- |||||||||| Erbitux (cetuximab) / Eli Lilly, EMD Serono
[VIRTUAL] Targeting MET and RON to overcome cetuximab resistance in colorectal cancer () - Mar 11, 2021 - Abstract #AACR2021AACR_3688; A comparative RNA-seq analysis showed that PDXs with high pMET/pRON levels could be segregated from PDXs with low pMET/pRON levels. Differential response of these PDXs and their organoid (PDO) derivatives for cetuximab resistance and response to crizotinib addition based on their pMET/pRON levels will be presented.
- |||||||||| APX701 / Apexigen, Erbitux (cetuximab) / Eli Lilly, EMD Serono, Herceptin (trastuzumab) / Roche
[VIRTUAL] Targeting SIRPα with APX701, a Novel Myeloid Checkpoint Inhibitor () - Mar 11, 2021 - Abstract #AACR2021AACR_3347; Together, these data demonstrate the unique binding profile of APX701 and its ability to potently reactivate myeloid cell-mediated anti-tumor immunity. Our data support the development of APX701, a promising myeloid checkpoint inhibitor, for the treatment of cancer.
- |||||||||| Ibrance (palbociclib) / Pfizer, Bavencio (avelumab) / EMD Serono, Pfizer, Erbitux (cetuximab) / Eli Lilly, EMD Serono
[VIRTUAL] A phase I study of avelumab, palbociclib, and cetuximab (APC) in recurrent or metastatic head and neck squamous cell carcinoma (RM HNSCC) () - Mar 11, 2021 - Abstract #AACR2021AACR_2577; P1 The RP2D is A 10 mg/kg every 2 wks, C 400 mg/m2 x 1 then 250 mg/m2 wkly, and P 125 mg daily, 3 wks on, one wk off. Promising response rates were seen, and several pts have had durable responses.
- |||||||||| Avastin (bevacizumab) / Roche, Erbitux (cetuximab) / Eli Lilly, EMD Serono
[VIRTUAL] 3D spheroid: A rapid drug screening model for epigenetic clinical targets against heterogenic cancer stem cells. () - Mar 11, 2021 - Abstract #AACR2021AACR_1891; The Cancer Stem Cells Therapeutic Target Database Version 2.0 (CSCTTv2.0) reported the highest expression of CSCs in glioblastomas, oral and CRCs that showed resistance to anticancer drugs (such as Bevacizumab, 5-FU, cisplatin, cetuximab, oxaliplatin)...We also found from Cytoscape analysis of Reactome network that UniProtKB - P61073 (CXCR4_HUMAN) has significant interaction with other target network genes from 106 network data and it has been mentioned that Plerixafor, an antagonist inhibits CXCR4 activity. Therefore, it is important in designing any small molecules or drugs against heterogenic CSCs of glioblastomas, oral, and CRC with epigenetic target of histone bivalent modifications using a 3D spheroid model which could be rapid screening model for anticancer drug discovery and our current study highlighted this important relationship.
- |||||||||| Erbitux (cetuximab) / Eli Lilly, EMD Serono
[VIRTUAL] Alterations of DNA damage response(DDR) signaling in the development of antibody-dependent cellular cytotoxicity (ADCC) resistance () - Mar 11, 2021 - Abstract #AACR2021AACR_1401; Here we describe a NK cell-mediated and cetuximab-dependent in vitro model of antibody-dependent cellular cytotoxicity (ADCC) to study alterations of DNA damage response signaling in the process of resistance development...Modulation of DDR signaling by ataxia telangiectasia mutated (ATM) or ATM-Rad3-related (ATR) inhibitors, p53 or STAT1 inhibition by siRNAs or the Janus Kinase 1(JAK1)/STAT1 inhibitor, ruxolitinib, potentiated ADCC activity in ADCC-sensitive A431 cells but not in their ADCC-resistant variants...Blocking DDR components might delay or prevent the evolution of the immunotherapy resistance. Further elucidation of critical signaling pathways involved in ADCC sensitivity and resistance will improve the ability to overcome antibody-based immunotherapy resistance.
- |||||||||| Erbitux (cetuximab) / Eli Lilly, EMD Serono
Journal: Role of NEU3 Overexpression in the Prediction of Efficacy of EGFR-Targeted Therapies in Colon Cancer Cell Lines. (Pubmed Central) - Mar 11, 2021 Consequently, we suggest that the evaluation of NEU3 expression cannot entirely substitute the evaluation of EGFR because EGFR-negative cases cannot be stimulated by NEU3. Furthermore, NEU3-mediated hyperactivation of EGFR is counterbalanced by the administration of cetuximab, hypothesizing that a combined treatment of NEU3- and EGFR-targeted therapies may represent a valid option for CRC patients, which must be investigated in the future.
- |||||||||| Keytruda (pembrolizumab) / Merck (MSD), Erbitux (cetuximab) / Eli Lilly, EMD Serono
Trial completion date, Trial primary completion date, Metastases: Pembrolizumab Combined With Cetuximab for Treatment of Recurrent/Metastatic Head & Neck Squamous Cell Carcinoma (clinicaltrials.gov) - Mar 11, 2021 P2, N=83, Recruiting, Furthermore, NEU3-mediated hyperactivation of EGFR is counterbalanced by the administration of cetuximab, hypothesizing that a combined treatment of NEU3- and EGFR-targeted therapies may represent a valid option for CRC patients, which must be investigated in the future. Trial completion date: May 2020 --> May 2022 | Trial primary completion date: Dec 2019 --> Dec 2021
- |||||||||| monalizumab (IPH2201) / AstraZeneca, Innate, Erbitux (cetuximab) / Eli Lilly, EMD Serono, Herceptin (trastuzumab) / Roche
[VIRTUAL] Monalizumab and trastuzumab in metastatic HER2-positive breast cancer: MIMOSA-trial () - Mar 9, 2021 - Abstract #ESMOBC2021ESMO_BC_250; P2 Before and on-treatment blood and biopsies will be used for translational research to explore treatment-induced intra-tumoral and systemic changes with a focus on NK-cells and CD8+ T-cells. The MIMOSA-trial is currently open for enrollment at the Netherlands Cancer Institute.
- |||||||||| simlukafusp alfa (RG7461) / Roche, Herceptin (trastuzumab) / Roche
Enrollment closed, Combination therapy: A Study Evaluating Safety, Pharmacokinetics, and Therapeutic Activity of RO6874281 as a Single Agent (Part A) or in Combination With Trastuzumab or Cetuximab (Part B or C) (clinicaltrials.gov) - Mar 9, 2021 P1a/1b, N=134, Active, not recruiting, The MIMOSA-trial is currently open for enrollment at the Netherlands Cancer Institute. Recruiting --> Active, not recruiting
- |||||||||| Journal: The Proteolytic Cleavage of Therapeutic Monoclonal Antibody Hinge Region: More Than a Matter of Subclass. (Pubmed Central) - Mar 9, 2021
Finally, with ELISA and flow cytometry, we observed that a single cleavage of IgG1 TmAbs greatly decreased their affinity for FcγRIIIA and C1q and their ability to induce FcγRIIIA-dependent functional responses of NK cells. Overall, our results indicate that the cleavage of the hinge region should be considered with TmAbs treatment and in the development of new molecules.
- |||||||||| Erbitux (cetuximab) / Eli Lilly, EMD Serono
Journal: The Multi-Level Mechanism of Action of a Pan-Ras Inhibitor Explains its Antiproliferative Activity on Cetuximab-Resistant Cancer Cells. (Pubmed Central) - Mar 9, 2021 A mathematical model of the Ras activation cycle predicts that the inhibitor severely reduces the proliferation of different Ras-driven cancer cells, effectively cooperating with Cetuximab to reduce proliferation even of Cetuximab-resistant cancer cell lines. Experimental data confirm the model prediction, indicating that the pan-Ras inhibitor is an appropriate candidate for medicinal chemistry efforts tailored at improving its currently unsatisfactory affinity.
- |||||||||| Erbitux (cetuximab) / Eli Lilly, EMD Serono
Journal: Recurrence of head and neck squamous cell carcinoma in relation to high-risk treatment volume. (Pubmed Central) - Mar 6, 2021 Biomarkers predicting radioresistance should be characterized in p16 positive tumors before widely embarking on de-escalated CRT protocols. Another concern is how to decrease the number of true or marginal misses in p16 negative cases despite multimodality imaging-based target delineation.
- |||||||||| Vistide (cidofovir) / Gilead, Erbitux (cetuximab) / Eli Lilly, EMD Serono
Preclinical, Journal: Differential Efficacy of Novel Antiviral Substances in 3D and Monolayer Cell Culture. (Pubmed Central) - Mar 4, 2021 Antiviral activity of erlotinib and osimertinib was nearly unaffected by the cultivation method similar to the virus-directed antivirals tecovirimat and cidofovir...100-fold more efficient against CPXV in the 3D infection model, similar to previous results with gefitinib...However, in contrast to virus-directed inhibitors, in vitro efficacy of host-directed antivirals might be seriously affected by cell cultivation. Results obtained for afatinib and cetuximab suggest that screening of such drugs in standard monolayer culture might underestimate their potential as antivirals.
- |||||||||| Erbitux (cetuximab) / Eli Lilly, EMD Serono, Herceptin (trastuzumab) / Roche
Journal: IgG-Engineered Protective Antigen for Cytosolic Delivery of Proteins into Cancer Cells. (Pubmed Central) - Mar 4, 2021 Each conjugate shows high specificity for cells expressing human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), respectively, and potent activity across six Tmab- and Cmab-resistant cell lines. The conjugates also exhibit increased pharmacokinetics and pronounced in vivo safety, which shows promise for further therapeutic development.
- |||||||||| Erbitux (cetuximab) / Eli Lilly, EMD Serono
Journal: Cetuximab enhances the anti-tumor function of macrophages in an IL-6 dependent manner. (Pubmed Central) - Mar 3, 2021 The conjugates also exhibit increased pharmacokinetics and pronounced in vivo safety, which shows promise for further therapeutic development. These results indicate a new macrophage-based molecular mechanism explaining the effect of cetuximab in treatment of colorectal cancer.
- |||||||||| EGFR bi-armed autologous activated T cells / Barbara Ann Karmanos Cancer Institute
Trial completion date, Metastases: Anti-CD3 x Anti-Erbitux (clinicaltrials.gov) - Mar 1, 2021 P1, N=30, Active, not recruiting, These results indicate a new macrophage-based molecular mechanism explaining the effect of cetuximab in treatment of colorectal cancer. Trial completion date: Jun 2021 --> Dec 2021
|