S. Yeleswaram

发表

The Janus Kinase 2 Inhibitor Fedratinib Inhibits Thiamine Uptake: A Putative Mechanism for the Onset of Wernicke’s Encephalopathy

R. Wynn, Phillip C. C. Liu, T. Burn, 2014, Drug Metabolism and Disposition.

Clinical Benefit of INCB7839, a Potent and Selective Inhibitor of ADAM10 and ADAM17, in Combination with Trastuzumab in Metastatic HER2 Positive Breast Cancer Patients.

D. Doval, S. Nag, G. Bhattacharyya, 2009 .

Abstract LB-268: Assessment of flat dosing strategy for INCMGA00012 in patients with advanced tumors

S. Kaul, Xuejun Chen, S. Yeleswaram, 2019, Experimental and Molecular Therapeutics.

The Effect of CYP3A4 Inhibition or Induction on the Pharmacokinetics and Pharmacodynamics of Orally Administered Ruxolitinib (INCB018424 Phosphate) in Healthy Volunteers

P. Scherle, Yvonne Lo, T. Emm, 2012, Journal of clinical pharmacology.

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

G. Trainor, R. Copeland, S. P. Seitz, 2005, Molecular Cancer Therapeutics.

Identification and Characterization of INCB 9471 , an Allosteric Noncompetitive Small-Molecule Antagonist of C-C Chemokine Receptor 5 with Potent Inhibitory Activity against Monocyte Migration and HIV-1 Infection

P. Scherle, N. Zhou, F. Baribaud, 2011 .

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

P. Scherle, N. Zhou, F. Baribaud, 2011, Journal of Pharmacology and Experimental Therapeutics.

Species-Specific Metabolism of SGX523 by Aldehyde Oxidase and the Toxicological Implications

T. Maduskuie, S. Diamond, J. Boer, 2010, Drug Metabolism and Disposition.

Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy

H. Koblish, M. Stubbs, Q. Wang, 2020, The Journal of Pharmacology and Experimental Therapeutics.

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

R. Wynn, A. Margulis, H. Koblish, 2018, PloS one.

Developing a JAK Inhibitor for Targeted Local Delivery: Ruxolitinib Cream

M. Covington, S. Shepard, S. Yeleswaram, 2021, Pharmaceutics.

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

P. Scherle, K. Vaddi, M. Covington, 2011, ACS medicinal chemistry letters.

The Pharmacokinetics, Pharmacodynamics, and Safety of Orally Dosed INCB018424 Phosphate in Healthy Volunteers

P. Scherle, Yvonne Lo, T. Emm, 2011, Journal of clinical pharmacology.

Population Pharmacokinetics Analysis of Pemigatinib in Patients With Advanced Malignancies

Xuejun Chen, S. Yeleswaram, Tao Ji, 2022, Clinical pharmacology in drug development.

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

G. Trainor, M. Covington, C. Decicco, 2005, Journal of medicinal chemistry.

Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.

R. Wynn, P. Scherle, K. Vaddi, 2022, Bioorganic & medicinal chemistry letters.

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

Xuejun Chen, S. Yeleswaram, N. Punwani, 2014, Clinical pharmacology in drug development.

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

I. Kariv, K. Vaddi, M. Covington, 2007, Bioorganic & medicinal chemistry letters.

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

A. Gottlieb, P. Scherle, S. Yeleswaram, 2012, Journal of the American Academy of Dermatology.

Parsaclisib Is a Next-Generation PI3Kδ Inhibitor With Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy a

Kathy, Qianqian Wang, H. Koblish, 2020 .

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

Haifeng Zhang, A. Menter, P. Scherle, 2016, The Journal of dermatological treatment.

Development of 2 Bromodomain and Extraterminal Inhibitors With Distinct Pharmacokinetic and Pharmacodynamic Profiles for the Treatment of Advanced Malignancies

David C. Smith, P. LoRusso, R. Kurzrock, 2019, Clinical Cancer Research.

Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050

J. Fridman, Jun Li, X. Wen, 2010, The Journal of Immunology.

Selective Inhibition of JAK 1 and JAK 2 Is Efficacious in Rodent Models of Arthritis : Preclinical Characterization of INCB 028050

J. Fridman, Jun Li, X. Wen, 2010 .

Preclinical Characterization of INCB 028050 Efficacious in Rodent Models of Arthritis : Selective Inhibition of JAK 1 and JAK 2 Is

J. Fridman, Jun Li, X. Wen, 2010 .

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

Xuejun Chen, S. Yeleswaram, Jack G. Shi, 2016, Journal of clinical pharmacology.

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

P. Scherle, L. Leffet, Yanlong Li, 2012, European journal of pharmacology.

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

A. Gottlieb, P. Scherle, K. Vaddi, 2015, The British journal of dermatology.

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

P. Scherle, Yvonne Lo, T. Emm, 2014, Journal of clinical pharmacology.

Design of Clinical Trials Evaluating Ruxolitinib, a JAK1/JAK2 Inhibitor, for Treatment of COVID-19–Associated Cytokine Storm

S. Yeleswaram, P. Langmuir, B. Knorr, 2020, Delaware journal of public health.

Evaluation of drug-drug interactions of pemigatinib in healthy participants

K. Rockich, Xuejun Chen, S. Yeleswaram, 2021, European Journal of Clinical Pharmacology.

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

J. Fridman, P. Scherle, C. Neilan, 2011, The Journal of investigative dermatology.

Discovery of 5,7-Dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones as Highly Selective CDK2 Inhibitors.

Yvonne Lo, M. Covington, S. Diamond, 2022, ACS medicinal chemistry letters.

INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).

H. Koblish, P. Scherle, T. Maduskuie, 2019, ACS medicinal chemistry letters.

Metabolism, Excretion, and Pharmacokinetics of [14C]INCB018424, a Selective Janus Tyrosine Kinase 1/2 Inhibitor, in Humans

S. Shepard, J. Rodgers, T. Emm, 2010, Drug Metabolism and Disposition.

Plasma pharmacokinetics and distribution of ruxolitinib into skin following oral and topical administration in minipigs.

S. Diamond, Jennifer J. Harris, S. Yeleswaram, 2020, International journal of pharmaceutics.

Population Pharmacokinetic Analysis of Orally‐Administered Ruxolitinib (INCB018424 Phosphate) in Patients With Primary Myelofibrosis (PMF), Post‐Polycythemia Vera Myelofibrosis (PPV‐MF) or Post‐Essential Thrombocythemia Myelofibrosis (PET MF)

Xuejun Chen, S. Yeleswaram, W. Williams, 2013, Journal of clinical pharmacology.

Discovery of a novel 2-spiro-proline steroid mimetic scaffold for the potent inhibition of 11β-HSD1.

R. Wynn, P. Scherle, Yanlong Li, 2022, Bioorganic & medicinal chemistry letters.

Effect of Itraconazole or Rifampin on Itacitinib Pharmacokinetics When Administered Orally in Healthy Subjects

Xuejun Chen, S. Yeleswaram, Phillip Wang, 2019, Journal of clinical pharmacology.

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

G. Trainor, S. P. Seitz, C. Albright, 2010, Bioorganic & medicinal chemistry letters.

Discovery and Pharmacological Characterization of a Novel Rodent-Active CCR2 Antagonist, INCB3344

P. Scherle, F. Baribaud, L. Leffet, 2005, The Journal of Immunology.

Evaluation of the pharmacokinetics of pemigatinib in patients with impaired hepatic or renal function

T. Ji, K. Rockich, Xuejun Chen, 2021, British journal of clinical pharmacology.

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

P. Scherle, K. Vaddi, Joseph Glenn, 2010, ACS medicinal chemistry letters.

A Maximum-Use Trial of Ruxolitinib Cream in Adolescents and Adults with Atopic Dermatitis

R. Bissonnette, S. Yeleswaram, R. Call, 2022, American Journal of Clinical Dermatology.

Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).

M. Covington, S. Diamond, E. Behshad, 2022, ACS medicinal chemistry letters.

Discovery of Pyrazolopyridine Derivatives as HPK1 Inhibitors.

M. Covington, S. Diamond, E. Behshad, 2022, ACS medicinal chemistry letters.

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

P. Scherle, K. Vaddi, M. Covington, 2010, Bioorganic & medicinal chemistry letters.

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

M. Bower, R. Wynn, Wenyu Zhu, 2006, Journal of medicinal chemistry.

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.

Astrid A. Ortiz, V. Gribkoff, J. Starrett, 2007, Journal of medicinal chemistry.

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

D. J. Rogier, P. Scherle, R. Devraj, 2011, Bioorganic & medicinal chemistry letters.

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.

I. Kariv, S. Mandlekar, A. Tebben, 2008, Bioorganic & medicinal chemistry letters.

Impact on Creatinine Renal Clearance by the Interplay of Multiple Renal Transporters: A Case Study with INCB039110

Bill Williams, Yan Zhang, S. Diamond, 2015, Drug Metabolism and Disposition.

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

Lixin Shao, Michael Xia, D. J. Rogier, 2011, ACS medicinal chemistry letters.

Discovery and Pharmacological Characterization of a Novel Rodent-Active CCR2 Antagonist, INCB3344

P. Scherle, F. Baribaud, T. Burn, 2005, The Journal of Immunology.

Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.

M. Covington, S. Diamond, S. Yeleswaram, 2022, ACS medicinal chemistry letters.

Bioanalysis of INCB000928 in human saliva: nonspecific binding and inhomogeneous concentration.

S. Yeleswaram, Phillip Wang, Zhiyin Xun, 2022, Bioanalysis.

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

Kevin J. Bowman, A. Combs, W. Frietze, 2016, Drug Metabolism and Disposition.

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

Jun Yu Li, Qianqian Wang, B. Rumberger, 2018, The Journal of Pharmacology and Experimental Therapeutics.

INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models

R. Wynn, H. Koblish, Yue Zhang, 2020, PloS one.

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

Jun Yu Li, R. Wynn, X. Liu, 2018, Clinical Cancer Research.

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

P. Scherle, T. Emm, Xuejun Chen, 2014, Clinical pharmacology in drug development.

An Open‐Label Study to Assess the Effect of Itraconazole and Rifampin on Parsaclisib Pharmacokinetics When Administered Orally in Healthy Participants

Gongfu Zhou, K. Rockich, Xuejun Chen, 2020, Journal of clinical pharmacology.

Abstract 2671: INCB050465, a novel PI3Kδ inhibitor, synergizes with PIM protein kinase inhibition to cause tumor regression in a model of DLBCL

H. Koblish, P. Scherle, T. Maduskuie, 2015 .

ONGOING PHASE 1/2 STUDY OF INCB050465, A SELECTIVE PI3Kδ INHIBITOR, FOR THE TREATMENT OF PATIENTS (PTS) WITH RELAPSED/REFRACTORY (R/R) B‐CELL MALIGNANCIES (CITADEL‐101)

D. Demarini, T. Phillips, L. Akard, 2017 .

Microsoft Word-26861637-file00

Bill Williams, Yan Zhang, S. Diamond, 2015 .

Abstract 5071: Preclinical characterization of the potent and selective BET inhibitor INCB057643 in models of hematologic malignancies

R. Wynn, X. Liu, X. Wen, 2017 .

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

J. Fridman, P. Scherle, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

Pharmacokinetics of Ruxolitinib in Patients with Atopic Dermatitis Treated With Ruxolitinib Cream: Data from Phase II and III Studies

Xuejun Chen, S. Yeleswaram, M. Kuligowski, 2021, American Journal of Clinical Dermatology.

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

Yan Zhang, S. Yeleswaram, Jack G. Shi, 2010, Nature Reviews Drug Discovery.

Effects of Epacadostat on Brain Extracellular Fluid Concentrations of Serotonin—an Intracerebral Microdialysis Study in Sprague-Dawley Rats

Kevin J. Bowman, J. Maleski, Yan Zhang, 2019, Drug Metabolism and Disposition.

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

T. Emm, S. Yeleswaram, Swamy Yeleswaram, 2011, Biomedical chromatography : BMC.

Evaluation of the clinical cardiac safety of pemigatinib, a fibroblast growth factor receptor inhibitor, in participants with advanced malignancies

Xuejun Chen, S. Yeleswaram, Xiaohua Gong, 2021, Pharmacology research & perspectives.

Evaluation of Clinical Cardiac Safety of Itacitinib, a JAK1 Inhibitor, in Healthy Participants

B. Darpo, Xuejun Chen, S. Yeleswaram, 2019, Clinical pharmacology in drug development.

Results from a Phase 1/2 Study of INCB050465, a Highly Selective and Highly Potent PI3Kδ Inhibitor, in Patients with Relapsed or Refractory B-Cell Malignancies (CITADEL-101)

D. Demarini, T. Phillips, L. Akard, 2017 .

Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.

R. Wynn, H. Koblish, Yue Zhang, 2021, Journal of medicinal chemistry.

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

S. Verstovsek, Xuejun Chen, S. Yeleswaram, 2018, Hematological oncology.

Abstract 1234: The novel FGFR4-selective inhibitor INCB062079 is efficacious in models of hepatocellular carcinoma harboring FGF19 amplification

X. Wen, M. Stubbs, P. Scherle, 2017 .

Predicting Drug–Drug Interactions Involving Multiple Mechanisms Using Physiologically Based Pharmacokinetic Modeling: A Case Study With Ruxolitinib

S. Yeleswaram, G. Fraczkiewicz, J G Shi, 2015, Clinical pharmacology and therapeutics.

Evaluation of drug–drug interaction potential for pemigatinib using physiologically based pharmacokinetic modeling

Xuejun Chen, S. Yeleswaram, Tao Ji, 2022, CPT: pharmacometrics & systems pharmacology.

Itacitinib Population Pharmacokinetics and Exposure‐Response in Patients With Acute Graft‐Versus‐Host Disease

Zhiyin Xun, Xuejun Chen, S. Yeleswaram, 2023, Journal of clinical pharmacology.

The Effect of Renal Impairment on the Pharmacokinetics and Safety of Itacitinib

Gongfu Zhou, T. Marbury, Xuejun Chen, 2020, Journal of clinical pharmacology.

Population Pharmacokinetic Analysis of Itacitinib, a Selective JAK-1 Inhibitor

Xuejun Chen, S. Yeleswaram, A. Barbour, 2019, Biology of Blood and Marrow Transplantation.

Effect of Hepatic Impairment on the Pharmacokinetics of Itacitinib

Gongfu Zhou, K. Rockich, Xuejun Chen, 2021, Journal of clinical pharmacology.

Inhibition of cytokine signaling by ruxolitinib and implications for COVID-19 treatment

T. Burn, Yanlong Li, M. Covington, 2020, Clinical Immunology.

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

J. Fridman, P. Scherle, K. Vaddi, 2008, Bioorganic & medicinal chemistry letters.

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

M. Bower, R. Wynn, J. Fridman, 2007, Journal of medicinal chemistry.

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

Qiang Zhang, Yan Zhang, S. Diamond, 2017, Drug Metabolism and Disposition.

Abstract 3523: Discovery of a novel BET inhibitor INCB054329

R. Wynn, X. Liu, Jun Li, 2015 .

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

L. Leopold, Kevin J. Bowman, Xuejun Chen, 2017, Journal of clinical pharmacology.

The Role of UGT, CYP and Gut Microbiota in the Metabolism of Epacadostat (EPA) in Humans

W. Frietze, S. Yeleswaram, L. Galya, 2016 .

Characterization of a Novel Rodent-Active Discovery and Pharmacological

P. Scherle, F. Baribaud, L. Leffet, 2013 .

R. Wynn, P. Scherle, K. Vaddi, 2022, Bioorganic & medicinal chemistry letters.

Preliminary Results from an Ongoing Phase 1/2 Study of INCB057643, a Bromodomain and Extraterminal (BET) Protein Inhibitor, in Patients (pts) with Advanced Malignancies

David C. Smith, P. LoRusso, R. Kurzrock, 2017 .