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Items: 1 to 20 of 102

1.

The pre-clinical absorption, distribution, metabolism and excretion properties of IPI-926, an orally bioavailable antagonist of the hedgehog signal transduction pathway.

Smith S, Hoyt J, Whitebread N, Manna J, Peluso M, Faia K, Campbell V, Tremblay M, Nair S, Grogan M, Castro A, Campbell M, Ferguson J, Arsenault B, Nevejans J, Carter B, Lee J, Dunbar J, McGovern K, Read M, Adams J, Constan A, Loewen G, Sydor J, Palombella V, Soglia J.

Xenobiotica. 2013 Oct;43(10):875-85. doi: 10.3109/00498254.2013.780671. Epub 2013 Mar 25.

PMID:
23527529
2.

Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor.

Wong H, Chen JZ, Chou B, Halladay JS, Kenny JR, La H, Marsters JC Jr, Plise E, Rudewicz PJ, Robarge K, Shin Y, Wong S, Zhang C, Khojasteh SC.

Xenobiotica. 2009 Nov;39(11):850-61. doi: 10.3109/00498250903180289.

PMID:
19845436
3.

Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL.

Kamath AV, Wang J, Lee FY, Marathe PH.

Cancer Chemother Pharmacol. 2008 Mar;61(3):365-76. Epub 2007 Apr 11.

PMID:
17429625
4.
5.

Disposition of CP-671, 305, a selective phosphodiesterase 4 inhibitor in preclinical species.

Kalgutkar AS, Choo E, Taylor TJ, Marfat A.

Xenobiotica. 2004 Aug;34(8):755-70.

PMID:
15690763
6.

Preclinical assessment of the absorption and disposition of the phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor GDC-0980 and prediction of its pharmacokinetics and efficacy in human.

Salphati L, Pang J, Plise EG, Lee LB, Olivero AG, Prior WW, Sampath D, Wong S, Zhang X.

Drug Metab Dispos. 2012 Sep;40(9):1785-96. doi: 10.1124/dmd.112.046052. Epub 2012 Jun 13.

7.

Discovery of a potent and orally active hedgehog pathway antagonist (IPI-926).

Tremblay MR, Lescarbeau A, Grogan MJ, Tan E, Lin G, Austad BC, Yu LC, Behnke ML, Nair SJ, Hagel M, White K, Conley J, Manna JD, Alvarez-Diez TM, Hoyt J, Woodward CN, Sydor JR, Pink M, MacDougall J, Campbell MJ, Cushing J, Ferguson J, Curtis MS, McGovern K, Read MA, Palombella VJ, Adams J, Castro AC.

J Med Chem. 2009 Jul 23;52(14):4400-18. doi: 10.1021/jm900305z.

PMID:
19522463
8.

In vitro phase I cytochrome P450 metabolism, permeability and pharmacokinetics of SB639, a novel histone deacetylase inhibitor in preclinical species.

Venkatesh PR, Goh E, Zeng P, New LS, Xin L, Pasha MK, Sangthongpitag K, Yeo P, Kantharaj E.

Biol Pharm Bull. 2007 May;30(5):1021-4.

9.

Preclinical drug metabolism and pharmacokinetic evaluation of GW844520, a novel anti-malarial mitochondrial electron transport inhibitor.

Xiang H, McSurdy-Freed J, Moorthy GS, Hugger E, Bambal R, Han C, Ferrer S, Gargallo D, Davis CB.

J Pharm Sci. 2006 Dec;95(12):2657-72.

PMID:
16892205
10.

Preclinical metabolism and disposition of SB939 (Pracinostat), an orally active histone deacetylase inhibitor, and prediction of human pharmacokinetics.

Jayaraman R, Pilla Reddy V, Pasha MK, Wang H, Sangthongpitag K, Yeo P, Hu CY, Wu X, Xin L, Goh E, New LS, Ethirajulu K.

Drug Metab Dispos. 2011 Dec;39(12):2219-32. doi: 10.1124/dmd.111.041558. Epub 2011 Aug 26.

11.

Pharmacokinetics and metabolism of AMG 232, a novel orally bioavailable inhibitor of the MDM2-p53 interaction, in rats, dogs and monkeys: in vitro-in vivo correlation.

Ye Q, Jiang M, Huang WT, Ling Y, Olson SH, Sun D, Xu G, Yan X, Wong BK, Jin L.

Xenobiotica. 2015;45(8):681-92. doi: 10.3109/00498254.2015.1010632. Epub 2015 Mar 23.

PMID:
25798742
13.

Pharmacokinetic characterization of a natural product-inspired novel MEK1 inhibitor E6201 in preclinical species.

Kumar V, Schuck EL, Pelletier RD, Farah N, Condon KB, Ye M, Rowbottom C, King BM, Zhang ZY, Saxton PL, Wong YN.

Cancer Chemother Pharmacol. 2012 Jan;69(1):229-37. doi: 10.1007/s00280-011-1687-8. Epub 2011 Jun 23.

PMID:
21698359
14.

Pre-clinical pharmacokinetics of UK-453,061, a novel non-nucleoside reverse transcriptase inhibitor (NNRTI), and use of in silico physiologically based prediction tools to predict the oral pharmacokinetics of UK-453,061 in man.

Allan G, Davis J, Dickins M, Gardner I, Jenkins T, Jones H, Webster R, Westgate H.

Xenobiotica. 2008 Jun;38(6):620-40. doi: 10.1080/00498250802069088 .

PMID:
18570162
15.

Preclinical pharmacokinetics of a novel HIV-1 attachment inhibitor BMS-378806 and prediction of its human pharmacokinetics.

Yang Z, Zadjura L, D'Arienzo C, Marino A, Santone K, Klunk L, Greene D, Lin PF, Colonno R, Wang T, Meanwell N, Hansel S.

Biopharm Drug Dispos. 2005 Dec;26(9):387-402.

PMID:
16142720
16.

Preclinical pharmacokinetics and oral bioavailability of BMS-310705, a novel epothilone B analog.

Kamath AV, Chang M, Lee FY, Zhang Y, Marathe PH.

Cancer Chemother Pharmacol. 2005 Aug;56(2):145-53. Epub 2005 Apr 14.

PMID:
15830240
17.

In vitro metabolism of BIIB021, an inhibitor of heat shock protein 90, in liver microsomes and hepatocytes of rats, dogs, and humans and recombinant human cytochrome P450 isoforms.

Xu L, Woodward C, Khan S, Prakash C.

Drug Metab Dispos. 2012 Apr;40(4):680-93. doi: 10.1124/dmd.111.043000. Epub 2012 Jan 4.

18.

Impact of the Smoothened inhibitor, IPI-926, on smoothened ciliary localization and Hedgehog pathway activity.

Peluso MO, Campbell VT, Harari JA, Tibbitts TT, Proctor JL, Whitebread N, Conley JM, White KF, Kutok JL, Read MA, McGovern K, Faia KL.

PLoS One. 2014 Mar 7;9(3):e90534. doi: 10.1371/journal.pone.0090534. eCollection 2014.

19.
20.

Semisynthetic cyclopamine analogues as potent and orally bioavailable hedgehog pathway antagonists.

Tremblay MR, Nevalainen M, Nair SJ, Porter JR, Castro AC, Behnke ML, Yu LC, Hagel M, White K, Faia K, Grenier L, Campbell MJ, Cushing J, Woodward CN, Hoyt J, Foley MA, Read MA, Sydor JR, Tong JK, Palombella VJ, McGovern K, Adams J.

J Med Chem. 2008 Nov 13;51(21):6646-9. doi: 10.1021/jm8008508. Epub 2008 Oct 9.

PMID:
18842035

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