-
Je něco špatně v tomto záznamu ?
Preclinical evaluation of radiolabelled nimotuzumab, a promising monoclonal antibody targeting the epidermal growth factor receptor
P. Barta, A. Laznickova, M. Laznicek, DR. Vera, M. Beran,
Jazyk angličtina Země Anglie, Velká Británie
Typ dokumentu časopisecké články, práce podpořená grantem
Odkazy
PubMed
24285372
DOI
10.1002/jlcr.2988
Knihovny.cz E-zdroje
- MeSH
- humanizované monoklonální protilátky chemie farmakokinetika farmakologie MeSH
- izotopové značení MeSH
- krysa rodu rattus MeSH
- lidé MeSH
- lutecium chemie farmakokinetika MeSH
- nádorové buněčné linie MeSH
- preklinické hodnocení léčiv MeSH
- radiofarmaka chemická syntéza farmakokinetika farmakologie MeSH
- radioizotopy jodu chemie farmakokinetika MeSH
- tkáňová distribuce MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
BACKGROUND: Radiolabelled monoclonal antibodies with affinity towards tumour-associated antigens may enhance the efficacy of cancer treatment with targeted radiotherapy. The humanized antibody nimotuzumab represents a promising vector to deliver radioactivity to tumours overexpressing epidermal growth factor receptor type 1 (ErbB1). We analysed the effect of radiolabelling nimotuzumab on its uptake in cancer cells and its biodistribution profile in preclinical experiments. METHODS: Nimotuzumab was labelled with (131) I by oxidative iodination and with (177) Lu using nimotuzumab conjugates with two different chelators (DTPA and DOTA) and two different spacers (p-SCN-Bn and NHS). For the receptor studies, two cell lines (HaCaT and A431) were used. Biodistribution studies were performed in male Wistar rats. RESULTS: The choice of radiolabel and the manner of its attachment to nimotuzumab had little effect on the internalization of the antibody into ErbB1-expressing cell lines. However, the type of radiolabel, the way in which it was attached to nimotuzumab and the radiolabelling procedure, significantly affected the blood clearance, liver uptake and liver persistence of radiolabelled nimotuzumab. (131) I-nimotuzumab had the longest elimination half-life and the lowest radioactivity uptake in the liver. (177) Lu-labelled nimotuzumab exhibited a shorter elimination half-life, high radioactivity and long-term retention in the liver.
- 000
- 00000naa a2200000 a 4500
- 001
- bmc14074465
- 003
- CZ-PrNML
- 005
- 20141009092422.0
- 007
- ta
- 008
- 141006s2013 enk f 000 0|eng||
- 009
- AR
- 024 7_
- $a 10.1002/jlcr.2988 $2 doi
- 035 __
- $a (PubMed)24285372
- 040 __
- $a ABA008 $b cze $d ABA008 $e AACR2
- 041 0_
- $a eng
- 044 __
- $a enk
- 100 1_
- $a Barta, Pavel $u Department of Pharmacology and Toxicology, Charles University in Prague, Czech Republic.
- 245 10
- $a Preclinical evaluation of radiolabelled nimotuzumab, a promising monoclonal antibody targeting the epidermal growth factor receptor / $c P. Barta, A. Laznickova, M. Laznicek, DR. Vera, M. Beran,
- 520 9_
- $a BACKGROUND: Radiolabelled monoclonal antibodies with affinity towards tumour-associated antigens may enhance the efficacy of cancer treatment with targeted radiotherapy. The humanized antibody nimotuzumab represents a promising vector to deliver radioactivity to tumours overexpressing epidermal growth factor receptor type 1 (ErbB1). We analysed the effect of radiolabelling nimotuzumab on its uptake in cancer cells and its biodistribution profile in preclinical experiments. METHODS: Nimotuzumab was labelled with (131) I by oxidative iodination and with (177) Lu using nimotuzumab conjugates with two different chelators (DTPA and DOTA) and two different spacers (p-SCN-Bn and NHS). For the receptor studies, two cell lines (HaCaT and A431) were used. Biodistribution studies were performed in male Wistar rats. RESULTS: The choice of radiolabel and the manner of its attachment to nimotuzumab had little effect on the internalization of the antibody into ErbB1-expressing cell lines. However, the type of radiolabel, the way in which it was attached to nimotuzumab and the radiolabelling procedure, significantly affected the blood clearance, liver uptake and liver persistence of radiolabelled nimotuzumab. (131) I-nimotuzumab had the longest elimination half-life and the lowest radioactivity uptake in the liver. (177) Lu-labelled nimotuzumab exhibited a shorter elimination half-life, high radioactivity and long-term retention in the liver.
- 650 _2
- $a zvířata $7 D000818
- 650 _2
- $a humanizované monoklonální protilátky $x chemie $x farmakokinetika $x farmakologie $7 D061067
- 650 _2
- $a nádorové buněčné linie $7 D045744
- 650 _2
- $a preklinické hodnocení léčiv $7 D004353
- 650 _2
- $a lidé $7 D006801
- 650 _2
- $a radioizotopy jodu $x chemie $x farmakokinetika $7 D007457
- 650 _2
- $a izotopové značení $7 D007553
- 650 _2
- $a lutecium $x chemie $x farmakokinetika $7 D008187
- 650 _2
- $a radiofarmaka $x chemická syntéza $x farmakokinetika $x farmakologie $7 D019275
- 650 _2
- $a krysa rodu Rattus $7 D051381
- 650 _2
- $a tkáňová distribuce $7 D014018
- 655 _2
- $a časopisecké články $7 D016428
- 655 _2
- $a práce podpořená grantem $7 D013485
- 700 1_
- $a Laznickova, Alice
- 700 1_
- $a Laznicek, Milan
- 700 1_
- $a Vera, Denis Rolando Beckford
- 700 1_
- $a Beran, Milos
- 773 0_
- $w MED00002760 $t Journal of labelled compounds & radiopharmaceuticals $x 1099-1344 $g Roč. 56, č. 5 (2013), s. 280-8
- 856 41
- $u https://pubmed.ncbi.nlm.nih.gov/24285372 $y Pubmed
- 910 __
- $a ABA008 $b sig $c sign $y a $z 0
- 990 __
- $a 20141006 $b ABA008
- 991 __
- $a 20141009092810 $b ABA008
- 999 __
- $a ok $b bmc $g 1042348 $s 873377
- BAS __
- $a 3
- BAS __
- $a PreBMC
- BMC __
- $a 2013 $b 56 $c 5 $d 280-8 $i 1099-1344 $m Journal of labelled compounds & radiopharmaceuticals $n J Labelled Comp Radiopharm $x MED00002760
- LZP __
- $a Pubmed-20141006