10281. Agatolimod

Nomenclature

CAS number: 207623-20-9
d(P-Thio)(T-C-G-T-C-G-T-T-T-T-G-T-C-G-T-T-T-T-G-T-C-G-T-T)DNA.
C236H326N70O133P23S23; mol wt 7721.39.
C 36.71%, H 4.26%, N 12.70%, O 27.56%, P 9.23%, S 9.55%.

Description and references

Synthetic, 24 base phosphothioate oligodeoxynucleotide containing multiple cytosine-phosphate-guanosine (CpG) motifs. Toll-like receptor 9 (TLR9) agonist that stimulates B-cells and plasmacytoid dendritic cells. Prepn: A. M. Krieg, WO 9818810; idem, US 7223741 (1998, 2007 both to Univ. Iowa Res. Foundn.). Immunostimulant effect on human dendritic cells: G. Hartmann et al., Proc. Natl. Acad. Sci. USA 96, 9305 (1999) DOI PubMed. CGE determn in plasma and metabolism study: B. O. Noll et al., Biochem. Pharmacol. 69, 981 (2005) DOI PubMed. Clinical evaluation as vaccine adjuvant: C. L. Cooper et al., J. Clin. Immunol. 24, 693 (2004) DOI PubMed; eidem, Vaccine 22, 3136 (2004) DOI PubMed; as immunostimulant in metastatic melanoma: M. Pashenkov et al., J. Clin. Oncol. 24, 5716 (2006) DOI PubMed. Review of clinical development in cancer therapy: Y. M. Murad et al., Expert Opin. Biol. Ther. 7, 1257-1266 (2007) DOI PubMed.

Derivative

Tricosasodium salt.

Nomenclature

CAS number: 541547-35-7
Agatolimod sodium; CpG-2006; CPG-7909; PF-3512676; VaxImmune (Coley).
C236H303N70Na23O133P23S23; mol wt 8226.98.
C 34.45%, H 3.71%, N 11.92%, Na 6.43%, O 25.87%, P 8.66%, S 8.96%.

Use

Vaccine adjuvant.

Therapeutic Category

Antineoplastic; immunomodulator.

Keywords

Antineoplastic; Oligonucleotides; Immunomodulator