4848. Hydroxyurea

Nomenclature

CAS number: 127-07-1
Hydroxycarbamide; Droxia (BMS); Hydrea (BMS); Litalir (BMS).
CH4N2O2; mol wt 76.05.
C 15.79%, H 5.30%, N 36.84%, O 42.08%.

Description and references

Ribonuleotide reductase inhibitor; blocks DNA synthesis and repair. Induces fetal hemoglobin production in patients with sickle cell anemia. Prepn: W. F. C. Dressler, R. Stein, Ann. 150, 242 (1869). Alternate route: P. J. Graham, US 2705727 (1955 to Du Pont). Symposium on mechanism of action and clinical experience in cancer: Semin. Oncol. 19, Suppl. 9, 1-116 (1992). Clinical trials in sickle cell crises in adults: S. Charache et al., N. Engl. J. Med. 332, 1317 (1995); in children: T. R. Kinney et al., Blood 94, 1550 (1999). Review of clinical pharmacokinetics: P. R. Gwilt, W. G. Tracewell, Clin. Pharmacokinet. 34, 347-358 (1998); of pharmacology and potential therapeutic indications: P. Navarra, P. Preziosi, Crit. Rev. Oncol. Hematol. 29, 249-255 (1999). Clinical trial in essential thrombocythemia: C. N. Harrison et al., N. Engl. J. Med. 353, 33 (2005).

Chemical structure

Properties

Needles from alc, mp 133-136°. Freely sol in water, hot alcohol.

Therapeutic Category

Antineoplastic; in treatment of sickle cell anemia.

Keywords

Antineoplastic