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PI3K pathway inhibitor

Members of the phosphatidylinositol 3-kinase (PI3K) pathway are frequently mutated or amplified in a broad range of cancers. Developing novel molecules that effectively and specifically block the PI3K pathway may inhibit the proliferation and growth of tumor cells and sensitize them to apoptosis. An inhibitor of class I PI3K, GDC-0941, is being developed in collaboration with Piramed Ltd.1

PI3K Pathway Inhibitor
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In preclinical studies, GDC-0941 exhibits selectivity for PI3K over other kinases and inhibits activation of downstream signaling components of the pathway.1 GDC-0941 leads to cell cycle arrest and apoptosis in certain human tumor cell lines.1 In preclinical studies, when administered as a single agent or in combination therapy with other anticancer agents, GDC-0941 has demonstrated significant antitumor activity.1

  1. GDC-0941 is a selective small molecule inhibitor of the kinase PI3K.1

    PI3K Vignette 1

  2. GDC-0941 is designed to bind the ATP-binding pocket of PI3K and prevent formation of the second messenger phosphatidylinositol-3,4,5-triphosphate (PIP3), a key signaling intermediate that transmits signals downstream of PI3K.1,2

    PI3K Vignette 2

  3. In preclinical tumor models, inhibition of PI3K resulted in tumor growth delays likely through the blockage of tumor growth and survival signaling.2,3

    PI3K Vignette 3

References:
1.
Folkes AJ, Ahmadi K, Alderton WK, et al. The identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. J Med Chem. 2008;51:5522-5532.
2.
Knight ZA, Shokat KM. Chemically targeting the PI3K family. Biochem Soc Trans. 2007;35:245-249.
3.
Yuan TL, Cantley LC. PI3K pathway alterations in cancer: variations on a theme. Oncogene. 2008;27:5497-5510.