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Adenosine Signaling Is Prognostic for Cancer Outcome and Has Predictive Utility for Immunotherapeutic Response.

Sidders B, Zhang P, Goodwin K, O'Connor G, Russell DL, Borodovsky A, Armenia J, McEwen R, Linghu B, Bendell JC, Bauer TM, Patel MR, Falchook GS, Merchant M, Pouliot G, Barrett JC, Dry JR, Woessner R, Sachsenmeier K.

Clin Cancer Res. 2020 Jan 17. doi: 10.1158/1078-0432.CCR-19-2183. [Epub ahead of print]


Comparison of pharmacokinetics, safety and tolerability of secukinumab administered subcutaneously using different delivery systems in healthy volunteers and in psoriasis patients.

Bruin G, Hockey HP, La Stella P, Sigurgeirsson B, Fu R, Patekar M, Charef P, Woessner R, Boutouyrie-Dumont B.

Br J Clin Pharmacol. 2020 Feb;86(2):338-351. doi: 10.1111/bcp.14155. Epub 2020 Jan 7.


Secukinumab Treatment Does Not Alter the Pharmacokinetics of the Cytochrome P450 3A4 Substrate Midazolam in Patients With Moderate to Severe Psoriasis.

Bruin G, Hasselberg A, Koroleva I, Milojevic J, Calonder C, Soon R, Woessner R, Pariser DM, Boutouyrie-Dumont B.

Clin Pharmacol Ther. 2019 Dec;106(6):1380-1388. doi: 10.1002/cpt.1558. Epub 2019 Aug 3.


Fevipiprant has a low risk of influencing co-medication pharmacokinetics: Impact on simvastatin and rosuvastatin in different SLCO1B1 genotypes.

Poller B, Woessner R, Barve A, Tillmann HC, Vemula J, Nica A, Elbast W, Schiller H, End P, Camenisch G, Weiss M.

Pulm Pharmacol Ther. 2019 Aug;57:101809. doi: 10.1016/j.pupt.2019.101809. Epub 2019 Jun 10.


STAT3 Modulation of Regulatory T Cells in Response to Radiation Therapy in Head and Neck Cancer.

Oweida AJ, Darragh L, Phan A, Binder D, Bhatia S, Mueller A, Court BV, Milner D, Raben D, Woessner R, Heasley L, Nemenoff R, Clambey E, Karam SD.

J Natl Cancer Inst. 2019 Dec 1;111(12):1339-1349. doi: 10.1093/jnci/djz036.


STAT3 antisense oligonucleotide AZD9150 in a subset of patients with heavily pretreated lymphoma: results of a phase 1b trial.

Reilley MJ, McCoon P, Cook C, Lyne P, Kurzrock R, Kim Y, Woessner R, Younes A, Nemunaitis J, Fowler N, Curran M, Liu Q, Zhou T, Schmidt J, Jo M, Lee SJ, Yamashita M, Hughes SG, Fayad L, Piha-Paul S, Nadella MVP, Xiao X, Hsu J, Revenko A, Monia BP, MacLeod AR, Hong DS.

J Immunother Cancer. 2018 Nov 16;6(1):119. doi: 10.1186/s40425-018-0436-5.


Development of a quantification method for adenosine in tumors by LC-MS/MS with dansyl chloride derivatization.

Goodwin KJ, Gangl E, Sarkar U, Pop-Damkov P, Jones N, Borodovsky A, Woessner R, Fretland AJ.

Anal Biochem. 2019 Mar 1;568:78-88. doi: 10.1016/j.ab.2018.11.004. Epub 2018 Nov 5.


Neomorphic PDGFRA extracellular domain driver mutations are resistant to PDGFRA targeted therapies.

Ip CKM, Ng PKS, Jeong KJ, Shao SH, Ju Z, Leonard PG, Hua X, Vellano CP, Woessner R, Sahni N, Scott KL, Mills GB.

Nat Commun. 2018 Nov 2;9(1):4583. doi: 10.1038/s41467-018-06949-w.


Antisense STAT3 inhibitor decreases viability of myelodysplastic and leukemic stem cells.

Shastri A, Choudhary G, Teixeira M, Gordon-Mitchell S, Ramachandra N, Bernard L, Bhattacharyya S, Lopez R, Pradhan K, Giricz O, Ravipati G, Wong LF, Cole S, Bhagat TD, Feld J, Dhar Y, Bartenstein M, Thiruthuvanathan VJ, Wickrema A, Ye BH, Frank DA, Pellagatti A, Boultwood J, Zhou T, Kim Y, MacLeod AR, Epling-Burnette PK, Ye M, McCoon P, Woessner R, Steidl U, Will B, Verma A.

J Clin Invest. 2018 Dec 3;128(12):5479-5488. doi: 10.1172/JCI120156. Epub 2018 Nov 5.


CYP3A but not P-gp plays a relevant role in the in vivo intestinal and hepatic clearance of the delta-specific phosphoinositide-3 kinase inhibitor leniolisib.

De Buck S, Kucher K, Hara H, Gray C, Woessner R.

Biopharm Drug Dispos. 2018 Sep;39(8):394-402. doi: 10.1002/bdd.2157.


Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.

Grimster NP, Anderson E, Alimzhanov M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Gero T, Harsch A, Huszar D, Kawatkar A, Kettle JG, Lyne P, Read JA, Rivard Costa C, Ruston L, Schroeder P, Shi J, Su Q, Throner S, Toader D, Vasbinder M, Woessner R, Wang H, Wu A, Ye M, Zheng W, Zinda M.

J Med Chem. 2018 Jun 28;61(12):5235-5244. doi: 10.1021/acs.jmedchem.8b00076. Epub 2018 Jun 13.


Absorption, Distribution, Metabolism, and Excretion of the Oral Prostaglandin D2 Receptor 2 Antagonist Fevipiprant (QAW039) in Healthy Volunteers and In Vitro.

Pearson D, Weiss HM, Jin Y, Jaap van Lier J, Erpenbeck VJ, Glaenzel U, End P, Woessner R, Eggimann F, Camenisch G.

Drug Metab Dispos. 2017 Jul;45(7):817-825. doi: 10.1124/dmd.117.075358. Epub 2017 Apr 25.


Cytokine receptor signaling is required for the survival of ALK- anaplastic large cell lymphoma, even in the presence of JAK1/STAT3 mutations.

Chen J, Zhang Y, Petrus MN, Xiao W, Nicolae A, Raffeld M, Pittaluga S, Bamford RN, Nakagawa M, Ouyang ST, Epstein AL, Kadin ME, Del Mistro A, Woessner R, Jaffe ES, Waldmann TA.

Proc Natl Acad Sci U S A. 2017 Apr 11;114(15):3975-3980. doi: 10.1073/pnas.1700682114. Epub 2017 Mar 29.


Pharmacokinetics and safety of indacaterol and glycopyrronium (IND/GLY) following repeated once daily inhalation from a fixed-dose combination in healthy Chinese subjects

Ren S, Sechaud R, Su Z, Tillmann HC, Hara H, Tan X, Hou J, Woessner R, Zhao R.

Int J Clin Pharmacol Ther. 2017 Feb;55(2):147-155. doi: 10.5414/CP202640.


Intravenous Dosing as an Alternate Approach to Safely Achieve Supratherapeutic Exposure for Assessments of Cardiac Repolarization: A Randomized Clinical Trial with Mavoglurant (AFQ056).

Ufer M, Sagkriotis A, Salunke A, Ganesan S, Tisserant A, Dodman A, Voltz E, Woessner R, Jordaan P, Legangneux E.

Clin Ther. 2016 Dec;38(12):2589-2597. doi: 10.1016/j.clinthera.2016.10.007. Epub 2016 Nov 4.


Inhibition of STAT3 with the Generation 2.5 Antisense Oligonucleotide, AZD9150, Decreases Neuroblastoma Tumorigenicity and Increases Chemosensitivity.

Odate S, Veschi V, Yan S, Lam N, Woessner R, Thiele CJ.

Clin Cancer Res. 2017 Apr 1;23(7):1771-1784. doi: 10.1158/1078-0432.CCR-16-1317. Epub 2016 Oct 19.


Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1.

Kettle JG, Åstrand A, Catley M, Grimster NP, Nilsson M, Su Q, Woessner R.

Expert Opin Ther Pat. 2017 Feb;27(2):127-143. doi: 10.1080/13543776.2017.1252753. Epub 2016 Nov 7. Review.


Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2.

Kettle JG, Åstrand A, Catley M, Grimster NP, Nilsson M, Su Q, Woessner R.

Expert Opin Ther Pat. 2017 Feb;27(2):145-161. doi: 10.1080/13543776.2017.1252754. Epub 2016 Nov 4. Review.


Population PK-PD Model for Tolerance Evaluation to the p38 MAP Kinase Inhibitor BCT197.

De Buck S, Hueber W, Vitaliti A, Straube F, Emotte C, Bruin G, Woessner R.

CPT Pharmacometrics Syst Pharmacol. 2015 Dec;4(12):691-700. doi: 10.1002/psp4.12037. Epub 2015 Nov 9.


Pharmacokinetics of indacaterol and mometasone furoate delivered alone or in a free or fixed dose combination in healthy subjects.

Vaidya SS, Khindri S, Calder N, Machineni S, Hara H, Majumdar T, Febbraro S, Fuhr R, Woessner R.

Pulm Pharmacol Ther. 2016 Apr;37:30-6. doi: 10.1016/j.pupt.2016.01.004. Epub 2016 Feb 1.


Identification of azabenzimidazoles as potent JAK1 selective inhibitors.

Vasbinder MM, Alimzhanov M, Augustin M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Goodwin K, Huszar D, Kawatkar A, Kawatkar S, Read J, Shi J, Steinbacher S, Steuber H, Su Q, Toader D, Wang H, Woessner R, Wu A, Ye M, Zinda M.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):60-7. doi: 10.1016/j.bmcl.2015.11.031. Epub 2015 Nov 12.


AZD9150, a next-generation antisense oligonucleotide inhibitor of STAT3 with early evidence of clinical activity in lymphoma and lung cancer.

Hong D, Kurzrock R, Kim Y, Woessner R, Younes A, Nemunaitis J, Fowler N, Zhou T, Schmidt J, Jo M, Lee SJ, Yamashita M, Hughes SG, Fayad L, Piha-Paul S, Nadella MV, Mohseni M, Lawson D, Reimer C, Blakey DC, Xiao X, Hsu J, Revenko A, Monia BP, MacLeod AR.

Sci Transl Med. 2015 Nov 18;7(314):314ra185. doi: 10.1126/scitranslmed.aac5272.


Secukinumab distributes into dermal interstitial fluid of psoriasis patients as demonstrated by open flow microperfusion.

Dragatin C, Polus F, Bodenlenz M, Calonder C, Aigner B, Tiffner KI, Mader JK, Ratzer M, Woessner R, Pieber TR, Cheng Y, Loesche C, Sinner F, Bruin G.

Exp Dermatol. 2016 Feb;25(2):157-9. doi: 10.1111/exd.12863. Epub 2015 Nov 23. No abstract available.


Effect of mavoglurant (AFQ056), a selective mGluR5 antagonist, on the pharmacokinetics of a combined oral contraceptive containing ethinyl estradiol and levonorgestrel in healthy women.

Sivasubramanian R, Chakraborty A, Rouzade-Dominguez ML, Neelakantham S, Jakab A, Mensinga T, Legangneux E, Woessner R, Ufer M.

Int J Clin Pharmacol Ther. 2015 Jul;53(7):550-6. doi: 10.5414/CP202321.


Pharmacokinetics of QMF149 in Japanese versus Caucasian subjects: an open-label, randomized phase I study.

Shimada S, Vaidya S, Khindri S, Tashiro N, Cheng Y, Hara H, Majumdar T, Woessner R, Furihata K, Kobayashi K.

Int J Clin Pharmacol Ther. 2015 May;53(5):398-407. doi: 10.5414/CP202239.


Model-based evaluation of the impact of formulation and food intake on the complex oral absorption of mavoglurant in healthy subjects.

Wendling T, Ogungbenro K, Pigeolet E, Dumitras S, Woessner R, Aarons L.

Pharm Res. 2015 May;32(5):1764-78. doi: 10.1007/s11095-014-1574-1. Epub 2014 Nov 26.


Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability.

Hicken EJ, Marmsater FP, Munson MC, Schlachter ST, Robinson JE, Allen S, Burgess LE, DeLisle RK, Rizzi JP, Topalov GT, Zhao Q, Hicks JM, Kallan NC, Tarlton E, Allen A, Callejo M, Cox A, Rana S, Klopfenstein N, Woessner R, Lyssikatos JP.

ACS Med Chem Lett. 2013 Nov 12;5(1):78-83. doi: 10.1021/ml4003953. eCollection 2014 Jan 9.


Single- and multiple-dose pharmacokinetics of inhaled indacaterol in healthy Chinese volunteers.

Jiang J, Li L, Yin H, Woessner R, Emotte C, Li R, Khindri S, Pei H.

Eur J Drug Metab Pharmacokinet. 2015 Jun;40(2):203-8. doi: 10.1007/s13318-014-0197-6. Epub 2014 Apr 6.


Metabolism and disposition of the metabotropic glutamate receptor 5 antagonist (mGluR5) mavoglurant (AFQ056) in healthy subjects.

Walles M, Wolf T, Jin Y, Ritzau M, Leuthold LA, Krauser J, Gschwind HP, Carcache D, Kittelmann M, Ocwieja M, Ufer M, Woessner R, Chakraborty A, Swart P.

Drug Metab Dispos. 2013 Sep;41(9):1626-41. doi: 10.1124/dmd.112.050716. Epub 2013 Jun 17.


Validation of an LC-MS/MS method for the quantitative determination of mavoglurant (AFQ056) in human plasma.

Jakab A, Winter S, Raccuglia M, Picard F, Dumitras S, Woessner R, Mistry S, Chudasama J, Guttikar S, Kretz O.

Anal Bioanal Chem. 2013 Jan;405(1):215-23. doi: 10.1007/s00216-012-6456-y. Epub 2012 Oct 13.


Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Blake JF, Xu R, Bencsik JR, Xiao D, Kallan NC, Schlachter S, Mitchell IS, Spencer KL, Banka AL, Wallace EM, Gloor SL, Martinson M, Woessner RD, Vigers GP, Brandhuber BJ, Liang J, Safina BS, Li J, Zhang B, Chabot C, Do S, Lee L, Oeh J, Sampath D, Lee BB, Lin K, Liederer BM, Skelton NJ.

J Med Chem. 2012 Sep 27;55(18):8110-27. Epub 2012 Sep 18.


Targeting the insulin-like growth factor-1 receptor to overcome bortezomib resistance in preclinical models of multiple myeloma.

Kuhn DJ, Berkova Z, Jones RJ, Woessner R, Bjorklund CC, Ma W, Davis RE, Lin P, Wang H, Madden TL, Wei C, Baladandayuthapani V, Wang M, Thomas SK, Shah JJ, Weber DM, Orlowski RZ.

Blood. 2012 Oct 18;120(16):3260-70. doi: 10.1182/blood-2011-10-386789. Epub 2012 Aug 29.


Systemic pharmacokinetics of indacaterol, an inhaled once-daily long-acting beta2-agonist, in different ethnic populations.

Matsushima S, Matthews I, Woessner R, Pinault G, Hara H, Wilkins J, Sekiguchi K.

Int J Clin Pharmacol Ther. 2012 Aug;50(8):545-56. doi: 10.5414/CP201719.


Validation of an on-line solid-phase extraction method coupled to liquid chromatography-tandem mass spectrometry detection for the determination of Indacaterol in human serum.

Emotte C, Heudi O, Deglave F, Bonvie A, Masson L, Picard F, Chaturvedi A, Majumdar T, Agarwal A, Woessner R, Kretz O.

J Chromatogr B Analyt Technol Biomed Life Sci. 2012 May 1;895-896:1-9. doi: 10.1016/j.jchromb.2012.02.025. Epub 2012 Feb 25.


Chk1 inhibition and Wee1 inhibition combine synergistically to impede cellular proliferation.

Davies KD, Cable PL, Garrus JE, Sullivan FX, von Carlowitz I, Huerou YL, Wallace E, Woessner RD, Gross S.

Cancer Biol Ther. 2011 Nov 1;12(9):788-96. doi: 10.4161/cbt.12.9.17673. Epub 2011 Nov 1.


Cardiac safety of indacaterol in healthy subjects: a randomized, multidose, placebo- and positive-controlled, parallel-group thorough QT study.

Khindri S, Sabo R, Harris S, Woessner R, Jennings S, Drollmann AF.

BMC Pulm Med. 2011 May 26;11:31. doi: 10.1186/1471-2466-11-31.


Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.

Wenglowsky S, Ren L, Ahrendt KA, Laird ER, Aliagas I, Alicke B, Buckmelter AJ, Choo EF, Dinkel V, Feng B, Gloor SL, Gould SE, Gross S, Gunzner-Toste J, Hansen JD, Hatzivassiliou G, Liu B, Malesky K, Mathieu S, Newhouse B, Raddatz NJ, Ran Y, Rana S, Randolph N, Risom T, Rudolph J, Savage S, Selby LT, Shrag M, Song K, Sturgis HL, Voegtli WC, Wen Z, Willis BS, Woessner RD, Wu WI, Young WB, Grina J.

ACS Med Chem Lett. 2011 Mar 8;2(5):342-7. doi: 10.1021/ml200025q. eCollection 2011 May 12.


Non-oxime pyrazole based inhibitors of B-Raf kinase.

Newhouse BJ, Hansen JD, Grina J, Welch M, Topalov G, Littman N, Callejo M, Martinson M, Galbraith S, Laird ER, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3488-92. doi: 10.1016/j.bmcl.2010.12.038. Epub 2010 Dec 17.


Efficacy, safety and pharmacokinetics of indacaterol in Caucasian and Japanese patients with chronic obstructive pulmonary disease: a comparison of data from two randomized, placebo-controlled studies.

Hosoe M, Woessner R, Matsushima S, Lawrence D, Kramer B.

Clin Drug Investig. 2011;31(4):247-55. doi: 10.2165/11586520-000000000-00000.


Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.

Bencsik JR, Xiao D, Blake JF, Kallan NC, Mitchell IS, Spencer KL, Xu R, Gloor SL, Martinson M, Risom T, Woessner RD, Dizon F, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ, Prior WW, Murray LJ.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7037-41. doi: 10.1016/j.bmcl.2010.09.112. Epub 2010 Sep 29.


Indacaterol once-daily is equally effective dosed in the evening or morning in COPD.

Magnussen H, Verkindre C, Jack D, Jadayel D, Henley M, Woessner R, Higgins M, Kramer B; INPUT study investigators.

Respir Med. 2010 Dec;104(12):1869-76. doi: 10.1016/j.rmed.2010.08.010. Epub 2010 Sep 20.


Discovery of pyrrolopyrimidine inhibitors of Akt.

Blake JF, Kallan NC, Xiao D, Xu R, Bencsik JR, Skelton NJ, Spencer KL, Mitchell IS, Woessner RD, Gloor SL, Risom T, Gross SD, Martinson M, Morales TH, Vigers GP, Brandhuber BJ.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5607-12. doi: 10.1016/j.bmcl.2010.08.053. Epub 2010 Aug 13.


Mcl-1 stability determines mitotic cell fate of human multiple myeloma tumor cells treated with the kinesin spindle protein inhibitor ARRY-520.

Tunquist BJ, Woessner RD, Walker DH.

Mol Cancer Ther. 2010 Jul;9(7):2046-56. doi: 10.1158/1535-7163.MCT-10-0033. Epub 2010 Jun 22.


ARRY-520, a novel KSP inhibitor with potent activity in hematological and taxane-resistant tumor models.

Woessner R, Tunquist B, Lemieux C, Chlipala E, Jackinsky S, Dewolf W Jr, Voegtli W, Cox A, Rana S, Lee P, Walker D.

Anticancer Res. 2009 Nov;29(11):4373-80.


KSP inhibitor ARRY-520 as a substitute for Paclitaxel in Type I ovarian cancer cells.

Kim KH, Xie Y, Tytler EM, Woessner R, Mor G, Alvero AB.

J Transl Med. 2009 Jul 20;7:63. doi: 10.1186/1479-5876-7-63.


Inhibition of KSP by ARRY-520 induces cell cycle block and cell death via the mitochondrial pathway in AML cells.

Carter BZ, Mak DH, Woessner R, Gross S, Schober WD, Estrov Z, Kantarjian H, Andreeff M.

Leukemia. 2009 Oct;23(10):1755-62. doi: 10.1038/leu.2009.101. Epub 2009 May 21.


Potent and selective pyrazole-based inhibitors of B-Raf kinase.

Hansen JD, Grina J, Newhouse B, Welch M, Topalov G, Littman N, Callejo M, Gloor S, Martinson M, Laird E, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5. doi: 10.1016/j.bmcl.2008.07.002. Epub 2008 Jul 5.


Trial and error versus errorless learning of functional skills in patients with acute stroke.

Mount J, Pierce SR, Parker J, DiEgidio R, Woessner R, Spiegel L.

NeuroRehabilitation. 2007;22(2):123-32.


Safety and tolerability of indacaterol in asthma: a randomized, placebo-controlled 28-day study.

Chuchalin AG, Tsoi AN, Richter K, Krug N, Dahl R, Luursema PB, Cameron R, Bao W, Higgins M, Woessner R, van As A.

Respir Med. 2007 Oct;101(10):2065-75. Epub 2007 Jul 20.


Long-term antibiotic treatment with roxithromycin in patients with multiple sclerosis.

Woessner R, Grauer MT, Frese A, Bethke F, Ginger T, Hans A, Treib J.

Infection. 2006 Dec;34(6):342-4.


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