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MK-1084 is a selective KRAS G12C inhibitor that is currently in Phase I clinical trial (NCT05067283). MK-1084 exhibits anticancer activity and can be used either alone or in combination with pembrolizumab (HY-P9902) for cancer research[1]. | [in vivo]
MK-1084 (10-30 mg/kg, po for 14 days) exhibits antitumor efficacy in mouse MiaPaCa-2 xenograft models[2].
MK-1084 exhibits a good pharmacokinetic characteristics with a plasma clearance of 22 mL/min/kg, a mean residence time MRT of 1.1 h and an oral bioavailability of 61%[2]. | Animal Model: | Mouse MiaPaCa-2 xenograft models[2] | | Dosage: | 10-30 mg/kg | | Administration: | po for 14 days | | Result: | Inhibited tumor growth. |
| [References]
[1] Rojas C, et al. 663P Safety and preliminary efficacy of the KRAS G12C inhibitor MK-1084 in solid tumors and in combination with pembrolizumab in NSCLC[J]. Annals of Oncology, 2023, 34: S466-S467.
[2] Ma X, et al., Discovery of MK-1084: An Orally Bioavailable and Low-Dose KRASG12C Inhibitor. J Med Chem. 2024 Jul 11;67(13):11024-11052. DOI:10.1021/acs.jmedchem.4c00572 |
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