Drug Discovery Today

Article	Citations
Advancing drug repurposing research: Trends, collaborative networks, innovation and knowledge leaders	267
Repurposing of parenterally administered active substances used to treat pain both systemically and locally	241
Contents page	178
CIPDB: A biological structure databank for studying cation and π interactions	173
The potential value of 5-androstenediol in countering acute radiation syndrome	149
The recent progress of deep-learning-based in silico prediction of drug combination	142
Next-generation lung-cancer-on-a-chip: Toward personalized therapy, AI, and CRISPR-driven models	137
General aspects of powder rheology applied to pharmaceutical formulations	135
Computational modeling approaches and regulatory pathways for drug combinations	125
Antibody–drug conjugates: What drives their progress?	125
Development of JmjC-domain-containing histone demethylase (KDM2-7) inhibitors for cancer therapy	124
Targeted drug delivery to the retinal pigment epithelium: Untapped therapeutic potential for retinal diseases	115
Accelerating the orphan GPCR pipeline: GPR149 as a case study in dual-domain target validation	112
Demystifying the potential of inhibitors targeting DNA topoisomerases in unicellular protozoan parasites	103
Opportunities and challenges in drug discovery targeting the orphan receptor GPR12	103
The global status of bioequivalence trials: a comprehensive clinical trial landscape analysis based on the Trialtrove database	98
Dysbiosis versus diabesity: Pathological signaling and promising therapeutic strategies	97
Artificial-intelligence-guided autophagy modulation and nanomedicine design for precision photodynamic cancer therapy	96
Generative AI: driving productivity and scientific breakthroughs in pharmaceutical R&D	96
Gastroretentive drug delivery systems: A holy grail in oral delivery	94
On-body drug delivery systems: State-of-the-art technologies, clinical application, and future perspectives	93
Models and approaches to comprehend and address glial inflammation following spinal cord injury	90
Bridging data and drug development: Machine learning approaches for next-generation ADMET prediction	90
From promise to progress: the dynamic landscape of glioblastoma immunotherapy	80
A global bibliometric and visualized analysis of bacteria-mediated cancer therapy	79

Redox active or thiol reactive? Optimization of rapid screens to identify less evident nuisance compounds	79
Tubulin targeting agents and their implications in non-cancer disease management	76
Trends in oral small-molecule drug discovery and product development based on product launches before and after the Rule of Five	75
Exploration of small-molecule inhibitors targeting Hsp110 as novel therapeutics	74
MRI assessment of cerebral perfusion in clinical trials	73
Metabolic reprogramming: Unveiling the therapeutic potential of targeted therapies against kidney disease	72
Regulatory approvals of therapeutic biologics: continuing progress or plateauing out compared with those of small molecules?	71
The evolution of ethical and legal regulations of drug research	71
Medicinal chemistry aspects of uracil containing dUTPase inhibitors targeting colorectal cancer	70
Mutation informatics: SARS-CoV-2 receptor-binding domain of the spike protein	70
Global landscape and translational trajectories of flavonoid-based wound-healing research	69
Engineering virus-like particles for lymph-node targeted cancer immunotherapy: strategies, challenges, and future prospects	69
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 States	69
Unlocking therapeutic frontiers: harnessing artificial intelligence in drug discovery for neurodegenerative diseases	68
Recent advances towards overcoming the blood–brain barrier	68
Therapeutic strategies targeting ocular vasculopathies: Current advances and emerging challenges	68
Randomized controlled trials do not always fit the purpose: A science-based response to Venetis and Mol’s editorial on biosimilars of follitropin alfa	67
Translational PK/PD: a retrospective analysis of performance and impact from a drug portfolio	67
The emerging role of fatty acid binding protein 7 (FABP7) in cancers	66
Investigating miRNA subfamilies: Can they assist in the early diagnosis of acute myocardial infarction?	66
Systematic review and QSPR analysis of chemical penetration through the nail to inform onychomycosis candidate selection	66
A review on the recent advances of interaction studies of anticancer metal-based drugs with therapeutic targets, DNA and RNAs	65
Steps toward nebulization in-use studies to understand the stability of new biological entities	65
Gaps between medical biology and AI drug discovery	64
Caught between a ROCK and a hard place: current challenges in structure-based drug design	63
Targeted protein degradation: current molecular targets, localization, and strategies	63
Peptide cheminformatics tools: making computational tasks accessible in peptide drug discovery	62
MTHFD2: A significant mitochondrial metabolic enzyme and a novel target for anticancer therapy	61
Targeting mutant EGFR in non-small cell lung cancer in the context of cell adaptation and resistance	60
Master protocols and other innovative trial designs in inflammation and immunology to expedite clinical drug development	60
Lactose in tablets: Functionality, critical material attributes, applications, modifications and co-processed excipients	59
Embryonic and larval zebrafish models for the discovery of new bioactive compounds against tuberculosis	59
PD-L1 small-molecule modulators: A new hope in epigenetic-based multidrug cancer therapy?	59
Oral delivery of nucleic acid therapeutics: Challenges, strategies, and opportunities	59
Pathogenic TDP-43 in amyotrophic lateral sclerosis	57
Advancing pharmacogenetics research in Africa: the “Project Africa GRADIENT” initiative	57
Lipid- and polymer-based formulations containing TNF-α inhibitors for the treatment of inflammatory bowel diseases	56
Organoids in drug development: from predictive models to regulatory integration	56
Regulatory readiness to facilitate the appropriate use of innovation in clinical trials: The case of decentralized clinical trial approaches	54
Hippo signaling in acute kidney injury to chronic kidney disease transition: Current understandings and future targets	54
Self-amplifying mRNA vaccines: Mode of action, design, development and optimization	54
Overview of new indications for novel drugs approved in China between 2018 and 2024	54
Elevating life science R&D success with AI: a framework	52
Contents page	52
PolyBodies for the Treatment of Respiratory Syncytial Virus Infection	52
Cubosome-based cosmeceuticals: A breakthrough in skincare	52
Advancements and challenges in using AI for biomarker detection in early Alzheimer’s disease	51
Global or local: The future of biotech	50
Structural biology of plant-derived antibacterials: opportunities for rational lead optimization	50
Decentralised, patient-centric, site-less, virtual, and digital clinical trials? From confusion to consensus	50

Indole therapeutics: Latest FDA updates, ongoing trials, and future directions	49
CPPsite3: An updated large repository of experimentally validated cell-penetrating peptides	49
UCP1 activation: Hottest target in the thermogenesis pathway to treat obesity using molecules of synthetic and natural origin	49
Vaginal drug delivery system: A promising route of drug administration for local and systemic diseases	49
Recent insights into viral infections as a trigger and accelerator in alzheimer's disease	49
Disruptions in bioactivity driven by dose: a challenge for drug discovery	48
Sustainability by design for recombinant protein therapeutics	48
Opioid epidemic and the urge to discover new treatment options	47
Potential nanocarrier-mediated miRNA-based therapy approaches for multiple sclerosis	47
Genetic–epigenetic targets for PCOS-associated diabesity	47
Back on the scene: Advances and challenges in CD3-related drugs in tumor therapy	47
Protein exosites as drug targets: from structural topology to therapeutic modality	47
Drugs from drugs: New chemical insights into a mature concept	47
In silico resources help combat cancer drug resistance mediated by target mutations	47
Impact of HDAC inhibitors on macrophage polarization to enhance innate immunity against infections	46
An overview of progress in human metapneumovirus (hMPV) research: Structure, function, and therapeutic opportunities	46
Open innovation: A paradigm shift in pharma R&D?	46
Pharmaceutical strategies for the treatment of bacterial biofilms in chronic wounds	46
Next-generation drug conjugates for breast cancer: Clinical prospects and mechanism-based strategies to overcome resistance	46
IRE1α-mediated UPR activation in gastrointestinal cancers: Adaptive mechanisms and therapeutic potential	45
50 shades of AI in regulatory science	45
Recent advances in dual-drug co-amorphous systems	44
Review of the impact of the FDA’s Fast Track Designation on biotechnology companies’ share prices	44
Recent advances in multitarget-directed ligands via in silico drug discovery	44
Health and Medical Research in Australia II: A Golden Egg Opportunity Too Valuable to Underfund	44
Exosomal heterogeneity and functional zonation in cancer drug resistance	44
Development of LRRK2 inhibitors through computational strategies: a promising avenue for Parkinson’s disease	43
Antibiotic repurposing as alternative therapeutic strategies for cancer and Alzheimer’s disease: A solution or conundrum?	43
The role of gut microbial β-glucuronidase in drug disposition and development	43
Illuminating function of the understudied druggable kinome	43
Targeting hepatitis B virus cccDNA levels: Recent progress in seeking small molecule drug candidates	42
Metabophore-mediated retro-metabolic (‘MeMeReMe’) approach in drug design	42
The Unitary Patent and UPC – Implications for the pharmaceutical sector	42
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 trial	41
Operational and path dependencies impede the feasibility of hospital-based production of individually engineered drugs	41
Corrigendum to “Role of transient receptor potential channels in the regulation of vascular tone” [Drug Discov. Today 29(7) (2024) 104051]	41
Corrigendum to “Therapeutic potential of fucosyltransferases in cancer and recent development of targeted inhibitors” [Drug Discov. Today 28(1) (2023) 103394]	41
Innovation testbeds as enabling ecosystems driving nanopharmaceuticals to market	41
Insight into the pivotal role of signaling pathways in psoriasis pathogenesis, potential therapeutic molecules and drug delivery approaches	40
Transforming patient engagement in clinical trials: Moving from a transactional relationship to human-centered care	40
Breakthrough in RAS targeting with pan-RAS(ON) inhibitors RMC-7977 and RMC-6236	40
Geometric deep learning methods and applications in 3D structure-based drug design	40
Oncological drug discovery: AI meets structure-based computational research	40
A new era for schizophrenia drug development – Lessons for the future	40
Nanoformulations of chemotherapeutic activators of the cGAS–STING pathway in tumor chemoimmunotherapy	40
Therapeutic targeting of the complement system in ocular disease	40
Antibacterial PROTACs: the road ahead for next-generation antibiotics?	40
Does pharma R&D need a strategic reset? Adapting to a changing US landscape	39
2023 in review: FDA approvals of new medicines	39
Artificially engineered bacteria to treat gastrointestinal disease and cancer	39
Neurotrophin peptidomimetics for the treatment of neurodegenerative diseases	39
Science of, and insights into, thermodynamic principles for dermal formulations	39
Advances in lipid-based nanoformulations for inhaled antibiotic therapy in respiratory infections	38
Artificial intelligence methods in kinase target profiling: Advances and challenges	38
Strategizing the human microbiome for small molecules: Approaches and perspectives	38
The expanding repertoire of covalent warheads for drug discovery	37
Therapeutic potential of targeting IL-17 and its receptor signaling in neuroinflammation	37
Molecular medicinal insights into scaffold hopping-based drug discovery success	37
Small molecules targeting canonical transient receptor potential channels: an update	37
Approaches to advance drug discovery for neglected tropical diseases	37
Recent advances in flavonoid-based nanocarriers as an emerging drug delivery approach for cancer chemotherapy	37
How health technology assessment can help to address challenges in drug repurposing: a conceptual framework	36
Corrigendum to “Pharmacological modulation of autophagy for epilepsy therapy: Opportunities and obstacles” [Drug Discov. Today 28(6) (2023) 103600]	36
The importance of a go-to-market strategy in the commercialisation of cellular immunotherapies	36
PROTAC technology: A new drug design for chemical biology with many challenges in drug discovery	36
Harnessing G-quadruplex ligands for lung cancer treatment: A comprehensive overview	36
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]	36
Druggable genome special issue: An introduction	35
Contents page	35
Small molecule inhibitors of the co-receptor neuropilin-1	35
Harnessing personalized tailored medicines to digital-based data-enriched edible pharmaceuticals	35
Advancing ocular gene therapy: a machine learning approach to enhance delivery, uptake and gene expression	35
A pipeline analysis of advanced therapy medicinal products	34
Advances in antibody-based strategies for targeting cancer-associated glycopeptide antigens	34
LYTACs and other extracellular targeted protein degradation TACnologies: guiding principles and potential clinical prospects	34
Piezo1 as a therapeutic target in kidney disease: emerging mechanistic insights and translational potential	34
Blocking platelet glycoprotein VI (GPVI) as a promising antithrombotic treatment	34
Peptide-derived ligands for the discovery of safer opioid analgesics	34
Expanding therapeutic potential of Bdellovibrio bacteriovorus against multidrug-resistant pathogens	33
Digital twins for accelerating drug discovery and development: opportunities and challenges	33

Targeting autophagy in colorectal cancer: An update on pharmacological small-molecule compounds	33
Toward generalizable predictive models for DNA-encoded libraries	33
Death ligand receptor (DLR) signaling: Its non-apoptotic functions in cancer and the consequences of DLR-directed therapies	33
Predictive value of the hERG assay for anticipating the arrhythmogenic potential of new drugs	33
A retrospective regulatory analysis of FDA recalls carried out by pharmaceutical companies from 2012 to 2023	32
Deadly interactions: Synergistic manipulations of concurrent pathogen infections potentially enabling future pandemics	32
Nanomedicine approaches to reduce cytokine storms in severe infections	32
A statewide multi-institutional model that de-risks academic drug discovery	32
‘Home inspections’ for life sciences companies going public before clinical proof-of-concept	32
Publisher’s Note	32
Early career researchers’ experiences in drug discovery in Africa	32
Surface-enhanced Raman scattering biosensors for detection of oncomiRs in breast cancer	32
Machine learning and natural language processing in clinical trial eligibility criteria parsing: a scoping review	31
TDP-43 protein interactome informs about perturbed canonical pathways and may help develop personalized medicine approaches for patients with TDP-43 pathology	31
Competition of regulatory ecosystems in approving medicines: policy implications in the case of Europe	31
Recent progress in covalent organic frameworks for cancer therapy	30
Opportunities and challenges of physiologically based pharmacokinetic modeling in drug delivery	30
Chiral-engineered supraparticles: Emerging tools for drug delivery	30
ADAM10: Function insights, disease implications, and promise of therapeutic targeting	30
Physics-inspired explainable AI for mechanistic and decision support in drug discovery	29
Effectiveness of histamine receptor antagonists in the treatment of histamine-driven clinical symptoms: do we have a histamine or, better, an anti-histamine problem?	29
Nanophotonic waveguide-based sensing of circulating cell-free mitochondrial DNA: implications for personalized medicine	29
Lysine lactylation: Regulatory mechanisms, role in health and disease, and its therapeutic potential	29
Recent discoveries of the role of histone modifications and related inhibitors in pathological cardiac hypertrophy	29
IdopNetwork as a genomic predictor of drug response	29
COVID-19 therapeutics: Small-molecule drug development targeting SARS-CoV-2 main protease	29
Antimicrobial and anti-biofilm activities of bio-inspired nanomaterials for wound healing applications	29
Drugging the entire human proteome: Are we there yet?	29
Targeting SIRT1-regulated autophagic cell death as a novel therapeutic avenue for cancer prevention	28
Patents, trade secrets and pricing	28
Optical tweezers for drug discovery	28
Exosome-mediated PROTAC delivery for treatment of RNA viral infections and zoonosis	28
Generic dry powder inhalers bioequivalence: Batch–to-batch variability insights	28
Sustaining pharmaceutical innovation after the Inflation Reduction Act: trends in R&D spending, equity investment, and business development	28
Orphan GPR52 as an emerging neurotherapeutic target	28
Translating precision medicine for autism spectrum disorder: A pressing need	28
Biopharmaceutical R&D outsourcing: Short-term gain for long-term pain?	28
Trends, challenges, and success factors in pharmaceutical portfolio management: Cognitive biases in decision-making and their mitigating measures	27
2025 In Review: Trends in Pharmaceutical Innovation	27
Electrospun proliposomes and the quest to overcome liposome instability	27
Therapeutic potential of fucosyltransferases in cancer and recent development of targeted inhibitors	27
Non-oncology orphan drug development: Productivity and probability of success	27
Methionine biosynthesis as a key metabolic pathway for antimicrobial drug discovery in Streptococcus mutans	27
Novel and investigational therapies for wet and dry age-related macular degeneration	27
A personalized pharmaco-epistatic network model of precision medicine	27
Targeting farnesyltransferase for cancer therapy and beyond	27
Evaluation of the implementation effectiveness of accelerated drug marketing registration procedures in China: lessons from the 2016–2024 regulatory review	27
Shining light on liquid–liquid phase separation in chronic liver disease	27
A review of the efficacy of prostate cancer therapies against castration-resistant prostate cancer	27
Recent trends in targeted delivery of smart nanocarrier-based microbial enzymes for therapeutic applications	26
Therapies for Inherited Retinal Dystrophies: What is Enough?	26
Benefits of hybrid QM/MM over traditional classical mechanics in pharmaceutical systems	26
Peptide modulators of cell migration: Overview, applications and future development	26
Comparative analysis of FDA approvals by top 20 pharma companies (2014–2023)	26
Differential immunogenicity of biosimilar monoclonal antibodies: overrated and overemphasized?	26
Humanized liver mouse models in preclinical drug development: current status, translation challenges and emerging technologies	26
ATP-binding cassette efflux transporters and MDR in cancer	26
Recent advances in the molecular design and applications of viral RNA-targeting antiviral modalities	26
Active pharmaceutical ingredients (APIs) in ionic liquids: An effective approach for API physiochemical parameter optimization	26
Concepts and applications of chemical fingerprint for hit and lead screening	25
Rational discovery of molecular glue degraders based on block chemistry	25
Contents page	25
Prospects of halofuginone as an antiprotozoal drug scaffold	25
Beyond CL and VSS: A comprehensive approach to human pharmacokinetic predictions	25
Epigenetic roles of lysine-specific demethylase 1 (LSD1) in cancer metabolism	25
SET7, a lysine-specific methyl transferase: An intriguing epigenetic target to combat diabetic nephropathy	25
Clinical significance and potential role of trimethylamine N-oxide in neurological and neuropsychiatric disorders	25
Commercialization of cell and gene therapy in Canada: Current landscape, challenges and opportunities	25
Contents page	25
Nanosponges: An overlooked promising strategy to combat SARS-CoV-2	25
Which cryptic sites are feasible drug targets?	25
Advantages, progress, and future trends in oral medicated jellies/gels: Focus on adherence aspects	24
Statins and angiogenesis in non-cardiovascular diseases	24
How missing value imputation is confounded with batch effects and what you can do about it	24
Treating liver cancer through arginine depletion	24
Rapid progress in neuroimaging technologies fuels central nervous system translational medicine	24
How can MSI enhance our understanding of ASO distribution?	24
DDR1-targeted therapies: current limitations and future potential	24
The role of venom proteomics and single-domain antibodies for antivenoms: Progress in snake envenoming treatment	24
Dual-action potential of cationic cryptides against infections and cancers	24
Informatic challenges and advances in illuminating the druggable proteome	24
Pivotal role of nitrogen heterocycles in Alzheimer’s disease drug discovery	24
An emerging MSC-exosome delivery strategy: injectable temperature-sensitive hydrogels encapsulate exosomes for enhanced therapeutic efficacy	23
Evolution of the division of labor for First-in-Class Drugs: A Quantitative Analysis of Trends across Company Types, Modalities, and Therapeutic Areas (2012–2024)	23
Circadian disruption in hepatocellular carcinoma: Current findings and future directions of molecular mechanisms	23
Aceclofenac and methotrexate combination therapy could influence Th1/Th17 axis to modulate rheumatoid-arthritis-induced inflammation	23
Metallocompounds as anticancer agents against osteosarcoma	23
New approaches for challenging therapeutic targets	23
Brain-derived neurotrophic factor (BDNF) in perinatal depression: Side show or pivotal factor?	23
The Wnt signaling cascade: a potential but untapped therapeutic target for monkeypox infection	22
Tracing drugs from discovery to disposal	22
Unleashing the power of generative AI in drug discovery	22
Drug repurposing against SARS-CoV-2 using computational approaches	22
All-in-one nanotheranostic platform based on tumor microenvironment: new strategies in multimodal imaging and therapeutic protocol	22
Therapeutic potential of acetyl-DL-leucine and its L-enantiomer in posterior fossa syndrome: Mechanistic insights	22