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DRUG CLASS:

RTK inhibitor

Associations
27d
OptiTROP-Lung04: A Phase III Study of SKB264 for EGFR Mutant NSCLC Patients (clinicaltrials.gov)
P3, N=376, Active, not recruiting, Sichuan Kelun Pharmaceutical Research Institute Co., Ltd. | Recruiting --> Active, not recruiting
Enrollment closed
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EGFR mutation
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cisplatin • carboplatin • pemetrexed • Jiataile (sacituzumab tirumotecan)
4ms
Tumor-Specific EphA2 Receptor Tyrosine Kinase Inhibits Anti-Tumor Immunity by Recruiting Suppressive Myeloid Populations in Murine Models of Non-Small Cell Lung Cancer. (PubMed, Cancers (Basel))
Our studies suggest EphA2 on tumor cells recruits monocytes and promotes their differentiation into TAMs that likely inhibit the activation and infiltration of cytotoxic lymphocytes, promoting tumor immune escape.
Preclinical • Journal • PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • CCL2 (Chemokine (C-C motif) ligand 2) • TGFB1 (Transforming Growth Factor Beta 1) • CCL8 (C-C Motif Chemokine Ligand 8)
4ms
From Lab to Target: Pyrazole, Pyrazoline and Fused Pyrazole Derivatives as Receptor Tyrosine Kinase Inhibitors in Cancer Therapy. (PubMed, Arch Pharm (Weinheim))
Furthermore, synthetic pathways for each series or key compounds are presented, offering a practical guide for researchers in the field. By integrating these elements, this review provides a solid foundation and rationale for the design, synthesis, and optimization of new pyrazole-based anticancer agents targeting receptor tyrosine kinases.
Review • Journal
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EGFR (Epidermal growth factor receptor) • FGFR (Fibroblast Growth Factor Receptor) • AXL (AXL Receptor Tyrosine Kinase) • KDR (Kinase insert domain receptor) • CSF1R (Colony stimulating factor 1 receptor)
4ms
Applying next-generation sequencing to predict short progression-free survival in patients with advanced EGFR-mutant lung adenocarcinoma receiving epidermal growth factor receptor tyrosine kinase inhibitors. (PubMed, Anticancer Drugs)
We identified three risk factors: (1) PIK3CA-AKT/RAS-RAF alterations, (2) age ≤50, and (3) PD-L1 ≥50%. Patients with these factors had poor PFS regardless of EGFR-TKI generation.
Journal • Next-generation sequencing • PD(L)-1 Biomarker • IO biomarker
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EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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EGFR mutation
4ms
Examining the 2-aryl-5-nitrobenzofuran-based hydrazones for anti-breast (MCF-7) cancer activity, potential to induce cell cycle arrest and inhibit receptor tyrosine kinases (VEGFR-2 & EGFR). (PubMed, Eur J Med Chem)
The ADMET predictions indicated excellent drug-like properties, particularly for the non-Pgp substrate series. The finding successfully identified compound 3k as a lead dual inhibitor of VEGFR-2 and EGFR with significant anticancer activity and selectivity.
Journal
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EGFR (Epidermal growth factor receptor) • KDR (Kinase insert domain receptor) • ANXA5 (Annexin A5)
5ms
Immune Checkpoint Inhibitors in Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitor-Resistant Chemotherapy-Naïve Advanced Non-Small Cell Lung Cancer: A Meta-Analysis Based on Eight Randomized Trials. (PubMed, JCO Precis Oncol)
This meta-analysis suggests that the addition of ICIs to C/A may improve survival outcomes in patients with advanced NSCLC after resistance to EGFR-TKIs, particularly in selected subpopulations such as those with high PD-L1 expression or specific EGFR mutations. However, careful monitoring for specific AEs is warranted.
Clinical • Retrospective data • Review • Journal • Checkpoint inhibition • PD(L)-1 Biomarker • IO biomarker
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EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1)
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PD-L1 expression • EGFR mutation • PD-L1 overexpression • EGFR expression
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pemetrexed
6ms
Drug-drug interactions between epidermal growth factor receptor tyrosine kinase inhibitors and rivaroxaban in vitro and in vivo. (PubMed, PLoS One)
These findings confirm the presence of DDIs between EGFR TKIs and rivaroxaban. Avitinib and gefitinib significantly inhibit rivaroxaban metabolism, and their co-administration may aggravate the risk of bleeding.
Preclinical • Journal
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EGFR (Epidermal growth factor receptor) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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gefitinib • Fujovee (abivertinib)
7ms
Halofuginone targets Serine/Glycine synthesis to reverse epidermal growth factor receptor Tyrosine Kinase inhibitor resistance in lung adenocarcinoma. (PubMed, Phytomedicine)
HF is a promising natural product for overcoming NSCLC resistance to third-generation epidermal growth factor receptors-TKIs.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation
8ms
Clinicopathologic features of histologic transformation in lung adenocarcinoma after treatment with epidermal growth factor receptor-tyrosine kinase inhibitors. (PubMed, Ann Diagn Pathol)
The analysis of mutation profiles and survival outcomes revealed that the transformation subtype affects prognosis. Additionally, the time taken to undergo transformation is critical for patient outcomes.
Journal
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EGFR (Epidermal growth factor receptor) • TP53 (Tumor protein P53) • PTEN (Phosphatase and tensin homolog) • RB1 (RB Transcriptional Corepressor 1) • KMT2D (Lysine Methyltransferase 2D)
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TP53 mutation • PTEN mutation
8ms
Safety, Tolerability, Pharmacokinetics and Anti-tumour Activity of Alflutinib in Advanced Non Small Cell Lung Cancer (clinicaltrials.gov)
P1, N=14, Terminated, Allist Pharmaceuticals, Inc. | Unknown status --> Terminated; Indications have been approved for marketing
Trial termination
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR L861Q • EGFR G719X
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Ivesa (firmonertinib)
10ms
Combination of Osimertinib and Aspirin to Treat 1st Generation EGFR-TKI Resistance in NSCLC (clinicaltrials.gov)
P2, N=115, Completed, Daping Hospital and the Research Institute of Surgery of the Third Military Medical University | Not yet recruiting --> Completed | Phase classification: PN/A --> P2 | N=330 --> 115 | Trial completion date: Dec 2022 --> Jun 2024
Trial completion • Phase classification • Enrollment change • Trial completion date
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EGFR mutation
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Tagrisso (osimertinib) • aspirin
10ms
FLAURA: AZD9291 Versus Gefitinib or Erlotinib in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer (clinicaltrials.gov)
P3, N=674, Active, not recruiting, AstraZeneca | Trial completion date: Jan 2025 --> Dec 2025
Trial completion date
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion
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Tagrisso (osimertinib) • erlotinib • gefitinib