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1. CAL-101: a phosphatidylinositol-3-kinase p110-delta inhibitor for the treatment of lymphoid malignancies. Expert Opin Investig Drugs. 2012 Jan;21(1):15-22. doi: 10.1517/13543784.2012.640318. Epub 2011 Nov 24.
CAL-101 is a highly selective inhibitor of p110δ.
2. The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood. 2011 Sep 29;118(13):3603-12. doi: 10.1182/blood-2011-05-352492. Epub 2011 Jul 29.
CAL-101 is a selective inhibitor of PI3Kδ that induces rapid lymph node shrinkage and a transient lymphocytosis in CLL cells. CAL-101 not only directly inhibits the pro-survival PI3K pathway but also disrupts CLL-microenvironment interactions, where it inhibits chemotaxis and migration of CLL cell, down-regulates BCR-induced chemokines secretion, reduces survival signals and suppresses ERK activation.
3. PI3Kδ inhibitor, GS-1101 (CAL-101), attenuates pathway signaling, induces apoptosis, and overcomes signals from the microenvironment in cellular models of Hodgkin lymphoma. Blood. 2012 Feb 23;119(8):1897-900. doi: 10.1182/blood-2011-10-386763. Epub 2011 Dec 30.
CAL-101, an oral inhibitor of PI3Kδ, inhibited AKT phosphorylation and stroma-induced Akt activation, reduced CCL5 production and dose-dependently induced apoptosis in HL cells. Moreover, addition of everolimu could enhance the anti-HL activity of CAL-101.
4. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 2011 Jan 13;117(2):591-4. doi: 10.1182/blood-2010-03-275305. Epub 2010 Oct 19.
CAL-101 is an inhibitor of p110δ that blocks phosphatidylinositol-3-kinase signaling in a wide range of B-cell malignancies leading to decreased phosphorylation of Akt and other downstream effectors, increased polu(ADP-ribose) polymerase and caspase cleavage and induced apoptosis.
5. Translating PI3K-Delta Inhibitors to the Clinic in Chronic Lymphocytic Leukemia: The Story of CAL-101 (GS1101). Am Soc Clin Oncol Educ Book. 2012;32:691-694. doi: 10.14694/EdBook_AM.2012.32.691.
CAL-101, a p110 delta inhibitor, has been developed fr the treatment of chronic lymphoid malignancies including CLL.
Brian J. Lannutti, Sarah A. Meadows, Sarah E. M. Herman, Adam Kashishian, Bart Steiner, Amy J. Johnson, John C. Byrd, Jeffrey W. Tyner, Marc M. Loriaux, Mike Deininger, Brian J. Druker, Kamal D. Puri, Roger G. Ulrich, and Neill A. Giese. CAL-101, a p110δ selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 2011; 117(2): 591 – 594.
Sarah E. M. Herman, Amber L. Gordon, Amy J. Wagner, Nyla A. Heerema, Weiqiang Zhao, Joseph M. Flynn, Jeffrey Jones, Leslie Andritsos, Kamal D. Puri, Brian J. Lannutti, Neill A. Giese, Xiaoli Zhang, Lai Wei, John C. Byrd, Amy J. Johnson. Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood. 2010; 116(12): 2078 – 88.