Lumakras (sotorasib) / Amgen 
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  • ||||||||||  Lumakras (sotorasib) / Amgen
    Review, Journal:  Targeting Ras with protein engineering. (Pubmed Central) -  Jul 7, 2023   
    These challenges were recently overcome by the development of the first covalent small-molecule anti-Ras drug, sotorasib, highlighting the efficacy of Ras inhibition as a therapeutic strategy...In parallel, significant advancements have been made in intracellular protein delivery, enabling the delivery of the engineered anti-Ras agents into the cellular cytoplasm. These advances offer a promising path for targeting Ras proteins and other challenging drug targets, opening up new opportunities for drug discovery and development.
  • ||||||||||  Lumakras (sotorasib) / Amgen
    Journal:  Sotorasib (Lumakras) for NSCLC. (Pubmed Central) -  Jun 24, 2023   
    These observations may help guide use of sotorasib in the clinic and may help inform the next generation of KRAS G12C-targeted clinical trials. No abstract available
  • ||||||||||  5-fluorouracil / Generic mfg., OTS514 / OncoTherapy, Lumakras (sotorasib) / Amgen
    Journal:  KRAS mutation-induced TOPK overexpression contributes to tumour progression in non-small cell lung cancer. (Pubmed Central) -  Jun 19, 2023   
    In the in vivo tumorigenesis model, the administration of TOPK inhibitor OTS514 enhanced the anticancer effect of 5-FU, and the combinatory use of OTS514 and KRAS inhibitor AMG510 showed synergistic anti-tumour effect. These results suggest that KRAS-TOPK axis contributes to the progression of NSCLC and targeting this axis could synergize with anticancer effect of the existing chemotherapeutics.
  • ||||||||||  Journal:  Discovery of a highly potent pan-RAF inhibitor IHMT-RAF-128 for cancer treatment. (Pubmed Central) -  Jun 19, 2023   
    In this study, we developed a highly potent pan-RAF inhibitor, IHMT-RAF-128, which exhibited similarly high efficacies in inhibiting both partners of the RAF dimer, and showed potent anti-tumor efficacy against a variety of cancer cells harboring either RAF or RAS mutations, especially Adagrasib and Sotorasib (AMG510) resistant-KRAS-G12C secondary mutations, such as KRAS-G12C-Y96C and KRAS-G12C-H95Q...Furthermore, IHMT-RAF-128 exhibited potent anti-tumor efficacy on xenograft mouse tumor models in a dose-dependent manner without any obvious toxicities. Together, these results support further investigation of IHMT-RAF-128 as a potential clinical drug candidate for the treatment of cancer patients with RAF or RAS mutations.
  • ||||||||||  Lumakras (sotorasib) / Amgen, ladarixin (DF-2156A) / Dompe
    Enrollment change, Trial completion date, Trial initiation date, Trial primary completion date, Metastases:  Ladarixin With Sotorasib in Advanced NSCLC (clinicaltrials.gov) -  Jun 15, 2023   
    P1,  N=40, Not yet recruiting, 
    These results demonstrate the long-term benefit of sotorasib, including in subgroups with poor prognosis. N=12 --> 40 | Trial completion date: Apr 2025 --> Jul 2026 | Initiation date: Apr 2023 --> Jul 2023 | Trial primary completion date: Apr 2024 --> Jul 2025
  • ||||||||||  DT2216 / Dialectic Therap, MRTX1133 / Mirati, Lumakras (sotorasib) / Amgen
    Journal:  Targeting KRAS in pancreatic cancer: Emerging therapeutic strategies. (Pubmed Central) -  Jun 7, 2023   
    The inhibitors targeting G12D mutation (such as MRTX1133) have been recently developed, whereas those targeting other mutations are still lacking...In addition, we recently demonstrated that the combination of sotorasib with DT2216 (a BCL-X-selective degrader) synergistically inhibits G12C-mutated pancreatic cancer cell growth in vitro and in vivo...This chapter will review KRAS biochemistry, signaling pathways, different mutations, emerging KRAS-targeted therapies, and combination strategies. Finally, we discuss challenges associated with KRAS targeting and future directions, emphasizing pancreatic cancer.
  • ||||||||||  JAB-3312 / Jacobio Pharma
    Trial completion date, Trial primary completion date, Metastases:  JAB-3312 Based Combination Therapy in Adult Patients With Advanced Solid Tumors (clinicaltrials.gov) -  May 18, 2023   
    P1/2,  N=200, Recruiting, 
    Trial primary completion date: May 2026 --> May 2027 Trial completion date: Jun 2023 --> Feb 2024 | Trial primary completion date: Mar 2023 --> Jan 2024
  • ||||||||||  Krazati (adagrasib) / Mirati, Lumakras (sotorasib) / Amgen
    Review, Journal, IO biomarker:  The Therapeutic Landscape for KRAS-Mutated Colorectal Cancers. (Pubmed Central) -  May 16, 2023   
    Treatment resistance remains an issue with combination treatment regimens including indirect pathway inhibition and immunotherapy providing possible ways to combat this. While KRAS-mutant selective therapy has come a long way, more work is required to make this an effective and viable option for patients with colorectal cancer.
  • ||||||||||  MODULE 4: Targeting MET, HER2 and KRAS Alterations in NSCLC (Hilton Chicago, Grand Ballroom ) -  May 15, 2023 - Abstract #ASCO2023ASCO_7040;    
    This event is organized and accredited by Research to Practice and supported through educational grants provided by AstraZeneca Pharmaceuticals LP, Daiichi Sankyo Inc, Janssen Biotech Inc, administered by Janssen Scientific Affairs LLC, Lilly, Novocure Inc, Regeneron Pharmaceuticals Inc, and Takeda Pharmaceuticals USA Inc. Key efficacy and safety findings with capmatinib or tepotinib for patients with NSCLC with MET exon 14 mutations; current clinical role and practical implementation Clinical activity observed with commercially available MET inhibitors in patients with high-level MET amplification Mechanism of action of telisotuzumab vedotin; available efficacy and safety findings with telisotuzumab vedotin for NSCLC with c-MET overexpression Available efficacy and safety outcomes from the Phase II DESTINY-Lung02 study evaluating trastuzumab deruxtecan (T-DXd) for previously treated NSCLC with a HER2 mutation Recent FDA approval of T-DXd and current role in therapy for HER2-mutated disease Efficacy outcomes with T-DXd for HER2-overexpressing NSCLC; potential role in this setting Principal efficacy and safety findings with sotorasib or adagrasib for patients with previously treated NSCLC with a KRAS G12C mutation
  • ||||||||||  D-1553 / InventisBio
    Preclinical, Journal:  D-1553: A novel KRAS inhibitor with potent and selective cellular and in vivo antitumor activity. (Pubmed Central) -  May 9, 2023   
    The combination of D-1553 with chemotherapy, MEK inhibitor, or SHP2 inhibitor showed stronger potency on tumor growth inhibition or regression compared to D-1553 alone. These findings support the clinical evaluation of D-1553 as an efficacious drug candidate, both as a single agent or in combination, for patients with solid tumors harboring KRAS mutation.
  • ||||||||||  Review, Journal:  Multiple Strategies to Develop Small Molecular KRAS Directly Bound Inhibitors. (Pubmed Central) -  May 2, 2023   
    Various KRAS-directed inhibitors have been developed, including the FDA-approved drugs sotorasib and adagrasib, KRAS-G12D inhibitor MRTX1133, and KRAS-G12V inhibitor JAB-23000, etc. The different strategies greatly promote the development of KRAS inhibitors. Herein, the strategies are summarized, which would shed light on the drug discovery for both KRAS and other "undruggable" targets.
  • ||||||||||  Cyramza (ramucirumab) / Eli Lilly, Lumakras (sotorasib) / Amgen
    Clinical data, Retrospective data, Review, Journal:  A Multicenter Retrospective Chart Review of Clinical Outcomes Among Patients With KRAS G12C Mutant Non-Small Cell Lung Cancer. (Pubmed Central) -  May 1, 2023   
    Herein, the strategies are summarized, which would shed light on the drug discovery for both KRAS and other "undruggable" targets. In this large, multicenter retrospective chart review of patients with KRAS G12C mutant NSCLC we observed a relatively short median rwPFS of 4.6 months among 10 patients with KRAS G12C mutant NSCLC treated with docetaxel with or without ramucirumab in the second-line setting, which aligns with the recently reported CodeBreak 200 dataset.
  • ||||||||||  Krazati (adagrasib) / Mirati, Lumakras (sotorasib) / Amgen
    Journal:  TEAD Inhibitors Sensitize KRAS Inhibitors via Dual Cell Cycle Arrest in KRAS-Mutant NSCLC. (Pubmed Central) -  Apr 28, 2023   
    Mechanistically, the dual inhibition of KRAS and TEAD results in the downregulation of MYC and E2F signatures and in the alteration of the G2/M checkpoint, converging in an increase in G1 and a decrease in G2/M cell cycle phases. Our data suggest that the co-inhibition of KRAS and TEAD leads to a specific dual cell cycle arrest in KRAS NSCLC cells.
  • ||||||||||  Lumakras (sotorasib) / Amgen
    Journal:  CodeBreaK 200: Sotorasib (AMG510) Has Broken the KRAS G12C+ NSCLC Enigma Code. (Pubmed Central) -  Apr 27, 2023   
    At the European Society of Medical Oncology (ESMO) 2022 annual meeting, sotorasib achieved a statistically significant improved PFS over docetaxel (HR = 0.66; 95% CI: 0...The modest magnitude of PFS improvement of 1.1 months (from 4.5 months to 5.6 months) and the ORR of 28% led to a vigorous debate on whether sotorasib was indeed a true breakthrough. In this pros and cons debate, we argue thatsotorasib has achieved a true breakthrough.
  • ||||||||||  Lumakras (sotorasib) / Amgen
    Journal:  CodeBreak 200: Sotorasib Has Not Broken the KRAS Enigma Code. (Pubmed Central) -  Apr 27, 2023   
    With novel agents and combinations, the field of KRAS G12C is quickly evolving. While sotorasib was an exciting start, there is more to do to break the KRAS G12C Enigma code.