OBX02-011 / Oncobix - LARVOL DELTA

OBX02-011, a Novel Oral ALK and EGFR Dual-target Tyrosine Kinase Inhibitor for the Treatment of Advanced NSCLC Patients (IASLC-WCLC 2024) - "In addition, OBX02-011 demonstrated superior inhibition compared to lorlatinib in ALK_C1156Y, G1202R, and L1196M mutations associated with clinical resistance to the first generation ALK inhibitor crizotinib and/or the second generation ALK inhibitors alectinib, brigatinib, and ceritinib...OBX02-011 also demonstrated tumor regression in the osimertinib-resistant lung cancer patient-derived xenograft model with EGFR_exon 19 deletion/T790M/C797S...In vitro cell-based assay results showed that OBX02-011 does not inhibit NTRK2 (TRKB), which causes neurological toxicity, and there were also no significant findings for OBX02-011 in the CNS safety pharmacology study. Based on these studies, a first-in-human study will be conducted in 2024 to address the current resistance mechanisms in ALK-positive or EGFR-positive NSCLC patients and prolong progression free survival."

Clinical • Metastases • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR • EML4 • NTRK2

C&R Research conducts phase 1 clinical trial for Oncobix non-small cell lung cancer [Google translation] (HIT News) - "C&R Research...announced on the 23rd that it is conducting a phase 1 clinical trial of Oncobix...for Non-Small Cell Lung Cancer...Currently, as OBX02-011 has received IND approval from the Ministry of Food and Drug Safety, clinical trials are scheduled to be conducted on patients with non-small cell lung cancer who have developed resistance or relapsed after being prescribed existing ALK or EGFR treatments....'The clinical trial design to be conducted together with C&R Research is a phase 1, first human subject, open-label, dose escalation and dose expansion clinical trial of OBX02-011, an oral ALK/EGFR inhibitor, targeting patients with advanced non-small cell lung cancer.'" "

Clinical protocol • New P1 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

The reversible fourth-generation EGFR tyrosine kinase inhibitor OBX02-011 overcomes C797S-mediated resistance in lung cancer. (PubMed, Cancer Res) - "Osimertinib is an irreversible third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that was initially developed to overcome the EGFR T790M mutation and is used as a standard therapy in patients with advanced non-small cell lung cancer (NSCLC) with EGFR-activating mutations. Additionally, in transgenic mouse models (EGFRL858R/T790M/C797S), OBX02-011 treatment effectively inhibited tumor growth and EGFR activity, leading to enhanced survival. Collectively, these results suggest that OBX02-011 may be a promising new EGFR TKI to overcome C797S-mediated resistance in NSCLC."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

OBX02-011, a reversible fourth-generation EGFR-TKI, overcomes C797S-mediated resistance in non-small cell lung cancer (AACR 2022) - "Osimertinib, an irreversible, third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) that is initially developed to overcome EGFR T790M mutation, and use as standard therapy in patients with advanced non-small cell lung cancer (NSCLC) including EGFR activating mutations as well as EGFR T790M mutation. Additionally, we evaluated the efficacy of OBX02-011 in transgenic models (EGFRL858R+T790M+C797S), showing the enhanced survival, and inhibition of tumor growth and EGFR activity. Collectively, our data suggest that OBX02-011 may be promising new EGFR-TKI to overcome C797S-mediated resistance in NSCLC."

Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR