title: Synthesis and in vivo antitumor activity of poly(l-glutamic acid) conjugates of 20S-camptothecin.
abstract: Poly-alpha-(l-glutamic acid) (PG) conjugates of 20(S)-camptothecin (1, CPT) displayed improved aqueous solubility compared to CPT, were stable in aqueous solution at neutral pH, and were potent antitumor agents in vivo. Evaluation of PG molecular weight, CPT loading, aqueous solubility, and CPT equivalent dosing with respect to in vivo antitumor potencies of various linked conjugates led to identification of a preferred conjugate composition.
authors.affiliation: Cell Therapeutics, Inc., 201 Elliott Avenue West, Seattle, Washington 98119, USA.
authors.forename: Rama
authors.initials: R
authors.lastname: Bhatt
authors.forename: Peter
authors.initials: P
authors.lastname: de Vries
authors.forename: John
authors.initials: J
authors.lastname: Tulinsky
authors.forename: Garland
authors.initials: G
authors.lastname: Bellamy
authors.forename: Brian
authors.initials: B
authors.lastname: Baker
authors.forename: Jack W
authors.initials: JW
authors.lastname: Singer
authors.forename: Peter
authors.initials: P
authors.lastname: Klein
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D004355:Drug Stability; D006863:Hydrogen-Ion Concentration; D051379:Mice; D008810:Mice, Inbred C57BL; D008819:Mice, Nude; D011099:Polyglutamic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D012996:Solutions; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D012996:Solutions; D011099:Polyglutamic Acid; D002166:Camptothecin