^
Association details:
| Biomarker: | KRAS G13D |
|---|---|
| Cancer: | Colorectal Cancer |
| Drug: | temuterkib (LY3214996) (ERK2 inhibitor, ERK1 inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Abstract 5225: Temporal inhibition of ERK is sufficient for tumor growth inhibition in KRAS-mutant or BRAF-mutant tumors
Published date:
05/15/2020
Excerpt:
...Colo205 BRAF V600E colorectal carcinoma and HCT116 KRAS G13D colorectal carcinoma...Additionally, an infusion study with LY3214996 was conducted in rats implanted with HCT116 colorectal carcinoma tumors…Overall assessment of the data in different models suggested that ≥50% target inhibition for 8-16h is enough for significant tumor growth inhibition and regressions by an ERK inhibitor in BRAF-mutant or KRAS-mutant tumors...Therefore, we believe that the PK profile of LY3214996 offers flexibility with dose and schedule to balance efficacy and safety, and to achieve a better therapeutic index in combination therapy for RAS/MAPK pathway altered cancers.
DOI:
10.1158/1538-7445.AM2020-5225
