Drug intelligence / Profile preview

GDC-6036 + inavolisib

Development stage
Unknown
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral
01

Overview

GDC-6036 + inavolisib is an investigational combination therapy comprising two targeted small molecule inhibitors: GDC-6036 (also known as divarasib), a potent and selective covalent inhibitor of KRAS G12C, and inavolisib (GDC-0077), an oral selective inhibitor of phosphoinositide 3-kinase alpha (PI3Kα). This combination aims to block key oncogenic drivers simultaneously—KRAS G12C-mediated signaling and PI3K pathway activation—which are implicated in the growth and survival of multiple solid tumors, especially those with respective KRAS G12C and PIK3CA mutations. Both agents are being studied primarily in patients with advanced or metastatic solid tumors such as non-small cell lung cancer (NSCLC) and other tumors harboring KRAS G12C mutations. The combination is under early-phase clinical evaluation for safety, pharmacokinetics, and preliminary antitumor activity[1][2][4][6][7][10].

Other names
GDC-6036 + GDC-0077
02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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