In vivo antitumor activity of novel water-soluble taxoids.
The antitumor activity of newly developed taxoids possessing a sugar moiety (glucose, galactose or mannose) to improve water solubility was evaluated. Galactose-bound taxoid (10-alpha-GAG-DT) proved superior to all other taxoids in both water solubility and antitumor activity. Therapeutic efficacy of 10-alpha-GAG-DT in terms of in vivo antitumor activity was found to be approximately equivalent to that of docetaxel, which is known to be superior to that of paclitaxel. The observation that the sugar moiety was gradually hydrolyzed in serum to release docetaxel indicates that 10-alpha-GAG-DT acts as a prodrug.
Mikuni
Katsuhiko
K
Ensuiko Sugar Refining Co., Ltd., Fukuura, Yokohama, Japan. mikuni_k@ensuiko.co.jp
Nakanishi
Katsuyoshi
K
Hara
Koji
K
Hara
Kozo
K
Iwatani
Wakao
W
Amano
Tetsuya
T
Nakamura
Kosho
K
Tsuchiya
Yoshinori
Y
Okumoto
Hiroshi
H
Mandai
Tadakatsu
T
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic; D001835:Body Weight / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D000077143:Docetaxel; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007202:Indicators and Reagents; D007941:Leukemia P388 / Q000188:drug therapy; D008297:Male; D051379:Mice; D012995:Solubility; D043823:Taxoids / Q000737:chemistry / Q000494:pharmacology*; D014867:Water
D000972:Antineoplastic Agents, Phytogenic; D007202:Indicators and Reagents; D043823:Taxoids; D014867:Water; D000077143:Docetaxel