Molecular Imaging and Pharmacokinetic Analysis of Carbon-11 Labeled Antisense Oligonucleotide LY2181308 in Cancer Patients.

Azeem Saleem; Julian C Matthews; Malcolm Ranson; Sophie Callies; Valérie André; Michael Lahn; Claire Dickinson; Christian Prenant; Gavin Brown; Adam McMahon; Denis C Talbot; Terry Jones; Patricia M Price

doi:10.7150/thno/v01p0290

Molecular Imaging and Pharmacokinetic Analysis of Carbon-11 Labeled Antisense Oligonucleotide LY2181308 in Cancer Patients.

Azeem Saleem, Julian C Matthews, Malcolm Ranson, Sophie Callies, Valérie André, Michael Lahn, Claire Dickinson, Christian Prenant, Gavin Brown, Adam McMahon, Denis C Talbot, Terry Jones, Patricia M Price

Research output: Contribution to journal › Article › peer-review

Abstract

Antisense oligonucleotides (ASOs) have potential as anti-cancer agents by specifically modulating genes involved in tumorigenesis. However, little is known about ASO biodistribution and tissue pharmacokinetics (PKs) in humans, including whether sufficient delivery to target tumor tissue may be achieved. In this preliminary study in human subjects, we used combined positron emission and computed tomography (PET-CT) imaging and subsequent modeling analysis of acquired dynamic data, to examine the in vivo biodistribution and PK properties of LY2181308 - a second generation ASO which targets the apoptosis inhibitor protein survivin. Following radiolabeling of LY2181308 with methylated carbon-11 ([(11)C]methylated-LY2181308), micro-doses (

Original language	English
Pages (from-to)	290-301
Number of pages	12
Journal	Theranostics
Volume	1
DOIs	https://doi.org/10.7150/thno/v01p0290
Publication status	Published - 2011

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.7150/thno/v01p0290

http://www.thno.org/v01p0290.htm

Cite this

@article{7601b7f0d28544fcbc99c8c3dd5798ff,

title = "Molecular Imaging and Pharmacokinetic Analysis of Carbon-11 Labeled Antisense Oligonucleotide LY2181308 in Cancer Patients.",

abstract = "Antisense oligonucleotides (ASOs) have potential as anti-cancer agents by specifically modulating genes involved in tumorigenesis. However, little is known about ASO biodistribution and tissue pharmacokinetics (PKs) in humans, including whether sufficient delivery to target tumor tissue may be achieved. In this preliminary study in human subjects, we used combined positron emission and computed tomography (PET-CT) imaging and subsequent modeling analysis of acquired dynamic data, to examine the in vivo biodistribution and PK properties of LY2181308 - a second generation ASO which targets the apoptosis inhibitor protein survivin. Following radiolabeling of LY2181308 with methylated carbon-11 ([(11)C]methylated-LY2181308), micro-doses (",

author = "Azeem Saleem and Matthews, {Julian C} and Malcolm Ranson and Sophie Callies and Val{\'e}rie Andr{\'e} and Michael Lahn and Claire Dickinson and Christian Prenant and Gavin Brown and Adam McMahon and Talbot, {Denis C} and Terry Jones and Price, {Patricia M}",

year = "2011",

doi = "10.7150/thno/v01p0290",

language = "English",

volume = "1",

pages = "290--301",

journal = "Theranostics",

issn = "1838-7640",

publisher = "Ivyspring International Publisher",

}

TY - JOUR

T1 - Molecular Imaging and Pharmacokinetic Analysis of Carbon-11 Labeled Antisense Oligonucleotide LY2181308 in Cancer Patients.

AU - Saleem, Azeem

AU - Matthews, Julian C

AU - Ranson, Malcolm

AU - Callies, Sophie

AU - André, Valérie

AU - Lahn, Michael

AU - Dickinson, Claire

AU - Prenant, Christian

AU - Brown, Gavin

AU - McMahon, Adam

AU - Talbot, Denis C

AU - Jones, Terry

AU - Price, Patricia M

PY - 2011

Y1 - 2011

N2 - Antisense oligonucleotides (ASOs) have potential as anti-cancer agents by specifically modulating genes involved in tumorigenesis. However, little is known about ASO biodistribution and tissue pharmacokinetics (PKs) in humans, including whether sufficient delivery to target tumor tissue may be achieved. In this preliminary study in human subjects, we used combined positron emission and computed tomography (PET-CT) imaging and subsequent modeling analysis of acquired dynamic data, to examine the in vivo biodistribution and PK properties of LY2181308 - a second generation ASO which targets the apoptosis inhibitor protein survivin. Following radiolabeling of LY2181308 with methylated carbon-11 ([(11)C]methylated-LY2181308), micro-doses (

AB - Antisense oligonucleotides (ASOs) have potential as anti-cancer agents by specifically modulating genes involved in tumorigenesis. However, little is known about ASO biodistribution and tissue pharmacokinetics (PKs) in humans, including whether sufficient delivery to target tumor tissue may be achieved. In this preliminary study in human subjects, we used combined positron emission and computed tomography (PET-CT) imaging and subsequent modeling analysis of acquired dynamic data, to examine the in vivo biodistribution and PK properties of LY2181308 - a second generation ASO which targets the apoptosis inhibitor protein survivin. Following radiolabeling of LY2181308 with methylated carbon-11 ([(11)C]methylated-LY2181308), micro-doses (

U2 - 10.7150/thno/v01p0290

DO - 10.7150/thno/v01p0290

M3 - Article

C2 - 21772926

SN - 1838-7640

VL - 1

SP - 290

EP - 301

JO - Theranostics

JF - Theranostics

ER -

Molecular Imaging and Pharmacokinetic Analysis of Carbon-11 Labeled Antisense Oligonucleotide LY2181308 in Cancer Patients.

Abstract

UN SDGs

Access to Document

Fingerprint

Cite this