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Last Updated: May 10, 2024

Claims for Patent: 8,697,031

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Summary for Patent: 8,697,031

Title:	Dual function polymer micelles
Abstract:	The invention relates to micelles that are elaborated with functionality useful for imaging and/or selectively targeting tissue, e.g., in the delivery of hydrophobic agents.
Inventor(s):	Ai; Hua (Sichuan, CN), Duerk; Jeffrey L. (Avon Lake, OH), Flask; Chris (Avon Lake, OH), Gao; Jinming (Plano, TX), Lewin; Jonathan S. (Baltimore, MD), Shuai; Xintao (Cleveland Heights, OH), Weinberg; Brent (Cleveland Heights, OH)
Assignee:	Case Western Reserve University (Cleveland, OH)
Application Number:	11/569,989
Patent Claims:	1. A micellar structure comprising a biocompatible amphiphilic block copolymer selected from PBLG-PEO, PEO-PPO-PEO, PEG-b-PBLA, and PCL-PEG, a hydrophobic chemotherapeutic agent encapsulated within the micellar structure, a functionalized corona comprising a tissue- or tumor-specific targeting peptide sequence, and an imaging agent comprising an MRI contrast agent encapsulated within the micellar structure, the MRI contrast agent comprising superparamagnetic iron oxide, wherein the tissue-specific targeting peptide sequence and the tumor-specific targeting peptide sequence is selected from SEQ ID Nos 1-756. 2. A micellar structure of claim 1, wherein the amphiphilic copolymer is PCL-PEG. 3. A micellar structure of claim 1, wherein the chemotherapeutic agent is selected from aminoglutethimide, amsacrine, anastrozole, asparaginase, bcg, bicalutamide, bleomycin, buserelin, busulfan, campothecin, capecitabine, carboplatin, carmustine, chlorambucil, cisplatin, cladribine, clodronate, colchicine, cyclophosphamide, cyproterone, cytarabine, dacarbazine, dactinomycin, daunorubicin, dienestrol, diethylstilbestrol, docetaxel, doxorubicin, epirubicin, estradiol, estramustine, etoposide, exemestane, filgrastim, fludarabine, fludrocortisone, fluorouracil, fluoxymesterone, flutamide, gemcitabine, genistein, goserelin, hydroxyurea, idarubicin, ifosfamide, imatinib, interferon, irinotecan, ironotecan, letrozole, leucovorin, leuprolide, levamisole, lomustine, mechlorethamine, medroxyprogesterone, megestrol, melphalan, mercaptopurine, mesna, methotrexate, mitomycin, mitotane, mitoxantrone, nilutamide, nocodazole, octreotide, oxaliplatin, paclitaxel, pamidronate, pentostatin, plicamycin, porfimer, procarbazine, raltitrexed, rituximab, streptozocin, suramin, tamoxifen, temozolomide, teniposide, testosterone, thioguanine, thiotepa, titanocene dichloride, topotecan, trastuzumab, tretinoin, vinblastine, vincristine, vindesine, and vinorelbine. 4. A micellar structure of claim 3, wherein the chemotherapeutic agent is selected from paclitaxel and doxorubicin. 5. A micellar structure of claim 1, wherein the peptide sequence is a .alpha..sub.v.beta..sub.3 ligand. 6. A micellar structure of claim 5, wherein the .alpha..sub.v.beta..sub.3 ligand is cRGD. 7. A micellar structure of claim 1, wherein the functionalized corona comprises a second imaging agent. 8. A micellar structure of claim 7, wherein the second imaging agent comprises a chelating agent. 9. A micellar structure of claim 8, wherein the chelating agent is selected from DOTA, DTPA-BMA, DTPA-BP, and CDTA. 10. A micellar structure of claim 8, further comprising a radioactive moiety that is chelated by the chelating agent. 11. A micellar structure of claim 10, wherein the radioactive moiety is selected from .sup.225Ac, .sup.227Ac, .sup.241Am, .sup.198Au, .sup.7Be, .sup.212Bi, .sup.48Ca, .sup.109Cd, .sup.139Ce, .sup.141Ce, .sup.252Cf, .sup.55Co, .sup.57Co, .sup.60Co, .sup.51Cr, .sup.130Cs, .sup.131Cs, .sup.137Cs, .sup.61Cu, .sup.62Cu, .sup.165Dy, .sup.152Eu, .sup.155Eu, .sup.18F, .sup.55Fe, .sup.59Fe, .sup.64Ga, .sup.67Ga, .sup.68Ga, .sup.153Gd, .sup.68Ge, .sup.111In, .sup.115mIn, .sup.191mIr, .sup.192Ir, .sup.177Lu, .sup.51Mn, .sup.52Mn, .sup.99Mo, .sup.95Nb, .sup.194Os, .sup.203Pb, .sup.212Pb, .sup.103Pd, .sup.109Pd, .sup.238Pu, .sup.223Ra, .sup.226Ra, .sup.82Rb, .sup.186Re, .sup.188Re, .sup.105Rh, .sup.97Ru, .sup.103Ru, .sup.145Sm, .sup.153Sm, .sup.117mSn, .sup.85Sr, .sup.89Sr, .sup.90Sr, .sup.178Ta, .sup.179Ta, .sup.182Ta, .sup.149Tb, .sup.96Tc, .sup.99mTc, .sup.228Th, .sup.229Th, .sup.201Tl, .sup.170Tm, .sup.171Tm, .sup.188W, .sup.88Y, .sup.90Y, .sup.91Y, .sup.169Yb, .sup.62Zn, .sup.65Zn, .sup.99mTc-labeled Annexin V.sup.28, and .sup.95Zr. 12. A micellar structure of claim 11, wherein the radioactive moiety is selected from .sup.99mTc-labeled Annexin V.sup.28, and .sup.111In. 13. A pharmaceutical composition comprising micelles of claim 1 and a pharmaceutically acceptable carrier.

Details for Patent 8,697,031

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Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Recordati Rare Diseases, Inc.	ELSPAR	asparaginase	For Injection	101063	01/10/1978	⤷ Try a Trial	2024-06-06
Amgen, Inc.	NEUPOGEN	filgrastim	Injection	103353	02/20/1991	⤷ Try a Trial	2024-06-06
Amgen, Inc.	NEUPOGEN	filgrastim	Injection	103353	06/28/2000	⤷ Try a Trial	2024-06-06
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997	⤷ Try a Trial	2024-06-06
Idec Pharmaceuticals Corp.	RITUXAN	rituximab	Injection	103737	02/19/2002	⤷ Try a Trial	2024-06-06
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998	⤷ Try a Trial	2024-06-06
>Applicant	>Tradename	>Biologic Ingredient	>Dosage Form	>BLA	>Approval Date	>Patent No.	>Expiredate

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