites are feasible drug targets?27
Active pharmaceutical ingredients (APIs) in ionic liquids: An effective approach for API physiochemical parameter optimization27
Trends, challenges, and success factors in pharmaceutical portfolio management: Cognitive biases in decision-making and their mitigating measures27
Comparative analysis of FDA approvals by top 20 pharma companies (2014–2023)26
Applications of density functional theory in COVID-19 drug modeling26
ATP-binding cassette efflux transporters and MDR in cancer26
Electrospun proliposomes and the quest to overcome liposome instability26
Beyond CL and VSS: A comprehensive approach to human pharmacokinetic predictions26
Recent advances in the molecular design and applications of viral RNA-targeting antiviral modalities26
Shining light on liquid–liquid phase separation in chronic liver disease26
Recent trends in targeted delivery of smart nanocarrier-based microbial enzymes for therapeutic applications26
Novel and investigational therapies for wet and dry age-related macular degeneration26
Clinical significance and potential role of trimethylamine N-oxide in neurological and neuropsychiatric disorders26
Benefits of hybrid QM/MM over traditional classical mechanics in pharmaceutical systems26
Rational discovery of molecular glue degraders based on block chemistry25
Informatic challenges and advances in illuminating the druggable proteome25
Contents page25
Contents page25
Non-oncology orphan drug development: Productivity and probability of success25
Aceclofenac and methotrexate combination therapy could influence Th1/Th17 axis to modulate rheumatoid-arthritis-induced inflammation25
Contents page25
Concepts and applications of chemical fingerprint for hit and lead screening25
How can MSI enhance our understanding of ASO distribution?25
Metallocompounds as anticancer agents against osteosarcoma25
Electron diffraction: Accelerating drug development25
SET7, a lysine-specific methyl transferase: An intriguing epigenetic target to combat diabetic nephropathy24
Treating liver cancer through arginine depletion24
Covalent ligand efficiency24
Epigenetic roles of lysine-specific demethylase 1 (LSD1) in cancer metabolism24
The forced swim test has poor accuracy for identifying novel antidepressants24
Grasping cryptic binding sites to neutralize drug resistance in the field of anticancer24
Advantages, progress, and future trends in oral medicated jellies/gels: Focus on adherence aspects24
The role of venom proteomics and single-domain antibodies for antivenoms: Progress in snake envenoming treatment24
New approaches for challenging therapeutic targets24
Brain-derived neurotrophic factor (BDNF) in perinatal depression: Side show or pivotal factor?23
Dual-action potential of cationic cryptides against infections and cancers23
DDR1-targeted therapies: current limitations and future potential23
Unleashing the power of generative AI in drug discovery23
Commercialization of cell and gene therapy in Canada: Current landscape, challenges and opportunities23
Statins and angiogenesis in non-cardiovascular diseases23
On the pivotal role of drug discovery in sustainable EU pharma reform23
Illuminating the druggable genome: Pathways to progress23
How missing value imputation is confounded with batch effects and what you can do about it23
Machine learning in targeted protein degradation drug design: a technical review of PROTACs and molecular glues23
Positron emission tomographic imaging in drug discovery23
Nanosponges: An overlooked promising strategy to combat SARS-CoV-223
Carbon dots in oncology: multifunctional nanoplatforms for diagnosis, targeted therapy, and drug discovery23
An overview of cancer drugs approved through expedited approval programs and orphan medicine designation globally between 2011 and 202023
How to build a tumor: An industry perspective22
Combining DELs and machine learning for toxicology prediction22
Combining repurposed drugs to treat colorectal cancer22
Kinase signaling as a drug target modality for regulation of vascular hyperpermeability: A case for ARDS therapy development22
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