Journal of Medicinal Chemistry Paper Reports Orally Bioavailable GSPT1 Degrader Active Against Glioblastoma
Start here
A study published in the Journal of Medicinal Chemistry describes LG-NE-29, a molecular glue degrader targeting GSPT1 that achieves 76% oral bioavailability and shows marked in vivo activity against glioblastoma. The compound also displays excellent metabolic stability. The authors note that earlier GSPT1 molecular glues were hampered by poor pharmacokinetic properties, limited oral exposure, and weak efficacy in solid tumors, positioning LG-NE-29 as an advance on those fronts. The findings are preclinical, based on the reported in vivo work, and no clinical data in patients are included in this coverage.
Written by a model from the reports · updated 2 hours ago
Coverage timeline
Follow the coverage to see the different angles.
- mp.weixin.qq.comJMC Paper Reports In Vivo Anti-GBM Activity and 76% Oral Bioavailability for GSPT1 Molecular Glue Degrader LG-NE-29
LG-NE-29 is a GSPT1 molecular glue degrader with high oral bioavailability that shows marked in vivo activity against glioblastoma. Its oral bioavailability is F = 76%, with excellent metabolic stability. The paper notes that early GSPT1 molecular glues suffered from poor pharmacokinetic properties, limited oral exposure, and weak efficacy in solid tumors.
Heat trend for this story
Heat now 9·Peak in the comparable set 10 (Oct 24 18:00)·Change over 24h in the comparable set –·Participants now 1
Participants counted above, heat below. The trend compares only the participants observed in full throughout, so its set can be smaller than the heat figure itself. Move the pointer or click the chart for an hour's reading; the left and right arrow keys work too.