# US 9,675,631 B2 · Dosing regimens for treatment of proliferative disorders comprising administration of sapacitabine > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 9,675,631 B2 - Document ID: US9675631B2 - Status: Granted - Kind: B2 - Application number: 13/967,901 - Filed: 2013-08-15 - Published: 2014-05-22 - Granted: 2017-06-13 - Earliest claimed: 2013-08-15 - Assignees: Cyclacel Limited - Applicants: Cyclacel Limited - Inventors: Judy H. Chiao - Web page: https://patentgrep.com/patent/US9675631B2 ## CPC - A61K 31/7068: having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid - A61K 31/513: having oxo groups directly attached to the heterocyclic ring, e.g. cytosine - A61P 11/00: Drugs for disorders of the respiratory system - A61P 35/00: Antineoplastic agents - A61P 35/02: specific for leukemia - 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) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract One aspect of the present invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating a proliferative disorder, wherein the sapacitabine or metabolite thereof is administered in a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine or metabolite thereof for about 2 to about 6 days per week, for 2 weeks out of 3 weeks. Another aspect of the invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating cutaneous T-cell lymphoma (CTCL). ## Claims ### Claim 1 A method of treating a proliferative disorder selected from the group consisting of acute lymphocytic leukemia (ALL), acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non small cell lung cancer (NSCLC), cutaneous T-cell lymphoma (CTCL), Mycosis fungoides (MF) and Sezary syndrome (SS) comprising administering a therapeutically effective amount of sapacitabine, or a metabolite thereof which is 2′-C-Cyano-2′-deoxy-β-D-arabinopentafuranosylcytosine (CNDAC), to a human subject in need thereof in accordance with a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle for the sapacitabine or the metabolites thereof consists of: (i) administering therapeutically effective amount of sapacitabine or the metabolite thereof for 5 consecutive days per week, for 2 weeks, wherein the sapacitabine or metabolite thereof is administered in a total daily dosage of from about 125 to about 375 mg, followed by; (ii) a rest period of 1 week during which no sapacitabine or metabolite thereof is administered. ### Claim 2 (depends on 1) The method of claim 1, wherein the treatment cycle for the sapacitabine or the metabolites thereof consists of administering sapacitabine for 5 consecutive days per week. ### Claim 3 (depends on 1) The method of claim 1, wherein the sapacitabine, or the metabolite thereof, is administered twice daily. ### Claim 4 (depends on 3) The method of claim 3, wherein the sapacitabine, or the metabolite thereof, is administered about every 12 hours. ### Claim 5 (depends on 3) The method of claim 3, wherein the sapacitabine, or the metabolite thereof is administered in approximately equal dosages. ### Claim 6 (depends on 1) The method of claim 1, wherein the dosing regimen comprises from two to twelve treatment cycles. ### Claim 7 (depends on 1) The method of claim 1, wherein the sapacitabine, or the metabolite thereof, is administered in unit dosage form of about 25 to about 225 mg. ### Claim 8 (depends on 1) The method of claim 1, wherein the sapacitabine, or the metabolite thereof, is administered in unit dosage form of about 50 to about 125 mg. ### Claim 9 (depends on 1) The method of claim 1, wherein the sapacitabine, or the metabolite thereof, is administered in unit dosage form of about 20, 25, 50, 60, 75, 100, 125, 150, 200 or 300 mg. ### Claim 10 (depends on 1) The method of claim 1, wherein the sapacitabine or the metabolite thereof, is administered orally. ### Claim 11 (depends on 7) The method of claim 7, wherein the unit dosage form is a capsule. ### Claim 12 (depends on 1) The method of claim 1, wherein the sapacitabine or the metabolite thereof, is crystalline. ### Claim 13 (depends on 1) The method of claim 1, wherein the subject is 60 years of age or more. ### Claim 14 (depends on 1) The method of claim 1, wherein the total dosage of sapacitabine or the metabolite thereof, is increased incrementally with each treatment cycle. ### Claim 15 (depends on 1) The method according to claim 1 wherein the treatment cycles are repeated sequentially with a time lag between sequential treatment cycles. ### Claim 16 (depends on 3) The method according to claim 3, wherein the sapacitabine, or the metabolite thereof, is administered twice daily in different dosages. ### Claim 17 (depends on 1) The method of claim 1 wherein the sapacitabine is administered in a dosing regimen comprising at least one 21 day treatment cycle, wherein said treatment cycle for the sapacitabine or the metabolites thereof consists of: (i) administering a therapeutically effective amount of sapacitabine on days 1 to 5 of the treatment cycle; discontinuing said administration for days 6 and 7 of the treatment cycle; administering a therapeutically effective amount of sapacitabine on days 8 to 12 of the treatment cycle; discontinuing said administration for days 13 and 14 of the treatment cycle; (ii) a rest period for days 15 to 21 of the treatment cycle during which no sapacitabine is administered. ### Claim 18 (depends on 1) The method of claim 1, wherein the sapacitabine, or the metabolite thereof, is administered in unit dosage form of about 20, 25, 50, 60, 75 or 100 mg. ### Claim 19 (depends on 1) The method of claim 1, wherein the sapacitabine, or the metabolite thereof, is administered in a total daily dosage of from about 125 to about 225 mg. ### Claim 20 (depends on 1) The method of claim 1, wherein the sapacitabine, or the metabolite thereof, is administered in a total daily dosage of from about 225 to about 375 mg.