Curtis J. Henrich - Rockville MD, US Heidi R. Bokesch - Frederick MD, US Susan E. Bates - Bethesda MD, US Robert W. Robey - Laurel MD, US Suneet Shukla - Rockville MD, US Suresh V. Ambudkar - Gaithersburg MD, US Michael C. Dean - Frederick MD, US James B. McMahon - Frederick MD, US
Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2 or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering peliomycin and other compounds described herein.
Method Of Inhibiting Abcg2 And Other Treatment Methods
Curtis J. Henrich - Rockville MD, US Heidi R. Bokesch - Frederick MD, US Laura K. Cartner - Middletown MD, US Richard W. Fuller - Fairfield PA, US Kirk R. Gustafson - Frederick MD, US Kentaro Takada - Yokohama, JP James B. McMahon - Frederick MD, US Susan E. Bates - Bethesda MD, US Robert W. Robey - Laurel MD, US Suneet Shukla - Rockville MD, US Suresh V. Ambudkar - Gaithersburg MD, US Michael C. Dean - Frederick MD, US
Assignee:
THE UNITED STATES OF AMERICA,AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICE - Bethesda MD
Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): Formula (I), wherein R, R, R, X, X, X, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.
Method Of Inhibiting Abcg2 And Other Treatment Methods
Heidi R. Bokesch - Frederick MD, US Laura K. Cartner - Middletown MD, US Richard W. Fuller - Fairfield PA, US Kirk R. Gustafson - Frederick MD, US Kentaro Takada - Chiba, JP James B. McMahon - Frederick MD, US Susan E. Bates - Bethesda MD, US Robert W. Robey - Laurel MD, US Suneet Shukla - Rockville MD, US Suresh V. Ambudkar - Gaithersburg MD, US Michael C. Dean - Frederick MD, US
Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I):wherein R, R, R, X, X, X, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.
- Bethesda MD, US Heidi R. Bokesch - Frederick MD, US Susan E. Bates - Bethesda MD, US Robert W. Robey - Laurel MD, US Suneet Shukla - Rockville MD, US Suresh V. Ambudkar - Gaithersburg MD, US Michael C. Dean - Frederick MD, US James B. McMahon - Frederick MD, US
Assignee:
The United States of America, as represented by the Secretary, Dept of Health and Human Services - Bethesda MD
Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2 or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering peliomycin and other compounds described herein.