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GDC-0349 is a potent, selective, ATP-competitive inhibitor of (Mammalian target of rapamycin) mTOR with Ki value of 3.8nM [1].

GDC-0349 is a remarkably selective mTOR inhibitor, with less than 25% inhibition of 266 kinases, including all isoforms of PI3K. GDC-0349 inhibited mTOR downstream markers , involving phospho-Akt(s473) and phospho-4EBP1 in an in vivo PK/PD study in mouse, consistent with an inhibition of mTORC1/mTORC2 complexes [1].

GDC-0349 inhibited tumor growth in a dose-dependent manner when dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation). GDC-0349 was also efficacious in other xenograft models, including PC3 (PTEN null) and 786-0 (VHL mutant). However, GDC-0349 showed only modest tumor growth delay in the A549 mouse xenograft model (KRas mutant, LKB1 deficient) [1].

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