6. Abetimus Sodium

Nomenclature

CAS number: 169147-32-4
d(C-A-C-A-C-A-C-A-C-A-C-A-C-A-C-A-C-A-C-A)DNA 5′,5,5′′′′′,5′′′′′′′-[[1,2-ethanediylbis[oxy-2,1-ethanediyloxycarbonylnitrilobis[2,1-ethanediylimino(6-oxo-6,1-hexanediyl)imino(2-oxo-2,1-ethanediyl)thio-6,1-hexanediyl]]] tetrakis(hydrogen phosphate)] complex with d(T-G-T-G-T-G-T-G-T-G-T-G-T-G-T-G-T-G-T-G)DNA (1:4) hexapentacontahectasodium salt; LJP-394; Riquent (La Jolla Pharmaceuticals).

Description and references

B-cell toleragen which prevents the expression of anti-ds-DNA. Consists of four identical ds-DNA oligonucleotides (20 basepairs) attached through a linker to a non-immunogenic modified triethylene glycol base. Relative mass of 54 kDa. Prepn: S. M. Coutts et al., EP 642798; eidem, US 5552391 (1995, 1996 both to La Jolla Pharm.); D. S. Jones et al., J. Med. Chem. 38, 2138 (1995) DOI PubMed. Clinical evaluation in systemic lupus erythematosus (SLE): R. A. Furie et al., J. Rheumatol. 28, 257 (2001) DOI PubMed; in prevention of SLE renal flare: D. Alarcon-Segovia et al., Arthritis Rheum. 48, 442 (2003) DOI PubMed. Review of clinical pharmacology: D. J. Wallace, Expert Opin. Invest. Drugs 10, 111-117 (2001) DOI PubMed; of clinical experience: M. H. Cardiel, ibid. 14, 77-88 (2005) DOI PubMed.

Properties

Colorless aqueous solution with an osmolality of 255-310 mmol/kg at pH 6.8-7.8.

Therapeutic Category

Immunosuppressant in treatment of SLE and associated nephritis.

Keywords

Immunosuppressant