Recent studies showed that the likelihood of drug approval can be predicted with clinical data and structure information of drug using computational approaches. Predicting the likelihood of drug approval can be innovative and of high impact. However, models that leverage clinical data are applicable only in clinical stages, which is not very practical. Prioritizing drug candidates and early-stage decision-making in the de novo drug development process is crucial in pharmaceutical research to optimize resource allocation. For early-stage decision-making, we need a computational model that uses only chemical structures. This seemingly impossible task may utilize the predictive power with multi-modal features including clinical data. In this work, we introduce ChemAP (Chemical structure-based drug Approval Predictor), a novel deep learning scheme for drug approval prediction in the early-stage drug discovery phase. ChemAP aims to enhance the possibility of early-stage decision-making by enriching semantic knowledge to fill in the gap between multi-modal and single-modal chemical spaces through knowledge distillation techniques. This approach facilitates the effective construction of chemical space solely from chemical structure data, guided by multi-modal knowledge related to efficacy, such as clinical trials and patents of drugs. In this study, ChemAP achieved state-of-the-art performance, outperforming both traditional machine learning and deep learning models in drug approval prediction, with AUROC and AUPRC scores of 0.782 and 0.842 respectively on the drug approval benchmark dataset. Additionally, we demonstrated its generalizability by outperforming baseline models on a recent external dataset, which included drugs from the 2023 FDA-approved list and the 2024 clinical trial failure drug list, achieving AUROC and AUPRC scores of 0.694 and 0.851. These results demonstrate that ChemAP is an effective method in predicting drug approval only with chemical structure information of drug so that decision-making can be done at the early stages of drug development process. To the best of our knowledge, our work is the first of its kind to show that prediction of drug approval is possible only with structure information of drug by defining the chemical space of approved and unapproved drugs using deep learning technology.
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http://dx.doi.org/10.1038/s41598-024-72868-0 | DOI Listing |
Clin Kidney J
January 2025
Department of General Internal Medicine and Nephrology, Robert Bosch Hospital Stuttgart, Stuttgart, Germany.
Background: Sparsentan, a dual-acting antagonist for both the angiotensin II receptor type 1 and the endothelin receptor type A, has emerged as a promising therapeutic agent for the treatment of IgA nephropathy (IgAN). Following the publication of the PROTECT trial, sparsentan recently received approval for the treatment of IgAN in Europe. However, it remains uncertain whether an additive effect can be observed in the context of existing treatment with sodium-glucose co-transporter 2 (SGLT2) inhibitors, given that the PROTECT study did not investigate this dual therapy approach.
View Article and Find Full Text PDFCureus
December 2024
Graduate Studies and Research Division at the Faculty of Dentistry, National Autonomous University of Mexico, Mexico City, MEX.
Introduction Dry eye and hyposalivation, often linked to Sjögren's syndrome (SS), are prevalent among adults. However, systemic diseases and their associated medications also play a role, as drug interactions can intensify the effects of certain medications. Objective To assess whether polypharmacy is associated with the co-occurrence of aqueous-deficient dry eye (ADDE) and hyposalivation in adults aged 50 years and older without SS.
View Article and Find Full Text PDFEur Cardiol
December 2024
Department of Respiratory Medicine, King George's Medical University Lucknow, Uttar Pradesh, India.
Pulmonary arterial hypertension (PAH) is a long-term condition characterised by increased resistance to blood flow in the pulmonary circulation. The disease has a progressive course and is associated with a poor prognosis. Without treatment, PAH is associated with mortality in <3 years.
View Article and Find Full Text PDFActa Neuropathol Commun
January 2025
Department of Neuroscience, Istituto di Ricerche Farmacologiche Mario Negri IRCCS, Via Mario Negri 2, 20156, Milan, Italy.
Deposition of abnormally phosphorylated tau aggregates is a central event leading to neuronal dysfunction and death in Alzheimer's disease (AD) and other tauopathies. Among tau aggregates, oligomers (TauOs) are considered the most toxic. AD brains show significant increase in TauOs compared to healthy controls, their concentration correlating with the severity of cognitive deficits and disease progression.
View Article and Find Full Text PDFCancer Imaging
January 2025
Department of Nuclear Medicine, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Hongkou District, No. 100, Haining Road, Shanghai, 200080, China.
Background: Programmed cell death 1/programmed death ligand-1 (PD-L1)-based immune checkpoint blockade is an effective treatment approach for non-small-cell lung cancer (NSCLC). However, immunohistochemistry does not accurately or dynamically reflect PD-L1 expression owing to its spatiotemporal heterogeneity. Herein, we assessed the feasibility of using a Ga-labeled anti-PD-L1 nanobody, Ga-NODAGA-NM-01, for PET imaging of PD-L1.
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