Quantification and reliability of [11C]VC - 002 binding to muscarinic acetylcholine receptors in the human lung — a test-retest PET study in control subjects

Autor: Zsolt Cselényi, Aurelija Jucaite, Cecilia Kristensson, Per Stenkrona, Pär Ewing, Andrea Varrone, Peter Johnström, Magnus Schou, Ana Vazquez-Romero, Mohammad Mahdi Moein, Martin Bolin, Jonathan Siikanen, Pär Grybäck, Bengt Larsson, Christer Halldin, Ken Grime, Ulf G. Eriksson, Lars Farde

Publikováno v: EJNMMI Research, Vol 10, Iss 1, Pp 1-13 (2020)

Abstract Background The radioligand [11C]VC-002 was introduced in a small initial study long ago for imaging of muscarinic acetylcholine receptors (mAChRs) in human lungs using positron emission tomography (PET). The objectives of the present study i

Externí odkaz: https://doaj.org/article/b57a1b395ada441a9bd3f59c5762420f

Figure S1 from Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs

Autor: Darren A.E. Cross, Zack Cheng, Lars Farde, Paul D. Smith, James W.T. Yates, Richard A. Ward, M. Raymond V. Finlay, Natasha A. Karp, Albert D. Windhorst, Mohammad Mahdi Moein, Ana Vazquez-Romero, Evgeny Revunov, Jonas Malmquist, Mikhail Kondrashov, Ryosuke Arakawa, Akihiro Takano, Aaron Smith, Joanne Wilson, Annika Janefeldt, Lin Zhang, James Atkinson, Peter Barton, Gareth Maglennon, Don X. Nguyen, Minghui Zhao, Sally J. Adua, Katarina Varnäs, Richard Goodwin, Magnus Schou, Gail L. Wrigley, Yumei Yan, Nicole Strittmatter, Peter Johnström, Kan Chen, Nicola Colclough

Supplementary Figure S1 - Structure and position of label for compounds assessed for BBB penetrance in non human primates (NHP). Majority of compounds were labelled with carbon-11 except afatinib which was labelled with fluorine-18. (*) Indicates pos

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f25e8e82af5345d6a7e68e8c3a46ea5
https://doi.org/10.1158/1078-0432.22473252

Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs

Autor: Aaron Smith, Peter Johnström, Katarina Varnäs, James Atkinson, Minghui Zhao, Nicole Strittmatter, Yumei Yan, Ryosuke Arakawa, Nicola Colclough, Annika Janefeldt, M. Raymond V. Finlay, Albert D. Windhorst, Evgeny Revunov, Natasha A. Karp, Kan Chen, Lin Zhang, Gareth Maglennon, Peter Barton, Richard J. A. Goodwin, Ana Vazquez-Romero, Magnus Schou, Akihiro Takano, Gail L. Wrigley, Darren Cross, Mikhail Kondrashov, Mohammad Mahdi Moein, Zack Cheng, Paul D. Smith, Sally J. Adua, Richard A. Ward, Lars Farde, James W.T. Yates, Joanne Wilson, Jonas Malmquist, Don X. Nguyen

Publikováno v: Colclough, N, Chen, K, Johnstrom, P, Strittmatter, N, Yan, Y, Wrigley, G L, Schou, M, Goodwin, R, Varnas, K, Adua, S J, Zhao, M, Nguyen, D X, Maglennon, G, Barton, P, Atkinson, J, Zhang, L, Janefeldt, A, Wilson, J, Smith, A, Takano, A, Arakawa, R, Kondrashov, M, Malmquist, J, Revunov, E, Vazquez-Romero, A, Moein, M M, Windhorst, A D, Karp, N A, Finlay, R V, Ward, R A, Yates, J W T, Smith, P D, Farde, L, Cheng, Z & Cross, D A E 2021, ' Preclinical comparison of the blood-brain barrier permeability of osimertinib with other EGFR TKIs ', Clinical Cancer Research, vol. 27, no. 1, pp. 189-201 . https://doi.org/10.1158/1078-0432.CCR-19-1871
Clinical Cancer Research, 27(1), 189-201. American Association for Cancer Research Inc.

Purpose: Osimertinib is a potent and selective EGFR tyrosine kinase inhibitor (EGFR-TKI) of both sensitizing and T790M resistance mutations. To treat metastatic brain disease, blood–brain barrier (BBB) permeability is considered desirable for incre

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d134e34f16839af3ef1a834fbea0f94
https://doi.org/10.1158/1078-0432.ccr-19-1871

Brain exposure of the ATM inhibitor AZD1390 in humans-a positron emission tomography study

Autor: Per Stenkrona, Zsolt Cselényi, Martin Pass, Mohammad Mahdi Moein, Andrea Varrone, Andy Sykes, Lars Farde, Christer Halldin, Chris Davison, Serena De Vita, Venkatesh Pilla Reddy, Núria Buil-Bruna, Melinda S. Merchant, Alicia Savage, Katarina Varnäs, Matthias Hoch, Magnus Schou, Peter Johnström, Aurelija Jucaite, Ana Vazquez-Romero

Publikováno v: Neuro Oncol

Background The protein kinase ataxia telangiectasia mutated (ATM) mediates cellular response to DNA damage induced by radiation. ATM inhibition decreases DNA damage repair in tumor cells and affects tumor growth. AZD1390 is a novel, highly potent, se

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbfb688a1e94c6c9ad2d65bea16ed066
https://pubmed.ncbi.nlm.nih.gov/33704490

A PET study in healthy subjects of brain exposure of (11)C-labelled osimertinib – A drug intended for treatment of brain metastases in non-small cell lung cancer

Autor: Christer Halldin, Andrew P. Brown, Peter Johnström, Mohammad Mahdi Moein, Karthick Vishwanathan, Magnus Schou, Lars Farde, Andrea Varrone, Aurelija Jucaite, Zsolt Cselényi, Ana Vazquez-Romero, Katarina Varnäs

Publikováno v: J Cereb Blood Flow Metab

Osimertinib is a tyrosine kinase inhibitor (TKI) of the mutated epidermal growth factor receptor (EGFRm) with observed efficacy in patients with brain metastases. Brain exposure and drug distribution in tumor regions are important criteria for evalua

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cefc739fda3d1a79bee1e8a3e1e389df
https://europepmc.org/articles/PMC7168784/