2024 World Conference on Lung Cancer (WCLC) - ePosters-EP.12E.01 OBX02-011, a Novel Oral ALK and EGFR Dual-target Tyrosine Kinase Inhibitor for the Treatment of Advanced NSCLC Patients

EP.12E.01 OBX02-011, a Novel Oral ALK and EGFR Dual-target Tyrosine Kinase Inhibitor for the Treatment of Advanced NSCLC Patients

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OBX02-011 is a novel oral tyrosine kinase inhibitor (TKI) developed as a dual targeting agent for ALK and EGFR mutations associated with advanced non-small-cell lung cancer (NSCLC). Traditional therapies targeting these mutations face limitations due to inevitable resistance, either through mutations within the kinase domains (on-target) or via bypass signaling pathways and phenotypic changes (off-target). Oncobix has addressed these limitations by developing OBX02-011 to overcome such resistance in both ALK and EGFR mutations.<br /><br />The in vitro tests demonstrated the potent inhibitory capabilities of OBX02-011 against a variety of ALK and EGFR mutations. These results showed that OBX02-011 outperformed existing medications like lorlatinib, particularly against resistant ALK mutations. The compound also significantly inhibited EGFR sensitizing and acquired mutations, while showing no significant inhibition of NTRK2 (TRKB), which reduces potential central nervous system side effects.<br /><br />In vivo studies confirmed OBX02-011's efficacy, showcasing its ability to regress tumors both in wild-type and resistant mutant models. These findings suggest a promising efficacy for osimertinib-resistant lung cancer patient-derived xenograft (PDX) models, notably with EGFR exon 19 deletion/T790M/C797S mutations.<br /><br />Overall, OBX02-011 has shown potential as an effective treatment option for NSCLC patients, particularly those exhibiting resistance to current ALK and EGFR inhibitors. It has opened up possibilities for improved management of EGFR and ALK mutation-related resistance in NSCLC, and plans for a first-in-human trial are underway. The novel TKI demonstrates a reduced likelihood of causing CNS-related side effects, a significant advancement in therapy for patients with advanced NSCLC.

Asset Subtitle

SuJin Heo

Meta Tag

Speaker SuJin Heo

Topic Metastatic Non-small Cell Lung Cancer – Targeted Therapy

Keywords

OBX02-011

tyrosine kinase inhibitor

ALK mutations

EGFR mutations

NSCLC

drug resistance

in vitro efficacy

in vivo studies

osimertinib-resistant

CNS side effects