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DRUG CLASS:

pan-HER inhibitor

2d
Afatinib Versus Osimertinib as First-Line Treatment for Advanced EGFR-Mutant Non-Small-Cell Lung Cancer: A 3-Year Follow-Up Overall Survival Analysis. (PubMed, Target Oncol)
Our study demonstrated that both afatinib and osimertinib as first-line treatments offer favorable median OS in patients with advanced EGFR-mutant NSCLC. In addition, we recommend that patients receiving afatinib as first-line therapy undergo sequential osimertinib treatment, regardless of their T790M mutation status.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M
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Tagrisso (osimertinib) • Gilotrif (afatinib)
8d
Afatinib Overcomes Osimertinib Resistance via Egfr V804F Mutation in a Syngeneic Egfr-Mutant Lung Cancer Mouse Model. (PubMed, Cancer Sci)
Consistently, afatinib treatment resulted in marked tumor shrinkage and suppression of EGFR signaling in the established mDEL OsiR #1/#3 in vivo. These findings establish secondary Egfr V804F/EGFR V802F as an on-target osimertinib resistance mechanism, providing a preclinical rationale for evaluating afatinib in biomarker-selected patients harboring this alteration.
Preclinical • Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR exon 19 deletion
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Tagrisso (osimertinib) • Gilotrif (afatinib)
9d
Initial Low-Dose Dacomitinib for First-Line Treatment of Patients With EGFR Exon 21-Mutated Non-Small-Cell Lung Cancer. (PubMed, Clin Med Insights Oncol)
Initial low-dose dacomitinib demonstrated promising efficacy with an improved safety profile in patients with EGFR exon 21-mutated NSCLC. These findings support the feasibility of a dose-optimization strategy, although further prospective studies are warranted.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation
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Vizimpro (dacomitinib)
9d
A targeted combination therapy achieves effective pancreatic cancer regression and prevents tumor resistance. (PubMed, Proc Natl Acad Sci U S A)
Likewise, a combination of selective inhibitors of KRAS (RMC-6236/daraxonrasib), EGFR family (afatinib), and STAT3 (SD36) induced the complete regression of orthotopic PDAC tumors with no evidence of tumor resistance for over 200 d posttreatment. Of importance, this combination therapy was well tolerated. In sum, these results should guide the development of new clinical trials that may benefit PDAC patients.
Journal
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EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53)
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TP53 mutation • KRAS mutation
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Gilotrif (afatinib) • daraxonrasib (RMC-6236)
10d
Afatinib Versus Osimertinib for Non-Small Cell Lung Cancer With Uncommon EGFR Mutations: Real-World Outcomes. (PubMed, Cancer Sci)
Among 56 patients who received subsequent systemic therapy, clinical outcomes were comparable between ICI plus platinum doublet and platinum doublet alone. These findings indicate that afatinib and osimertinib provide comparable survival outcomes as first-line therapies for NSCLC with UMs, with treatment effects varying by molecular subtype, while subsequent ICI-based regimens may confer limited additional benefit.
Journal • Real-world evidence • IO biomarker
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR T790M
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Tagrisso (osimertinib) • Gilotrif (afatinib)
12d
A Study to Learn About Dacomitinib in Patients With Non-small Cell Lung Cancer. (clinicaltrials.gov)
P=N/A, N=29, Completed, Pfizer | Active, not recruiting --> Completed | Trial completion date: Dec 2026 --> Sep 2025 | Trial primary completion date: Dec 2026 --> Sep 2025
Trial completion • Trial completion date • Trial primary completion date • HEOR • Real-world evidence
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EGFR (Epidermal growth factor receptor)
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EGFR mutation
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Vizimpro (dacomitinib)
12d
Network toxicology and bioinformatics reveal potential molecular links between cadmium exposure and pancreatic cancer. (PubMed, BMC Pharmacol Toxicol)
This study reveals that Cd may promote the malignant progression of PC by regulating ECM remodeling through key genes such as FN1. Dacomitinib shows promise as an FN1-associated therapy, offering new insights for the precise prevention and treatment of Cd-associated PC.
Journal
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FN1 (Fibronectin 1) • TIMP1 (Tissue inhibitor of metalloproteinases 1) • COL3A1 (Collagen Type III Alpha 1 Chain) • COL5A1 (Collagen Type V Alpha 1 Chain)
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Vizimpro (dacomitinib)
12d
An Effective and Systematic Strategy for Metabolic Profiling of Golvatinib In Vitro by Combining UHPLC-MS/MS and UHPLC-Q-Orbitrap-HRMS. (PubMed, J Sep Sci)
Detection was carried out by multiple reaction monitoring mode using the transitions m/z 634.3→184.2 for golvatinib and m/z 650.3→200.2 for golvatinib N-oxide. Further study demonstrated that CYP3A4 was the principal enzyme involved in metabolizing golvatinib. To the best of our knowledge, this is the first report combining ultra-high-performance liquid chromatography-tandem MS (UHPLC-MS/MS) with UHPLC-Quadrupole-Orbitrap-HRMS for profiling golvatinib metabolism in vitro, thereby laying a foundation for subsequent pharmacokinetic study.
Preclinical • Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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larotinib (Z650) • golvatinib (E7050)
14d
A novel quinazolinone insulin receptor inhibitor and its synergy with an EGFR inhibitor in glucose-driven glioblastoma. (PubMed, Mol Oncol)
Combination studies revealed that W1B acts synergistically with the EGFR inhibitor dacomitinib, effectively overcoming compensatory activation of parallel pathways...The in vivo studies on Danio rerio have shown a good safety profile, as well as strong antitumor potential of the tested compound. Therefore, these findings establish W1B as a promising derivative for the development of next-generation dual IGF1R/EGFR inhibitors in GBM.
Journal
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IR (Insulin receptor)
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Vizimpro (dacomitinib)
16d
Establishing the role of the neurotransmitter receptor-related gene GABRD in the diagnosis, prognosis and immune infiltrates of colorectal cancer by bioinformatics analysis and experimental validation. (PubMed, Transl Cancer Res)
Molecular docking simulations suggested promising drug repurposing avenues, particularly with afatinib and crizotinib, for GABRD inhibition. GABRD gene may serve as a novel biomarker in the diagnosis, prognosis and immune infiltrates of CRC patients.
Journal
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CTNNB1 (Catenin (cadherin-associated protein), beta 1) • TGFB1 (Transforming Growth Factor Beta 1) • GABRD (Gamma-Aminobutyric Acid Type A Receptor Subunit Delta)
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Xalkori (crizotinib) • Gilotrif (afatinib)
16d
Lysine crotonylation-related long non-coding RNAs: a novel prognostic framework for gastric carcinoma. (PubMed, Transl Cancer Res)
Additionally, the model accurately predicted patient sensitivity to specific chemotherapeutic agents like afatinib and dasatanib...We developed a signature of lncRNAs linked to crotonylation that offers dependable prognostic insights and characterizes the immune microenvironment within GC. However, additional investigation is necessary to confirm its practical applications in clinical settings.
Journal • Tumor mutational burden • IO biomarker
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TMB (Tumor Mutational Burden)
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Gilotrif (afatinib)
20d
Dacomitinib in Combination with chemotherapy is effective in lung adenocarcinoma with rare EGFR L747P mutation and bone metastases: a case report. (PubMed, Front Oncol)
The patient initially received pemetrexed plus carboplatin chemotherapy. The treatment efficacy was evaluated as a partial response (PR), with manageable adverse events including skin rash and paronychia. Dacomitinib may provide sustained clinical benefit and an acceptable safety profile in lung adenocarcinoma patients with L747P mutation and bone metastases.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation
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carboplatin • pemetrexed • Vizimpro (dacomitinib)