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Items: 45

1.

The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies.

Stubbs MC, Burn TC, Sparks RB, Maduskuie T, Diamond S, Rupar M, Wen X, Volgina A, Zolotarjova N, Waeltz P, Favata M, Jalluri R, Liu H, Liu XM, Li J, Collins R, Falahatpisheh N, Polam P, DiMatteo D, Feldman P, Dostalik V, Thekkat P, Gardiner C, He X, Li Y, Covington M, Wynn R, Ruggeri B, Yeleswaram S, Xue C, Yao W, Combs AP, Huber R, Hollis G, Scherle P, Liu P.

Clin Cancer Res. 2018 Sep 11. pii: clincanres.0098.2018. doi: 10.1158/1078-0432.CCR-18-0098. [Epub ahead of print]

PMID:
30206163
2.

Sustained-release ruxolitinib: Findings from a phase 1 study in healthy subjects and a phase 2 study in patients with myelofibrosis.

Verstovsek S, Yeleswaram S, Hou K, Chen X, Erickson-Viitanen S.

Hematol Oncol. 2018 Aug 13. doi: 10.1002/hon.2544. [Epub ahead of print]

PMID:
30105794
3.

Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies.

Koblish H, Li YL, Shin N, Hall L, Wang Q, Wang K, Covington M, Marando C, Bowman K, Boer J, Burke K, Wynn R, Margulis A, Reuther GW, Lambert QT, Dostalik Roman V, Zhang K, Feng H, Xue CB, Diamond S, Hollis G, Yeleswaram S, Yao W, Huber R, Vaddi K, Scherle P.

PLoS One. 2018 Jun 21;13(6):e0199108. doi: 10.1371/journal.pone.0199108. eCollection 2018.

4.

INCB040093 Is a Novel PI3Kδ Inhibitor for the Treatment of B Cell Lymphoid Malignancies.

Shin N, Li YL, Mei S, Wang KH, Hall L, Katiyar K, Wang Q, Yang G, Rumberger B, Leffet L, He X, Rupar M, Bowman K, Favata M, Li J, Liu M, Li Y, Covington M, Koblish H, Soloviev M, Shuey D, Burn T, Diamond S, Fridman J, Combs A, Yao W, Yeleswaram S, Hollis G, Vaddi K, Huber R, Newton R, Scherle P.

J Pharmacol Exp Ther. 2018 Jan;364(1):120-130. doi: 10.1124/jpet.117.244947. Epub 2017 Nov 10.

PMID:
29127109
5.

In Vitro Interactions of Epacadostat and its Major Metabolites with Human Efflux and Uptake Transporters: Implications for Pharmacokinetics and Drug Interactions.

Zhang Q, Zhang Y, Boer J, Shi JG, Hu P, Diamond S, Yeleswaram S.

Drug Metab Dispos. 2017 Jun;45(6):612-623. doi: 10.1124/dmd.116.074609. Epub 2017 Mar 10.

6.

Population Pharmacokinetic and Pharmacodynamic Modeling of Epacadostat in Patients With Advanced Solid Malignancies.

Shi JG, Bowman KJ, Chen X, Maleski J, Leopold L, Yeleswaram S.

J Clin Pharmacol. 2017 Jun;57(6):720-729. doi: 10.1002/jcph.855. Epub 2016 Dec 19.

PMID:
27990653
7.

Roles of UGT, P450, and Gut Microbiota in the Metabolism of Epacadostat in Humans.

Boer J, Young-Sciame R, Lee F, Bowman KJ, Yang X, Shi JG, Nedza FM, Frietze W, Galya L, Combs AP, Yeleswaram S, Diamond S.

Drug Metab Dispos. 2016 Oct;44(10):1668-74. doi: 10.1124/dmd.116.070680. Epub 2016 Jul 25.

8.

Potential Underprediction of Warfarin Drug Interaction From Conventional Interaction Studies and Risk Mitigation: A Case Study With Epacadostat, an IDO1 Inhibitor.

Shi JG, Chen X, Punwani NG, Williams WV, Yeleswaram S.

J Clin Pharmacol. 2016 Nov;56(11):1344-1354. doi: 10.1002/jcph.737.

PMID:
26990117
9.

A randomized, double-blind, placebo-controlled, dose-escalation study of the safety and efficacy of INCB039110, an oral janus kinase 1 inhibitor, in patients with stable, chronic plaque psoriasis.

Bissonnette R, Luchi M, Fidelus-Gort R, Jackson S, Zhang H, Flores R, Newton R, Scherle P, Yeleswaram S, Chen X, Menter A.

J Dermatolog Treat. 2016 Aug;27(4):332-8. doi: 10.3109/09546634.2015.1115819. Epub 2016 Jan 14.

PMID:
26769332
10.

Downmodulation of key inflammatory cell markers with a topical Janus kinase 1/2 inhibitor.

Punwani N, Burn T, Scherle P, Flores R, Shi J, Collier P, Hertel D, Haley P, Lo Y, Waeltz P, Rodgers J, Shepard S, Vaddi K, Yeleswaram S, Levy R, Williams W, Gottlieb AB.

Br J Dermatol. 2015 Oct;173(4):989-97. doi: 10.1111/bjd.13994. Epub 2015 Oct 14.

PMID:
26123031
11.

Predicting drug-drug interactions involving multiple mechanisms using physiologically based pharmacokinetic modeling: a case study with ruxolitinib.

Shi JG, Fraczkiewicz G, Williams WV, Yeleswaram S.

Clin Pharmacol Ther. 2015 Feb;97(2):177-85. doi: 10.1002/cpt.30. Epub 2014 Dec 15.

PMID:
25670523
12.

Impact on creatinine renal clearance by the interplay of multiple renal transporters: a case study with INCB039110.

Zhang Y, Warren MS, Zhang X, Diamond S, Williams B, Punwani N, Huang J, Huang Y, Yeleswaram S.

Drug Metab Dispos. 2015 Apr;43(4):485-9. doi: 10.1124/dmd.114.060673. Epub 2015 Jan 20.

13.

The Janus kinase 2 inhibitor fedratinib inhibits thiamine uptake: a putative mechanism for the onset of Wernicke's encephalopathy.

Zhang Q, Zhang Y, Diamond S, Boer J, Harris JJ, Li Y, Rupar M, Behshad E, Gardiner C, Collier P, Liu P, Burn T, Wynn R, Hollis G, Yeleswaram S.

Drug Metab Dispos. 2014 Oct;42(10):1656-62. doi: 10.1124/dmd.114.058883. Epub 2014 Jul 25.

14.

The pharmacokinetics, pharmacodynamics, and safety of baricitinib, an oral JAK 1/2 inhibitor, in healthy volunteers.

Shi JG, Chen X, Lee F, Emm T, Scherle PA, Lo Y, Punwani N, Williams WV, Yeleswaram S.

J Clin Pharmacol. 2014 Dec;54(12):1354-61. doi: 10.1002/jcph.354.

PMID:
24965573
15.

Evaluation of the effect of ruxolitinib on cardiac repolarization: A thorough QT study.

Punwani N, Yeleswaram S, Chen X, Bowman J, Soloviev M, Williams W.

Clin Pharmacol Drug Dev. 2014 May;3(3):207-14. doi: 10.1002/cpdd.90. Epub 2014 Feb 6.

PMID:
27128611
16.

Pharmacokinetics and pharmacodynamics of orally administered ruxolitinib (INCB018424 phosphate) in renal and hepatic impairment patients.

Chen X, Shi JG, Emm T, Scherle PA, McGee RF, Lo Y, Landman RR, Punwani NG, Williams WV, Yeleswaram S.

Clin Pharmacol Drug Dev. 2014 Jan;3(1):34-42. doi: 10.1002/cpdd.77. Epub 2013 Oct 19.

PMID:
27128228
18.

Preliminary clinical activity of a topical JAK1/2 inhibitor in the treatment of psoriasis.

Punwani N, Scherle P, Flores R, Shi J, Liang J, Yeleswaram S, Levy R, Williams W, Gottlieb A.

J Am Acad Dermatol. 2012 Oct;67(4):658-64. doi: 10.1016/j.jaad.2011.12.018. Epub 2012 Jan 24.

PMID:
22281165
19.

INCB38579, a novel and potent histamine H₄ receptor small molecule antagonist with anti-inflammatory pain and anti-pruritic functions.

Shin N, Covington M, Bian D, Zhuo J, Bowman K, Li Y, Soloviev M, Qian DQ, Feldman P, Leffet L, He X, He Wang K, Krug K, Bell D, Czerniak P, Hu Z, Zhao H, Zhang J, Yeleswaram S, Yao W, Newton R, Scherle P.

Eur J Pharmacol. 2012 Jan 30;675(1-3):47-56. doi: 10.1016/j.ejphar.2011.11.027. Epub 2011 Nov 27.

PMID:
22155710
20.

Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Xue CB, Wang A, Han Q, Zhang Y, Cao G, Feng H, Huang T, Zheng C, Xia M, Zhang K, Kong L, Glenn J, Anand R, Meloni D, Robinson DJ, Shao L, Storace L, Li M, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Metcalf B.

ACS Med Chem Lett. 2011 Oct 5;2(12):913-8. doi: 10.1021/ml200199c. eCollection 2011 Dec 8.

21.

Preclinical evaluation of local JAK1 and JAK2 inhibition in cutaneous inflammation.

Fridman JS, Scherle PA, Collins R, Burn T, Neilan CL, Hertel D, Contel N, Haley P, Thomas B, Shi J, Collier P, Rodgers JD, Shepard S, Metcalf B, Hollis G, Newton RC, Yeleswaram S, Friedman SM, Vaddi K.

J Invest Dermatol. 2011 Sep;131(9):1838-44. doi: 10.1038/jid.2011.140. Epub 2011 Jun 16.

22.

Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.

Xue CB, Feng H, Cao G, Huang T, Glenn J, Anand R, Meloni D, Zhang K, Kong L, Wang A, Zhang Y, Zheng C, Xia M, Chen L, Tanaka H, Han Q, Robinson DJ, Modi D, Storace L, Shao L, Sharief V, Li M, Galya LG, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B.

ACS Med Chem Lett. 2011 Mar 31;2(6):450-4. doi: 10.1021/ml200030q. eCollection 2011 Jun 9.

23.

The effect of CYP3A4 inhibition or induction on the pharmacokinetics and pharmacodynamics of orally administered ruxolitinib (INCB018424 phosphate) in healthy volunteers.

Shi JG, Chen X, Emm T, Scherle PA, McGee RF, Lo Y, Landman RR, McKeever EG Jr, Punwani NG, Williams WV, Yeleswaram S.

J Clin Pharmacol. 2012 Jun;52(6):809-18. doi: 10.1177/0091270011405663. Epub 2011 May 20.

PMID:
21602517
24.

Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection.

Shin N, Solomon K, Zhou N, Wang KH, Garlapati V, Thomas B, Li Y, Covington M, Baribaud F, Erickson-Viitanen S, Czerniak P, Contel N, Liu P, Burn T, Hollis G, Yeleswaram S, Vaddi K, Xue CB, Metcalf B, Friedman S, Scherle P, Newton R.

J Pharmacol Exp Ther. 2011 Jul;338(1):228-39. doi: 10.1124/jpet.111.179531. Epub 2011 Apr 1.

25.

Simultaneous determination of fluoxetine and its major active metabolite norfluoxetine in human plasma by LC-MS/MS using supported liquid extraction.

Li Y, Emm T, Yeleswaram S.

Biomed Chromatogr. 2011 Nov;25(11):1245-51. doi: 10.1002/bmc.1597. Epub 2011 Feb 10.

PMID:
21308704
26.

Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.

Zheng C, Cao G, Xia M, Feng H, Glenn J, Anand R, Zhang K, Huang T, Wang A, Kong L, Li M, Galya L, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Baribaud F, Shin N, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B, Xue CB.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1442-6. doi: 10.1016/j.bmcl.2011.01.015. Epub 2011 Jan 11.

PMID:
21295478
27.

The pharmacokinetics, pharmacodynamics, and safety of orally dosed INCB018424 phosphate in healthy volunteers.

Shi JG, Chen X, McGee RF, Landman RR, Emm T, Lo Y, Scherle PA, Punwani NG, Williams WV, Yeleswaram S.

J Clin Pharmacol. 2011 Dec;51(12):1644-54. doi: 10.1177/0091270010389469. Epub 2011 Jan 21.

PMID:
21257798
28.

The relevance of assessment of intestinal P-gp inhibition using digoxin as an in vivo probe substrate.

Shi JG, Zhang Y, Yeleswaram S.

Nat Rev Drug Discov. 2011 Jan;10(1):75; author reply 75. doi: 10.1038/nrd3028-c1. No abstract available.

PMID:
21193869
29.

Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.

Xue CB, Chen L, Cao G, Zhang K, Wang A, Meloni D, Glenn J, Anand R, Xia M, Kong L, Huang T, Feng H, Zheng C, Li M, Galya L, Zhou J, Shin N, Baribaud F, Solomon K, Scherle P, Zhao B, Diamond S, Emm T, Keller D, Contel N, Yeleswaram S, Vaddi K, Hollis G, Newton R, Friedman S, Metcalf B.

ACS Med Chem Lett. 2010 Aug 25;1(9):483-7. doi: 10.1021/ml1001536. eCollection 2010 Dec 9.

30.

Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

Xue CB, Wang A, Meloni D, Zhang K, Kong L, Feng H, Glenn J, Huang T, Zhang Y, Cao G, Anand R, Zheng C, Xia M, Han Q, Robinson DJ, Storace L, Shao L, Li M, Brodmerkel CM, Covington M, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7473-8. doi: 10.1016/j.bmcl.2010.10.020. Epub 2010 Oct 13.

PMID:
21036044
31.

Metabolism, excretion, and pharmacokinetics of [14C]INCB018424, a selective Janus tyrosine kinase 1/2 inhibitor, in humans.

Shilling AD, Nedza FM, Emm T, Diamond S, McKeever E, Punwani N, Williams W, Arvanitis A, Galya LG, Li M, Shepard S, Rodgers J, Yue TY, Yeleswaram S.

Drug Metab Dispos. 2010 Nov;38(11):2023-31. doi: 10.1124/dmd.110.033787. Epub 2010 Aug 10.

32.

Species-specific metabolism of SGX523 by aldehyde oxidase and the toxicological implications.

Diamond S, Boer J, Maduskuie TP Jr, Falahatpisheh N, Li Y, Yeleswaram S.

Drug Metab Dispos. 2010 Aug;38(8):1277-85. doi: 10.1124/dmd.110.032375. Epub 2010 Apr 26.

33.

Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.

Fridman JS, Scherle PA, Collins R, Burn TC, Li Y, Li J, Covington MB, Thomas B, Collier P, Favata MF, Wen X, Shi J, McGee R, Haley PJ, Shepard S, Rodgers JD, Yeleswaram S, Hollis G, Newton RC, Metcalf B, Friedman SM, Vaddi K.

J Immunol. 2010 May 1;184(9):5298-307. doi: 10.4049/jimmunol.0902819. Epub 2010 Apr 2.

34.

Discovery of matrix metalloproteases selective and activated peptide-doxorubicin prodrugs as anti-tumor agents.

Hu Z, Jiang X, Albright CF, Graciani N, Yue E, Zhang M, Zhang SY, Bruckner R, Diamond M, Dowling R, Rafalski M, Yeleswaram S, Trainor GL, Seitz SP, Han W.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):853-6. doi: 10.1016/j.bmcl.2009.12.084. Epub 2010 Jan 4.

PMID:
20060717
35.

From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.

Santella JB 3rd, Gardner DS, Yao W, Shi C, Reddy P, Tebben AJ, DeLucca GV, Wacker DA, Watson PS, Welch PK, Wadman EA, Davies P, Solomon KA, Graden DM, Yeleswaram S, Mandlekar S, Kariv I, Decicco CP, Ko SS, Carter PH, Duncia JV.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):576-85. Epub 2007 Nov 22.

PMID:
18096386
36.

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.

Burns DM, He C, Li Y, Scherle P, Liu X, Marando CA, Covington MB, Yang G, Pan M, Turner S, Fridman JS, Hollis G, Vaddi K, Yeleswaram S, Newton R, Friedman S, Metcalf B, Yao W.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):560-4. Epub 2007 Nov 28.

PMID:
18068976
37.

Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.

Yao W, Zhuo J, Burns DM, Li YL, Qian DQ, Zhang C, He C, Xu M, Shi E, Li Y, Marando CA, Covington MB, Yang G, Liu X, Pan M, Fridman JS, Scherle P, Wasserman ZR, Hollis G, Vaddi K, Yeleswaram S, Newton R, Friedman S, Metcalf B.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):159-63. Epub 2007 Nov 4.

PMID:
18036818
38.

CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.

Pruitt JR, Batt DG, Wacker DA, Bostrom LL, Booker SK, McLaughlin E, Houghton GC, Varnes JG, Christ DD, Covington M, Das AM, Davies P, Graden D, Kariv I, Orlovsky Y, Stowell NC, Vaddi KG, Wadman EA, Welch PK, Yeleswaram S, Solomon KA, Newton RC, Decicco CP, Carter PH, Ko SS.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):2992-7. Epub 2007 Mar 24.

PMID:
17418570
39.

3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl ]-1,3,4-oxadiazol-2(3H)-one, BMS-191011: opener of large-conductance Ca(2+)-activated potassium (maxi-K) channels, identification, solubility, and SAR.

Romine JL, Martin SW, Meanwell NA, Gribkoff VK, Boissard CG, Dworetzky SI, Natale J, Moon S, Ortiz A, Yeleswaram S, Pajor L, Gao Q, Starrett JE Jr.

J Med Chem. 2007 Feb 8;50(3):528-42.

PMID:
17266205
40.

Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

Yao W, Zhuo J, Burns DM, Xu M, Zhang C, Li YL, Qian DQ, He C, Weng L, Shi E, Lin Q, Agrios C, Burn TC, Caulder E, Covington MB, Fridman JS, Friedman S, Katiyar K, Hollis G, Li Y, Liu C, Liu X, Marando CA, Newton R, Pan M, Scherle P, Taylor N, Vaddi K, Wasserman ZR, Wynn R, Yeleswaram S, Jalluri R, Bower M, Zhou BB, Metcalf B.

J Med Chem. 2007 Feb 22;50(4):603-6. Epub 2007 Jan 26.

PMID:
17256836
41.

Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic.

Combs AP, Zhu W, Crawley ML, Glass B, Polam P, Sparks RB, Modi D, Takvorian A, McLaughlin E, Yue EW, Wasserman Z, Bower M, Wei M, Rupar M, Ala PJ, Reid BM, Ellis D, Gonneville L, Emm T, Taylor N, Yeleswaram S, Li Y, Wynn R, Burn TC, Hollis G, Liu PC, Metcalf B.

J Med Chem. 2006 Jun 29;49(13):3774-89.

PMID:
16789735
42.

Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344.

Brodmerkel CM, Huber R, Covington M, Diamond S, Hall L, Collins R, Leffet L, Gallagher K, Feldman P, Collier P, Stow M, Gu X, Baribaud F, Shin N, Thomas B, Burn T, Hollis G, Yeleswaram S, Solomon K, Friedman S, Wang A, Xue CB, Newton RC, Scherle P, Vaddi K.

J Immunol. 2005 Oct 15;175(8):5370-8.

43.

Matrix metalloproteinase-activated doxorubicin prodrugs inhibit HT1080 xenograft growth better than doxorubicin with less toxicity.

Albright CF, Graciani N, Han W, Yue E, Stein R, Lai Z, Diamond M, Dowling R, Grimminger L, Zhang SY, Behrens D, Musselman A, Bruckner R, Zhang M, Jiang X, Hu D, Higley A, Dimeo S, Rafalski M, Mandlekar S, Car B, Yeleswaram S, Stern A, Copeland RA, Combs A, Seitz SP, Trainor GL, Taub R, Huang P, Oliff A.

Mol Cancer Ther. 2005 May;4(5):751-60.

44.

Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.

De Lucca GV, Kim UT, Vargo BJ, Duncia JV, Santella JB 3rd, Gardner DS, Zheng C, Liauw A, Wang Z, Emmett G, Wacker DA, Welch PK, Covington M, Stowell NC, Wadman EA, Das AM, Davies P, Yeleswaram S, Graden DM, Solomon KA, Newton RC, Trainor GL, Decicco CP, Ko SS.

J Med Chem. 2005 Mar 24;48(6):2194-211.

PMID:
15771462

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