US2010316567A1PendingUtilityA1
Ether and alkyl phospholipid compounds for treating cancer and imaging and detection of cancer stem cells
Individually held — no corporate assignee on recordPriority: Jun 12, 2009Filed: Jun 11, 2010Published: Dec 16, 2010
Est. expiryJun 12, 2029(~2.9 yrs left)· nominal 20-yr term from priority
A61P 35/00A61P 35/04A61P 43/00A61P 25/00C07B 59/00A61P 1/00A61K 31/661A61P 17/00A61K 45/06A61K 51/0489A61K 51/0408A61P 11/00A61P 15/00A61P 13/08A61P 13/12A61P 1/18A61K 31/685A61N 5/1001A61N 2005/1021A61N 5/02
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Claims
Abstract
Methods and compositions utilizing ether and alkyl phospholipid ether analog compounds for treating cancer and imaging, monitoring, and detecting cancer stem cells in humans.
Claims
exact text as granted — not AI-modified1 . A method of treating cancer comprising administering to a patient in need thereof a therapeutically effective amount of a radiolabeled ether or alkyl phospholipid compound of Formula I
where X is an isotope of iodine; n is an integer between 12 and 30; and Y is selected from the group comprising N + H 3 , HN + (R) 2 , N + H 2 R, and N + (R) 3 , wherein R is an alkyl or arylalkyl substituent,
or Formula II
where X is an isotope of iodine; n is an integer between 12 and 30; Y is selected from the group consisting of H, OH, COOH, COOR and OR, and Z is selected from the group comprising N + H 3 , HN + (R) 2 , N + H 2 R, and N + (R) 3 , wherein R is an alkyl or arylalkyl substituent,
wherein said therapeutically effective amount of said radiolabeled ether or alkyl phospholipid compound is sufficient to penetrate into said cancer stem cells and wherein a population of said cancer stem cells is reduced.
2 . The method of claim 1 , wherein said population of cancer stem cells comprises stem cells of the following cancers: glioma, lung cancer, squamous cell carcinoma, renal cancer, melanoma, colorectal cancer, ovarian cancer, prostate cancer, breast cancer, and pancreatic cancer.
3 . The method of claim 1 , wherein said isotope of iodine is 131 I.
4 . The method of claim 1 , wherein said radiolabeled ether or alkyl phospholipid compound is 18-(p-iodophenyl)octadecyl phosphocholine and X is 131 I.
5 . The method of claim 1 , wherein X is two or three isotopes of iodine.
6 . The method of claim 1 , wherein said method further comprises another cancer therapy selected from the group consisting of chemotherapy, radiation therapy, tumor resection, ablative therapy, and local physical treatment on the basis of cold (cryo), heat (thermal), radiofrequency, and microwave.
7 . A method of imaging a population of cancer stem cells in vivo comprising administering to a patient in need thereof an effective amount of a radiolabeled alkyl phospholipid compound of Formula I
where X is an isotope of iodine; n is an integer between 12 and 30; and Y is selected from the group comprising N + H 3 , HN + (R) 2 , N + H 2 R, and N + (R) 3 , wherein R is an alkyl or arylalkyl substituent,
Formula II
where X is an isotope of iodine; n is an integer between 12 and 30; Y is selected from the group consisting of H, OH, COOH, COOR and OR, and Z is selected from the group comprising N + H 3 , HN + (R) 2 , N + H 2 R, and N + (R) 3 , wherein R is an alkyl or arylalkyl substituent,
or a fluorescent analog of said radiolabeled ether or alkyl phospholipid compound,
wherein said radioactive ether or alkyl phospholipid compound or said fluorescent analog penetrates said cancer stem cells.
8 . The method of claim 7 , wherein said imaging is performed through a hybrid scanning utilizing single photon emission computed tomography (SPECT) or positron emission tomography (PET) and computed tomography (CT) or magnetic resonance imaging (MRI) techniques.
9 . The method of claim 7 , wherein said isotope of iodine is 124 I.
10 . The method of claim 7 , wherein said radiolabeled ether or alkyl phospholipid compound is 18-(p-iodophenyl)octadecyl phosphocholine and X is 124 I.
11 . The method of claim 7 , wherein X is two or three isotopes of iodine.
12 . The method of claim 7 , wherein said fluorescent analog has the following structure:
13 . The method of claim 7 , wherein said population of cancer stem cells comprises stem cells of the following cancers: glioma, lung cancer, squamous cell carcinoma, renal cancer, melanoma, colorectal cancer, ovarian cancer, prostate cancer, breast cancer, and pancreatic cancer.
14 . A method of ex vivo or in vitro labeling cancer stem cells comprising administering to cells suspected of comprising cancer stem cells an effective amount of a radiolabeled ether or alkyl phospholipid compound of Formula I
where X is an isotope of iodine; n is an integer between 12 and 30; and Y is selected from the group comprising N + H 3 , HN + (R) 2 , N + H 2 R, and N + (R) 3 , wherein R is an alkyl or arylalkyl substituent,
or Formula II
where X is an isotope of iodine; n is an integer between 12 and 30; Y is selected from the group consisting of H, OH, COOH, COOR and OR, and Z is selected from the group comprising N + H 3 , HN + (R) 2 , N + H 2 R, and N + (R) 3 , wherein R is an alkyl or arylalkyl substituent,
or a fluorescent analog of said radiolabeled ether or alkyl phospholipid compound,
wherein said cancer stem cells are labeled with said radiolabeled ether or alkyl phospholipid compound or said fluorescent analog.
15 . The method of claim 14 , wherein said isotope of iodine is 124 I.
16 . The method of claim 14 , wherein said radiolabeled ether or alkyl phospholipid compound is 18-(p-iodophenyl)octadecyl phosphocholine and X is 124 I.
17 . The method of claim 14 , wherein X is two or three isotopes of iodine.
18 . The method of claim 14 , wherein said fluorescent analog has the following structure:
19 . The method of claim 14 , wherein said cancer stem cells comprise stem cells of one or more of the following cancers: glioma, lung cancer, squamous cell carcinoma, renal cancer, melanoma, colorectal cancer, ovarian cancer, prostate cancer, breast cancer, and pancreatic cancer.
20 . The method of claim 14 , further comprising a step of distinguishing said cancer stem cells from non-cancer cells.Join the waitlist — get patent alerts
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