title: Preclinical anticancer activity of cryptophycin-8.
abstract: Cryptophycin-8 was prepared by the conversion of the epoxide group on cryptophycin-1 to a chlorohydrin. In the studies reported here, cryptophycin-8 was evaluated for preclinical activity against subcutaneous tumors of both mouse and human origin. At the highest non-toxic single course treatment, the following results were obtained (Table A). Cryptophycin-8 was less potent than cryptophycin-1 by approximately 4-fold; however, it was both more water soluble and had greater therapeutic efficacy, as demonstrated by % T/C, tumor cell log kill values, range of dose effectiveness and host cures.
authors.affiliation: Department of Internal Medicine, Wayne State University School of Medicine, Detroit, MI 48201, USA.
authors.forename: T H
authors.initials: TH
authors.lastname: Corbett
authors.forename: F A
authors.initials: FA
authors.lastname: Valeriote
authors.forename: L
authors.initials: L
authors.lastname: Demchik
authors.forename: L
authors.initials: L
authors.lastname: Polin
authors.forename: C
authors.initials: C
authors.lastname: Panchapor
authors.forename: S
authors.initials: S
authors.lastname: Pugh
authors.forename: K
authors.initials: K
authors.lastname: White
authors.forename: J
authors.initials: J
authors.lastname: Knight
authors.forename: J
authors.initials: J
authors.lastname: Jones
authors.forename: L
authors.initials: L
authors.lastname: Jones
authors.forename: P
authors.initials: P
authors.lastname: LoRusso
authors.forename: B
authors.initials: B
authors.lastname: Foster
authors.forename: R A
authors.initials: RA
authors.lastname: Wiegand
authors.forename: L
authors.initials: L
authors.lastname: Lisow
authors.forename: T
authors.initials: T
authors.lastname: Golakoti
authors.forename: C E
authors.initials: CE
authors.lastname: Heltzel
authors.forename: J
authors.initials: J
authors.lastname: Ogino
authors.forename: G M
authors.initials: GM
authors.lastname: Patterson
authors.forename: R E
authors.initials: RE
authors.lastname: Moore
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use* / Q000633:toxicity; D047630:Depsipeptides; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D006801:Humans; D007769:Lactams / Q000627:therapeutic use* / Q000633:toxicity; D007783:Lactones / Q000627:therapeutic use* / Q000633:toxicity; D007928:Lethal Dose 50; D051379:Mice; D008815:Mice, Inbred Strains; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology
chemical_list: D000970:Antineoplastic Agents; D047630:Depsipeptides; D007769:Lactams; D007783:Lactones; C107304:cryptophycin 8