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4d
ImesAgCl/TBHP Promoted Aqueous Synthesis of Isatin-Amide Derivatives: Anti-proliferative, Anti-Vascular Endothelial Growth Factor Receptor 2, Bioavailability and Molecular Docking Studies. (PubMed, Chem Biodivers)
Few FDA approved drugs (such as Sorafenib, Sunitinib, Nintedanib and Cabotanzinib), which target VEGFRs, however, a significant issue with the monotherapy of these agents is drug resistance. Finally, in silico molecular docking studies on VEGFR-2 (PDB ID 3VHE) revealed that compounds 5d, 5j, and 5q showed encouraging inhibition constants (68.5-154.92 nM) and binding energies (-9.29 to -9.77 kcal/mol) compared to Sunitinib (inhibition constant = 248.72 nM) and binding energy = -9.01 kcal/mol). Specifically, compounds 5d and 5j established an H-bond with the ASP1046 residue, similar to the standard drug Sunitinib.
Journal
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KDR (Kinase insert domain receptor)
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sorafenib • sunitinib • nintedanib
5d
The emerging role of pancreatic exocrine fibrosis as a common aetiological driver of islet dysfunction and diabetes: opportunities for novel disease-modifying interventions. (PubMed, Diabetologia)
The antifibrotic agents pirfenidone and nintedanib, thought to work primarily through suppression of TGF-β function, are used routinely in clinical practice for non-pancreatic indications, with a first trial in pancreatitis underway. Trials evaluating these licensed therapeutics that include primary diabetes-related endpoints and measures aiming to elucidate the underlying mechanisms of action merit consideration in type 3c diabetes and ultimately in type 2 diabetes and in combinatorial regimens in type 1 diabetes.
Review • Journal
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TGFB1 (Transforming Growth Factor Beta 1)
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nintedanib
6d
Management of Progressive Disease in Idiopathic Pulmonary Fibrosis (clinicaltrials.gov)
P4, N=279, Completed, Hospices Civils de Lyon | Recruiting --> Completed
Trial completion
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nintedanib
8d
RNA-Seq Analysis of Nintedanib Effects on Interstitial Pneumonia in Preoperative NSCLC Patients. (PubMed, Respir Med)
xCell2 analysis indicated reduced plasma cells and increased smooth muscle, muscle, adipocyte, and endothelial cells, suggesting normalization of tissue remodeling. Nintedanib appears to exert anti-inflammatory effects and promote tissue repair in non-tumor lung, while facilitating tissue remodeling in fibrotic areas, indicating potential benefits in patients with interstitial pneumonia and lung cancer.
Journal
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AREG (Amphiregulin) • MMP11 (Matrix Metallopeptidase 11) • MUC6 (Mucin 6)
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nintedanib
9d
GARD: Genomic Data based Drug Repurposing in Head and Neck Cancer with Large Language Model Validation. (PubMed, bioRxiv)
Drug-gene mapping revealed candidates spanning already in clinical trials for HNC (e.g. Afatinib, Cabozantinib, Dasatinib, Brigatinib, Lenvatinib, Capivasertib, Erdafitinib) and emerging or repurposing candidates (Amuvatinib, XL765 (Voxtalisib), Golotimod, Artenimol, Quercetin, and Acetylsalicylic Acid), offering opportunities for precision repurposing...These included targeted therapies such as Fostamatinib, Nintedanib, Brigatinib, Regorafenib, and Lenvatinib, as well as emerging compounds like Artenimol, Quercetin, and Acetylsalicylic Acid (Aspirin). Through a combination of genomic analysis, network expansion, and literature validation, the GARD pipeline offers a powerful way to accelerate personalized cancer treatments while reducing cost and development time.
Journal • IO biomarker
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • SOX2 • CLDN1 (Claudin 1) • TLR7 (Toll Like Receptor 7) • EIF4G1 (Eukaryotic translation initiation factor 4 gamma, 1)
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Gilotrif (afatinib) • dasatinib • Lenvima (lenvatinib) • Cabometyx (cabozantinib tablet) • Balversa (erdafitinib) • Stivarga (regorafenib) • Alunbrig (brigatinib) • Truqap (capivasertib) • nintedanib • Tavalisse (fostamatinib) • amuvatinib (MP470) • aspirin • voxtalisib (SAR245409)
13d
Improving the bioavailability of nintedanib by formulating inhalable ufasomes as a targeted therapy for non-small cell lung cancer. (PubMed, Int J Pharm X)
The histopathological analysis confirmed these results. The safety and efficacy studies demonstrated that the nebulized NLU formulation at a dose of 100 mg/kg could serve as a viable therapy for NSCLC.
Journal
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TNFA (Tumor Necrosis Factor-Alpha) • IL1B (Interleukin 1, beta)
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nintedanib
15d
New P2 trial
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nintedanib
24d
Phase I/II Study of Nivolumab and Ipilimumab Combined With Nintedanib in Non Small Cell Lung Cancer (clinicaltrials.gov)
P1/2, N=66, Active, not recruiting, H. Lee Moffitt Cancer Center and Research Institute | Trial completion date: Nov 2025 --> Aug 2026
Trial completion date
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EGFR (Epidermal growth factor receptor) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase)
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BRAF V600E • EGFR mutation • BRAF V600 • EGFR T790M • ALK rearrangement • ROS1 rearrangement
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Opdivo (nivolumab) • Yervoy (ipilimumab) • nintedanib
25d
Multimodal profiling of pancreatic cancer reveals a TIMP-1-dominated secretory profile determining pro-tumor immunoinstruction in human cancers. (PubMed, Cell Rep Med)
In pre-clinical PC, TIMP-1/CISS proves targetable through combined inhibition of upstream kinases with clinically approved drugs trametinib and nintedanib. Collectively, CISS represents a ubiquitous signature of pro-tumor immunoinstruction with actionable diagnostic and therapeutic potential across human cancers.
Journal
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IL2 (Interleukin 2) • TIMP1 (Tissue inhibitor of metalloproteinases 1)
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Mekinist (trametinib) • nintedanib
26d
Nintedanib Attenuates Epidural Fibrosis After Laminectomy in Rats. (PubMed, J Korean Neurosurg Soc)
By improving the dural structure and reducing key molecules that contribute to scar formation, NIN shows significant promise as a treatment to prevent postoperative epidural adhesions. Future studies with extended follow-up may help clarify its clinical relevance.
Preclinical • Journal
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TNFA (Tumor Necrosis Factor-Alpha) • TGFB1 (Transforming Growth Factor Beta 1) • IL1B (Interleukin 1, beta)
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nintedanib
26d
PEMBIB: Trial Of Pembrolizumab And Nintedanib (clinicaltrials.gov)
P1, N=196, Completed, Gustave Roussy, Cancer Campus, Grand Paris | Recruiting --> Completed | Trial completion date: Nov 2028 --> Jan 2026
Trial completion • Trial completion date • Tumor mutational burden
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Keytruda (pembrolizumab) • nintedanib
1m
Early Clinical and Molecular Biomarkers in Patients With Advanced Ovarian Cancer Undergoing Neoadjuvant Chemotherapy: CHIVA Phase II GINECO Trial. (PubMed, JCO Precis Oncol)
HRD status, KELIM, and TILs are key independent biomarkers in advanced OC. CCNE1 amplifications, although typically associated with platinum resistance, were linked to moderate chemotherapy sensitivity, defining an intermediate prognostic subgroup.
P2 data • Journal • BRCA Biomarker
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HRD (Homologous Recombination Deficiency) • CCNE1 (Cyclin E1)
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HRD
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nintedanib