The United States of America, as Represented by the Secretary, Department of Health and Human Services

Celgene Corporation

Astellas Pharma Gmbh

Gelgene Corporation

Susan Elaine Bates

Michael C Dean

Robert W Robey

James Brislin McMahon

Curtis J Henrich

Heidi R Bokesch

Suneet Shukla

Suresh V Ambudkar

Kirk R Gustafson

Richard W Fuller

David Covell

Melinda G Hollingshead

William McCulloch

Susan D Mertins

Geoffrey W Patton

Rao Vishnuvajjalla

Laura K Cartner

Kentaro Takada

Richard L Piekarz

Rando L Allikmets

Wyndham H Wilson

Yoshinori Naoe

Antonio T Fojo

Robert E Wittes

Antonio Tito Fojo

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 related treatments

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.

Method of inhibiting ABCG2 and other treatment methods

The present invention relates to deacetylase inhibitor (e.g., histone deacetylase inhibitor) therapies and demonstrates that individuals with low electrolyte levels may have increased susceptibility to certain unwanted side effects such as cardiac side effects. In some embodiments, the invention provides methods of administering DAC or DAC inhibitor therapy that includes electrolyte supplementation.

Deacetylase inhibitor therapy

The present invention provides a therapeutic agent of kidney cancer, which comprises FK228 of the formula (I) or a salt thereof. FK228 or a salt thereof, which is an active ingredient in the present invention, shows a superior antitumor activity in vivo against kidney cancer. 

Depsipeptide for therapy of kidney cancer

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. 

Botryllamides and method of inhibiting PGP in a mammal afflicted with cancer

The present invention features methods of treating a mammalian subject having renal cancer by administration of 4-[bis[2-[(methylsulfonyl)oxy]ethyl]amino]-benzaldehyde. The present invention further features administration protocols and dosing schedules for methods of treating patients having renal cancer and pharmaceutical compositions suitable for use in the treatment methods provided herein.

Treating renal cancer using 4-[bis[2-[(methylsulfonyl)oxy]ethyl]amino]-2-methyl-benzaldehyde

The present invention features methods of treating a mammalian subject having renal cancer by administration of certain dimethylsulfonate compounds, such as a 4-[bis[2-[(methylsulfonyl)oxy]ethyl]amino]-benzaldehyde. The present invention further features administration protocols and dosing schedules for methods of treating patients having renal cancer and pharmaceutical compositions suitable for use in the treatment methods provided herein.

Treating renal cancer using a 4-[bis[2-[(methylsulfonyl)oxy]ethyl]amino]-benzaldehyde

The present invention is a method of treatment for a patient with cancer. In particular, it is a method of treating patients havinglymphomas andbreast cancer using the microtubule agent, Taxol. The present method of administration, serves to prevent or retard the adverse side effects associated with Taxol and reduces the chances of a patient developing mdr Taxol resistance. The novel method of treatment provides a low-dose, long-term exposure to Taxol in a patient.

Taxol treatment of cancer

This invention provides for a novel ATP-binding cassette protein which is responsible for cytotoxin resistance. The invention also provides for methods of expressing the protein and assays for identification of inhibitors of the protein.

ATP-binding cassette protein responsible for cytotoxin resistance

This invention provides methods that are useful for inhibiting a MXR transporter in a cell overexpressing a MXR gene but not overexpressing a Pgp gene by contacting the cell with an acridine derivative. The invention also provides for a method of treating a mammal suffering from a cancer, which overexpressing a MXR gene but not overexpress a Pgp gene, by the co-administration of a chemotherapeutic and an acridine derivative.

Growing community of inventors

Bethesda, MD, United States of America

Susan Elaine Bates