Exelixis, Inc.

Genentech, Inc.

F. Hoffmann-la Roche Ag

Marcia Belvin

Lori Friedman

Gregory D Plowman

Helen Louise Francis-Lang

Roel P Funke

Danxi Li

Deepak Sampath

Jeffrey Wallin

Mallika Singh

Klaus Hoeflich

Stephanie A Robertson

Mario N Lioubin

Sonal Patel

Leisa Johnson

Ulka Vijapurkar

Jeffrey Scott Larson

Timothy S Heuer

David K Bol

Matthew V Lorenzi

Mark Merchant

Danix Li

Wen Shi

Rolf Peter Ryseck

Lata Jayaraman

John Moffat

Jeffery S Larson

Changyou Chen

Jocelyn Chan

Klaus P Hoeflich

Iris T Chan

John Prescott

Helen Francis-Lang

The invention provides combinations comprising a MEK inhibitor (such as GDC-0973 or GDC-0623), or a pharmaceutically acceptable salt thereof and an ERK inhibitor (such as GDC-0994). The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.

Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases

Methods and compositions are provided for treating hyperproliferative disorders in patients with a PI3K inhibitor, GDC-0032 as a single agent or in combination with chemotherapeutic agents. 

Mutant selectivity and combinations of a phosphoinositide 3-kinase inhibitor compound and chemotherapeutic agents for the treatment of cancer

Human SCD genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of SCD are provided.

SCDs as modifiers of the p53 pathway and methods of use

Combinations of PI3K inhibitor compounds having Formulas I and II and chemotherapeutic agents, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for treating hyperproliferative disorders such as cancer. Methods of using such combinations for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Combinations of phosphoinositide 3-kinase inhibitor compounds chemotherapeutic agents, and methods of use

Human MAP3K genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of MAP3K are provided.

MAP3Ks as modifiers of the p53 pathway and methods of use

Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use

Human MARK genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of MARK are provided.

Marks as modifiers of the p53 pathway and methods of use

Human PRMT genes are identified as modulators of the p53 pathway, and thus are therapeutic targets for disorders associated with defective p53 function. Methods for identifying modulators of p53, comprising screening for agents that modulate the activity of PRMT are provided.

PRMTs as modifiers of the p53 pathway and methods of use

RRP genes are identified as modulators of the p53 or p21 pathway, and thus are therapeutic targets for disorders associated with defective p53 or p21 function. Methods for identifying modulators of p53 or p21, comprising screening for agents that modulate the activity of RRP are provided. Modulating agents identified using the methods of the invention can be used to specifically inhibit growth of tumor cells that overexpress an RRP protein. mRRP1 knockout mice are also provided.

RRP sequences and knockout mice and uses thereof

Human HADH genes are identified as modulators of the p21 pathway, and thus are therapeutic targets for disorders associated with defective p21 function. Methods for identifying modulators of p21, comprising screening for agents that modulate the activity of HADH are provided.

HADHs as modifiers of the p21 pathway and methods of use

Rhomboid Related Proteins (RRPs), involved in the EGFR signaling pathway, are provided. Transgenic, nonhuman mammals containing a transgene encoding an RRP polypeptide or a gene effecting the expression of an RRP polypeptide, along with methods of modulating the interaction of RRP proteins with their pathway members, and methods of screening for agents that modulate the interaction of an RRP polypeptide with an RRP binding target, such as RRP-specific antibodies and small molecules identified in high throughput screens, are also provided. Modulating agents identified using the methods of the invention can be used to specifically inhibit growth of tumor cells that overexpress an RRP protein.

Human RRP sequences and methods of use

Growing community of inventors

Albany, CA, United States of America

Marcia Belvin