IP Library Granted Patent US 10,099,996
Granted Patent B2
US 10,099,996 · App. 14/025,206 · Granted Oct 16, 2018

Compositions and methods of use of phorbol esters in the treatment of neoplasms

Inventors: Zheng Tao Han (Eugene, OR); Hung-Fong Chen (Taipei, TW)
Assignee: Biosuccess Biotech Co. Ltd.
C07C69/614A61K31/191A61K31/194A61K31/215A61K31/22A61K31/23A61K31/235A61K31/573A61K31/575A61K31/60A61K45/06C07C69/21C07C69/33C07C69/533C07C69/716C07C69/78C07C2103/40
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Quick Facts
Patent No.
US 10,099,996
App. No.
14/025,206
Granted
Oct 16, 2018
Kind
B2
Abstract

Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of chronic and acute conditions. Such conditions may be caused by disease, be symptoms, treatments, or sequelae of disease. The phorbol esters described are particularly useful in the treatment of neoplastic diseases and/or managing the side effects of chemotherapeutic and radiotherapeutic treatments of neoplastic diseases.

Claims (26)

1. A method of treating neoplasms comprising administering parenterally to a mammalian subject with lung cancer, an effective amount of a phorbol ester of Formula II, or a pharmaceutically acceptable salt, isomer, or enantiomer thereof,

and at least one secondary or adjunctive therapeutic agent;

wherein said effective amount is between about 10 μg to about 1500 μg of said phorbol ester of Formula II, administered every other day, and for at least a total of 5 times; and

wherein one or more symptoms or conditions suffered by the mammalian subject is alleviated or treated, the one or more symptoms being selected from the group consisting of chronic fatigue, excessive or easy bleeding, easy bruising, shortness of breath, petechiae, recurrent fever, swollen gums, slow healing of cuts, bone and joint discomfort, recurrent infections, weight loss, itching, night sweats, lymph node swelling, fever, abdominal pain and discomfort, disturbances in vision, coughing, loss of appetite, pain in the chest, difficulty swallowing, swelling, a need to urinate frequently, difficulty starting urination, difficulty holding back urine, weak or interrupted flow of urine, painful or burning urination, difficulty in having an erection, painful ejaculation, blood in urine or semen, frequent pain or stiffness, and weakness.

2. The method of claim 1 , wherein two secondary or adjunctive therapeutic agents are administered to said subject.

3. The method of claim 2 , wherein the two secondary or adjunctive therapeutic agents are dexamethasone and choline magnesium trisalicylate.

4. A method of treating neoplasms comprising administering parenterally to a mammalian subject with lymphoma, an effective amount of a phorbol ester of Formula II, or a pharmaceutically acceptable salt, isomer, or enantiomer thereof,

and at least one secondary or adjunctive therapeutic agent; wherein said effective amount is between about 10 μg to about 1500 μg of said phorbol ester of Formula II, administered every other day and wherein said phorbol ester of Formula II is administered for at least a total of 5 times; and

wherein one or more symptoms or conditions suffered by the mammalian subject is alleviated or treated, the one or more symptoms being selected from the group consisting of chronic fatigue, excessive or easy bleeding, easy bruising, shortness of breath, petechiae, recurrent fever, swollen gums, slow healing of cuts, bone and joint discomfort, recurrent infections, weight loss, itching, night sweats, lymph node swelling, fever, abdominal pain and discomfort, disturbances in vision, coughing, loss of appetite, pain in the chest, difficulty swallowing, swelling, a need to urinate frequently, difficulty starting urination, difficulty holding back urine, weak or interrupted flow of urine, painful or burning urination, difficulty in having an erection, painful ejaculation, blood in urine or semen, frequent pain or stiffness, and weakness.

5. A method of treating neoplasms comprising administering parenterally to a mammalian subject with breast cancer, an effective amount of a phorbol ester of Formula II, or a pharmaceutically acceptable salt, isomer, or enantiomer thereof,

and at least one secondary or adjunctive therapeutic agent; wherein said effective amount is between about 10 μg to about 1500 μg of said phorbol ester of Formula II, administered every other day and wherein said phorbol ester of Formula II is administered for at least a total of 5 times; and

wherein one or more symptoms or conditions suffered by the mammalian subject is alleviated or treated, the one or more symptoms being selected from the group consisting of chronic fatigue, excessive or easy bleeding, easy bruising, shortness of breath, petechiae, recurrent fever, swollen gums, slow healing of cuts, bone and joint discomfort, recurrent infections, weight loss, itching, night sweats, lymph node swelling, fever, abdominal pain and discomfort, disturbances in vision, coughing, loss of appetite, pain in the chest, difficulty swallowing, swelling, a need to urinate frequently, difficulty starting urination, difficulty holding back urine, weak or interrupted flow of urine, painful or burning urination, difficulty in having an erection, painful ejaculation, blood in urine or semen, frequent pain or stiffness, and weakness.

6. A method of treating neoplasms comprising administering parenterally to a mammalian subject with liver cancer, an effective amount of a phorbol ester of Formula II, or a pharmaceutically acceptable salt, isomer, or enantiomer thereof,

and at least one secondary or adjunctive therapeutic agent; wherein said effective amount is between about 10 μg to about 1500 μg of said phorbol ester of Formula II, administered every other day and wherein said phorbol ester of Formula II is administered for at least a total of 5 times; and

wherein one or more symptoms or conditions suffered by the mammalian subject is alleviated or treated, the one or more symptoms being selected from the group consisting of chronic fatigue, excessive or easy bleeding, easy bruising, shortness of breath, petechiae, recurrent fever, swollen gums, slow healing of cuts, bone and joint discomfort, recurrent infections, weight loss, itching, night sweats, lymph node swelling, fever, abdominal pain and discomfort, disturbances in vision, coughing, loss of appetite, pain in the chest, difficulty swallowing, swelling, a need to urinate frequently, difficulty starting urination, difficulty holding back urine, weak or interrupted flow of urine, painful or burning urination, difficulty in having an erection, painful ejaculation, blood in urine or semen, frequent pain or stiffness, and weakness.

7. A method of treating neoplasms comprising administering parenterally to a mammalian subject with pancreatic cancer, an effective amount of a phorbol ester of Formula II, or a pharmaceutically acceptable salt, isomer, or enantiomer thereof,

and at least one secondary or adjunctive therapeutic agent; wherein said effective amount is between about 10 μg to about 1500 μg of said phorbol ester of Formula II, administered every other day and wherein said phorbol ester of Formula II is administered for at least a total of 5 times; and

wherein one or more symptoms or conditions suffered by the mammalian subject is alleviated or treated, the one or more symptoms being selected from the group consisting of chronic fatigue, excessive or easy bleeding, easy bruising, shortness of breath, petechiae, recurrent fever, swollen gums, slow healing of cuts, bone and joint discomfort, recurrent infections, weight loss, itching, night sweats, lymph node swelling, fever, abdominal pain and discomfort, disturbances in vision, coughing, loss of appetite, pain in the chest, difficulty swallowing, swelling, a need to urinate frequently, difficulty starting urination, difficulty holding back urine, weak or interrupted flow of urine, painful or burning urination, difficulty in having an erection, painful ejaculation, blood in urine or semen, frequent pain or stiffness, and weakness.

8. A method of treating neoplasms comprising administering parenterally to a mammalian subject with cervical cancer, an effective amount of a phorbol ester of Formula II, or a pharmaceutically acceptable salt, isomer, or enantiomer thereof,

and at least one secondary or adjunctive therapeutic agent; wherein said effective amount is between about 10 μg to about 1500 μg of said phorbol ester of Formula II, administered every other day and wherein said phorbol ester of Formula II is administered for at least a total of 5 times; and

wherein one or more symptoms or conditions suffered by the mammalian subject is alleviated or treated, the one or more symptoms being selected from the group consisting of chronic fatigue, excessive or easy bleeding, easy bruising, shortness of breath, petechiae, recurrent fever, swollen gums, slow healing of cuts, bone and joint discomfort, recurrent infections, weight loss, itching, night sweats, lymph node swelling, fever, abdominal pain and discomfort, disturbances in vision, coughing, loss of appetite, pain in the chest, difficulty swallowing, swelling, a need to urinate frequently, difficulty starting urination, difficulty holding back urine, weak or interrupted flow of urine, painful or burning urination, difficulty in having an erection, painful ejaculation, blood in urine or semen, frequent pain or stiffness, and weakness.

9. A method of treating neoplasms comprising administering parenterally to a mammalian subject with multiple myeloma, an effective amount of a phorbol ester of Formula II, or a pharmaceutically acceptable salt, isomer, or enantiomer thereof,

and at least one secondary or adjunctive therapeutic agent; wherein said effective amount is between about 10 μg to about 1500 μg of said phorbol ester of Formula II, administered every other day and wherein said phorbol ester of Formula II is administered for at least a total of 5 times; and

wherein one or more symptoms or conditions suffered by the mammalian subject is alleviated or treated, the one or more symptoms being selected from the group consisting of chronic fatigue, excessive or easy bleeding, easy bruising, shortness of breath, petechiae, recurrent fever, swollen gums, slow healing of cuts, bone and joint discomfort, recurrent infections, weight loss, itching, night sweats, lymph node swelling, fever, abdominal pain and discomfort, disturbances in vision, coughing, loss of appetite, pain in the chest, difficulty swallowing, swelling, a need to urinate frequently, difficulty starting urination, difficulty holding back urine, weak or interrupted flow of urine, painful or burning urination, difficulty in having an erection, painful ejaculation, blood in urine or semen, frequent pain or stiffness, and weakness.

10. The method of any one of claim 1 , 5 , 6 , 7 , 8 , or 9 , wherein the at least one secondary or adjunctive therapeutic agent is administered to said subject in a coordinate administration protocol, simultaneously with, prior to, or after, administration of said phorbol ester to said subject.

11. The method of any one of claim 1 , 4 , 5 , 6 , 7 , 8 , or 9 , wherein the at least one secondary or adjunctive therapeutic agent is selected from the group consisting of: doxorubicin, vitamin D3, cytarabine, cytosine arabinoside, daunorubicin, cyclophosphamide, gemtuzumab ozogamicin, idarubicin, mercaptopurine, mitoxantrone, thioguanine, aldesleukin, asparaginase, carboplatin, etoposide phosphate, fludarabine, methotrexate, etoposide, dexamethasone, and choline magnesium trisalicylate.

Assignments (2)
SECURITY INTEREST Recorded Dec 31, 2018
From: BIOSUCCESS BIOTECH CO., LTD.
To: SUGHRUE MION, PLLC
Reel/Frame 047997/0405 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 24, 2013
From: HAN, ZHENG TAO; CHEN, HUNG-FONG
To: BIOSUCCESS BIOTECH CO., LTD.
Reel/Frame 031467/0623 →
Continuity (4)
Continuation 13745745 · Jan 18, 2013
Provisional Application 61588165 · Jan 18, 2012
Related Publication 20150072960A1 · Mar 12, 2015
Related Publication 20160332955A9 · Nov 17, 2016
Cited By (1)
US 12,502,369