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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: brodfuehrer ji. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
The Interleukin-1 Receptor-Associated Kinase 4 Inhibitor PF-06650833 Blocks Inflammation in Preclinical Models of Rheumatic Disease and in Humans Enrolled in a Randomized Clinical Trial.
Winkler A, Sun W, De S, Jiao A, Sharif MN, Symanowicz PT, Athale S, Shin JH, Wang J, Jacobson BA, Ramsey SJ, Dower K, Andreyeva T, Liu H, Hegen M, Homer BL, Brodfuehrer J, Tilley M, Gilbert SA, Danto SI, Beebe JJ, Barnes BJ, Pascual V, Lin LL, Kilty I, Fleming M, Rao VR. Winkler A, et al. Arthritis Rheumatol. 2021 Dec;73(12):2206-2218. doi: 10.1002/art.41953. Epub 2021 Nov 1. Arthritis Rheumatol. 2021. PMID: 34423919 Free PMC article. Clinical Trial.
A Phase 1 Study to Assess Mass Balance and Absolute Bioavailability of Zimlovisertib in Healthy Male Participants Using a 14 C-Microtracer Approach.
Singh RSP, Dowty ME, Salganik M, Brodfuehrer JI, Walker GS, Sharma R, Beebe JS, Danto SI. Singh RSP, et al. Among authors: brodfuehrer ji. Clin Pharmacol Drug Dev. 2022 Jul;11(7):815-825. doi: 10.1002/cpdd.1109. Epub 2022 May 4. Clin Pharmacol Drug Dev. 2022. PMID: 35506501 Free PMC article. Clinical Trial.
Pharmacokinetics of clinafloxacin after single and multiple doses.
Randinitis EJ, Brodfuehrer JI, Eiseman I, Vassos AB. Randinitis EJ, et al. Among authors: brodfuehrer ji. Antimicrob Agents Chemother. 2001 Sep;45(9):2529-35. doi: 10.1128/AAC.45.9.2529-2535.2001. Antimicrob Agents Chemother. 2001. PMID: 11502525 Free PMC article. Clinical Trial.
Pharmacokinetics of clinafloxacin enantiomers in humans.
Humphrey GH, Shapiro MA, Randinitis EJ, Guttendorf RJ, Brodfuehrer JI. Humphrey GH, et al. Among authors: brodfuehrer ji. J Clin Pharmacol. 1999 Nov;39(11):1143-50. J Clin Pharmacol. 1999. PMID: 10579144
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