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Association details:
Biomarker:KRAS mutation
Cancer:Pancreatic Cancer
Drug:RGT-018 (SOS1 inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
Source:
Title:

477 / 8 - Discovery of RGT-018: A potent, selective and orally bioavailable SOS1 inhibitor for mutant KRAS-driven cancers

Published date:
03/15/2023
Excerpt:
In vivo efficacy study data were generated using lung and pancreatic cancer xenograft mouse models with KRAS mutation….Robust anti-proliferation activity was observed when RGT-018 was combined with MEK, KRASG12C, EGFR or CDK2/4/6 inhibitors in vitro. Oral administration of RGT-018 inhibited tumor growth and suppressed KRAS signaling pathway activation in tumor xenografts. Furthermore, combination with MEK or KRASG12C inhibitors led to profound tumor regression.
Secondary therapy:
CDK6 inhibitor; Undisclosed EGFR inhibitor; FWD-K01; MEK Inhibitor; RLY-2139; CDK4 inhibitor