Oral Tegafur/Uracil
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Drugs Aging 2001; 18 (12): 935-948 1170-229X/01/0012-0935/$22.00/0 © Adis International Limited. All rights reserved.
Oral Tegafur/Uracil Keri Wellington and Karen L. Goa Adis International Limited, Auckland, New Zealand
Contents Abstract . . . . . . . . . . . . . . 1. Pharmacodynamic Profile . . . . 2. Pharmacokinetic Profile . . . . . . 3. Therapeutic Efficacy . . . . . . . . 4. Tolerability . . . . . . . . . . . . . . 5. Oral Tegafur/Uracil: Current Status
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Abstract Tegafur is a prodrug of the antineoplastic agent fluorouracil, and is administered in a 1:4 molar ratio with the fluorouracil modulator uracil. Oral tegafur/uracil 300 mg/m2/day plus calcium folinate 75 or 90 mg/day for 28 days every 35 days was as effective as intravenous (IV) fluorouracil 425 mg/m2/day plus folinic acid 20 mg/m2/day for 5 days every 28 or 35 days in the treatment of patients with metastatic colorectal cancer in two large, randomised, nonblind, multicentre trials (n = 816 and 380). Median survival time among patients treated with tegafur/ uracil or fluorouracil was approximately 12 months in both trials. Results from both trials also demonstrated no significant between-group differences in overall response rates among patients treated with oral tegafur/uracil (12 and 11%) or IV fluorouracil (15 and 9%). In elderly patients (aged ≥70 years) with metastatic colorectal cancer, results from small noncomparative studies showed that treatment with oral tegafur/uracil afforded overall response rates of 12.5 to 29% and was well tolerated. During preoperative treatment with oral tegafur/uracil plus calcium folinate as an adjunct to radiotherapy in patients with stage II or III rectal cancer, the maximum tolerated dosage of tegafur/uracil was 350 mg/m2/day (administered 5 days per week for 5 weeks). Among the 15 patients who were followed for 5 to 8 months, three had a complete response to treatment. Treatment with tegafur/uracil was also given postoperatively The most common adverse events associated with oral tegafur/uracil were anaemia, nausea/vomiting, diarrhoea, thrombocytopenia, mucositis, neutropenia, asthenia, anorexia and abdominal pain. Oral tegafur/uracil was associated with a significantly more favourable tolerability profile than IV fluorouracil in the two large randomised trials. In particular, stomatitis and most adverse haematological events were less frequent.
Features and properties of tegafur/uracil Indication Treatment of metastatic colorectal cancer in combination with oral calcium folinate Mechanism of action Tegafur is a
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