Drug Discovery Today

Article	Citations
Repurposing of parenterally administered active substances used to treat pain both systemically and locally	293
Contents page	257
CIPDB: A biological structure databank for studying cation and π interactions	196
The potential value of 5-androstenediol in countering acute radiation syndrome	163
The recent progress of deep-learning-based in silico prediction of drug combination	146
Demystifying the potential of inhibitors targeting DNA topoisomerases in unicellular protozoan parasites	146
Antibody–drug conjugates: What drives their progress?	142
A global bibliometric and visualized analysis of bacteria-mediated cancer therapy	141
Models and approaches to comprehend and address glial inflammation following spinal cord injury	133
Tubulin targeting agents and their implications in non-cancer disease management	124
Artificial-intelligence-guided autophagy modulation and nanomedicine design for precision photodynamic cancer therapy	108
Accelerating the orphan GPCR pipeline: GPR149 as a case study in dual-domain target validation	108
The global status of bioequivalence trials: a comprehensive clinical trial landscape analysis based on the Trialtrove database	107
On-body drug delivery systems: State-of-the-art technologies, clinical application, and future perspectives	106
General aspects of powder rheology applied to pharmaceutical formulations	105
Advancing drug repurposing research: Trends, collaborative networks, innovation and knowledge leaders	102
Dysbiosis versus diabesity: Pathological signaling and promising therapeutic strategies	99
Next-generation lung-cancer-on-a-chip: Toward personalized therapy, AI, and CRISPR-driven models	98
Development of JmjC-domain-containing histone demethylase (KDM2-7) inhibitors for cancer therapy	97
Opportunities and challenges in drug discovery targeting the orphan receptor GPR12	95
Gastroretentive drug delivery systems: A holy grail in oral delivery	90
Generative AI: driving productivity and scientific breakthroughs in pharmaceutical R&D	84
Computational modeling approaches and regulatory pathways for drug combinations	83
From promise to progress: the dynamic landscape of glioblastoma immunotherapy	82
Targeted drug delivery to the retinal pigment epithelium: Untapped therapeutic potential for retinal diseases	82

Trends in oral small-molecule drug discovery and product development based on product launches before and after the Rule of Five	79
Exploration of small-molecule inhibitors targeting Hsp110 as novel therapeutics	79
Bridging data and drug development: Machine learning approaches for next-generation ADMET prediction	79
MRI assessment of cerebral perfusion in clinical trials	78
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	77
Randomized controlled trials do not always fit the purpose: A science-based response to Venetis and Mol’s editorial on biosimilars of follitropin alfa	75
Investigating miRNA subfamilies: Can they assist in the early diagnosis of acute myocardial infarction?	75
Systematic review and QSPR analysis of chemical penetration through the nail to inform onychomycosis candidate selection	74
Master protocols and other innovative trial designs in inflammation and immunology to expedite clinical drug development	73
Engineering virus-like particles for lymph-node targeted cancer immunotherapy: strategies, challenges, and future prospects	73
The evolution of ethical and legal regulations of drug research	73
Gaps between medical biology and AI drug discovery	72
Mutation informatics: SARS-CoV-2 receptor-binding domain of the spike protein	72
Embryonic and larval zebrafish models for the discovery of new bioactive compounds against tuberculosis	69
Unlocking therapeutic frontiers: harnessing artificial intelligence in drug discovery for neurodegenerative diseases	69
Translational PK/PD: a retrospective analysis of performance and impact from a drug portfolio	68
MTHFD2: A significant mitochondrial metabolic enzyme and a novel target for anticancer therapy	68
Global landscape and translational trajectories of flavonoid-based wound-healing research	67
Recent advances towards overcoming the blood–brain barrier	66
Steps toward nebulization in-use studies to understand the stability of new biological entities	65
Caught between a ROCK and a hard place: current challenges in structure-based drug design	65
Estimating the global inventory of deprioritized clinical-stage drug development programs: Toward a market for shelved assets	65
A review on the recent advances of interaction studies of anticancer metal-based drugs with therapeutic targets, DNA and RNAs	64
Advancing pharmacogenetics research in Africa: the “Project Africa GRADIENT” initiative	63
Pathogenic TDP-43 in amyotrophic lateral sclerosis	61
Metabolic reprogramming: Unveiling the therapeutic potential of targeted therapies against kidney disease	61
PD-L1 small-molecule modulators: A new hope in epigenetic-based multidrug cancer therapy?	61
Lipid- and polymer-based formulations containing TNF-α inhibitors for the treatment of inflammatory bowel diseases	61
Targeting mutant EGFR in non-small cell lung cancer in the context of cell adaptation and resistance	59
Regulatory approvals of therapeutic biologics: continuing progress or plateauing out compared with those of small molecules?	59
The emerging role of fatty acid binding protein 7 (FABP7) in cancers	58
Targeted protein degradation: current molecular targets, localization, and strategies	58
Medicinal chemistry aspects of uracil containing dUTPase inhibitors targeting colorectal cancer	58
Lactose in tablets: Functionality, critical material attributes, applications, modifications and co-processed excipients	57
Therapeutic strategies targeting ocular vasculopathies: Current advances and emerging challenges	57
Organoids in drug development: from predictive models to regulatory integration	56
Peptide cheminformatics tools: making computational tasks accessible in peptide drug discovery	55
Targeting ADAM15 in cancer: from dual-faced biology to emerging therapies	55
Recent advances in multitarget-directed ligands via in silico drug discovery	54
Oral delivery of nucleic acid therapeutics: Challenges, strategies, and opportunities	54
An overview of progress in human metapneumovirus (hMPV) research: Structure, function, and therapeutic opportunities	54
Indole therapeutics: Latest FDA updates, ongoing trials, and future directions	53
Next-generation drug conjugates for breast cancer: Clinical prospects and mechanism-based strategies to overcome resistance	53
Cubosome-based cosmeceuticals: A breakthrough in skincare	52
Regulatory readiness to facilitate the appropriate use of innovation in clinical trials: The case of decentralized clinical trial approaches	52
Pharmaceutical strategies for the treatment of bacterial biofilms in chronic wounds	52
Decentralised, patient-centric, site-less, virtual, and digital clinical trials? From confusion to consensus	51
Illuminating function of the understudied druggable kinome	51
Advancements and challenges in using AI for biomarker detection in early Alzheimer’s disease	51
Hippo signaling in acute kidney injury to chronic kidney disease transition: Current understandings and future targets	50

Contents page	50
Disruptions in bioactivity driven by dose: a challenge for drug discovery	49
PolyBodies for the Treatment of Respiratory Syncytial Virus Infection	49
Overview of new indications for novel drugs approved in China between 2018 and 2024	49
Sustainability by design for recombinant protein therapeutics	49
Elevating life science R&D success with AI: a framework	49
Development of LRRK2 inhibitors through computational strategies: a promising avenue for Parkinson’s disease	49
Recent insights into viral infections as a trigger and accelerator in alzheimer's disease	49
In silico resources help combat cancer drug resistance mediated by target mutations	48
Review of the impact of the FDA’s Fast Track Designation on biotechnology companies’ share prices	48
50 shades of AI in regulatory science	48
Opioid epidemic and the urge to discover new treatment options	48
Potential nanocarrier-mediated miRNA-based therapy approaches for multiple sclerosis	48
Back on the scene: Advances and challenges in CD3-related drugs in tumor therapy	48
IRE1α-mediated UPR activation in gastrointestinal cancers: Adaptive mechanisms and therapeutic potential	48
UCP1 activation: Hottest target in the thermogenesis pathway to treat obesity using molecules of synthetic and natural origin	47
Open innovation: A paradigm shift in pharma R&D?	47
Health and Medical Research in Australia II: A Golden Egg Opportunity Too Valuable to Underfund	47
Exosomal heterogeneity and functional zonation in cancer drug resistance	46
Vaginal drug delivery system: A promising route of drug administration for local and systemic diseases	45
Impact of HDAC inhibitors on macrophage polarization to enhance innate immunity against infections	45
Drugs from drugs: New chemical insights into a mature concept	45
Protein exosites as drug targets: from structural topology to therapeutic modality	44
Structural biology of plant-derived antibacterials: opportunities for rational lead optimization	44
Genetic–epigenetic targets for PCOS-associated diabesity	43
CPPsite3: An updated large repository of experimentally validated cell-penetrating peptides	43
Self-amplifying mRNA vaccines: Mode of action, design, development and optimization	43
Targeting hepatitis B virus cccDNA levels: Recent progress in seeking small molecule drug candidates	42
The role of gut microbial β-glucuronidase in drug disposition and development	42
Recent advances in dual-drug co-amorphous systems	42
Global or local: The future of biotech	42
The Unitary Patent and UPC – Implications for the pharmaceutical sector	41
Innovation testbeds as enabling ecosystems driving nanopharmaceuticals to market	41
Antibiotic repurposing as alternative therapeutic strategies for cancer and Alzheimer’s disease: A solution or conundrum?	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
Small molecules targeting canonical transient receptor potential channels: an update	41
Operational and path dependencies impede the feasibility of hospital-based production of individually engineered drugs	41
Nanoformulations of chemotherapeutic activators of the cGAS–STING pathway in tumor chemoimmunotherapy	41
Antibacterial PROTACs: the road ahead for next-generation antibiotics?	41
Metabophore-mediated retro-metabolic (‘MeMeReMe’) approach in drug design	40
Does pharma R&D need a strategic reset? Adapting to a changing US landscape	40
Strategizing the human microbiome for small molecules: Approaches and perspectives	40
2023 in review: FDA approvals of new medicines	40
Geometric deep learning methods and applications in 3D structure-based drug design	40
Advances in lipid-based nanoformulations for inhaled antibiotic therapy in respiratory infections	40
Approaches to advance drug discovery for neglected tropical diseases	40
Artificially engineered bacteria to treat gastrointestinal disease and cancer	40
A new era for schizophrenia drug development – Lessons for the future	40
Therapeutic targeting of the complement system in ocular disease	39
Neurotrophin peptidomimetics for the treatment of neurodegenerative diseases	39
Therapeutic potential of targeting IL-17 and its receptor signaling in neuroinflammation	39
Artificial intelligence methods in kinase target profiling: Advances and challenges	39
Insight into the pivotal role of signaling pathways in psoriasis pathogenesis, potential therapeutic molecules and drug delivery approaches	38
The expanding repertoire of covalent warheads for drug discovery	37
PROTAC technology: A new drug design for chemical biology with many challenges in drug discovery	37
Recent advances in flavonoid-based nanocarriers as an emerging drug delivery approach for cancer chemotherapy	37
Science of, and insights into, thermodynamic principles for dermal formulations	37
Breakthrough in RAS targeting with pan-RAS(ON) inhibitors RMC-7977 and RMC-6236	37
Protein–ligand interactions by QCM: challenges and resolutions	37
Corrigendum to “Pharmacological modulation of autophagy for epilepsy therapy: Opportunities and obstacles” [Drug Discov. Today 28(6) (2023) 103600]	36
Transforming patient engagement in clinical trials: Moving from a transactional relationship to human-centered care	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
Molecular medicinal insights into scaffold hopping-based drug discovery success	36
Druggable genome special issue: An introduction	35
Death ligand receptor (DLR) signaling: Its non-apoptotic functions in cancer and the consequences of DLR-directed therapies	35
Advancing ocular gene therapy: a machine learning approach to enhance delivery, uptake and gene expression	35
Harnessing G-quadruplex ligands for lung cancer treatment: A comprehensive overview	35
Contents page	35
The importance of a go-to-market strategy in the commercialisation of cellular immunotherapies	35
Blocking platelet glycoprotein VI (GPVI) as a promising antithrombotic treatment	35
Small molecule inhibitors of the co-receptor neuropilin-1	34
Expanding therapeutic potential of Bdellovibrio bacteriovorus against multidrug-resistant pathogens	34
Harnessing personalized tailored medicines to digital-based data-enriched edible pharmaceuticals	34
Piezo1 as a therapeutic target in kidney disease: emerging mechanistic insights and translational potential	34
Targeting autophagy in colorectal cancer: An update on pharmacological small-molecule compounds	34
From trial-and-error to inverse design: how AI is redefining drug delivery systems	33
A pipeline analysis of advanced therapy medicinal products	33
Predictive value of the hERG assay for anticipating the arrhythmogenic potential of new drugs	33
A statewide multi-institutional model that de-risks academic drug discovery	33

How health technology assessment can help to address challenges in drug repurposing: a conceptual framework	33
Toward generalizable predictive models for DNA-encoded libraries	33
A retrospective regulatory analysis of FDA recalls carried out by pharmaceutical companies from 2012 to 2023	33
Digital twins for accelerating drug discovery and development: opportunities and challenges	32
Single-cell and spatial transcriptomic insights into fibrotic mechanisms and therapeutic opportunities	32
Advances in antibody-based strategies for targeting cancer-associated glycopeptide antigens	32
‘Home inspections’ for life sciences companies going public before clinical proof-of-concept	32
Peptide-derived ligands for the discovery of safer opioid analgesics	32
LYTACs and other extracellular targeted protein degradation TACnologies: guiding principles and potential clinical prospects	32
Early career researchers’ experiences in drug discovery in Africa	31
Competition of regulatory ecosystems in approving medicines: policy implications in the case of Europe	31
Publisher’s Note	31
Surface-enhanced Raman scattering biosensors for detection of oncomiRs in breast cancer	31
Deadly interactions: Synergistic manipulations of concurrent pathogen infections potentially enabling future pandemics	31
Chiral-engineered supraparticles: Emerging tools for drug delivery	31
Translating precision medicine for autism spectrum disorder: A pressing need	30
Nanomedicine approaches to reduce cytokine storms in severe infections	30
Nanophotonic waveguide-based sensing of circulating cell-free mitochondrial DNA: implications for personalized medicine	30
COVID-19 therapeutics: Small-molecule drug development targeting SARS-CoV-2 main protease	30
Targeting SIRT1-regulated autophagic cell death as a novel therapeutic avenue for cancer prevention	30
Recent discoveries of the role of histone modifications and related inhibitors in pathological cardiac hypertrophy	30
Drugging the entire human proteome: Are we there yet?	30
Orphan GPR52 as an emerging neurotherapeutic target	29
Machine learning and natural language processing in clinical trial eligibility criteria parsing: a scoping review	29
Antimicrobial and anti-biofilm activities of bio-inspired nanomaterials for wound healing applications	29
ADAM10: Function insights, disease implications, and promise of therapeutic targeting	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
TDP-43 protein interactome informs about perturbed canonical pathways and may help develop personalized medicine approaches for patients with TDP-43 pathology	29
Physics-inspired explainable AI for mechanistic and decision support in drug discovery	29
Interplay between RNA m6A modification and transglutaminase 2 inhibitor effects on mitophagy dysfunction in Alzheimer’s disease	29
Opportunities and challenges of physiologically based pharmacokinetic modeling in drug delivery	29
Lysine lactylation: Regulatory mechanisms, role in health and disease, and its therapeutic potential	29
IdopNetwork as a genomic predictor of drug response	29
Recent progress in covalent organic frameworks for cancer therapy	28
2025 In Review: Trends in Pharmaceutical Innovation	28
Sustaining pharmaceutical innovation after the Inflation Reduction Act: trends in R&D spending, equity investment, and business development	28
Shining light on liquid–liquid phase separation in chronic liver disease	28
Exosome-mediated PROTAC delivery for treatment of RNA viral infections and zoonosis	28
Evaluation of the implementation effectiveness of accelerated drug marketing registration procedures in China: lessons from the 2016–2024 regulatory review	28
Generic dry powder inhalers bioequivalence: Batch–to-batch variability insights	28
Peptide modulators of cell migration: Overview, applications and future development	27
Comparative analysis of FDA approvals by top 20 pharma companies (2014–2023)	27
Beyond CL and VSS: A comprehensive approach to human pharmacokinetic predictions	27
Therapies for Inherited Retinal Dystrophies: What is Enough?	27
Targeting farnesyltransferase for cancer therapy and beyond	27
Differential immunogenicity of biosimilar monoclonal antibodies: overrated and overemphasized?	27
Trends, challenges, and success factors in pharmaceutical portfolio management: Cognitive biases in decision-making and their mitigating measures	27
Humanized liver mouse models in preclinical drug development: current status, translation challenges and emerging technologies	26
Novel and investigational therapies for wet and dry age-related macular degeneration	26
Biopharmaceutical R&D outsourcing: Short-term gain for long-term pain?	26
Rational discovery of molecular glue degraders based on block chemistry	26
A review of the efficacy of prostate cancer therapies against castration-resistant prostate cancer	25
Methionine biosynthesis as a key metabolic pathway for antimicrobial drug discovery in Streptococcus mutans	25
Recent trends in targeted delivery of smart nanocarrier-based microbial enzymes for therapeutic applications	25
ATP-binding cassette efflux transporters and MDR in cancer	25
Therapeutic potential of fucosyltransferases in cancer and recent development of targeted inhibitors	25
Prospects of halofuginone as an antiprotozoal drug scaffold	25
Benefits of hybrid QM/MM over traditional classical mechanics in pharmaceutical systems	25
Concepts and applications of chemical fingerprint for hit and lead screening	25
Recent advances in the molecular design and applications of viral RNA-targeting antiviral modalities	25
A personalized pharmaco-epistatic network model of precision medicine	25
Non-oncology orphan drug development: Productivity and probability of success	25
Which cryptic sites are feasible drug targets?	24
Active pharmaceutical ingredients (APIs) in ionic liquids: An effective approach for API physiochemical parameter optimization	24
Covalent ligand efficiency	24
Clinical significance and potential role of trimethylamine N-oxide in neurological and neuropsychiatric disorders	24
Electrospun proliposomes and the quest to overcome liposome instability	24
Grasping cryptic binding sites to neutralize drug resistance in the field of anticancer	24
Optical tweezers for drug discovery	24
On the pivotal role of drug discovery in sustainable EU pharma reform	24
Nanosponges: An overlooked promising strategy to combat SARS-CoV-2	24
How missing value imputation is confounded with batch effects and what you can do about it	23
SET7, a lysine-specific methyl transferase: An intriguing epigenetic target to combat diabetic nephropathy	23
Rapid progress in neuroimaging technologies fuels central nervous system translational medicine	23
Informatic challenges and advances in illuminating the druggable proteome	23
Pivotal role of nitrogen heterocycles in Alzheimer’s disease drug discovery	23
Contents page	23
Dual-action potential of cationic cryptides against infections and cancers	23
Treating liver cancer through arginine depletion	23
The role of venom proteomics and single-domain antibodies for antivenoms: Progress in snake envenoming treatment	23
Statins and angiogenesis in non-cardiovascular diseases	23
Aceclofenac and methotrexate combination therapy could influence Th1/Th17 axis to modulate rheumatoid-arthritis-induced inflammation	23
Advantages, progress, and future trends in oral medicated jellies/gels: Focus on adherence aspects	23
How can MSI enhance our understanding of ASO distribution?	23
Metallocompounds as anticancer agents against osteosarcoma	22
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)	22
Epigenetic roles of lysine-specific demethylase 1 (LSD1) in cancer metabolism	22
DDR1-targeted therapies: current limitations and future potential	22
Circadian disruption in hepatocellular carcinoma: Current findings and future directions of molecular mechanisms	22
Artificial protein scaffolds for human therapeutics: drug discovery and delivery strategies	22
An emerging MSC-exosome delivery strategy: injectable temperature-sensitive hydrogels encapsulate exosomes for enhanced therapeutic efficacy	22
Brain-derived neurotrophic factor (BDNF) in perinatal depression: Side show or pivotal factor?	22
New approaches for challenging therapeutic targets	22
Carbon dots in oncology: multifunctional nanoplatforms for diagnosis, targeted therapy, and drug discovery	22
Commercialization of cell and gene therapy in Canada: Current landscape, challenges and opportunities	22