Antisense phosphorothioate oligodeoxyribonucleotide targeted against ICAM-1: synthetic and biological characterization of a process-related impurity formed during oligonucleotide synthesis.
A phosphorothioate-linked oligonucleotide bearing a 3'-terminal phosphorothioate monoester has been synthesized and characterized. This oligonucleotide has been identified as a process-related impurity formed during synthesis of ISIS 2302. Biological properties of the compound have been determined. Based on these data, it can be concluded that this species (3'-TPT) has biological properties similar to parent drug.
Ravikumar
Vasulinga T
VT
Isis Pharmaceuticals, Inc., 2292 Faraday Avenue, Carlsbad, CA 92008, USA. vravikumar@isiph.com
Capaldi
Daniel C
DC
Lima
Walt F
WF
Lesnik
Elena
E
Turney
Brett
B
Cole
Douglas L
DL
D000818:Animals; D020811:Biomedical Technology; D016503:Drug Delivery Systems; D008401:Gas Chromatography-Mass Spectrometry; D007166:Immunosuppressive Agents / Q000138:chemical synthesis / Q000302:isolation & purification / Q000378:metabolism; D018799:Intercellular Adhesion Molecule-1 / Q000235:genetics* / Q000378:metabolism; D007700:Kinetics; D020319:Oligodeoxyribonucleotides, Antisense / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D009841:Oligonucleotides / Q000138:chemical synthesis / Q000737:chemistry; D016376:Oligonucleotides, Antisense / Q000138:chemical synthesis / Q000302:isolation & purification / Q000378:metabolism; D054735:Phosphorothioate Oligonucleotides; D011786:Quality Control; D016914:Ribonuclease H / Q000502:physiology; D013873:Thionucleotides / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism
D007166:Immunosuppressive Agents; D020319:Oligodeoxyribonucleotides, Antisense; D009841:Oligonucleotides; D016376:Oligonucleotides, Antisense; D054735:Phosphorothioate Oligonucleotides; D013873:Thionucleotides; D018799:Intercellular Adhesion Molecule-1; D016914:Ribonuclease H; C089753:alicaforsen