lifirafenib (BGB-283)

P1, N=91, Completed, BeiGene | Trial completion date: Feb 2026 --> Oct 2025 | Active, not recruiting --> Completed

RAMRGs serve as useful biomarkers to predict prognosis in LUAD patients, and may guide the immunotherapy regimen.

Lifirafenib (Type II) + encorafenib (Type I½) was highly synergistic against both NRAS - and KRAS -mutant lines, while synergy of lifirafenib + SB590885 (Type I) was specific to NRAS -mutants. Assessment of leukemia burden in bone marrow and spleen during treatment further showed site-specific efficacy against circulating and spleen-resident blasts for both combinations. In summary, we report that our structure based-modelling approach can effectively identify novel, non-obvious, and well-tolerated RAFi combinations that are highly effective against in vitro and in vivo models, thereby suggesting alternative potential therapeutic strategies for high-risk RAS -mutant AML.

This study provided potential prognostic biomarkers for LUAD and might facilitate the development of effective immunotherapy strategies for LUAD patients.

BGB-283 was a candidate for LUAD targeting VGF. Our study elucidates the impact of GCGs on LUAD prognosis and immune responses, offering insights for prognostic forecasting and immunotherapeutic strategies for LUAD patients.

P1, N=93, Active, not recruiting, BeiGene | Recruiting --> Active, not recruiting

Therefore, this study aims to disover potential TMPRSS4 inhibitors that have better binding affinity than the approved inhibitors: 2-hydroxydiarylamide and tyroserleutide...Moreover, through a systematic analysis, MD simulations and MM-GBSA binding free energy calculations revealed that the best candidates Ergotamine, S55746, NPC478048, Lifirafenib, and NPC77101 are highly stable drug candidates in complex with TMPRSS4, displaying low RMSD and RMSF values with strong binding stability. Among these compounds, Ergotamine showed the most favorable binding energy (-33.73 kcal/mol). Overall, our in silico results revealed that these compounds could act as potent TMPRSS4 inhibitors and need to be validated by future experimental studies.

P1, N=105, Recruiting, BeiGene | Phase classification: P1b --> P1

P1, N=131, Completed, BeiGene | Phase classification: P1a/1b --> P1

A T-cell mediated killing sensitivity gene-based prognostic score TTKPI showed good accuracy in predicting survival in AML. TTKPI corresponded to functional and immunological features of the tumor microenvironment including checkpoint expression patterns and should be investigated for precision medicine approaches.

P1b, N=105, Recruiting, BeiGene | Trial completion date: Apr 2024 --> Feb 2026 | Trial primary completion date: Mar 2024 --> Sep 2025

This led to the development of sotorasib as a second-line treatment of KRAS mutant non-small cell lung cancer. Considerable effort also has been expended to develop MAP kinase and PI3-kinase pathway inhibitors as indirect RAS antagonists.