^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG CLASS:

EGFR inhibitor

Related drugs:
2d
Design, synthesis, and biological evaluation of quinazoline-benzohydrazide and quinazoline-benzothiazole hybrids uncovering a dual EGFR/VEGFR-2 inhibitor with pronounced cytotoxic activity against triple-negative breast Cancer. (PubMed, Bioorg Med Chem)
Among the tested compounds, 7a demonstrated the most potent activity, with IC₅₀ values ranging from 3.98 to 9.67 μM, comparable with doxorubicin...It also markedly inhibited EGFR and VEGFR-2 with IC₅₀ values of 1.67 and 6.72 μM, compared to Erlotinib and Sorafenib, respectively...Molecular docking studies confirmed the strong binding affinity of 7a within the active sites of both EGFR and VEGFR-2, supporting its proposed mechanism of action. These findings position compound 7a as a promising lead for further development as a dual EGFR/VEGFR-2-targeting anticancer agent, particularly for aggressive cancers such as TNBC.
Journal • IO biomarker
|
EGFR (Epidermal growth factor receptor) • BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • CASP9 (Caspase 9)
|
erlotinib • sorafenib • doxorubicin hydrochloride
2d
New P4 trial
|
cisplatin • Tagrisso (osimertinib) • carboplatin • pemetrexed
2d
EMB-01, a Tetravalent Bispecific Antibody, Inducing Co-Degradation of EGFR and c-Met for Enhanced Anti-Tumor Efficacy. (PubMed, Cancer Sci)
Furthermore, EMB-01 demonstrates potent anti-tumor activity across multiple tumor models, outperforming existing EGFR-targeted therapies and other bispecific antibodies, while maintaining favorable pharmacokinetics with good tolerability in cynomolgus monkeys. These findings support the clinical development of EMB-01 as a promising therapeutic for EGFR/c-Met-driven cancers.
Journal
|
EGFR (Epidermal growth factor receptor) • MET (MET proto-oncogene, receptor tyrosine kinase) • CXCL8 (Chemokine (C-X-C motif) ligand 8)
|
bafisontamab (EMB-01)
3d
Case Report: Two cases of non-small cell lung cancer with coexistence of NTRK2 fusion and EGFR mutations. (PubMed, Front Oncol)
Case 1 received osimertinib combined with savolitinib, had 33 months of follow-up, and achieved a partial response. Case 2 received furmonertinib and achieved a complete response. NTRK2 fusion coexisting with EGFR mutations is a rare molecular characteristic of non-small cell lung cancer, accompanied by positive PD-L1 expression, and may serve as a promising biomarker for targeted therapy.
Journal • Tumor mutational burden • PD(L)-1 Biomarker • IO biomarker
|
EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • TMB (Tumor Mutational Burden) • MET (MET proto-oncogene, receptor tyrosine kinase) • FGFR1 (Fibroblast growth factor receptor 1) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2) • NKX2-1 (NK2 Homeobox 1) • NAPSA (Napsin A Aspartic Peptidase)
|
PD-L1 expression • EGFR mutation • MET amplification • TMB-L • MET mutation
|
Tagrisso (osimertinib) • Orpathys (savolitinib) • Ivesa (firmonertinib)
3d
New P2 trial
|
gemcitabine • albumin-bound paclitaxel • TheraCIM (nimotuzumab)
3d
Almonertinib inhibits liver cancer progression by triggering autophagy-dependent ferroptosis through inhibition of the PI3K/Akt1/mTOR pathway. (PubMed, Biochem Pharmacol)
Interestingly, we demonstrated that Almonertinib-activated autophagy directly participates in ferroptosis activation by promoting Fe2+ release upstream and influencing lipid peroxidation, elucidating the occurrence of autophagy-dependent ferroptosis. In summary, these findings indicate that Almonertinib suppresses liver cancer progression by inducing autophagy-dependent ferroptosis in HepG2 and MHCC-97H cells, potentially providing insights for positioning Almonertinib as a novel therapeutic candidate for future liver cancer treatment.
Journal • IO biomarker
|
GPX4 (Glutathione Peroxidase 4) • SLC7A11 (Solute Carrier Family 7 Member 11)
|
Ameile (aumolertinib)
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
|
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)
|
EGFR mutation • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Zegfrovy (sunvozertinib)
3d
New P3 trial
|
Keytruda (pembrolizumab) • cisplatin • carboplatin • 5-fluorouracil • Rybrevant (amivantamab-vmjw)
3d
Increased Cardiovascular Risk With Lorlatinib in Patients With ALK-Mutated Lung Cancer: A Real-World Comparative Study. (PubMed, J Am Heart Assoc)
These findings underscore the importance of routine cardiovascular monitoring, particularly in older patients and those with atrial arrhythmias.
Journal • Real-world evidence
|
ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
|
ALK rearrangement • ALK mutation
|
Alecensa (alectinib) • Lorbrena (lorlatinib) • Alunbrig (brigatinib)
3d
Evaluation of Pafolacianine (Cytalux®) for Fluorescence-Guided Surgery in Head and Neck Squamous Cell Carcinoma: A Negative Study with Important Clinical Implications. (PubMed, Mol Imaging Biol)
Negative studies such as this are essential for evidence-based clinical decision-making, preventing unnecessary resource allocation and potential patient exposure to ineffective interventions. These findings inform the broader fluorescence-guided surgery field and support continued investigation of alternative targeting strategies for HNSCC.
Journal
|
FOLR1 ( Folate receptor alpha )
|
Vectibix (panitumumab)
3d
ELK3-SERPINE1-PCBP2 axis promotes gefitinib resistance in lung cancer by inhibiting ferroptosis. (PubMed, Int Immunopharmacol)
The ELK3-SERPINE1-PCBP2 axis promotes GEF resistance in lung cancer by inhibiting ferroptosis, providing a potential new therapeutic strategy for overcoming chemoresistance.
Journal
|
SERPINE1 (Serpin Family E Member 1) • PCBP2 (Poly(RC) Binding Protein 2)
|
gefitinib