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[FO-152].

Abstract
5'-O-(L-valyl)-5-fluorouridine hydrochloride (FO-152) is a derivative of 5-fluorouridine. In preclinical studies, FO-152 has demonstrated more favorable antitumor effect with greater therapeutic index compared with the parent compound, 5-fluorouridine. A phase I study was performed in 38 cases with advanced cancer. Myelosuppression was dose limiting, with leukopenia more pronounced than thrombocytopenia. Other side effects included mild hot feeling of the body during infusion and slight G.I. toxicities. Clinical responses were seen in patients with adenocarcinoma of the stomach, lung, etc. FO-152 has major advantages over 5-fluorouridine in terms of reduced toxicity. The recommended phase II dose for patients with solid tumors is 250 mg/m2 X 1, or 35 mg/m2 X 5 consecutive days with a 4-week rest, provided there is reversal of drug related myelosuppression.
AuthorsH Furue, H Niitani, M Kurihara, K Hasegawa, I Nakao, S Tsukagoshi, H Fujita
JournalGan to kagaku ryoho. Cancer & chemotherapy (Gan To Kagaku Ryoho) Vol. 14 Issue 7 Pg. 2251-6 (Jul 1987) ISSN: 0385-0684 [Print] Japan
PMID3111381 (Publication Type: English Abstract, Journal Article)
Chemical References
  • Antineoplastic Agents
  • Tegafur
  • 5'-O-(L-valyl)-5-fluorouridine hydrochloride
  • Fluorouracil
  • Uridine
Topics
  • Absorption
  • Adenocarcinoma (drug therapy)
  • Animals
  • Antineoplastic Agents (therapeutic use)
  • Cell Line
  • Dogs
  • Drug Evaluation
  • Female
  • Fluorouracil (therapeutic use)
  • Humans
  • Leukemia L1210 (drug therapy)
  • Lung Neoplasms (drug therapy)
  • Male
  • Mice
  • Stomach Neoplasms (drug therapy)
  • Tegafur (therapeutic use)
  • Uridine (analogs & derivatives, metabolism, therapeutic use)

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