Glutathione-activated anti-tumor prodrugs of 6-mercaptopurine and 6-thioguanine
OwnerAdnan A. Elfarra, Sjofn Gunnarsdottirinventors
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Abstract
The present invention relates to a method for treating a tumor in a tissue of a human or non-human animal, the tumor having an elevated level of glutathione relative to the tissue, the method comprising the steps of administering to the animal a prodrug comprising a thiopurine having a sulfur heteroatom conjugated to an alpha-, beta-unsaturated carbonyl moiety, in combination with a pharmaceutically acceptable carrier, the moiety comprising a double bond having an alpha end and a beta end, the beta end being accessible to glutathione in an addition-elimination reaction, the prodrug lacking an ionizable carboxylic acid group; and observing a reduction in growth of the tumor.
Claims18
A prodrug comprising:
- a pharmaceutically acceptable carrier;
- and
- a thiopurine having a sulfur heteroatom conjugated to an alpha-, beta-unsaturated carbonyl moiety, the moiety comprising a double bond having an alpha end and a beta end, the beta end being accessible to glutathione in an addition-elimination reaction, the prodrug lacking an ionizable carboxylic acid group.
A method for treating a tumor in a tissue of a human or non-human animal, the tumor having an elevated level of glutathione relative to the tissue, the method comprising the steps of:
- administering to the animal a prodrug comprising a thiopurine having a sulfur heteroatom conjugated to an alpha-, beta-unsaturated carbonyl moiety, in combination with a pharmaceutically acceptable carrier, the moiety comprising a double bond having an alpha end and a beta end, the beta end being accessible to glutathione in an addition-elimination reaction, the prodrug lacking an ionizable carboxylic acid group;
- and
- observing a reduction in growth of the tumor.
Dependencies are inferred from the claim text.