Drug intelligence / Profile preview

GDC-0980 + rabeprazole

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

Overview

**GDC-0980 + rabeprazole** is a drug combination studied to evaluate the effects of rabeprazole, a proton pump inhibitor, on the pharmacokinetics of GDC-0980 (apitolisib), a dual inhibitor of class I phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) kinase[1][3][4]. **GDC-0980 (apitolisib)** modulates cancer cell proliferation by blocking PI3K/mTOR signaling, thus suppressing tumor growth[3][4]. **Rabeprazole** decreases gastric acid secretion by irreversible inhibition of H+,K+-ATPase in parietal cells, used for acid-related gastrointestinal disorders[2][5]. The combination drug has been evaluated in a phase 1 pharmacokinetic study in healthy volunteers to assess its effect on GDC-0980 bioavailability[1].

Brand names
AciphexPariet
Other names
rabeprazoleapitolisib
02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)Fgr proto-oncogene tyrosine-protein kinaseMAP3K9 (Mixed lineage kinase 1)SYK (Spleen Tyrosine Kinase)YES1 (YES proto-oncogene 1 tyrosine kinase)ATP4A (Potassium–transporting ATPase alpha chain 1)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CD (Phosphatidylinositol 3-kinase delta)mTOR (Mammalian target of rapamycin kinase)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PAK4

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