Title: Everolimus
CAS Registry Number: 159351-69-6
CAS Name: 42-
O-(2-Hydroxyethyl)rapamycin
Synonyms: 40-
O-(2-hydroxyethyl)rapamycin
Manufacturers' Codes: RAD-001; SDZ RAD
Trademarks: Certican (Novartis)
Molecular Formula: C53H83NO14
Molecular Weight: 958.22
Percent Composition: C 66.43%, H 8.73%, N 1.46%, O 23.38%
Literature References: Macrolide immunosuppressant; derivative of rapamycin,
q.v. Inhibits 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). Whole blood determn by LC/MS: N. Brignol
et al., Rapid Commun. Mass Spectrom. 15, 898 (2001); by HPLC: S. Baldelli
et al.,
J. Chromatogr. B 816, 99 (2005). Clinical pharmacokinetics in combination with cyclosporine: J. M. Kovarik
et al., Clin. Pharmacol. Ther. 69, 48 (2001). Clinical study in prevention of cardiac-allograft vasculopathy: H. J. Eisen
et al., N. Engl. J. Med. 349, 847 (2003).
Review: F. J. Dumont
et al., Curr. Opin. Invest. Drugs 2, 1220-1234 (2001); B. Nashan,
Ther. Drug Monit. 24, 53-58 (2002).
Therap-Cat: Immunosuppressant.
Keywords: Immunosuppressant.