Treatment of cancers, tumors and malignancies using amphiphilic prodrugs
AssigneeNobex Corporation
InventorsNnochiri Ekwuribe, Christopher H. Price, Tatyana A. Dyakonov
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Abstract
The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the central nervous system.
Claims34
A method of treating a mammalian subject having a disease condition selected from the group consisting of cancers, tumors, and malignancies, said method comprising administering to the subject of an effective disease treating amount of a prodrug comprising:
- (a) at least one therapeutic compound selected from the group consisting of a therapeutic compound comprising etoposide and a therapeutic compound comprising an etoposide analog which retains some or all of the therapeutic activity of etoposide;
- and
- (b) one or more PEG polymers and/or oligomers, each joined to a bonding site on the therapeutic compound by a hydrolyzable bond, said PEG polymers and/or oligomers each:
- (i) comprising a straight or branched PEG segment consisting of 1 to 25 polyethylene glycol units;
- and
- (ii) comprising a salt-forming moiety.
A method of treating a mammalian subject having a disease condition selected from the group consisting of cancers, tumors and malignancies, said method comprising administering to the subject of an effective disease treating amount of a prodrug comprising a therapeutic compound selected from the group consisting of a therapeutic compound comprising etoposide and a therapeutic compound comprising an etoposide analog which retains some or all of the therapeutic activity of etoposide and wherein the therapeutic compound is joined by hydrolyzable bond(s) to one or more PEG oligomer(s) selected from the group consisting of:
- wherein n is from 1 to 7, m is from 2 to 25, and R is hydrogen or a lower alkyl;
- wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25, and R is hydrogen or a lower alkyl;
- wherein n is from 1 to 6, m and r are each independently from 2 to 25, and R is hydrogen or a lower alkyl;
- wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25 and R is hydrogen or a lower alkyl;
- wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25, X− is a negative ion and R is hydrogen or a lower alkyl;
- wherein n is from 1 to 6, p is from 2 to 8, m is from 2 to 25, and R1 and R2 are each independently hydrogen or a lower alkyl;
- wherein n is from 1 to 6, p is from 2 to 8 and m is from 2 to 25;
- wherein n and p are each independently from 1 to 6, m is from 2 to 25 and X+ is a positive ion;
- wherein n is from 1 to 5, m is from 2 to 25, and wherein R1 and R2 are each independently hydrogen or lower alkyl;
- and
- wherein n is from 1 to 6, m is from 2 to 25 and X− is a negative ion.
Dependencies are inferred from the claim text.