Phase I and pharmacokinetic study of Bay 38-3441, a camptothecin glycoconjugate, administered as a 30-minute infusion daily for five days every 3 weeks in patients with advanced solid malignancies.

Abstract	Bay 38-3441 is a camptothecin glycoconjugate which stabilizes the active lactone form of camptothecin and allows selective uptake into tumor cells. We conducted a phase I study of Bay 38-3441 administered as a 30-minute infusion daily for five consecutive days every 21 days. Thirty-one patients were enrolled at 8 dose levels. Most common nonhematologic side effects were diarrhea (29%), vomiting (19%), nausea (19%), lethargy (13%), and abdominal pain (10%). The main hematologic toxicity was prolonged neutropenia. Nine patients had a best response of stable disease with a median duration of 2.7 months (range: 2.3-20.6 months). The study was closed without reaching the maximum tolerated dose (MTD) due to excessive toxicity in a companion trial resulting in termination of development of this agent. Bay 38-3441 was well tolerated in this study with granulocytopenia as the main hematologic toxicity. This study showed that glycoconjugation is a feasible delivery technique for camptothecin.
Authors	Eric X Chen, Gerald Batist, Lillian L Siu, Naeema Bangash, Martha Maclean, Lynn McIntosh, Wilson H Miller Jr, Amit M Oza, Chetan Lathia, Oana Petrenciuc, Lesley Seymour
Journal	Investigational new drugs (Invest New Drugs) Vol. 23 Issue 5 Pg. 455-65 (Oct 2005) ISSN: 0167-6997 [Print] United States
PMID	16133797 (Publication Type: Clinical Trial, Phase I, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	20-O-(Nalpha-(4-(3-O-methylfucopyranosyloxy)phenylaminothiocarbonyl)histidylvalyl)camptothecin Antineoplastic Agents, Phytogenic Dipeptides Glycoconjugates Camptothecin
Topics	Adult Aged Agranulocytosis (chemically induced) Antineoplastic Agents, Phytogenic (administration & dosage, adverse effects, pharmacokinetics) Area Under Curve Camptothecin (administration & dosage, adverse effects, analogs & derivatives, pharmacokinetics) Diarrhea (chemically induced) Dipeptides (administration & dosage, adverse effects, pharmacokinetics) Drug Administration Schedule Female Glycoconjugates (administration & dosage, adverse effects, pharmacokinetics) Half-Life Humans Male Middle Aged Neoplasms (drug therapy, metabolism)

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