Hydrophobic cis-platinum complexes efficiently incorporated into liposomes
AssigneeBoard of Regents, The University of Texas System
InventorsAbdul R. Khokhar, Gabriel Lopez-Berestein, Roman Perez-Soler
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AssigneeBoard of Regents, The University of Texas System
InventorsAbdul R. Khokhar, Gabriel Lopez-Berestein, Roman Perez-Soler
Estimating the term…
The present invention involves the synthesis and use of new platinum compounds. These new platinum compounds are easy to encapsulate in liposomes at high efficiencies. They are further characterized as platinum (II) four coordinate complex having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are carboxylato monoanions bearing a hydrophobic radical function or a single carboxylato dianion bearing a hydrophobic radical function and R.sub.3 is a vicinal diaminoalkane or vicinal diaminocycloalkane. The complex is substantially soluble in methanol or chloroform and substantially insoluble in water. Said complex may be incorporated into phospholipid liposomes. Such platinum complexes encapsulated in phospholipid liposomes are useful for chemotherapy of platinum complex-sensitive tumors.
A method of treating an animal afflicted with tumor cells sensitive to a platinum (II) four-coordinate complex, comprising administering to the animal a pharmaceutically effective amount of a liposome which comprises a phospholipid and a platinum (II) four-coordinate complex having the formula:
Dependencies are inferred from the claim text.