(WO/2009/011702) SELF-ASSEMBLING AMPHIPHILIC POLYMERS AS ANTICANCER AGENTS
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| Latest bibliographic data on file with the International Bureau | ||||||||||||
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| IPC: | A61K 31/74 (2006.01) | |||||||||||
| Applicants: | ALLEXCEL, INC. [US/US]; 135 Wood Street, Suite 200, West Haven, CT 06516 (US) (All Except US). DIWAN, Anil, R. [US/US]; (US) (US Only). ONTON, Ann, Louise [US/US]; (US) (US Only). | |||||||||||
| Inventors: | DIWAN, Anil, R.; (US). ONTON, Ann, Louise; (US). | |||||||||||
| Agent: | DEMERS, James, P.; Kenyon & Kenyon LLP, One Broadway, New York, NY 10004 (US). | |||||||||||
| Title: | SELF-ASSEMBLING AMPHIPHILIC POLYMERS AS ANTICANCER AGENTS |
| Abstract: |  The invention provides amphiphilic biocompatible copolymers which have a hydrophilic backbone and pendant hydrophobic groups. The polymers form nanoscale molecular aggregates in aqueous environments, which have hydrophobic interiors within which anticancer drugs may be solubilized. The polymers optionally feature attached antibodies, receptor ligands, and other targeting moieties which mediate adherence of the drug-carrying aggregates to targeted cancer cells. |
Anticancer drugs that can be encapsulated and delivered by these polymers include but are not limited to doxorubicin, camptothecin, docetaxel, paclitaxel, topotecan, irinotecan, imatinib, sunitinib, sorafenib, axitinib, pazopanib, etoposide, methotrexate, methopterin, dichloromethotrexate, 5-fluorouracil, 6-mercaptopurine, cladribine, cladribine, staurosporine, cytarabine, melphalan, leurosine, actinomycin, daunorubicin, epirubicin, idarubicin, mitomycin D, mitomycin A, carninomycin, aminopterin, tallysomycin, podophyllotoxin,
cisplatinum, carboplatin, vinblastine, vincristine, vindesin, retinoic acid, colchicine, dexamethasone, and tamoxifen, and derivatives and analogs of these drugs, as well as photodynamic agents, nucleic acids, nucleic acid analogues, and nucleic acid complexes. Nucleic acid analogues include species such as thiophosphates, phosphoramidates, and peptide nucleic acids. Nucleic acid complexes are ionic complexes of oligonucleic acids or analogues thereof with substantially charge-neutralizing amounts of cationic or polycationic species.
As a result of the ability of the polymers of the invention to encapsulate anticancer drugs, the present invention also provides pharmaceutical compositions, which comprise one or more π-polymers of the invention in combination with a therapeutically effective amount of one or more pharmacologically active anticancer agents, and a pharmaceutically acceptable carrier or excipient. Suitable carriers and excipients include water and saline, and solid additives such as buffers, salts, sugars, polysaccharides such as cellulose and derivatives thereof, and various humectants, glidants, preservatives, binding and dispersing agents known in the art. The polymers of the invention can render effective what would otherwise, in the prior art, have been an ineffective amount of an anticancer agent. For purposes of this disclosure, therefore, a "therapeutically effective amount" is the amount of agent that renders the overall composition effective.
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