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DRUG CLASS:

HER2 inhibitor

Related drugs:
24h
Efficacy and Safety of Different Treatment Regimens for Previously Untreated Patients with HER2-positive Advanced Gastric Cancer: A Meta-Analysis of Randomized Controlled Trials. (PubMed, J Gastrointest Cancer)
No first-line regimen significantly improved OS or PFS in HER2-positive advanced gastric cancer. However, HLX22-based and immune-combination strategies show potential clinical value-particularly in enhancing ORR-and merit further investigation.
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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Keytruda (pembrolizumab) • Hercessi (trastuzumab-strf)
2d
Adjuvant ovarian function suppression and aromatase inhibitors in premenopausal patients with hormone receptor and HER2 positive breast cancer, by timing of chemotherapy and trastuzumab and response to neoadjuvant therapy. (PubMed, Breast)
OFS + AI were associated with better DDFS in patients with RD after neoadjuvant therapy. Our findings can assist shared decision-making on adjuvant endocrine therapy of these patients.
Journal
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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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Herceptin (trastuzumab) • tamoxifen • Perjeta (pertuzumab)
2d
CPT1A exacerbates trastuzumab-induced cardiotoxicity via promotion of mitochondrial dysfunction. (PubMed, Int J Biol Macromol)
In vitro mechanistic studies revealed that CPT1A may promote mitochondrial damage and induce cardiomyocyte injury by interacting with Parkin. This study underscores the utility of multi-omics integration in elucidating TIC mechanisms and paves the way for personalized cardioprotective strategies in HER2-targeted therapy.
Journal
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CPT1A (Carnitine Palmitoyltransferase 1A) • ACSL1 (Acyl-CoA Synthetase Long Chain Family Member 1)
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HER-2 positive
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Herceptin (trastuzumab)
2d
Mechanism exploration of Salvia miltiorrhiza Bunge against trastuzumab induced cardiotoxicity via multi-omics. (PubMed, J Ethnopharmacol)
DS extract alleviates TRZ-induced cardiotoxicity, manifested by improved cardiac function, reduced myocardial injury markers, and mitigated tissue and mitochondrial damage. Its mechanism of action is associated with regulating proteins in the ferroptosis pathway (upregulating GPX4 and downregulating ACSL4). Additionally, tanshinone I, IIA, and IIB have been identified as potential active components.
Journal
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GPX4 (Glutathione Peroxidase 4) • ACSL4 (Acyl-CoA Synthetase Long Chain Family Member 4)
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Herceptin (trastuzumab)
2d
A nyelőcső-, GEJ- és gyomordaganatok immunterápiája. (PubMed, Magy Onkol)
In esophageal tumors, adjuvant nivolumab is used. Among HER2-positive patients, adding pembrolizumab to trastuzumab and chemotherapy - in PDL1 CPS ≥1 cases - has become a new standard. A special mention must be made of MSI-H tumors, in which immunotherapy is highly effective, and adjuvant chemotherapy is not recommended according to current guidelines.
Review • Journal
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HER-2 (Human epidermal growth factor receptor 2) • MSI (Microsatellite instability)
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HER-2 positive • MSI-H/dMMR
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Keytruda (pembrolizumab) • Opdivo (nivolumab) • Herceptin (trastuzumab)
3d
Structure-guided screening identifies Tucatinib as dual inhibitor for MCT1/2. (PubMed, EMBO Rep)
We show that Tucatinib potently inhibits the proliferation and migration of cervical tumor cells in vitro and tumor growth in a mouse xenograft model, while exhibiting excellent biological safety. These findings offer molecular insights into the structural and functional mechanism of MCT2 and identify Tucatinib as novel dual inhibitor of both transporters.
Journal
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BSG (Basigin (Ok Blood Group))
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Tukysa (tucatinib)
3d
Genetic modulation of ABCB1: Sunvozertinib reverses ABCB1-mediated multidrug resistance in cancer cells. (PubMed, Cancer Genet)
Furthermore, treatment with sunvozertinib did not change protein expression or subcellular localization of ABCB1. Altogether, these data demonstrate that sunvozertinib, when combined with other conventional chemotherapeutic agents, can overcome MDR and improve therapeutic effect.
Journal
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EGFR (Epidermal growth factor receptor) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • ABCC1 (ATP Binding Cassette Subfamily C Member 1)
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EGFR mutation • EGFR exon 20 insertion • EGFR exon 20 mutation
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Zegfrovy (sunvozertinib)
3d
Targeting tumor microenvironment-derived NRG1-HER2/3 signaling with zenocutuzumab restores sensitivity to AR inhibition in PTEN wild-type prostate cancer. (PubMed, Mol Cancer Ther)
In the context of PTEN loss and AR inhibitor resistance, zenocutuzumab did not restore sensitivity. These findings highlight the critical molecular context in which tumor microenvironment (TME)-derived NRG1 impacts responsiveness to AR inhibition and suggest that targeting NRG1 is a promising strategy for overcoming resistance to androgen blockade in PTEN-wildtype prostate cancers.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • PTEN (Phosphatase and tensin homolog) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • NRG1 (Neuregulin 1)
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Bizengri (zenocutuzumab-zbco)
4d
Clinical efficacy and safety of pyrotinib as the first-line treatment of HER2-positive advanced breast cancer in Xinjiang Uygur Autonomous Region of China. (PubMed, Transl Cancer Res)
Pyrotinib showed good antitumor activity in the treatment of patients with HER2-positive advanced breast cancer and displayed a degree of efficacy in patients with brain metastases. The main adverse reaction was diarrhea, which was mostly low to moderate in severity, and the incidence of high-grade AEs was generally low, with controllable toxicity.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • EGFR positive
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Irene (pyrotinib)
4d
A serum biomarker panel for early detection of treatment-related cardiotoxicity in early HER2-positive breast cancer patients. (PubMed, Ann Med Surg (Lond))
All enrolled patients received the full treatment protocol consisting of anthracycline followed by 12 months of trastuzumab alone or with pertuzumab. The highest risk was observed when both elevated hs-Tn I (≥82 ng/L after four cycles of anti-HER2 agents) and elevated hs-CRP (after four cycles of anthracyclines) were present. The interaction between both hs-Tn I and hs-CRP demonstrates significant predictive value for cardiotoxicity risk related to HER2+ breast cancer treatment.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • IL6 (Interleukin 6)
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HER-2 positive • HER-2 elevation
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Herceptin (trastuzumab) • Perjeta (pertuzumab)
4d
TrasTUCAN: Efficacy and Safety of the Combination of Trastuzumab Plus TUCAtinib Plus viNorelbine in Patients With HER2-positive Non-resectable Locally Advanced or Metastatic Breast Cancer (clinicaltrials.gov)
P2, N=13, Terminated, Spanish Breast Cancer Research Group | Trial completion date: Aug 2026 --> May 2025 | Active, not recruiting --> Terminated | Trial primary completion date: Aug 2026 --> May 2025; The study was closed early due to safety concerns and an unfavorable benefit-risk balance. Unexpected high neutropenia rates required a costly sub-study, which was not feasible, forcing the sponsor to terminate the trial prematurely.
Trial completion date • Trial termination • Trial primary completion date
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HER-2 positive
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Herceptin (trastuzumab) • Tukysa (tucatinib) • vinorelbine tartrate
4d
New P2 trial
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Zegfrovy (sunvozertinib)