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DRUG CLASS:

HER4 inhibitor

1d
Study of Afatinib in Advanced Cutaneous Squamous Cell Carcinoma (clinicaltrials.gov)
P2, N=25, Recruiting, H. Lee Moffitt Cancer Center and Research Institute | Trial primary completion date: Mar 2026 --> Sep 2026
Trial primary completion date
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Gilotrif (afatinib)
2d
Neoadjuvant Pyrotinib in HR-positive and HER2-low High-risk Early Breast Cancer (clinicaltrials.gov)
P3, N=160, Active, not recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University | Recruiting --> Active, not recruiting
Enrollment closed
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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MammaPrint®
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paclitaxel • doxorubicin hydrochloride • Irene (pyrotinib) • cyclophosphamide • epirubicin
3d
Radiation therapy combined with tyrosine kinase inhibitors in 826 patients with HER2-positive breast cancer brain metastases: a systematic review and network meta-analysis. (PubMed, Neurosurg Rev)
Bayesian network meta-analysis (NMA) was conducted to integrate direct and indirect comparisons, addressing the lack of head-to-head trials. Eleven studies (2 RCTs, 9 retrospective; 826 patients) evaluated four treatment strategies: pyrotinib + RT, pyrotinib alone, RT alone, and lapatinib + RT. In contrast, lapatinib + RT appeared to offer limited benefit and a higher risk of SAEs. Further randomized controlled trials are needed to validate these findings.
Clinical • Retrospective data • Review • Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive
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lapatinib • Irene (pyrotinib)
3d
Exploration of Targeted Therapy Regimens for Triple-Positive Breast CancerExploration of Targeted Therapy Regimens for Triple-Positive Breast Cancer (ChiCTR2500113410)
P=N/A, N=200, Not yet recruiting, The First Affiliated Hospital of Xi'an Jiaotong University; The First Affiliated Hospital of Xi'an Jiaotong University
New trial
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HR positive • HR positive + HER-2 positive
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Prosigna™ Breast Cancer Prognostic Gene Signature Assay
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Herceptin (trastuzumab) • carboplatin • docetaxel • Perjeta (pertuzumab) • Irene (pyrotinib)
3d
New trial
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HER-2 positive
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paclitaxel • Irene (pyrotinib)
4d
First-Line Afatinib 30 mg Versus 40 mg in Non-small Cell Lung Cancer Patients With Uncommon EGFR Mutations: Real-world Efficacy and Tolerability in Taiwan. (PubMed, Anticancer Res)
Afatinib 30 mg daily achieved comparable efficacy and better tolerability than 40 mg, with significantly longer PFS and OS in patients harboring compound or double-rare EGFR mutations. These findings suggest that lower-dose afatinib may optimize efficacy and safety in patients with uncommon EGFR-mutant NSCLC.
Retrospective data • Journal • Real-world evidence
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EGFR (Epidermal growth factor receptor)
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EGFR mutation
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Gilotrif (afatinib)
4d
Afatinib alters DNA methylation and Paneth-like differentiation markers in Caco-2 cells. (PubMed, Adv Biol Regul)
These findings suggest that DNMT1/3B-skewed methylation at the SOX9/DEFA5 promoters may be counteracted by ten-eleven translocation-mediated counter-demethylation. Collectively, our data indicate that afatinib modulates Paneth-like differentiation markers via DNA methylation-dependent repression of SOX9/DEFA5 and DNA methylation-independent induction of OSR1/RIP140 in Caco-2 cells, which may be relevant to crypt-associated epithelial function and gastrointestinal safety.
Journal
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EGFR (Epidermal growth factor receptor) • DNMT1 (DNA methyltransferase 1) • SOX9 (SRY-Box Transcription Factor 9) • YBX1 (Y-Box Binding Protein 1) • RIPK1 (Receptor Interacting Serine/Threonine Kinase 1)
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EGFR mutation
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Gilotrif (afatinib)
7d
NCI 10495: Testing the Safety and Tolerability of the Anti-cancer Drugs Trastuzumab Deruxtecan and Neratinib for Cancers With Changes in the HER2 Gene (clinicaltrials.gov)
P1, N=33, Suspended, National Cancer Institute (NCI) | Trial completion date: Dec 2025 --> Jan 2027 | Recruiting --> Suspended
Trial completion date • Trial suspension
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CD4 (CD4 Molecule)
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HER-2 positive • HER-2 overexpression • HER-2 amplification • HER-2 mutation
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Nerlynx (neratinib) • Enhertu (fam-trastuzumab deruxtecan-nxki)
7d
NCI-2017-00831: Poziotinib in EGFR Exon 20 Mutant Advanced NSCLC (clinicaltrials.gov)
P2, N=93, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Dec 2025 --> Dec 2027 | Trial primary completion date: Dec 2025 --> Dec 2027
Trial completion date • Trial primary completion date
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
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EGFR mutation • EGFR exon 20 insertion • HER-2 exon 20 insertion • EGFR exon 20 mutation
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FoundationOne® CDx • Guardant360® CDx • cobas® EGFR Mutation Test v2 • therascreen® EGFR RGQ PCR Kit
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Pozenveo (poziotinib)
9d
TMIGD2 in Bladder Cancer: A Bioinformatics and Experimental Approach to Understanding its Prognostic and Therapeutic Potential. (PubMed, Curr Top Med Chem)
This study demonstrates that TMIGD2 is downregulated in BLCA and correlates with adverse prognosis and immune regulation. Its potential as a prognostic biomarker and therapeutic target is underscored by its involvement in key pathways, immune infiltration, and drug sensitivity. Further research is essential to fully realize the clinical potential of TMIGD2 in the management of BLCA.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • LAG3 (Lymphocyte Activating 3) • CTLA4 (Cytotoxic T-Lymphocyte Associated Protein 4) • TIGIT (T Cell Immunoreceptor With Ig And ITIM Domains 2) • MIR1304 (MicroRNA 1304)
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PD-L1 expression
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Gilotrif (afatinib) • sorafenib • paclitaxel
11d
TBCRC 022: HKI-272 for HER2-Positive Breast Cancer and Brain Metastases (clinicaltrials.gov)
P2, N=140, Completed, Dana-Farber Cancer Institute | Active, not recruiting --> Completed
Trial completion
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HER-2 amplification
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Nerlynx (neratinib) • Kadcyla (ado-trastuzumab emtansine) • capecitabine
13d
Novel syngeneic cell lines for studying high-risk BRAFV600E-driven colorectal cancer in vivo. (PubMed, Cancer Res Commun)
Interestingly, these so-called NaJa lines displayed distinct differentiation states and responses to the clinically relevant RAF inhibitors (RAFi) encorafenib and exarafenib, thereby resembling the clinical heterogeneity of BRAFV600E-driven CRC. RAFi resistance was overcome by the EGFR-family inhibitor afatinib...Upon re-transplantation into syngeneic mice, all NaJa lines established aggressive tumors with distinct tumor microenvironments matching to their differentiation states. Thus, the NaJa lines provide a unique tool to study tumor heterogeneity, drug resistance and the interplay between tumor, stroma and immune cells in BRAFV600E-driven CRC.
Preclinical • Journal • IO biomarker
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BRAF (B-raf proto-oncogene) • APC (APC Regulator Of WNT Signaling Pathway)
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BRAF V600E • BRAF V600
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Gilotrif (afatinib) • Braftovi (encorafenib) • exarafenib (KIN-2787)