David Grayzel
Harvard University
23 Papers
181 Citations
David Grayzel is an academic researcher from Harvard University. The author has contributed to research in topics: Hsp90 inhibitor & Hsp90. The author has an hindex of 12, co-authored 23 publications.
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Papers
Activity of IPI-504, a novel heat-shock protein 90 inhibitor, in patients with molecularly defined non-small-cell lung cancer.
Lecia V. Sequist,Scott N. Gettinger,Neil Senzer,Renato G. Martins,Pasi A. Jänne,Rogerio Lilenbaum,Jhanelle E. Gray,A. John Iafrate,Ryohei Katayama,Nafeeza Hafeez,Jennifer Sweeney,John R. Walker,Christian C. Fritz,Robert W. Ross,David Grayzel,Jeffrey A. Engelman,Darrell R. Borger,Guillermo Paez,Ronald B. Natale +18 more
TL;DR: IPI-504 has clinical activity in patients with NSCLC, particularly among patients with ALK rearrangements, and was below the target ORR of 20%, among the three patients with an ALK gene rearrangement.
Inhibition of heat shock protein 90 prolongs survival of mice with BCR-ABL-T315I-induced leukemia and suppresses leukemic stem cells
Cong Peng,Julia Brain,Yiguo Hu,Ami Goodrich,Linghong Kong,David Grayzel,Roger H. Pak,Margaret Ruth Read,Shaoguang Li +8 more
TL;DR: Rather than inhibiting kinase activity, elimination of mutant kinases provides a new therapeutic strategy for treating BCR-ABL-induced leukemia as well as other cancers resistant to treatment with tyrosine kinase inhibitors.
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A Phase I Study of the HSP90 Inhibitor Retaspimycin Hydrochloride (IPI-504) in Patients with Gastrointestinal Stromal Tumors or Soft-Tissue Sarcomas
Andrew J. Wagner,Rashmi Chugh,Lee S. Rosen,Jeffrey A. Morgan,Suzanne George,Michael S. Gordon,Joi Dunbar,Emmanuel Normant,David Grayzel,George D. Demetri +9 more
TL;DR: In this study of advanced GIST or other STS, IPI-504 was generally well-tolerated with some evidence of antitumor activity, serving as a clinical proof-of-concept that HSP90 inhibition remains a promising strategy.
Inhibition of heat shock protein 90 (Hsp90) with the novel agent IPI-504 in metastatic GIST following failure of tyrosine kinase inhibitors (TKIs) or other sarcomas: Clinical results from phase I trial
Andrew J. Wagner,Jeffrey A. Morgan,Rashmi Chugh,Lee S. Rosen,Suzanne George,Michael S. Gordon,C. M. Devine,A. D. Van Den Abbeele,David Grayzel,George D. Demetri +9 more
TL;DR: This data indicates that inhibition of the Hsp90 chaperone protein results in selective destruction of the mutated KIT kinase in human GIST cell lines across multispecies studies.
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A phase 1 study of IPI-504 (retaspimycin hydrochloride) in patients with relapsed or relapsed and refractory multiple myeloma.
David Siegel,Sundar Jagannath,David H. Vesole,Ivan Borello,Amitabha Mazumder,Constantine S. Mitsiades,Jill Goddard,Joi Dunbar,Emmanuel Normant,Julian Adams,David Grayzel,Kenneth C. Anderson,Paul G. Richardson +12 more
TL;DR: The most common treatment-related adverse event was grade 1 infusion site pain (four patients), and the area under the curve (AUC) increased with increasing dose, and the mean half-life was approximately 2–4 h for IPI-504 and its metabolites.
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