# US 2021/0275562 A1 · Cancer treatment methods

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- Number: US 2021/0275562 A1
- Document ID: US20210275562A1
- Status: Published application
- Kind: A1
- Application number: 17/249,528
- Filed: 2021-03-04
- Published: 2021-09-09
- Earliest claimed: 2020-03-05
- Inventors: Dennis W. Stacey
- Web page: https://patentgrep.com/patent/US20210275562A1

## CPC

- A61K 31/7072: having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/0095: {Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006)}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/475: having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine (vincamine A61K31/4375)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

A cancer treatment method includes administering a first dose of a drug selectively targeting cells in a particular phase (e.g., S phase cells); and administering an additional dose of the drug after waiting a full normal cell cycle. The method takes advantage of the uniformity of cell cycle length in normal cells (e.g., normal small intestine cells) and the and the lack of this uniformity, or variation in cell cycle length of cancer cells.

## Claims

### Claim 1

A method for selectively killing cells in S phase, the method comprising:
administering a first dose of a drug selectively targeting S phase cells; and
administering an additional dose of the drug after waiting a full normal cell cycle.

### Claim 2 (depends on 1)

The method of claim 1, further comprising:
repeating the administration of the additional dose at least one time.

### Claim 3 (depends on 1)

The method of claim 1, wherein the full normal cell cycle is a normal human intestine cell cycle or a lymphoid cell cycle.

### Claim 4 (depends on 1)

The method of claim 1, wherein the drug selectively targeting S phase cells is selected from the group consisting of bromodeoxyuridine (BRDU) and 5-ethynyl-2′-deoxyuridine (EDU).

### Claim 5 (depends on 1)

The method of claim 1, wherein the drug selectively targeting S phase cells is related to a dideoxynucleoside, or a derivative of such a drug specifically designed to enter tissues and be incorporated efficiently into DNA, and then block chain elongation.

### Claim 6 (depends on 1)

The method of claim 1, wherein the drug selectively targeting S phase cells is related to a thymidine analogous, or a derivative of such a drug, specifically designed to enter tissues and be incorporated efficiently into DNA, and then render the DNA unstable or toxic within the next few cell cycles.

### Claim 7 (depends on 1)

The method of claim 1, wherein the drug selectively targeting S phase cells is selected from the group consisting of methotrexate, pemetrexed, pralatrexate, cytarabine, gemcitabine, clofarabine, fludarabine, mercaptopurine, nelarabine, pentostatin, thioguanine, azacytidine, decitabine, irinotecan, and teniposide.

### Claim 8 (depends on 1)

The method of claim 1, wherein drug selectively targeting S phase cells is administered orally.

### Claim 9 (depends on 1)

The method of claim 1, wherein drug selectively targeting S phase cells is administered via injection.

### Claim 10 (depends on 1)

The method of claim 1, wherein the drug selectively targeting S phase cells is tritiated thymidine.

### Claim 11 (depends on 1)

The method of claim 1, wherein the method disproportionately kills cancer cells.

### Claim 12

A process for treating small intestine cancer comprising in sequence: administering a first dose of a drug selectively targeting S phase cells, wherein the drug kills cancer cells in the S phase and normal small intestine cells in the S phase and wherein the drug does not kill cells that are not in the S phase; waiting a full normal small intestine cell cycle; and administering an additional dose of the drug.

### Claim 13 (depends on 12)

The process of claim 12, further comprising: repeating the administration of the additional dose at least one time after waiting at least one more full normal small intestine cell cycle.

### Claim 14 (depends on 12)

The process of claim 12, wherein the drug selectively targeting S phase cells is selected from the group consisting of bromodeoxyuridine (BRDU), 5-ethynyl-2′-deoxyuridine (EDU), deoxynucleosides, methotrexate, pemetrexed, pralatrexate, cytarabine, gemcitabine, clofarabine, fludarabine, mercaptopurine, nelarabine, pentostatin, thioguanine, azacytidine, decitabine, irinotecan, and teniposide.

### Claim 15 (depends on 12)

The process of claim 12, wherein the administration is oral or via injection.

### Claim 16

A cancer treatment method comprising: administering a first dose of a drug selectively targeting M phase cells; and administering an additional dose of the drug after waiting a full normal cell cycle.

### Claim 17 (depends on 16)

The cancer treatment method of claim 16, wherein the drug is vinblastine.

### Claim 18 (depends on 16)

The cancer treatment method of claim 16, wherein the drug is selected from the group consisting of 5-fluorouracil (5-FU), tegafur, capecitabine, 5-fluorouridine 5′-triphosphate (FUTP), 5-fluoro-2′-deoxyuridine 5′-triphosphate (FdUTP), and 5-fluoro-2′-deoxyuridine 5′-monophosphate (FdUMP).

### Claim 19 (depends on 16)

The cancer treatment method of claim 16, wherein the drug comprises 5-(dihydroxyboryl)-2′-deoxyuridine.

### Claim 20 (depends on 16)

The cancer treatment method of claim 16, wherein the drug comprises a thymidine analogue in which the 3′ —OH group is replaced by a group selected from the group consisting of a methyl (—CH3), an ethyl (—CH2—CH3), an amine (—NH2), a sulfhydryl (—SH), fluorine at position 3 (—F), (—C═CH2), (—CH2—CH2-OH), (—CH═CH—OH), (—Br), and (—Se).