Oregon Health & Science University

Dana-farber-cancer Institute Inc.

The Brigham and Women's Hospital, Inc.

The United States Government As Represented by the Department of Veterans Affairs

Novartis Ag

Bristol-myers Squibb Compnay

Michael C Heinrich

Jonathan A Fletcher

George Daniel Demetri

Christopher C Corless

Francis Lee

Brian Jay Druker

Elisabeth Buchdunger

Heikki Joensuu

Sandra Leta Silberman

Sasa Dimitrijevic

David Tuveson

Renaud Capdeville

Francis Y Lee

The invention described herein relates to methods of identifying and treating individuals with protein tyrosine kinase associated disorders that have, or may, become resistant to treatment with a kinase inhibitor such as imatinib due to a gain-of-function mutation in KIT tyrosine kinase.

Methods of identifying and treating individuals exhibiting mutant kit protein

This disclosure provides tyrosine kinase protein and nucleic acid variants, particularly PDGFRA variants, which are activating forms of these molecules and are linked to neoplasms and/or the development or progression of cancer. The disclosure further provides methods of diagnosis and prognosis, and development of new therapeutic agents using these molecules and fragments thereof, and kits for employing these methods and compositions.

Platelet derived growth factor receptor alpha (PDGFRA) polypeptides comprising activating mutation(s)

Nucleic acids encoding platelet derived growth factor receptor alpha (PDGFRA) activating mutations

Method of detecting a neoplasia associated with an activating platelet derived growth factor receptor alpha (PDGFRA) mutation

4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of the formula Ior a pharmaceutically acceptable salt thereof can be used in the treatment of gastrointestinal stromal tumours.

Treatment of gastrointestinal stromal tumors

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Lake Oswego, OR, United States of America

Michael C Heinrich