5-FU is metabolized to FUTP and FdUMP in tumor cells and exhibits RNA- and DNA-directed cytotoxicity. Biochemical modulation of the intracellular metabolic pathways of 5-FU result in either selective enhancement of the antitumor effect or protection of the host. 1. Administration of pro-drugs of the active intermediates of 5-FU (FO-152, FF-705, TK-117, T-506) 2. Increase in PRPP level by inhibition of the de novo purine synthetic pathway, and greater production of cytotoxic 5-FU-containing nucleotides (MTX, MMPR) 3. Lowering of intracellular UTP pools by inhibition of de novo pyrimidine biosynthesis and enhancement of antitumor activity of 5-FU (PALA, Acivicin) 4. Increase in the UTP level and protection against 5-FU toxicity in normal host tissue (Uridine, Uridine + BAU, Cytidine) 5. Enhanced and prolonged inhibition of thymidylate synthetase by FdUMP (Leucovorin, MTX) 6. Inhibition of 5-FU degradation and increase in the 5-FU tissue level (Thymidine, Uracil)

01 Jul 1987·Gan to kagaku ryoho. Cancer & chemotherapy

[FO-152].

Article

Author: Tsukagoshi, S ; Fujita, H ; Kurihara, M ; Furue, H ; Niitani, H ; Nakao, I ; Hasegawa, K

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.

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Phase 2	JP	Daiichi Fine Chemical Co., Ltd.	-
Neoplasms	Phase 2	JP	Sankyo & Co. Ltd.	-

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