3907. Everolimus

Nomenclature

CAS number: 159351-69-6
42-O-(2-Hydroxyethyl)rapamycin; 40-O-(2-hydroxyethyl)rapamycin; RAD-001; SDZ RAD; Afinitor (Novartis); Certican (Novartis).
C53H83NO14; mol wt 958.22.
C 66.43%, H 8.73%, N 1.46%, O 23.38%.

Description and references

Macrolide immunosuppressant; derivative of rapamycin, q.v. Inhibitor of the serine-threonine kinase, mTOR. Suppresses cytokine-mediated lymphocyte proliferation. Prepn: S. Cottens, R. Sedrani, WO 9409010; eidem, US 5665772 (1994, 1997 both to Sandoz). Pharmacology: W. Schuler et al., Transplantation 64, 36 (1997) DOI PubMed. Whole blood determn by LC/MS: N. Brignol et al., Rapid Commun. Mass Spectrom. 15, 898 (2001) DOI PubMed; by HPLC: S. Baldelli et al., J. Chromatogr. B 816, 99 (2005) DOI. Clinical pharmacokinetics in combination with cyclosporine: J. M. Kovarik et al., Clin. Pharmacol. Ther. 69, 48 (2001) DOI PubMed. Clinical study in prevention of cardiac-allograft vasculopathy: H. J. Eisen et al., N. Engl. J. Med. 349, 847 (2003) DOI PubMed; in advanced renal cell carcinoma: R. J. Motzer et al., Lancet 372, 449 (2008) DOI PubMed. Review: F. J. Dumont et al., Curr. Opin. Investig. Drugs 2, 1220-1234 (2001); B. Nashan, Ther. Drug Monit. 24, 53-58 (2002) DOI PubMed.

Chemical structure

Therapeutic Category

Immunosuppressant; antineoplastic.

Keywords

Immunosuppressant; Antineoplastic