249. Alitretinoin

Description and references

Naturally occurring derivative of vitamin A, q.v. Morphogenic agent that modulates cell growth and differentiation; activates both retinoic acid (RAR) and retinoid X (RXR) receptors. Prepn: C. D. Robeson et al., J. Am. Chem. Soc. 77, 4111 (1955); M. Matsui et al., J. Vitaminol. 4, 178 (1958); M. F. Boehm et al., J. Med. Chem. 37, 408 (1994). Identification as physiological ligand of RXR: R. A. Heyman et al., Cell 68, 397 (1992); A. A. Levin et al., Nature 355, 359 (1992). Role in morphogenesis: C. Thaller et al., Development 118, 957 (1993). Biosynthesis from all-trans-retinoic acid: J. Urbach, R. R. Rando, Biochem. J. 299, 459 (1994). HPLC determn in plasma: A. M. Dzerk et al., J. Pharm. Biomed. Anal. 16, 1013 (1998). Clinical pharmacokinetics: C. Weber, E. Dumont, J. Clin. Pharmacol. 37, 566 (1997). Clinical evaluation in acute promyelocytic leukemia: S. L. Soignet et al., Leukemia 12, 1518 (1998); in advanced cancers: N. A. Rizvi et al., Clin. Cancer Res. 4, 1437 (1998). Review of role as hormone: B. F. Tate et al., Trends Endocrinol. Metab. 5, 189-194 (1994); of clinical development: J. Cell. Biochem. Suppl. 26, 158-167 (1996).

Properties