Title: Edotreotide
CAS Registry Number: 204318-14-9
CAS Name: N-[[4,7,10-Tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]-D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-threonyl-N-[(1R,2R)-2-hydroxy-1-(hydroxymethyl)propyl]-L-cysteinamide cyclic(2®7)-disulfide
Additional Names: (DOTA D-Phe1,Tyr3)octreotide; DOTATOC
Manufacturers' Codes: SMT-487
Molecular Formula: C65H92N14O18S2
Molecular Weight: 1421.64
Percent Composition: C 54.92%, H 6.52%, N 13.79%, O 20.26%, S 4.51%
Literature References: Octapeptide analog of somatostatin, q.v. Designed for targeted radiotherapy vs somatostatin receptor-expressing tumors. Prepn: R. Albert et al., EP 714911; eidem, US 6183721 (1996, 2001 both to Novartis); idem, et al., Bioorg. Med. Chem. Lett. 8, 1207 (1998). Solution-phase synthesis: M. Schottelius et al., Tetrahedron Lett. 44, 2393 (2003). In vivo antineoplastic activity: B. Stolz et al., Eur. J. Nucl. Med. 25, 668 (1998). Receptor binding study: J. C. Reubi et al., ibid. 27, 273 (2000). Clinical pharmacokinetics: F. Jamar et al., Eur. J. Nucl. Med. Mol. Imaging 30, 510 (2003). Clinical evaluation in neuroendocrine tumors: C. Waldherr et al., J. Nucl. Med. 43, 610 (2002).
Properties: Prepd as acetate. [a]22D -14.75° (c = 0.52 in 95% acetic acid).
Optical Rotation: [a]22D -14.75° (c = 0.52 in 95% acetic acid)
Derivative Type: 90Y chelate
CAS Registry Number: 322407-70-5
Manufacturers' Codes: 90Y-SMT-487
Trademarks: OctreoTher (Novartis)
Therap-Cat: 90Y chelate as antineoplastic.
Keywords: Somatostatin Analog. |