Drug intelligence / Profile preview

NTQ3617

Development stage
Unknown
Lead developer
Chia Tai-Tianqing Pharmaceutical Group
Modality
Small Molecules
Administration
Oral
01

Overview

NTQ3617 is an orally bioavailable small molecule inhibitor specifically targeting the KRAS G12C mutation, developed by Nanjing Chia Tai Tianqing Pharmaceutical. KRAS is a GTPase that functions as a molecular switch in signaling pathways like MAPK/ERK, which regulate cell proliferation and survival. The G12C mutation results in a constitutive activation of the protein, driving the growth of various malignancies, including non-small cell lung cancer and colorectal cancer. NTQ3617 works by covalently binding to the cysteine residue at position 12 in the inactive GDP-bound state of the KRAS protein, effectively locking it in an off conformation and blocking downstream oncogenic signaling. It is currently in early-stage clinical development for the treatment of advanced solid tumors harboring the KRAS G12C mutation.

02

Targets

KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)MAT2A (Methionine adenosyltransferase 2A)

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