Title: Motexafin Lutetium
CAS Registry Number: 246252-04-0; 156436-90-7 (hydrate)
CAS Name: (PB-7-11-233¢2¢4)-Bis(acetato-kO)[9,10-diethyl-20,21-bis[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]-4,15-dimethyl-8,11-imino-3,6:16,13-dinitrilo-1,18-benzodiazacycloeicosine-5,14-dipropanolato-kN1,kN18,kN23,kN24,kN25]lutetium
Additional Names: 4,5-diethyl-10,23-dimethyl-9,24-bis(3-hydroxypropyl)-16,17-bis[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]pentaazapentacyclo[20.2.1.13,6.18.11. 014,19]heptacosa-1,3,5,7,9,11(27),12,14,16,18,20,22(25),23-tridecaene lutetium(III) complex; lutetium texaphyrin; Lu-Tex
Manufacturers' Codes: PCI-0123
Trademarks: Antrin (Pharmacyclics); Lutrin (Pharmacyclics); Optrin (Pharmacyclics)
Molecular Formula: C52H72LuN5O14
Molecular Weight: 1166.12
Percent Composition: C 53.56%, H 6.22%, Lu 15.00%, N 6.01%, O 19.21%
Literature References: Synthetic metal-coordinating expanded porphyrin. Diamagnetic photosensitizer that is activated using far-red light to generate cytotoxic singlet oxygen. Prepn: J. L. Sessler et al., US 5801229 (1998 to Board of Regents Univ. of Texas); S. W. Young et al., Photochem. Photobiol. 63, 892 (1996). Electrochemical characteristics: J. L. Sessler et al., J. Alloys Compds. 249, 146 (1997); and singlet oxygen generation: L. I. Grossweiner et al., Photochem. Photobiol. 70, 138 (1999). LC-MS/MS and ICP-AES determn in plasma: D. Miles et al., AAPS PharmSci. 5, 1 (2003). Preclinical studies in cancer and atheromatous plaque: K. W. Woodburn et al., J. Clin. Laser Med. Surg. 14, 343 (1996); in ocular angiography: M. S. Blumenkranz et al., Am. J. Ophthalmol. 129, 353 (2000). Clinical evaluation in coronary arterial photodynamic therapy: D. J. Kereiakes et al., Circulation 108, 1310 (2003). Review of chemistry and therapeutic potential: T. D. Mody, J. L. Sessler, J. Porphr. Phthalocyan. 5, 134-142 (2001).
Properties: Prepd as hydrate, shiny green solid. Sol in water, acetonitrile, methanol, N,N-dimethylformamide. Aqueous solns (100 mM) stable at 2<pH<11 for several months. uv max (methanol): 354, 414, 474, 732 nm (log e 4.33, 4.67, 5.10, 4.62).
Absorption maximum: Sol in water, acetonitrile, methanol, N,N-dimethylformamide. Aqueous solns (100 mM) stable at 2<pH<11 for several months. uv max (methanol): 354, 414, 474, 732 nm (log e 4.33, 4.67, 5.10, 4.62)
Therap-Cat: Antiatherosclerotic, antineoplastic (photosensitizer). In treatment of age-related macular degeneration.
Keywords: Antiatherosclerotic; Antineoplastic (Photosensitizer); Macular Degeneration Treatment. |