Výsledky vyhledávání - "Peter D. Gorycki"

First‐in‐Human Studies for a Selective RET Tyrosine Kinase Inhibitor, GSK3179106, to Investigate the Safety, Tolerability, and Pharmacokinetics in Healthy Volunteers

Autor: Peter D. Gorycki, Kristen E. Pannullo, Melisa Cooper, Robin O'Connor-Semmes, Beth Ann Reedy, Kimberley Hacquoil, Sepehr Shakib, Adeline Verticelli

Publikováno v: Clinical Pharmacology in Drug Development. 8:234-245

Rearranged during transfection (RET), a neuronal growth factor receptor tyrosine kinase, regulates the development of the sympathetic, parasympathetic, motor, and sensory neurons in the enteric nervous system. GSK3179106 is a RET kinase inhibitor tha

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::596390355047b625fe67f7430123fd73
https://doi.org/10.1002/cpdd.600

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First-in-Human Study for a Selective Rearranged During Transfection Tyrosine Kinase Inhibitor, GSK3352589, to Investigate the Safety, Tolerability, and Pharmacokinetics in Healthy Volunteers

Autor: Robin O'Connor-Semmes, Adeline Verticelli, Kimberley Hacquoil, Beth Ann Reedy, Peter D. Gorycki, Angela Molga

Publikováno v: Clinical pharmacology in drug developmentReferences. 10(4)

Rearranged during transfection (RET), a neuronal growth factor receptor tyrosine kinase, regulates the development of sympathetic, parasympathetic, motor, and sensory neurons in the enteric nervous system. The intended site of action for GSK3352589 i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a808c60983edfc3909439ddd99256616
https://pubmed.ncbi.nlm.nih.gov/33606922

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Bioactivation of herbal constituents: mechanisms and toxicological relevance

Autor: Peter D. Gorycki, Bo Wen

Publikováno v: Drug metabolism reviews. 51(4)

The increase in the application of herbal medicines and dietary products over the last decades has been accompanied with a substantial increase in case reports of herb-induced toxicities. Metabolic activation of relatively inert functional groups to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8d7c58a27fd1450faf0947088c729b5f
https://pubmed.ncbi.nlm.nih.gov/31448961

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1315. No Dose Adjustment of Metformin with Fostemsavir Coadministration Based on Mechanistic Static and Physiologically Based Pharmacokinetic Models

Autor: Guoying Tai, Peter D. Gorycki, Mindy Magee, Katy H. P. Moore, Dung N Nguyen, Xiusheng Miao

Publikováno v: Open Forum Infectious Diseases

Background Fostemsavir (FTR) is an oral prodrug of the first-in-class attachment inhibitor temsavir (TMR) which is being evaluated in patients with multidrug resistant HIV-1 infection. In vitro studies indicated that TMR and its 2 major metabolites a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d0416d7fdc59f6f53de226d895739cb
https://doi.org/10.1093/ofid/ofaa439.1497

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2500. Fostemsavir Drug–Drug Interaction Profile, an Attachment Inhibitor and Oral Prodrug of Temsavir, for Heavily Treatment Experienced HIV-1-Infected Patients

Autor: Katy H. P. Moore, Peter D. Gorycki, Mindy Magee, Peter Ackerman, Cyril Llamoso, A Savannah Mageau

Publikováno v: Open Forum Infectious Diseases

Background Fostemsavir (FTR) is a first-in-class attachment inhibitor being evaluated in heavily treatment-experienced (HTE) HIV-1-infected patients. Active temsavir (TMR) binds to viral envelope glycoprotein 120 and prevents viral attachment and ent

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::069c47a973fc6dbc08be16fe5bd1b067
http://europepmc.org/articles/PMC6810480

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Metabolism and Disposition of Oral Dabrafenib in Cancer Patients: Proposed Participation of Aryl Nitrogen in Carbon-Carbon Bond Cleavage via Decarboxylation following Enzymatic Oxidation

Autor: Dana Knecht, Samuel C. Blackman, Kristen E Jurusik, Lauren E. Richards-Peterson, Peter D. Gorycki, Jerry L. Adams, Donna Mamaril-Fishman, David A. Bershas, Noelia Nebot, Royce A. Morrison, Stanley W. Carson, Daniele Ouellet

Publikováno v: Drug Metabolism and Disposition. 41:2215-2224

A phase I study was conducted to assess the metabolism and excretion of [(14)C]dabrafenib (GSK2118436; N-{3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzene sulfonamide, methanesulfonate salt), a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::20c9d2e4a5b1542ed07fbedd81036ccb
https://doi.org/10.1124/dmd.113.053785

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Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer

Autor: Emile P. Chen, Mohammed M. Dar, Yanwen Qian, Peter D. Gorycki, Yanli Deng, A. Benjamin Suttle, Kitaw Negash, May Y. K. Ho, Caroline Sychterz, David A. Bershas

Publikováno v: Xenobiotica. 43:443-453

1. Pazopanib (Votrient) is an oral tyrosine kinase inhibitor that was recently approved for the treatment of renal cell carcinoma and soft tissue sarcoma. 2. In this two-part study, we investigated the metabolism, disposition of [(14)C]pazopanib, and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3afb5d9e737fb0795d5057fc96e8b8b3
https://doi.org/10.3109/00498254.2012.734642

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Investigations of Hydrazine Cleavage of Eltrombopag in Humans

Autor: Emile P. Chen, Cosette J. Serabjit-Singh, David A. Bershas, May Ho, Yanli Deng, Yanwen Qian, Caroline Sychterz, Peter D. Gorycki, Martin Rogers, Wei Shi, Kimberly Talley

Publikováno v: Drug Metabolism and Disposition. 39:1747-1754

After oral administration to humans, eltrombopag undergoes extensive cleavage of its hydrazine linkage to metabolites, which are exclusively eliminated in urine. In vitro, the cleavage pathway was not detected in systems using cytochrome P450 enzymes

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::27c8210af8aacf34e21a15b6d74a5bf2
https://doi.org/10.1124/dmd.111.040188

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Metabolism of [14C]GSK977779 in Rats and Its Implication with the Observed Covalent Binding

Autor: William M. Hardesty, Fangming Xia, Armina Madatian, Ernest M. Schubert, Peter D. Gorycki, Yanli Deng, Jennifer L. Seymour, Catherine D. Tsalta

Publikováno v: Drug Metabolism and Disposition. 39:1620-1632

GSK977779 is a potent HM74a agonist evaluated for the treatment of dyslipidemia. The disposition and metabolism of [(14)C]GSK977779 (67.6 μmol/kg p.o.) was studied in male and female rats. The compound was well absorbed and its primary route of elim

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09774896aa3f9dafaf3900a6619ec5ab
https://doi.org/10.1124/dmd.110.036467

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SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. II: In vitro and in vivo metabolism studies and pharmacokinetic extrapolation to man

Autor: Brian R. Smith, Keith W. Ward, J. W. Proksch, M. A. Levy, C.-P. Yu, B. D. Bush, Peter D. Gorycki, May Y. K. Ho

Publikováno v: Xenobiotica. 32:235-250

1. Inhibition of p38 MAP kinase has been investigated extensively as a potential therapy for cytokine-mediated diseases such as autoimmune and inflammatory diseases. SB-242235 (1-(4-piperidinyl)-4-(4-fluorophenyl)-5-(2-methoxy-4-pyrimidinyl) imidazol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::025b2487aa720d19b891030018a96290
https://doi.org/10.1080/00498250110100711

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