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CCR 20th Anniversary Commentary: Determining a Pharmacokinetic/Pharmacodynamic Relationship for Sunitinib—A Look Back.

Mendel DB, Cherrington JM, Laird AD.

Clin Cancer Res. 2015 Jun 1;21(11):2415-7. doi: 10.1158/1078-0432.CCR-14-2557.


Evaluation of the potential for pharmacokinetic and pharmacodynamic interactions between dutogliptin, a novel DPP4 inhibitor, and metformin, in type 2 diabetic patients.

Li J, Klemm K, O'Farrell AM, Guler HP, Cherrington JM, Schwartz S, Boyea T.

Curr Med Res Opin. 2010 Aug;26(8):2003-10. doi: 10.1185/03007995.2010.491266.


Dutogliptin, a selective DPP4 inhibitor, improves glycaemic control in patients with type 2 diabetes: a 12-week, double-blind, randomized, placebo-controlled, multicentre trial.

Pattzi HM, Pitale S, Alpizar M, Bennett C, O'Farrell AM, Li J, Cherrington JM, Guler HP; PHX1149-PROT202 Study Group.

Diabetes Obes Metab. 2010 Apr;12(4):348-55. doi: 10.1111/j.1463-1326.2010.01195.x.


The dipeptidyl peptidase-4 inhibitor PHX1149 improves blood glucose control in patients with type 2 diabetes mellitus.

Garcia-Soria G, Gonzalez-Galvez G, Argoud GM, Gerstman M, Littlejohn TW 3rd, Schwartz SL, O'Farrell AM, Li X, Cherrington JM, Bennett C, Guler HP.

Diabetes Obes Metab. 2008 Apr;10(4):293-300. doi: 10.1111/j.1463-1326.2008.00868.x.


Pharmacokinetic and pharmacodynamic assessments of the dipeptidyl peptidase-4 inhibitor PHX1149: double-blind, placebo-controlled, single- and multiple-dose studies in healthy subjects.

O'Farrell AM, van Vliet A, Abou Farha K, Cherrington JM, Campbell DA, Li X, Hanway D, Li J, Guler HP.

Clin Ther. 2007 Aug;29(8):1692-705.


FLT3 K663Q is a novel AML-associated oncogenic kinase: Determination of biochemical properties and sensitivity to Sunitinib (SU11248).

Schittenhelm MM, Yee KW, Tyner JW, McGreevey L, Haley AD, Town A, Griffith DJ, Bainbridge T, Braziel RM, O'Farrell AM, Cherrington JM, Heinrich MC.

Leukemia. 2006 Nov;20(11):2008-14. Epub 2006 Sep 14.


SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity.

Patyna S, Laird AD, Mendel DB, O'farrell AM, Liang C, Guan H, Vojkovsky T, Vasile S, Wang X, Chen J, Grazzini M, Yang CY, Haznedar JO, Sukbuntherng J, Zhong WZ, Cherrington JM, Hu-Lowe D.

Mol Cancer Ther. 2006 Jul;5(7):1774-82.


Contribution of individual targets to the antitumor efficacy of the multitargeted receptor tyrosine kinase inhibitor SU11248.

Potapova O, Laird AD, Nannini MA, Barone A, Li G, Moss KG, Cherrington JM, Mendel DB.

Mol Cancer Ther. 2006 May;5(5):1280-9.


A phase 1 study of SU11248 in the treatment of patients with refractory or resistant acute myeloid leukemia (AML) or not amenable to conventional therapy for the disease.

Fiedler W, Serve H, Döhner H, Schwittay M, Ottmann OG, O'Farrell AM, Bello CL, Allred R, Manning WC, Cherrington JM, Louie SG, Hong W, Brega NM, Massimini G, Scigalla P, Berdel WE, Hossfeld DK.

Blood. 2005 Feb 1;105(3):986-93. Epub 2004 Sep 30.


Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells.

Yee KW, Schittenhelm M, O'Farrell AM, Town AR, McGreevey L, Bainbridge T, Cherrington JM, Heinrich MC.

Blood. 2004 Dec 15;104(13):4202-9. Epub 2004 Aug 10.


Effects of SU5416, a small molecule tyrosine kinase receptor inhibitor, on FLT3 expression and phosphorylation in patients with refractory acute myeloid leukemia.

O'Farrell AM, Yuen HA, Smolich B, Hannah AL, Louie SG, Hong W, Stopeck AT, Silverman LR, Lancet JE, Karp JE, Albitar M, Cherrington JM, Giles FJ.

Leuk Res. 2004 Jul;28(7):679-89.


Gene expression profiling of human colon xenograft tumors following treatment with SU11248, a multitargeted tyrosine kinase inhibitor.

Morimoto AM, Tan N, West K, McArthur G, Toner GC, Manning WC, Smolich BD, Cherrington JM.

Oncogene. 2004 Feb 26;23(8):1618-26.


SU11248 inhibits tumor growth and CSF-1R-dependent osteolysis in an experimental breast cancer bone metastasis model.

Murray LJ, Abrams TJ, Long KR, Ngai TJ, Olson LM, Hong W, Keast PK, Brassard JA, O'Farrell AM, Cherrington JM, Pryer NK.

Clin Exp Metastasis. 2003;20(8):757-66.


Proof of target for SU11654: inhibition of KIT phosphorylation in canine mast cell tumors.

Pryer NK, Lee LB, Zadovaskaya R, Yu X, Sukbuntherng J, Cherrington JM, London CA.

Clin Cancer Res. 2003 Nov 15;9(15):5729-34.


An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients.

O'Farrell AM, Foran JM, Fiedler W, Serve H, Paquette RL, Cooper MA, Yuen HA, Louie SG, Kim H, Nicholas S, Heinrich MC, Berdel WE, Bello C, Jacobs M, Scigalla P, Manning WC, Kelsey S, Cherrington JM.

Clin Cancer Res. 2003 Nov 15;9(15):5465-76.


A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo.

Christensen JG, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R, Lipson KE, Ramphal J, Do S, Cui JJ, Cherrington JM, Mendel DB.

Cancer Res. 2003 Nov 1;63(21):7345-55.


Preclinical evaluation of the tyrosine kinase inhibitor SU11248 as a single agent and in combination with "standard of care" therapeutic agents for the treatment of breast cancer.

Abrams TJ, Murray LJ, Pesenti E, Holway VW, Colombo T, Lee LB, Cherrington JM, Pryer NK.

Mol Cancer Ther. 2003 Oct;2(10):1011-21.


Hair depigmentation is a biological readout for pharmacological inhibition of KIT in mice and humans.

Moss KG, Toner GC, Cherrington JM, Mendel DB, Laird AD.

J Pharmacol Exp Ther. 2003 Nov;307(2):476-80. Epub 2003 Sep 9.


The combination of the tyrosine kinase receptor inhibitor SU6668 with paclitaxel affects ascites formation and tumor spread in ovarian carcinoma xenografts growing orthotopically.

Garofalo A, Naumova E, Manenti L, Ghilardi C, Ghisleni G, Caniatti M, Colombo T, Cherrington JM, Scanziani E, Nicoletti MI, Giavazzi R.

Clin Cancer Res. 2003 Aug 15;9(9):3476-85.


Phase I dose-escalating study of SU11654, a small molecule receptor tyrosine kinase inhibitor, in dogs with spontaneous malignancies.

London CA, Hannah AL, Zadovoskaya R, Chien MB, Kollias-Baker C, Rosenberg M, Downing S, Post G, Boucher J, Shenoy N, Mendel DB, McMahon G, Cherrington JM.

Clin Cancer Res. 2003 Jul;9(7):2755-68.


SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer.

Abrams TJ, Lee LB, Murray LJ, Pryer NK, Cherrington JM.

Mol Cancer Ther. 2003 May;2(5):471-8.


Phase II study of SU5416--a small-molecule, vascular endothelial growth factor tyrosine-kinase receptor inhibitor--in patients with refractory myeloproliferative diseases.

Giles FJ, Cooper MA, Silverman L, Karp JE, Lancet JE, Zangari M, Shami PJ, Khan KD, Hannah AL, Cherrington JM, Thomas DA, Garcia-Manero G, Albitar M, Kantarjian HM, Stopeck AT.

Cancer. 2003 Apr 15;97(8):1920-8.


Expression profiling of blood samples from an SU5416 Phase III metastatic colorectal cancer clinical trial: a novel strategy for biomarker identification.

DePrimo SE, Wong LM, Khatry DB, Nicholas SL, Manning WC, Smolich BD, O'Farrell AM, Cherrington JM.

BMC Cancer. 2003 Feb 7;3:3. Epub 2003 Feb 7.


SU5416, a small molecule tyrosine kinase receptor inhibitor, has biologic activity in patients with refractory acute myeloid leukemia or myelodysplastic syndromes.

Giles FJ, Stopeck AT, Silverman LR, Lancet JE, Cooper MA, Hannah AL, Cherrington JM, O'Farrell AM, Yuen HA, Louie SG, Hong W, Cortes JE, Verstovsek S, Albitar M, O'Brien SM, Kantarjian HM, Karp JE.

Blood. 2003 Aug 1;102(3):795-801. Epub 2003 Mar 20.


In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship.

Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB, Murray LJ, Carver J, Chan E, Moss KG, Haznedar JO, Sukbuntherng J, Blake RA, Sun L, Tang C, Miller T, Shirazian S, McMahon G, Cherrington JM.

Clin Cancer Res. 2003 Jan;9(1):327-37.


SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo.

O'Farrell AM, Abrams TJ, Yuen HA, Ngai TJ, Louie SG, Yee KW, Wong LM, Hong W, Lee LB, Town A, Smolich BD, Manning WC, Murray LJ, Heinrich MC, Cherrington JM.

Blood. 2003 May 1;101(9):3597-605. Epub 2003 Jan 16.


Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents.

Laird AD, Cherrington JM.

Expert Opin Investig Drugs. 2003 Jan;12(1):51-64. Review.


SU5416 and SU5614 inhibit kinase activity of wild-type and mutant FLT3 receptor tyrosine kinase.

Yee KW, O'Farrell AM, Smolich BD, Cherrington JM, McMahon G, Wait CL, McGreevey LS, Griffith DJ, Heinrich MC.

Blood. 2002 Oct 15;100(8):2941-9.


Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors.

Liao AT, Chien MB, Shenoy N, Mendel DB, McMahon G, Cherrington JM, London CA.

Blood. 2002 Jul 15;100(2):585-93. Erratum in: Blood 2002 Oct 15;100(8):2696.


SU6668 inhibits Flk-1/KDR and PDGFRbeta in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice.

Laird AD, Christensen JG, Li G, Carver J, Smith K, Xin X, Moss KG, Louie SG, Mendel DB, Cherrington JM.

FASEB J. 2002 May;16(7):681-90.


The antiangiogenic agents SU5416 and SU6668 increase the antitumor effects of fractionated irradiation.

Ning S, Laird D, Cherrington JM, Knox SJ.

Radiat Res. 2002 Jan;157(1):45-51.


High levels of HER-2 expression alter the ability of epidermal growth factor receptor (EGFR) family tyrosine kinase inhibitors to inhibit EGFR phosphorylation in vivo.

Christensen JG, Schreck RE, Chan E, Wang X, Yang C, Liu L, Cui J, Sun L, Wei J, Cherrington JM, Mendel DB.

Clin Cancer Res. 2001 Dec;7(12):4230-8.


Adefovir and tenofovir susceptibilities of HIV-1 after 24 to 48 weeks of adefovir dipivoxil therapy: genotypic and phenotypic analyses of study GS-96-408.

Miller MD, Margot NA, Lamy PD, Fuller MD, Anton KE, Mulato AS, Cherrington JM.

J Acquir Immune Defic Syndr. 2001 Aug 15;27(5):450-8.


The angiogenesis inhibitor SU5416 has long-lasting effects on vascular endothelial growth factor receptor phosphorylation and function.

Mendel DB, Schreck RE, West DC, Li G, Strawn LM, Tanciongco SS, Vasile S, Shawver LK, Cherrington JM.

Clin Cancer Res. 2000 Dec;6(12):4848-58.


Effects of SU101 in combination with cytotoxic agents on the growth of subcutaneous tumor xenografts.

Strawn LM, Kabbinavar F, Schwartz DP, Mann E, Shawver LK, Slamon DJ, Cherrington JM.

Clin Cancer Res. 2000 Jul;6(7):2931-40.


Development of SU5416, a selective small molecule inhibitor of VEGF receptor tyrosine kinase activity, as an anti-angiogenesis agent.

Mendel DB, Laird AD, Smolich BD, Blake RA, Liang C, Hannah AL, Shaheen RM, Ellis LM, Weitman S, Shawver LK, Cherrington JM.

Anticancer Drug Des. 2000 Feb;15(1):29-41. Review.


New paradigms for the treatment of cancer: the role of anti-angiogenesis agents.

Cherrington JM, Strawn LM, Shawver LK.

Adv Cancer Res. 2000;79:1-38. Review.


In vitro selection and characterization of HIV-1 with reduced susceptibility to PMPA.

Wainberg MA, Miller MD, Quan Y, Salomon H, Mulato AS, Lamy PD, Margot NA, Anton KE, Cherrington JM.

Antivir Ther. 1999;4(2):87-94.


Prophylactic and therapeutic benefits of short-term 9-[2-(R)-(phosphonomethoxy)propyl]adenine (PMPA) administration to newborn macaques following oral inoculation with simian immunodeficiency virus with reduced susceptibility to PMPA.

Van Rompay KK, Miller MD, Marthas ML, Margot NA, Dailey PJ, Canfield DR, Tarara RP, Cherrington JM, Aguirre NL, Bischofberger N, Pedersen NC.

J Virol. 2000 Feb;74(4):1767-74.


Quantitative changes in cytomegalovirus DNAemia and genetic analysis of the UL97 and UL54 genes in AIDS patients receiving cidofovir following ganciclovir therapy.

Bowen EF, Cherrington JM, Lamy PD, Griffiths PD, Johnson MA, Emery VC.

J Med Virol. 1999 Aug;58(4):402-7.


9-[2-(Phosphonomethoxy)propyl]adenine (PMPA) therapy prolongs survival of infant macaques inoculated with simian immunodeficiency virus with reduced susceptibility to PMPA.

Van Rompay KK, Cherrington JM, Marthas ML, Lamy PD, Dailey PJ, Canfield DR, Tarara RP, Bischofberger N, Pedersen NC.

Antimicrob Agents Chemother. 1999 Apr;43(4):802-12.


Early short-term 9-[2-(R)-(phosphonomethoxy)propyl]adenine treatment favorably alters the subsequent disease course in simian immunodeficiency virus-infected newborn Rhesus macaques.

van Rompay KK, Dailey PJ, Tarara RP, Canfield DR, Aguirre NL, Cherrington JM, Lamy PD, Bischofberger N, Pedersen NC, Marthas ML.

J Virol. 1999 Apr;73(4):2947-55.


In vitro antiviral susceptibilities of isolates from cytomegalovirus retinitis patients receiving first- or second-line cidofovir therapy: relationship to clinical outcome.

Cherrington JM, Fuller MD, Lamy PD, Miner R, Lalezari JP, Nuessle S, Drew WL.

J Infect Dis. 1998 Dec;178(6):1821-5.


Human immunodeficiency virus type 1 reverse transcriptase expressing the K70E mutation exhibits a decrease in specific activity and processivity.

Miller MD, Lamy PD, Fuller MD, Mulato AS, Margot NA, Cihlar T, Cherrington JM.

Mol Pharmacol. 1998 Aug;54(2):291-7.


Genotypic and phenotypic characterization of human immunodeficiency virus type 1 variants isolated from AIDS patients after prolonged adefovir dipivoxil therapy.

Mulato AS, Lamy PD, Miller MD, Li WX, Anton KE, Hellmann NS, Cherrington JM.

Antimicrob Agents Chemother. 1998 Jul;42(7):1620-8.

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