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Description of GDC-0980: GDC-0980 is a dual PI3 kinase/mTOR inhibitor, is also an orally available agent targeting phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinase in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR kinase inhibitor GDC-0980 inhibits both PI3K kinase and mTOR kinase, which may result in tumor cell apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
Current developer: Roche/Genentech.
GCD-0980 is potent across PI3K class I isoforms with IC(50)s of 5, 27, 7, and 14 nM for PI3Kα, β, δ, and γ, respectively, inhibits mTOR with a K(i) of 17 nM yet is highly selective versus a large panel of kinases including others in the PIKK family. On the basis of the cell potency, low clearance in mouse, and high free fraction, 2 demonstrated significant efficacy in mouse xenografts when dosed as low as 1 mg/kg orally and is currently in phase I clinical trials for cancer. [source: J Med Chem. 2011 Nov 10;54(21):7579-87.]
1: Wallin JJ, Edgar KA, Guan J, Berry M, Prior WW,
Lee L, Lesnick JD, Lewis C, Nonomiya J, Pang J, Salphati L, Olivero AG,
Sutherlin DP, O'Brien C, Spoerke JM, Patel S, Lensun L, Kassees R, Ross
L, Lackner MR, Sampath D, Belvin M, Friedman LS. GDC-0980 is a novel
class I PI3K/mTOR kinase inhibitor with robust activity in cancer models
driven by the PI3K pathway. Mol Cancer Ther. 2011 Oct 13. [Epub ahead of
print] PubMed PMID: 21998291.
(Keyword; CAS#; MedKoo code#)
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