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Record W4407140906 · doi:10.1186/s13321-025-00962-0

Improving drug repositioning with negative data labeling using large language models

2025· article· en· W4407140906 on OpenAlex

Why this work is in the frame

A frame that forgets how it found something cannot be audited. These are the routes that admitted this work.

affAt least one author lists a Canadian institution in the pinned OpenAlex snapshot.

Bibliographic record

VenueJournal of Cheminformatics · 2025
Typearticle
Languageen
FieldComputer Science
TopicComputational Drug Discovery Methods
Canadian institutionsUniversité Laval
Fundersnot available
KeywordsComputer scienceDrug repositioningDrugData miningNatural language processingData scienceMedicinePharmacology

Abstract

fetched live from OpenAlex

INTRODUCTION: Drug repositioning offers numerous advantages, such as faster development timelines, reduced costs, and lower failure rates in drug development. Supervised machine learning is commonly used to score drug candidates but is hindered by the lack of reliable negative data-drugs that fail due to inefficacy or toxicity- which is difficult to access, lowering their prediction accuracy and generalization. Positive-Unlabeled (PU) learning has been used to overcome this issue by either randomly sampling unlabeled drugs or identifying probable negatives but still suffers from misclassification or oversimplified decision boundaries. RESULTS: We proposed a novel strategy using Large Language Models (GPT-4) to analyze all clinical trials on prostate cancer and systematically identify true negatives. This approach showed remarkable improvement in predictive accuracy on independent test sets with a Matthews Correlation Coefficient of 0.76 (± 0.33) compared to 0.55 (± 0.15) and 0.48 (± 0.18) for two commonly used PU learning approaches. Using our labeling strategy, we created a training set of 26 positive and 54 experimentally validated negative drugs. We then applied a machine learning ensemble to this new dataset to assess the repurposing potential of the remaining 11,043 drugs in the DrugBank database. This analysis identified 980 potential candidates for prostate cancer. A detailed review of the top 30 revealed 9 promising drugs targeting various mechanisms such as genomic instability, p53 regulation, or TMPRSS2-ERG fusion. CONCLUSION: By expanding our negative data labeling approach to all diseases within the ClinicalTrials.gov database, our method could greatly advance supervised drug repositioning, offering a more accurate and data-driven path for discovering new treatments.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.001
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Simulation or modeling · Consensus signal: Simulation or modeling
GenreCandidate signal: Methods · Consensus signal: Methods
Teacher disagreement score0.187
Threshold uncertainty score0.368

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0010.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.003
Open science0.0010.001
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.025
GPT teacher head0.320
Teacher spread0.295 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it