COMPLEX OF RAS-FARNESYLTRANSFERASE INHIBITOR AND SULFOBUTYLETHER-7- beta -CYCLODEXTRIN OR 2-HYDROXYPROPYL- beta -CYCLODEXTRIN AND METHOD

摘要

A ras-farnesyltransferase inhibitor complex formed of ras-farnesyltransferase inhibitor or a pharmaceutically acceptable salt thereof, of formula (I), wherein n is 0 or 1; R1 is selected from Cl, Br, phenyl, pyridyl or cyano; R2 is aralkyl; R3 is selected from lower alkyl, aryl or substituted aryl or heterocyclo; Z1 is selected from CO, SO2, CO2 or SO2NR5, R5 is selected from hydrogen, lower alkyl or substituted alkyl; and sulfobutylether-7- beta -cyclodextrin or 2-hydroxypropyl- beta -cyclodextrin is provided. The complex has unexpectedly high aqueous solubility of the ras-farnesyltransferase inhibitor and is useful for its intravenous delivery to humans with cancer. Also provided is a method for forming the complex. The ras-farnesyltransferase inhibitors are useful as anti-tumor agents.