cobimetinib + ipatasertib

Cobimetinib + ipatasertib is an investigational oral combination of a selective allosteric MEK1/2 inhibitor (cobimetinib) with an ATP-competitive pan-AKT inhibitor (ipatasertib) intended to achieve dual blockade of the MAPK (RAS/RAF/MEK/ERK) and PI3K/AKT signaling pathways in cancers with pathway activation such as PTEN loss or PIK3CA/AKT1 alterations. In a phase Ib study in advanced solid tumors (NCT01562275), dose-escalation identified maximum tolerated doses and an intermittent-dosing recommended phase II dose; pharmacodynamic analyses showed pathway blockade and increased IFNγ/PD-L1 expression, with partial responses observed in PTEN-low, KRAS-mutant gynecologic cancers, though overall tolerability and efficacy were limited.[1][3][2][4]

Other names

MEK inhibitor cobimetinib + AKT inhibitor ipatasertibcobimetinib plus ipatasertib