References/Library
Clinical
Clinical Management I
Clinical Trial Results
I Epidemiology I Genotyping I Imaging
I Pathology/Diagnosis I Prognosis I Reviews I Surgery I Neoadjuvant I Adjuvant
Research
Biology I Gene Mutations I GIST Resistance I GIST Signaling I Immunotherapy I KIT Inhibitors I MDR Proteins/Pumps I Pharmacokinetics I Model Targeted Therapy
Drugs
AMG706 I AMN107
I BAY 43-9006 I BMS-354825 I Genasense I Gleevec
I IPI-504 I PKC412 I Perifosine
I RAD001 I Sutent
Clinical
Clinical
Management (also see all other "Clinical" sections)
Treatment Guidelines I
Overview/Review I Dose I Managing Progression
National Comprehensive Cancer Network
(NCCN),NCCN Clinical
Practice Guidelines in Oncology - GIST: NCCN Clinical
Practice Guidelines in Oncology v.1.2005, 2-16-0005, Pages:
15-20,
Web Page: http://www.nccn.org/professionals/physician_gls/PDF/sarcoma.pdf
BLAY, J. Y., Bonvalot, S. et al, Consensus meeting
for the management of gastrointestinal stromal tumors. Report of
the GIST Consensus Conference of 20-21 March 2004, under the
auspices of ESMO: Ann.Oncol., Vol. 16, Iss. 4, 2005, Pages:
566-578,
Abstract: http://annonc.oxfordjournals.org/cgi/content/abstract/16/4/566
PDF: http://www.glivec.at/servlet/image?id=522
PubMed: PM:15781488
REID, R., Warren, B., et al, Guidelines for the
management of Gastrointestinal Stromal Tumours (GISTs)
http://www.augis.org/augis/upload/GIST Mngmnt Gdlns 071205
FINAL.pdf
Clinical Management of GIST: Understanding the New
Paradigms Helsinki & Barcelona 2003: Connective Tissue Oncology
Society (CTOS), 2004,
PDF Link: http://www.ctos.org/newsletter/GIST_Newsletter0404.pdf
DEMATTEO, R. P., Heinrich, M. C. et al, Clinical
management of gastrointestinal stromal tumors: before and after
STI-571: Hum.Pathol., Vol. 33, Iss. 5, 2002, Pages: 466-477,
Abstract:
PubMed: PM:12094371
JOENSUU, H., Fletcher, C. et al, Management of
malignant gastrointestinal stromal tumours: Lancet Oncol., Vol. 3,
Iss. 11, 2002, Pages: 655-664,
Abstract:
PDF: http://km.lsh.is/nam/nlif/gist.pdf
PubMed: PM:12424067
BLACKSTEIN, M. E., Rankin, C. et al, Clinical
benefit of Imatinib in patients (pts) with metastatic
Gastrointestinal Stromal Tumors (GIST) negative for the expression
of CD117 in the S0033 trial (Oral Presentation: Abstract # 9010):
Proc Am Soc Clin Oncol, Iss. 2005, 5-14-2005,
2005 ASCO Abstract and presentation
VAN OOSTEROM, Allan T.,Gastrointestinal Stromal
Tumors: Proc Am Soc Clin Oncol, 6-6-2004,
ASCO 2004 Presentation:
http://asco.org/ac/1,1003,_12-002511-00_18-0026-00_19-0011080,00.asp
Dose (also see Clinical Trial Results, especially phase III results)
VAN OOSTEROM, Allan T.,Gastrointestinal Stromal
Tumors: Proc Am Soc Clin Oncol, 6-6-2004,
Presentation:
http://asco.org/ac/1,1003,_12-002511-00_18-0026-00_19-0011080,00.asp
ZALCBERG, J. R., Verweij, J. et al, Outcome of
patients with advanced gastro-intestinal stromal tumors (GIST)
crossing over to a daily imatinib dose of 800mg (HD) after
progression on 400mg (LD) - an international, intergroup study of
the EORTC, ISG and AGITG. (Oral Presentation: Abstract # 9004):
Proc Am Soc Clin Oncol, Vol. 22, Iss. 2004, 6-6-2004,
2004 ASCO abstract and presentation
RANKIN, C., von Mehren, M. et al, Dose effect of imatinib (IM) in
patients (pts) with metastatic GIST - Phase III Sarcoma Group Study
S0033 (Oral Presentation: Abstract # 9005): Proc Am Soc Clin
Oncol, Vol. 22, Iss. 14S (July 15 Supplement), 6-6-2004,
2004 ASCO abstract and presentation
SCHERZER, N. J., Barkett, P. et al, Disease
Progression in Patients with Metastatic Gastrointestinal Stromal
Tumor (GIST) Receiving Gleevec (imatinib): The Effect of Drug
Dosage (Oral Presentation: Abstract # 227): 11-12-2004,
Presentation:
http://www.ctos.org/meeting/2004/presentations/friday/scherzer.ppt
|
Initial Therapy (Gleevec) - |
Phase I I Phase II I Phase III |
|
Gleevec-Resistant Therapy - |
Phase I I Phase II I Phase III |
Initial Therapy (Gleevec) -Phase I
JOENSUU, H., Roberts, P., et al, Effect of the
Tyrosine Kinase Inhibitor STI571 in a Patient with a Metastatic
Gastrointestinal Stromal Tumor NEJM, (This is the report of
the first GIST patient to ever take Gleevec).
Full-text (requires registration)
VAN OOSTEROM, A. T., Judson, I. et al, Safety and
efficacy of imatinib (STI571) in metastatic gastrointestinal
stromal tumours: a phase I study: Lancet, Vol. 358, Iss. 9291,
10-27-2001, Pages: 1421-1423,
Abstract:
PubMed: PM:11705489
|
STI 571, an Active Drug in Metastatic Gastro Intestinal Stromal
Tumors (GIST), an EORTC Phase I Study.
Abstract No: 2 2001 ASCO Author(s): Allan T. Van Oosterom, I. Judson, J. Verweij, E. Di Paola, M. van Glabbeke, S. Dimitrijevic, O. Nielsen, UZ Gasthuisberg KULeuven, Leuven, Belgium; EORTC Soft Tissue and Bone Sarcoma Group, Brussels, Belgium.
Update of the Imatinib (STI571, Glivec) phase I study in gastro
intestinal stromal tumours (GISTs). |
Initial Therapy (Gleevece) -Phase II
|
Outcome of Advanced Gastrointestinal Stromal
Tumor (GIST) Patients Treated With Imatinib Mesylate:Four-Year
Follow-Up of a Phase II Randomized Trial
Poster PDF 71KB ASCO 2006 Abstract* ASCO 2006 Presentation C. D. Blanke, H. Joensuu, G. D. Demetri, M. C. Heinrich, B. Eisenberg, J. Fletcher, C. L. Corless, E. Wehrle, K. B. Sandau, M. von Mehren NOTE: *The submitted abstract mistakenly stated that 63% of patients have died of Progressive Disease. The correct value is 40%. |
BLANKE, Charles D., von Mehren, Margaret et al,
Evaluation Of The Safety And Efficacy Of An Oral
Molecularly-targeted Therapy, STI571, In Patients (pts) With
Unresectable Or Metastatic Gastrointestinal Stromal Tumors GISTs)
Expressing C-kit (cd117) (Abstract #1): Proc Am Soc Clin Oncol,
Vol. 20, 5-14-2001,
2001 ASCO
Abstract:
Presentation:
DEMETRI, G. D., von, Mehren M. et al, Efficacy and
safety of imatinib mesylate in advanced gastrointestinal stromal
tumors: N.Engl.J.Med., Vol. 347, Iss. 7, 8-15-2002, Pages:
472-480,
Abstract: http://content.nejm.org/cgi/content/abstract/347/7/472
PubMed: PM:12181401
BLANKE, Charles., Joensuu, H. et al, Long-term
follow up of advanced gastrointestinal stromal tumor (GIST)
patients treated with imatinib mesylate. (Oral Presentation:
Abstract # 2): 1-22-2004,
2004 ASCO
Abstract:
Presentation:
High incidence of durable responses induced by imatinib mesylate
(Gleevec) in patients with unresectable and metastatic
gastrointestinal stromal tumors (GISTs)
Abstract No: 1608 2002 ASCO
Author(s): Margaret von Mehren, Charles Blanke, Heikki Joensuu,
Mike C Heinrich, Peter Roberts, Burton Eisenberg, Sandra Silberman,
Sasa Dimitrijevic, Beate Kiese, Jonathan Fletcher, Christopher
Fletcher, George D Demetri, Fox Chase Cancer Ctr, Philadelphia, PA;
OHSU, Portland, OR; University Hospital, Helsinki, Finland;
Novartis Oncology, E. Hanover, NJ; Novartis Oncology, Basel,
Switzerland; Dana-Farber Cancer Inst, Boston, MA.
|
KIT mutational status predicts clinical response to STI571 in
patients with metastatic gastrointestinal stromal tumors
(GISTs)
Abstract No. 6 2002 ASCO Michael C Heinrich, Christopher L Corless, Charles Blanke, George D Demetri, Heikki Joensuu, Meg von Mehren, Laura S McGreevey, Cecily L Wait, Diana Griffith, C-J Chen, Andrea Haley, Beate Kiese, Brian Druker, Peter Roberts, Burt Eisenberg, Sam Singer, Sandra Silberman, Sasa Dimitrijevic, Christopher D Fletcher, Jonathan A Fletcher, Oregon Health & Science University, Portland, OR; Dana-Farber Cancer Inst, Boston, MA; Helsinki University Central Hospital, Helsinki, Finland; Fox Chase Cancer Center, Philadelphia, PA; Novartis Oncology, Basel, Switzerland; University of Turku, Turku, Finland; Novartis Oncology, E. Hanover, NJ |
Phase II clinical study of STI571 in Japanese (Jpn) patients (pts)
with malignant gastrointestinal stromal tumors (GIST): Results of
the B 1201 study.
Abstract No: 4078 2004 ASCO
Citation: Journal of Clinical Oncology, 2004 ASCO Annual Meeting
Proceedings (Post-Meeting Edition). Vol 22, No 14S (July 15
Supplement), 2004: 4078
Author(s):
T. Doi, T. Nishida, S. Hirota, T. Sugiyama, K. Yamao, M. Koseki, T.
Okamura, K. Shirao, A. Ohtsu; National Cancer Center Hospital East,
Kashiwa, Japan; Osaka University Graduate School of Medicine,
Suita, Japan; Hokkaido University Medical Hospital, Sapporo, Japan;
Aichi Cancer Center, Nagoya, Japan; National Kure Medical Center,
Kure, Japan; National Kyusyu Cancer Center, Fukuoka, Japan;
National Cancer Center Hospotal, Tokyo, Japan
|
Efficacy of imatinib mesylate in metastatic or unresectable
malignant gastrointestinal stromal tumor (GIST)
Abstract No: 3312 M.-H. Ryu, T.-W. Kim, H.-M. Chang, H. Lee, J.-S. Kim, W.-K. Kim, J.-S. Lee, Y.-K. Kang; Asan Medical Center, University of Ulsan College of Medicine, Seoul, South Korea
A two arm phase 2 study of temozolomide (T) in gastrointestinal
stromal tumors (GISTs) and other soft-tissue sarcomas
(STS). |
VERWEIJ, J., Casali, P. G. et al, Progression-free
survival in gastrointestinal stromal tumours with high-dose
imatinib: randomized trial: Lancet, Vol. 364, Iss. 9440, 9-25-2004,
Pages: 1127-1134, (Phase III EORTC trial)
Abstract:
PubMed: PM:15451219
VERWEIJ, J., Early efficacy comparison of two doses
of imatinib for the treatment of advanced gastro-intestinal stromal
tumors (GIST): Interim results of a randomized phase III trial from
the EORTC-STBSG, ISG and AGITG (Oral Presentation: Abstract #
3272): 6-1-2003,
Abstract and presentation
RANKIN, C., von Mehren, M. et al, Dose effect of imatinib (IM) in
patients (pts) with metastatic GIST - Phase III Sarcoma Group Study
S0033 (Oral Presentation: Abstract # 9005): Proc Am Soc Clin
Oncol, Vol. 22, Iss. 14S (July 15 Supplement), 6-6-2004,
2004 ASCO
Abstract:
Presentation:
BLAY, J.-Y., Berthaud, P. et al, Continuous vs
intermittent imatinib treatment in advanced GIST after one year: A
prospective randomized phase III trial of the French Sarcoma Group.
(Oral Presentation: Abstract # 9006): Proc Am Soc Clin Oncol, Vol.
22, Iss. 2004, 6-6-2004,
2004 ASCO
Abstract:
Presentation:
Le Cesne, A. Perol, I. et al, Interruption of
imatinib (IM) in GIST patients with advanced disease: Updated
results of the prospective French Sarcoma Group randomized phase
III trial on survival and quality of life.
2005 ASCO
Abstract:
BENJAMIN, R. S., Rankin, C. et al, Phase III
dose-randomized study of imatinib mesylate (STI571) for GIST:
Intergroup S0033 early results (Oral Presentation: Abstract #
3271): Proc Am Soc Clin Oncol, Vol. 22, Iss. 2003, 6-1-2003, Pages:
814,
2003 ASCO
Abstract:
Presentation:
Demetri, G. D., Rankin, C., et at, Phase III
dose-randomized study of imatinib mesylate (Gleevec, STI571) for
GIST: intergroup S0033 early results
2002 ASCO Abstract 1651
ZALCBERG, J. R., Verweij, J. et al, Outcome of
patients with advanced gastro-intestinal stromal tumors (GIST)
crossing over to a daily imatinib dose of 800mg (HD) after
progression on 400mg (LD) - an international, intergroup study of
the EORTC, ISG and AGITG. (Oral Presentation: Abstract # 9004):
Proc Am Soc Clin Oncol, Vol. 22, Iss. 2004, 6-6-2004,
2004 ASCO
Abstract:
Presentation:
Pubmed:
CASALI, P., Verweij, J., et al Imatinib (Glivec)
400 vs 800 mg daily in patients with gastrointestinal stromal
tumors (GIST): a randomized phase III trial from the EORTC Soft
Tissue and Bone Sarcoma Group, the Italian Sarcoma Group (ISG), and
the Australasian Gastro-Intestinal Trials Group (AGITG). A toxicity
report.
Abstract No. 1650 2002 ASCO
Gleevec-resistant Therapy Phase I or Phase I/II
|
Gleevec-resistant Therapy Phase II
MAKI, R. G., Fletcher, J. A. et al, Results from a
continuation trial of SU11248 in patients (pts) with imatinib
(IM)-resistant gastrointestinal stromal tumor (GIST) (Oral
Presentation: Abstract # 9011): 5-14-0005,
2005 ASCO
Abstract:
Presentation:
Gleevec-resistant Therapy Phase III
|
Phase 3, multicenter, randomized, double-blind,
placebo-controlled trial of SU11248 in patients (pts)
following failure of imatinib for metastatic GIST
ASCO 2005 abstract ASCO 2005 presentation Abstract No: 4000 Author(s): G. D. Demetri, A. T. van Oosterom, M. Blackstein, C. Garrett, M. Shah, M. Heinrich, G. McArthur, I. Judson, C. M. Baum, P. G. Casali |
HEINRICH, M. C., Corless, C. L. et al, PDGFRA and
KIT mutations correlate with the clinical responses to imatinib
mesylate in patients with advanced gastrointestinal stromal tumors
(GIST) (Oral Presentation: Abstract # 3274): Proc Am Soc Clin
Oncol, Vol. 22, Iss. 2003, 6-1-2003, Pages: 815,
Abstract and presentation
HEINRICH, M. C.
and Corless, C.,KIT & PDGFRA Gene Mutation Screening For GI
Stromal Tumors: Heinrich-Corless Laboratories Website,
12-6-2005,
HEINRICH, M. C., Shomaker, C. L et al, Correlation
of target kinase genotype with clinical activity of imatinib
mesylate (IM) in patients with metastatic GI stromal tumors (GISTs)
expressing KIT (KIT+) (Oral Presentation: Abstract # 7):
5-15-2005,
Abstract and presentation
LINTON, K. M., Taylor, M. B., and Radford, J. A.,
Response evaluation in GIST treated with imatinib - misdiagnosis of
disease progression on CT due to cystic change in liver metastases
(Poster: Abstract # 9047): Proc Am Soc Clin Oncol, Iss. 2005,
5-16-2005,
Abstract and presentation
DESAI, Jayesh, Shankar, Sridhar et al, The Nodule
Within a Mass": A Unique Pattern of Disease Progression Seen in
Patients with Metastatic Gastrointestinal Stromal Tumors (GIST) Not
Predicted for by Standard Tumor Response Criteria: 11-8-2003,
Abstract:
http://ctos-abstracts.ctsnet.org/abstractsprogram/ctos/3?view=displayoverview&RequestTimeOut=2000&hidebuttons=yes
Pathology/Diagnosis
Rediscovering GIST: Differential Diagnosis of GIST
in the Era of Molecularly Targeted Therapy: Novartis Oncology,
2002,
PDF Link: http://www.glivec.com/pdfs/PathBgdr.pdf
CHECK, W.,GI stromal tumors 'a model for what's
coming': CAP Today, 2004,
Web Page:
http://www.cap.org/apps/docs/cap_today/cover_stories/0904GIST.html
FLETCHER, C. D., Berman, J. J. et al, Diagnosis of
gastrointestinal stromal tumors: A consensus approach: Hum.Pathol.,
Vol. 33, Iss. 5, 2002, Pages: 459-465,
Abstract: PubMed: PM:12094370
PAUWELS, P., diec-Rychter, M. et al, Changing
phenotype of gastrointestinal stromal tumours under imatinib
mesylate treatment: a potential diagnostic pitfall: Histopathology,
Vol. 47, Iss. 1, 2005, Pages: 41-47,
Abstract:
http://www.blackwell-synergy.com/doi/abs/10.1111/j.1365-2559.2005.02179.x
MIETTINEN, M. and Lasota, J., Gastrointestinal
stromal tumors (GISTs): definition, occurrence, pathology,
differential diagnosis and molecular genetics
11: Pol.J Pathol., Vol. 54, Iss. 1, 2003, Pages: 3-24,
Abstract: PM:12817876
PDF: http://www.poljpathol.cm-uj.krakow.pl/03_1/03_1MIE.pdf
PubMed: PM:15982322
WEST, Robert B., Corless, Christopher L. et al, The
Novel Marker, DOG1, Is Expressed Ubiquitously in Gastrointestinal
Stromal Tumors Irrespective of KIT or PDGFRA Mutation Status
4: American Journal of Pathology, Vol. 165, Iss. 1, 7-1-2004,
Pages: 107-113,
Abstract: http://ajp.amjpathol.org/cgi/content/abstract/165/1/107
PDF: http://ajp.amjpathol.org/cgi/reprint/165/1/107
Full Text: http://ajp.amjpathol.org/cgi/content/full/165/1/107
PubMed: PM15215166
BERMAN, J. and O'Leary, T. J., Gastrointestinal
stromal tumor workshop: Hum.Pathol., Vol. 32, Iss. 6, 2001, Pages:
578-582,
Abstract: PubMed: PM:11431711
FLETCHER, C. D., Berman, J. J. et al, Diagnosis of
gastrointestinal stromal tumors: A consensus approach: Hum.Pathol.,
Vol. 33, Iss. 5, 2002, Pages: 459-465,
Abstract: PubMed: PM:12094370
SINGER, S., Rubin, B. P. et al, Prognostic value of
KIT mutation type, mitotic activity, and histologic subtype in
gastrointestinal stromal tumors: J.Clin.Oncol., Vol. 20, Iss. 18,
9-15-2002, Pages: 3898-3905,
Abstract: http://www.jco.org/cgi/content/abstract/20/18/3898
PDF: http://www.jco.org/cgi/reprint/20/18/3898
Full Text: http://www.jco.org/cgi/content/full/20/18/3898
PubMed: PM:12228211
HEINRICH, M. C., Shomaker, C. L et al, Correlation
of target kinase genotype with clinical activity of imatinib
mesylate (IM) in patients with metastatic GI stromal tumors (GISTs)
expressing KIT (KIT+) (Oral Presentation: Abstract # 7):
5-15-2005,
Abstract and presentation
First Successful Systemic Treatment For GIST
(Metastatic and/or Unresectable) Glivec Imatinib: Symposium
Highlights, London, U.K. September 18-20, 2002: Novartis Oncology,
2003,
PDF Link: http://www.glivec.com/pdfs/X0061_London.pdf
CASPER, E. S., Gastrointestinal stromal tumors:
Curr.Treat.Options.Oncol., Vol. 1, Iss. 3, 2000, Pages:
267-273,
Full Text:
http://www.treatment-options.com/article.cfm?KeyWords=&PubID=ON01-3-2-04&Type=Article
PubMed: PM:12057170
PIDHORECKY, I., Cheney, R. T. et al,
Gastrointestinal stromal tumors: current diagnosis, biologic
behavior, and management: Ann.Surg.Oncol., Vol. 7, Iss. 9, 2000,
Pages: 705-712,
PDF: http://www.annalssurgicaloncology.org/cgi/reprint/7/9/705
PubMed: PM:11034250
MIETTINEN, M. and Lasota, J., Gastrointestinal
stromal tumors (GISTs): definition, occurrence, pathology,
differential diagnosis and molecular genetics
11: Pol.J Pathol., Vol. 54, Iss. 1, 2003, Pages: 3-24,
Abstract: PM:12817876
PDF: http://www.poljpathol.cm-uj.krakow.pl/03_1/03_1MIE.pdf
VAN OOSTEROM, Allan T.,Gastrointestinal Stromal
Tumors: Proc Am Soc Clin Oncol, 6-6-2004,
2004 ASCO
Presentation:
KNOOP, M., St, Friedrichs K., and Dierschke, J.,
Surgical management of gastrointestinal stromal tumors of the
stomach: Langenbecks Arch.Surg., Vol. 385, Iss. 3, 2000, Pages:
194-198,
Abstract: PubMed: PM:10857490
PIERIE, J. P., Choudry, U. et al, The effect of
surgery and grade on outcome of gastrointestinal stromal tumors:
Arch.Surg., Vol. 136, Iss. 4, 2001, Pages: 383-389,
Abstract: http://archsurg.ama-assn.org/cgi/content/abstract/136/4/383
PubMed: PM:11296107
DEMATTEO, R. P., Antonescu, C. R. et al, Adjuvant
imatinib mesylate in patients with primary high risk
gastrointestinal stromal tumor (GIST) following complete resection:
Safety results from the U.S. Intergroup Phase II trial ACOSOG Z9000
(Oral Presentation: Abstract # 9009): Proc Am Soc Clin Oncol, Iss.
2005, 5-14-2005,
2005 ASCO
Abstract and presentation:
GRONCHI, A., Fiore, M. et al, Surgery of residual
disease following Imatinib mesylate in advanced gastrointestinal
stromal tumors (GIST) (Poster Discussion: Abstract # 9038): Proc Am
Soc Clin Oncol, Iss. 2005, 5-15-2005,
Abstract:
http://www.asco.org/ac/1,1003,_12-002643-00_18-0034-00_19-0033394,00.asp
Presentation:
http://www.asco.org/ac/1,1003,_12-002511-00_18-0034-00_19-004324,00.asp
GRONCHI, Alessandro, Fiore, Marco et al, Advanced
Gastro-Intestinal Stromal Tumor: Molecular, Pathological and
Clinical Pattern in Post-Imatinib Surgery (Oral Presentation:
Abstract # 399): 11-20-2005,
Presentation:
http://www.ctos.org/meeting/2005/presentations/Sunday/am0945_Gronchi399.ppt
RAUT, Chandrajit, Posner, Matthew et al, Surgical
Management of Gastro-Intestinal Stromal Tumors (GIST) Following
Treatment with KIT-Directed Chemotherapy (Oral Presentation:
Abstract # 459): 11-20-2005,
Presentation:
http://www.ctos.org/meeting/2005/presentations/Sunday/am0945_Raut459.ppt
RAUT, C., P., Posner, M., et al Surgical management
of gastrointestinal stromal tumors (GIST) following systemic
therapy with kinase-targeted
2006 ASCO GI cancers symposium
Abstract and presentation
RUTKOWSKI, P., Nowecki, Z. et al, Surgical
treatment of patients (pts) with gastrointestinal stromal tumors
(GIST) after imatinib mesylate (IM) therapy (Poster: Abstract #
9037): Proc Am Soc Clin Oncol, Iss. 2005, 5-14-2005,
Abstract and presentation
RUTKOWSKI, P., Nowecki, Z. et al, Surgical
treatment of patients (pts) with gastrointestinal stromal tumors
(GIST) after imatinib mesylate (IM) therapy (Poster: Abstract #
9037): Proc Am Soc Clin Oncol, Iss. 2005, 5-14-2005,
2005 ASCO
Abstract and presentation:
DEMATTEO, R. P., Antonescu, C. R. et al, Adjuvant
imatinib mesylate in patients with primary high risk
gastrointestinal stromal tumor (GIST) following complete resection:
Safety results from the U.S. Intergroup Phase II trial ACOSOG Z9000
(Oral Presentation: Abstract # 9009): Proc Am Soc Clin Oncol, Iss.
2005, 5-14-2005,
2005 ASCO
Abstract and presentation
HEINRICH, M. C., Rubin, B. P. et al, Biology and
genetic aspects of gastrointestinal stromal tumors: KIT activation
and cytogenetic alterations: Hum.Pathol., Vol. 33, Iss. 5, 2002,
Pages: 484-495,
Abstract:
PDF: http://heinrich-corless.net/pdfs/humanpath.pdf
PubMed: PM:12094373
HEINRICH, M. C., Corless, C. L. et al, Kinase
mutations and imatinib response in patients with metastatic
gastrointestinal stromal tumor: J.Clin.Oncol., Vol. 21, Iss. 23,
12-1-2003, Pages: 4342-4349,
PDF: http://heinrich-corless.net/pdfs/jcomutationpaper.pdf
Full Text: http://www.jco.org/cgi/content/full/21/23/4342
PubMed: PM:14645423
HEINRICH, M. C., Corless, C. L. et al, PDGFRA
activating mutations in gastrointestinal stromal tumors: Science,
Vol. 299, Iss. 5607, 1-31-2003, Pages: 708-710,
PDF: http://heinrich-corless.net/pdfs/science.pdf
Full Text: http://www.sciencemag.org/cgi/content/full/299/5607/708
PubMed: PM:12522257
HIROTA, S., Isozaki, K. et al, Gain-of-function
mutations of c-kit in human gastrointestinal stromal tumors:
Science, Vol. 279, Iss. 5350, 1-23-1998, Pages: 577-580,
Full Text: http://www.sciencemag.org/cgi/content/full/279/5350/577
PubMed: PM:9438854
MIETTINEN, M., Sarlomo-Rikala, M., and Lasota, J.,
Gastrointestinal stromal tumors: recent advances in understanding
of their biology: Hum.Pathol., Vol. 30, Iss. 10, 1999, Pages:
1213-1220,
Abstract:
PubMed: PM:10534170
RUBIN, B. P., Singer, S. et al, KIT activation is a
ubiquitous feature of gastrointestinal stromal tumors: Cancer Res.,
Vol. 61, Iss. 22, 11-15-2001, Pages: 8118-8121,
Abstract:
http://cancerres.aacrjournals.org/cgi/content/abstract/61/22/8118
Full Text: http://cancerres.aacrjournals.org/cgi/content/full/61/22/8118
PubMed: PM:11719439
PLAAT, B. E., Hollema, H. et al, Soft tissue
leiomyosarcomas and malignant gastrointestinal stromal tumors:
differences in clinical outcome and expression of multidrug
resistance proteins: J.Clin.Oncol., Vol. 18, Iss. 18, 9-15-2000,
Pages: 3211-3220,
Abstract: http://www.jco.org/cgi/content/abstract/18/18/3211
Full Text: http://www.jco.org/cgi/content/full/18/18/3211
PubMed: PM:10986053
WU, Kai, Xing, Leon et al, Detecting copy number
aberrations in DNA from gastrointestinal stromal tumors with
Affymetrix gene expression microarrays (Abstract # LB-47): Proc
Amer Assoc Cancer Res, Vol. 46, Iss. 2005, 4-16-2005,
Abstract:
BRUCE ALBERTS, Alexander Johnson Julian Lewis
Martin Raff Keith Roberts Peter Walter,Molecular Biology of the
Cell, 4th Edition: Vol. Fourth, 2002, Pages: 1-1616,
Amazon.com:
http://www.amazon.com/gp/product/0815332181/qid=1134091535/sr=2-1/ref=pd_bbs_b_2_1/104-4860748-6394304?s=books&v=glance&n=283155
GSCHWIND, A., Fischer, O. M., and Ullrich, A., The
discovery of receptor tyrosine kinases: targets for cancer therapy:
Nat.Rev.Cancer, Vol. 4, Iss. 5, 2004, Pages: 361-370,
Abstract:
PubMed: PM:15122207
HEINRICH, M. C., Corless, C. L. et al, Kinase
mutations and imatinib response in patients with metastatic
gastrointestinal stromal tumor: J.Clin.Oncol., Vol. 21, Iss. 23,
12-1-2003, Pages: 4342-4349,
PDF: http://heinrich-corless.net/pdfs/jcomutationpaper.pdf
Full Text: http://www.jco.org/cgi/content/full/21/23/4342
PubMed: PM:14645423
HEINRICH, M. C. and Corless, C.,KIT & PDGFRA Gene Mutation Screening For GI Stromal Tumors: Heinrich-Corless Laboratories Website, 12-6-2005,
RUBIN, Brian P., Antonescu, Cristina R. et al, A
Knock-In Mouse Model of Gastrointestinal Stromal Tumor Harboring
Kit K641E: Cancer Research, Vol. 65, Iss. 15, 8-1-2005, Pages:
6631-6639,
Abstract:
http://cancerres.aacrjournals.org/cgi/content/abstract/65/15/6631
PubMed: PM:16061643
WU, Kai, Xing, Leon et al, Detecting copy number
aberrations in DNA from gastrointestinal stromal tumors with
Affymetrix gene expression microarrays (Abstract # LB-47): Proc
Amer Assoc Cancer Res, Vol. 46, Iss. 2005, 4-16-2005,
Abstract:
Primary Resistance I Secondary Resistance I Residual Disease (Stable lesions) I CML Resistance/General Imatinib Resistance
DEBIEC-RYCHTER, Maria, Cools, Jan et al, Mechanisms
of resistance to imatinib mesylate in gastrointestinal stromal
tumors and activity of the PKC412 inhibitor against
imatinib-resistant mutants: Gastroenterology, Vol. 128, Iss. 2,
2005, Pages: 270-279,
Abstract: http://linkinghub.elsevier.com/retrieve/pii/s0016508504020311
PubMed: PM:15685537
FLETCHER, J. A., Corless, C. L. et al, Mechanisms
of resistance to imatinib mesylate (IM) in advanced
gastrointestinal stromal tumor (GIST) (Oral Presentation: Abstract
# 3275): Proc Am Soc Clin Oncol, Vol. 22, Iss. 2003, 6-1-2003,
Pages: 815,
2003 ASCO
abstract and presentation
VAN GLABBEKE, M., Verweij, J. et al, Early and Late
Resistance to Imatinib (IM) in Advanced Gastro-Intestinal Stromal
Tumors (GIST) Are Predicted By Different Prognostic Factors: an
Analysis of the EORTC-ISG-AGITG Randomized Trial: 11-12-2004,
Presentation:
http://www.ctos.org/meeting/2004/presentations/friday/vanGlabbeke.ppt
FLETCHER, J. A., Corless, C. L. et al, Mechanisms
of resistance to imatinib mesylate (IM) in advanced
gastrointestinal stromal tumor (GIST) (Oral Presentation: Abstract
# 3275): Proc Am Soc Clin Oncol, Vol. 22, Iss. 2003, 6-1-2003,
Pages: 815,
2003 ASCO
abstract and presentation
VAN GLABBEKE, M., Verweij, J. et al, Early and Late
Resistance to Imatinib (IM) in Advanced Gastro-Intestinal Stromal
Tumors (GIST) Are Predicted By Different Prognostic Factors: an
Analysis of the EORTC-ISG-AGITG Randomized Trial: 11-12-2004,
Presentation:
http://www.ctos.org/meeting/2004/presentations/friday/vanGlabbeke.ppt
VAN GLABBEKE, Martine, Verweij, Jaap et al, Initial
and Late Resistance to Imatinib in Advanced Gastrointestinal
Stromal Tumors Are Predicted by Different Prognostic Factors: A
European Organization for Research and Treatment of Cancer-Italian
Sarcoma Group-Australasian Gastrointestinal Trials Group Study:
Journal of Clinical Oncology, Vol. 23, Iss. 24, 8-20-2005, Pages:
5795-5804,
Abstract: http://www.jco.org/cgi/content/abstract/23/24/5795
PubMed: PM:16110036
WAKAI, T, Kanda, T. et al, Late resistance to
imatinib therapy in a metastatic gastrointestinal stromal tumour is
associated with a second KIT mutation.: British Journal of Cancer,
Vol. 90, Iss. 11, 6-1-2004, Pages: 2059-2061,
Abstract: http://www.nature.com/bjc/journal/v90/n11/abs/6601819a.html
PubMed: PM:15150562
DESAI, Jayesh, Shankar, Sridhar et al, The Nodule
Within a Mass": A Unique Pattern of Disease Progression Seen in
Patients with Metastatic Gastrointestinal Stromal Tumors (GIST) Not
Predicted for by Standard Tumor Response Criteria: 11-8-2003,
Abstract:
http://ctos-abstracts.ctsnet.org/abstractsprogram/ctos/3?view=displayoverview&RequestTimeOut=2000&hidebuttons=yes
DEMETRI, G. D., Desai, J. et al, SU11248, a
multi-targeted tyrosine kinase inhibitor, can overcome imatinib
(IM) resistance caused by diverse genomic mechanisms in patients
(pts) with metastatic gastrointestinal stromal tumor (GIST). (Oral
Presentation: Abstract # 3001): 6-6-2004,
2004 ASCO
abstract and presentation
DEMETRI, G. D., van Oosterom, A. T. et al, Phase 3,
multicenter, randomized, double-blind, placebo-controlled trial of
SU11248 in patients (pts) following failure of imatinib for
metastatic GIST (Oral Presentation; Abstract # 4000):
5-14-2005,
2005 ASCO
abstract and presentation
BAUER, Sebastian and Yu, Lynn,Targeting HSP90 In
IM-Resistant GIST: KIT Degradation As A Broadly Relevant Salvage
Strategy.(Oral Presentation: Abstract # 457): 11-21-2005,
Presentation:
http://www.ctos.org/meeting/2005/presentations/Monday/am0800_Bauer457.ppt
DEBIEC-RYCHTER, Maria, Cools, Jan et al, Mechanisms
of resistance to imatinib mesylate in gastrointestinal stromal
tumors and activity of the PKC412 inhibitor against
imatinib-resistant mutants: Gastroenterology, Vol. 128, Iss. 2,
2005, Pages: 270-279,
Abstract: http://linkinghub.elsevier.com/retrieve/pii/s0016508504020311
PubMed: PM:15685537
GROWNEY, Joseph D., Clark, Jennifer J. et al,
Activation mutations of human c-KIT resistant to imatinib mesylate
are sensitive to the tyrosine kinase inhibitor PKC412: Blood, Vol.
106, Iss. 2, 7-15-2005, Pages: 721-724,
Abstract: http://www.bloodjournal.org/cgi/content/abstract/106/2/721
PubMed: PM:15790786
CHEN, Lei L., Trent, Jonathan C. et al, A Missense
Mutation in KIT Kinase Domain 1 Correlates with Imatinib Resistance
in Gastrointestinal Stromal Tumors
1: Cancer Research, Vol. 64, Iss. 17, 9-1-2004, Pages:
5913-5919,
Abstract:
http://cancerres.aacrjournals.org/cgi/content/abstract/64/17/5913
PDF: http://cancerres.aacrjournals.org/cgi/reprint/64/17/5913
Full Text: http://cancerres.aacrjournals.org/cgi/content/full/64/17/5913
BURGER, H., vanTol, H. et al, Chronic Imatinib
Mesylate Exposure Leads to Reduced Intracellular Drug
Accumulation by Induction of the ABCG2 (BCRP) and ABCB1 (MDR1) Drug
Transport
Pumps.: Cancer Biol & Therapy, Vol. 4, Iss. 7, 2005, Pages:
747-752,
Abstract:
http://www.landesbioscience.com/journals/cbt/abstract.php?id=1826
PubMed: PM:15970668
HOHENBERGER, P., Wardelman, E. et al, Acquired
Resistance to Imatinib in Progressive Gastrointestinal Stromal
Tumors Due to Multiple Synchronous Kinase Mutations in Different
Exons of KIT (Oral Presentation: Abstract # 347): 11-12-2004,
Presentation:
http://ctos.org/meeting/2004/presentations/friday/hohenberger.ppt
SCHERZER, N. J., Barkett, P. et al, Disease
Progression in Patients with Metastatic Gastrointestinal Stromal
Tumor (GIST) Receiving Gleevec (imatinib): The Effect of Drug
Dosage (Oral Presentation: Abstract # 227): 11-12-2004,
Presentation:
http://www.ctos.org/meeting/2004/presentations/friday/scherzer.ppt
SCHITTENHELM, Marcus M., Shiraga, Sharon et al,
Dasatinib (BMS-354825), a Dual SRC/ABL Kinase Inhibitor, Inhibits
the Kinase Activity of Wild-Type, Juxtamembrane, and Activation
Loop Mutant KIT Isoforms Associated with Human Malignancies
2: Cancer Research, Vol. 66, Iss. 1, 1-1-2006, Pages:
473-481,
Abstract: http://cancerres.aacrjournals.org/cgi/content/abstract/66/1/473
PubMed: PM:16397263
Residual Disease (Stable lesions)
ELRICK, Lucy J., Jorgensen, Heather G. et al,
Punish the parent not the progeny: Blood, Vol. 105, Iss. 5,
3-1-2005, Pages: 1862-1866,
Abstract: http://www.bloodjournal.org/cgi/content/abstract/105/5/1862
PubMed: PM:15528314
CHURCH, Sally, Imatinib and Beyond -- New
Developments in the Treatment of CML: An Interview With Brian
Druker, MD: Medscape Today, 2004,
Web Page: http://www.medscape.com/viewarticle/496015?src=search
COGHLAN, Andy, New tests identify cancer
"ringleaders": NewScientist.com, 1-20-2005,
Web Page: http://www.newscientist.com/channel/health/dn6904
TRAVIS, John, The Bad Seed: Rare stem cells appear
to drive cancers: Science News, Vol. 165, Iss. 12, 3-20-2004,
Pages: 184,
Web Page: http://www.sciencenews.org/articles/20040320/bob8.asp
GRONCHI, A., Fiore, M. et al, Surgery of residual
disease following Imatinib mesylate in advanced gastrointestinal
stromal tumors (GIST) (Poster Discussion: Abstract # 9038): Proc Am
Soc Clin Oncol, Iss. 2005, 5-15-2005,
2005 ASCO
abstract and presentation
21. GUZMAN, M. L. and Jordan, C. T., Considerations
for targeting malignant stem cells in leukemia.: Cancer Control,
Vol. 11, Iss. (2) Mar-Apr, 2004, Pages: 97-104,
Web Page: http://www.moffitt.usf.edu/pubs/ccj/v11n2/pdf/97.pdf
CML Resistance/General Imatinib Resistance
NIMMANAPALLI, Ramadevi, Fuino, Lianne et al,
Histone Deacetylase Inhibitor LAQ824 Both Lowers Expression and
Promotes Proteasomal Degradation of Bcr-Abl and Induces Apoptosis
of Imatinib Mesylate-sensitive or -refractory Chronic Myelogenous
Leukemia-Blast Crisis Cells
12: Cancer Research, Vol. 63, Iss. 16, 8-15-2003, Pages:
5126-5135,
Abstract:
PDF:
Full Text:
PubMed:
GOLEMOVIC, Mirna, Verstovsek, Srdan et al, AMN107,
a Novel Aminopyrimidine Inhibitor of Bcr-Abl, Has In vitro Activity
against Imatinib-Resistant Chronic Myeloid Leukemia: Clinical
Cancer Research, Vol. 11, Iss. 13, 7-1-2005, Pages:
4941-4947,
Abstract:
http://clincancerres.aacrjournals.org/cgi/content/abstract/11/13/4941
PubMed: PM:16000593
O'HARE, Thomas, Walters, Denise K. et al, In vitro
Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against
Clinically Relevant Imatinib-Resistant Abl Kinase Domain Mutants:
Cancer Research, Vol. 65, Iss. 11, 6-1-2005, Pages:
4500-4505,
Abstract:
http://cancerres.aacrjournals.org/cgi/content/abstract/65/11/4500
PubMed: PM:15930265
SHAH, Neil P., Tran, Chris et al, Overriding
Imatinib Resistance with a Novel ABL Kinase Inhibitor
1: Science, Vol. 305, Iss. 5682, 7-16-2004, Pages: 399-401,
Abstract: http://www.sciencemag.org/cgi/content/abstract/305/5682/399
RUBIN, B. P., Singer, S. et al, KIT activation is a
ubiquitous feature of gastrointestinal stromal tumors: Cancer Res.,
Vol. 61, Iss. 22, 11-15-2001, Pages: 8118-8121,
Abstract:
http://cancerres.aacrjournals.org/cgi/content/abstract/61/22/8118
Full Text: http://cancerres.aacrjournals.org/cgi/content/full/61/22/8118
PubMed: PM:11719439
BLASKOVICH, M. A., Sun, J. et al, Discovery of
JSI-124 (cucurbitacin I), a selective Janus kinase/signal
transducer and activator of transcription 3 signaling pathway
inhibitor with potent antitumor activity against human and murine
cancer cells in mice: Cancer Research, Vol. 63, Iss. 6, 3-15-2003,
Pages: 1270-1279,
Abstract: http://cancerres.aacrjournals.org/cgi/content/abstract/63/6/1270
PDF: http://cancerres.aacrjournals.org/cgi/reprint/63/6/1270
Full Text: http://cancerres.aacrjournals.org/cgi/content/full/63/6/1270
PubMed: PM:12649187
DUENSING, Anette, Joseph, Nora E. et al, Protein
Kinase C {theta} (PKC{theta}) Expression and Constitutive
Activation in Gastrointestinal Stromal Tumors (GISTs)
1: Cancer Research, Vol. 64, Iss. 15, 8-1-2004, Pages:
5127-5131,
Abstract:
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PDF: http://cancerres.aacrjournals.org/cgi/content/full/64/15/5127
Full Text: http://cancerres.aacrjournals.org/cgi/content/full/64/15/5127
PubMed: PM:15289315
TARN, Chi and Godwin, Andrew K., Glucose uptake is
altered in gastrointestinal stromal tumors in Response to imatinib
mesylate therapy via phospho-inositol-3 kinase (Board #1): Proc
Amer Assoc Cancer Res, Vol. 46, Iss. 2005, 4-19-2005,
Abstract:
BORG, C., TERME, M., Novel mode of action of c-kit
tyrosine kinase inhibitors leading to NK cell–dependent
antitumor effects J. Clin. Invest. 114:379-388 (2004)
doi:10.1172/JCI200421102
Full text: http://www.jci.org/cgi/content/full/114/3/379
ZITVOGEL, L., Ghiringhelli, M., A Novel Mode of
Antitumor Activity For Imatinib Mesylate: Consequences for the
design of surrogate markers of efficacy and combination
therapies.
2005 ASCO abstract
DEMETRI, G. D., Targeting c-kit mutations in solid
tumors: scientific rationale and novel therapeutic options:
Semin.Oncol., Vol. 28, Iss. 5 Suppl 17, 2001, Pages: 19-26,
Abstract:
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PubMed: PM:11740803
BAUER, S., Hubert, C. et al, KIT hyperactivation in
imatinib-resistant GIST: Implications for salvage therapies (Poster
Discussion: Abstract No: 9034): Proc Am Soc Clin Oncol, Iss. 2005,
5-15-0005,
2005 ASCO
abstract and presentation
BAUER, Sebastian and Yu, Lynn, Targeting HSP90 In
IM-Resistant GIST: KIT Degradation As A Broadly Relevant Salvage
Strategy. (Oral Presentation: Abstract # 457): 11-21-2005,
Presentation:
http://www.ctos.org/meeting/2005/presentations/Monday/am0800_Bauer457.ppt
SUN, L., Liang, C. et al, Discovery of
5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4-
dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a
novel tyrosine kinase inhibitor targeting vascular endothelial and
platelet-derived growth factor receptor tyrosine kinase:
J.Med.Chem., Vol. 46, Iss. 7, 3-27-2003, Pages: 1116-1119,
Abstract:
http://pubs.acs.org/cgi-bin/abstract.cgi/jmcmar/2003/46/i07/abs/jm0204183.html
PDF:
http://pubs.acs.org/subscribe/journals/jmcmar/suppinfo/jm0204183/jm0204183_s.pdf
PubMed: PM:12646019
O'HARE, Thomas, Walters, Denise K. et al, In vitro
Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against
Clinically Relevant Imatinib-Resistant Abl Kinase Domain Mutants:
Cancer Research, Vol. 65, Iss. 11, 6-1-2005, Pages:
4500-4505,
Abstract:
http://cancerres.aacrjournals.org/cgi/content/abstract/65/11/4500
PubMed: PM:15930265
SAMBOL, Elliot B., Motwani, Monica et al,
Flavopiridol is an active agent in the treatment of
gastrointestinal stromal tumor (GIST) cells with relative
resistance to imatinib mesylate via both transcriptional
suppression and inhibition of autophosphorylation of KIT (Abstract
# 1710): Proc Amer Assoc Cancer Res, Vol. 46, Iss. 2005,
4-17-2005,
Abstract:
BORDEN, E., Jacobs, B. et al, Induction of TRAIL
and XAF-1 and inhibition of p-Akt and c-Kit expression by
interferons (IFNs) is associated with apoptosis in GIST cells.
(Poster: Abstract # 9027): Proc Am Soc Clin Oncol, Vol. 22, Iss.
2004, 6-6-2004,
2004 ASCO
abstract and presentation
PLAAT, B. E., Hollema, H. et al, Soft tissue
leiomyosarcomas and malignant gastrointestinal stromal tumors:
differences in clinical outcome and expression of multidrug
resistance proteins: J.Clin.Oncol., Vol. 18, Iss. 18, 9-15-2000,
Pages: 3211-3220,
Abstract: http://www.jco.org/cgi/content/abstract/18/18/3211
Full Text: http://www.jco.org/cgi/content/full/18/18/3211
PubMed: PM:10986053
BURGER, H., vanTol, H. et al, Chronic Imatinib
Mesylate Exposure Leads to Reduced Intracellular Drug Accumulation
by Induction of the ABCG2 (BCRP) and ABCB1 (MDR1) Drug Transport
Pumps.: Cancer Biol & Therapy, Vol. 4, Iss. 7, 2005, Pages:
747-752,
Abstract:
http://www.landesbioscience.com/journals/cbt/abstract.php?id=1826
PubMed: PM:15970668
CROSSMAN, Lucy C., Druker, Brian J. et al, hOCT 1
and resistance to imatinib: Blood, Vol. 106, Iss. 3, 8-1-2005,
Pages: 1133-1134,
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DAI, HaiQing, Marbach, Peter et al, Distribution of
STI-571 to the Brain Is Limited by P-Glycoprotein-Mediated Efflux:
Journal of Pharmacology And Experimental Therapeutics, Vol. 304,
Iss. 3, 3-1-2003, Pages: 1085-1092,
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PDF: http://jpet.aspetjournals.org/cgi/reprint/304/3/1085
Full Text: http://jpet.aspetjournals.org/cgi/content/full/304/3/1085
PubMed: PM:12604685
FERRAO, Petranel T., Frost, Michelle J. et al,
Overexpression of P-glycoprotein in K562 cells does not confer
resistance to the growth inhibitory effects of imatinib (STI571) in
vitro: Blood, Vol. 102, Iss. 13, 12-15-2003, Pages:
4499-4503,
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PDF: http://www.bloodjournal.org/cgi/reprint/102/13/4499
Full Text: http://www.bloodjournal.org/cgi/content/full/102/13/4499
PubMed: PM:12881321
MAHON, Francois Xavier, Belloc, Francis et al, MDR1
gene overexpression confers resistance to imatinib mesylate in
leukemia cell line models: Blood, Vol. 101, Iss. 6, 3-15-2003,
Pages: 2368-2373,
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PDF: http://www.bloodjournal.org/cgi/content/full/101/6/2368
Full Text: http://www.bloodjournal.org/cgi/content/full/101/6/2368
PubMed: PM:12609962
THOMAS, J., Wang, L. et al, Active transport of
imatinib into and out of cells: implications for drug resistance:
Blood, Vol. 104, Iss. 12, 12-12-0005, Pages: 3739-3745,
PDF: http://www.bloodjournal.org/cgi/reprint/104/12/3739
PubMed: PM:15315971
BURGER, H., vanTol, H. et al, Chronic Imatinib
Mesylate Exposure Leads to Reduced Intracellular Drug
Accumulation by Induction of the ABCG2 (BCRP) and ABCB1 (MDR1) Drug
Transport
Pumps.: Cancer Biol & Therapy, Vol. 4, Iss. 7, 2005, Pages:
747-752,
Abstract:
http://www.landesbioscience.com/journals/cbt/abstract.php?id=1826
PubMed: PM:15970668
PRENEN, H, de Bruijn E. et al, Cellular Uptake
of the Tyrosine Kinase Inhibitors Imatinib and AMN107 in
Gastrointestinal Stromal Tumor Cell Lines.
http://content.karger.com/ProdukteDB/produkte.asp?Aktion=ShowAbstract&ArtikelNr=91943&ProduktNr=224274&Ausgabe=231729
to top
DAI, HaiQing, Marbach, Peter et al, Distribution of
STI-571 to the Brain Is Limited by P-Glycoprotein-Mediated Efflux:
Journal of Pharmacology And Experimental Therapeutics, Vol. 304,
Iss. 3, 3-1-2003, Pages: 1085-1092,
Abstract: http://jpet.aspetjournals.org/cgi/content/abstract/304/3/1085
PDF: http://jpet.aspetjournals.org/cgi/reprint/304/3/1085
Full Text: http://jpet.aspetjournals.org/cgi/content/full/304/3/1085
PubMed: PM:12604685
JUDSON, Ian, Ma, Peiming et al, Imatinib
pharmacokinetics in patients with gastrointestinal stromal tumour:
a retrospective population pharmacokinetic study over time. EORTC
Soft Tissue and Bone Sarcoma Group: Cancer Chemotherapy and
Pharmacology, Vol. 55, Iss. 4, 2005, Pages: 379-386,
Abstract:
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PubMed: PM:15592836
KHAN, A., Efficacy of Imatinib Mesylate in
Metastatic GIST to the Brain (Poster: Abstract # 9050): Proc Am Soc
Clin Oncol, Iss. 2005, 5-14-2005,
2005 ASCO
Abstract
BURGER, H., vanTol, H. et al, Chronic Imatinib
Mesylate Exposure Leads to Reduced Intracellular Drug Accumulation
by Induction of the ABCG2 (BCRP) and ABCB1 (MDR1) Drug
Transport
Pumps.: Cancer Biol & Therapy, Vol. 4, Iss. 7, 2005, Pages:
747-752,
Abstract:
http://www.landesbioscience.com/journals/cbt/abstract.php?id=1826
PubMed: PM:15970668
GURNEY, H., Wong, M. et al, Imatinib elimination:
Characterization by in vivo testing of phenotype and genotype.(Oral
Presentation: Abstract # 775): Proc Am Soc Clin Oncol, Vol. 22,
Iss. 2003, 6-1-2003, Pages: 193,
2003 ASCO
Abstract and presentation:
TONG, Ricky T., Winkler, Frank et al, Vascular
normalization by VEGFR2 blockade improves drug penetration and
radiation response in two tumor models (Abstract # 6135): Proc Amer
Assoc Cancer Res, Vol. 46, Iss. 2005, 4-20-2005,
Abstract:
RUBIN, Brian P., Antonescu, Cristina R. et al, A
Knock-In Mouse Model of Gastrointestinal Stromal Tumor Harboring
Kit K641E: Cancer Research, Vol. 65, Iss. 15, 8-1-2005, Pages:
6631-6639,
Abstract:
http://cancerres.aacrjournals.org/cgi/content/abstract/65/15/6631
PubMed: PM:16061643
Drugs
ROSEN, L., Kurzrock, R. et al, Safety and
pharmacokinetics of AMG 706 in patients with advanced solid tumors
(Oral Presentation: Abstract # 3013): Proc Am Soc Clin Oncol, Iss.
2005, 5-14-2005,
2005 ASCO
Abstract and presentation
O'HARE, Thomas, Walters, Denise K. et al, In vitro
Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against
Clinically Relevant Imatinib-Resistant Abl Kinase Domain Mutants:
Cancer Research, Vol. 65, Iss. 11, 6-1-2005, Pages:
4500-4505,
Abstract:
http://cancerres.aacrjournals.org/cgi/content/abstract/65/11/4500
PubMed: PM:15930265
GOLEMOVIC, Mirna, Verstovsek, Srdan et al, AMN107,
a Novel Aminopyrimidine Inhibitor of Bcr-Abl, Has In vitro Activity
against Imatinib-Resistant Chronic Myeloid Leukemia: Clinical
Cancer Research, Vol. 11, Iss. 13, 7-1-2005, Pages:
4941-4947,
Abstract:
http://clincancerres.aacrjournals.org/cgi/content/abstract/11/13/4941
PubMed: PM:16000593
PRENEN, H, de Bruijn E. et al, Cellular Uptake
of the Tyrosine Kinase Inhibitors Imatinib and AMN107 in
Gastrointestinal Stromal Tumor Cell Lines.
http://content.karger.com/ProdukteDB/produkte.asp?Aktion=ShowAbstract&ArtikelNr=91943&ProduktNr=224274&Ausgabe=231729
AHMAD, Tanya and Eisen, Tim, Kinase Inhibition with
BAY 43-9006 in Renal Cell Carcinoma: Clinical Cancer Research, Vol.
10, Iss. 18, 9-15-2004, Pages: 6388S-66392,
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WILHELM, Scott M., Carter, Christopher et al, BAY
43-9006 Exhibits Broad Spectrum Oral Antitumor Activity and Targets
the RAF/MEK/ERK Pathway and Receptor Tyrosine Kinases Involved in
Tumor Progression and Angiogenesis
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7099-7109,
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Full Text:
PubMed: PM:15466206
O'HARE, Thomas, Walters, Denise K. et al, In vitro
Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against
Clinically Relevant Imatinib-Resistant Abl Kinase Domain Mutants:
Cancer Research, Vol. 65, Iss. 11, 6-1-2005, Pages:
4500-4505,
Abstract:
PubMed: PM:15930265
SCHITTENHELM, Marcus M., Shiraga, Sharon et al,
Dasatinib (BMS-354825), a Dual SRC/ABL Kinase Inhibitor, Inhibits
the Kinase Activity of Wild-Type, Juxtamembrane, and Activation
Loop Mutant KIT Isoforms Associated with Human Malignancies
2: Cancer Research, Vol. 66, Iss. 1, 1-1-2006, Pages:
473-481,
Abstract: http://cancerres.aacrjournals.org/cgi/content/abstract/66/1/473
PubMed: PM:16397263
Gleevec (imatinib mesylate) Tablets Rx Only
Prescribing Information: Novartis, 2005,
PDF Link:
http://www.pharma.us.novartis.com/product/pi/pdf/gleevec_tabs.pdf
DEMETRI, G. D., von, Mehren M. et al, Efficacy and
safety of imatinib mesylate in advanced gastrointestinal stromal
tumors: N.Engl.J.Med., Vol. 347, Iss. 7, 8-15-2002, Pages:
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NAGAR, B., Bornmann, W. G. et al, Crystal
structures of the kinase domain of c-Abl in complex with the small
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PubMed: PM:12154025
DEMATTEO, R. P., Antonescu, C. R. et al, Adjuvant
imatinib mesylate in patients with primary high risk
gastrointestinal stromal tumor (GIST) following complete resection:
Safety results from the U.S. Intergroup Phase II trial ACOSOG Z9000
(Oral Presentation: Abstract # 9009): Proc Am Soc Clin Oncol, Iss.
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2005 ASCO
Abstract and presentation
GRONCHI, Alessandro, Fiore, Marco et al, Advanced
Gastro-Intestinal Stromal Tumor: Molecular, Pathological and
Clinical Pattern in Post-Imatinib Surgery (Oral Presentation:
Abstract # 399): 11-20-2005,
Presentation:
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KIKUCHI, Saturo, Muroi, Kazuo et al, Severe
Hepatitis and Complete Molecular Response Caused by Imatinib
Mesylate: Possible Association of Its Serum Concentration with
Clinical Outcomes: Leukemia & Lymphoma, Vol. 45, Iss. 11, 2004,
Pages: 2349-2351,
Abstract:
http://taylorandfrancis.metapress.com/link.asp?id=x8pg80mlha4gaw2b
PubMed: PM:15512829
PAUWELS, P., diec-Rychter, M. et al, Changing
phenotype of gastrointestinal stromal tumours under imatinib
mesylate treatment: a potential diagnostic pitfall: Histopathology,
Vol. 47, Iss. 1, 2005, Pages: 41-47,
Abstract:
http://www.blackwell-synergy.com/doi/abs/10.1111/j.1365-2559.2005.02179.x
PubMed: PM:15982322
SCHERZER, N. J., Barkett, P. et al, Diseaes
Progression in Patients with Metastatic Gastrointestinal Stromal
Tumor (GIST) Receiving Gleevec (imatinib): The Effect of Drug
Dosage (Oral Presentation: Abstract # 227): 11-12-2004,
Presentation:
http://www.ctos.org/meeting/2004/presentations/friday/scherzer.ppt
TARN, Chi and Godwin, Andrew K., Glucose uptake is
altered in gastrointestinal stromal tumors in Response to imatinib
mesylate therapy via phospho-inositol-3 kinase (Board #1): Proc
Amer Assoc Cancer Res, Vol. 46, Iss. 2005, 4-19-2005,
Abstract:
TRENT, J. C., Choi, H. et al, Apoptotic and
anti-vascular activity of imatinib in GIST patients (Oral
Presentation: Abstract # 9001): Proc Am Soc Clin Oncol, Iss. 2005,
5-14-2005,
2005 ASCO
Abstract and presentation
BLACKSTEIN, M. E., Rankin, C. et al, Clinical
benefit of Imatinib in patients (pts) with metastatic
Gastrointestinal Stromal Tumors (GIST) negative for the expression
of CD117 in the S0033 trial (Oral Presentation: Abstract # 9010):
Proc Am Soc Clin Oncol, Iss. 2005, 5-14-2005,
ASCO 2005
Abstract and presentation
BLANKE, Charles D., Developmental Therapeutics:
Molecular Therapeutics (Oral Presentation: No Abstract): Proc Am
Soc Clin Oncol, 6-6-2004,
2004 ASCO
Presentation:
BLANKE, Charles., Joensuu, H. et al, Long-term
follow up of advanced gastrointestinal stromal tumor (GIST)
patients treated with imatinib mesylate. (Oral Presentation:
Abstract # 2): 1-22-2004,
2004 ASCO
Abstract and presentation
HEINRICH, M. C., Corless, C. L. et al, PDGFRA and
KIT mutations correlate with the clinical responses to imatinib
mesylate in patients with advanced gastrointestinal stromal tumors
(GIST) (Oral Presentation: Abstract # 3274): Proc Am Soc Clin
Oncol, Vol. 22, Iss. 2003, 6-1-2003, Pages: 815,
2003 ASCO
Abstract and presentation
JUDSON, Ian, Ma, Peiming et al, Imatinib
pharmacokinetics in patients with gastrointestinal stromal tumour:
a retrospective population pharmacokinetic study over time. EORTC
Soft Tissue and Bone Sarcoma Group: Cancer Chemotherapy and
Pharmacology, Vol. 55, Iss. 4, 2005, Pages: 379-386,
Abstract:
http://springerlink.com/openurl.asp?genre=article&id=doi:10.1007/s00280-004-0876-0
PubMed: PM:15592836
KANTARJIAN, Hagop, Talpaz, Moshe et al, High-dose
imatinib mesylate therapy in newly diagnosed Philadelphia
chromosome-positive chronic phase chronic myeloid leukemia: Blood,
Vol. 103, Iss. 8, 4-15-2004, Pages: 2873-2878,
Abstract: http://www.bloodjournal.org/cgi/content/abstract/103/8/2873
PDF: http://www.bloodjournal.org/cgi/reprint/103/8/2873
PubMed: PM:15070658
KHAN, A., Efficacy of Imatinib Mesylate in
Metastatic GIST to the Brain (Poster: Abstract # 9050): Proc Am Soc
Clin Oncol, Iss. 2005, 5-14-2005,
2005 ASCO
Abstract:
IPI-504 and other HSP90 inhibitors
BAUER, Sebastian and Yu, Lynn, Targeting HSP90 In
IM-Resistant GIST: KIT Degradation As A Broadly Relevant Salvage
Strategy. (Oral Presentation: Abstract # 457): 11-21-2005,
Presentation:
http://www.ctos.org/meeting/2005/presentations/Monday/am0800_Bauer457.ppt
TONG, Jeffrey K., Sydor, Jens R. et al, Anti-tumor
activity of a novel, water soluble Hsp90 inhibitor IPI-504 in
multiple myeloma (Abstract # 6160): Proc Amer Assoc Cancer Res,
Vol. 46, Iss. 2005, 4-20-2005,
Abstract:
BULL, Elizabeth E. A., Dote, Hideaki et al,
Enhanced Tumor Cell Radiosensitivity and Abrogation of G2 and S
Phase Arrest by the Hsp90 Inhibitor
17-(Dimethylaminoethylamino)-17-demethoxygeldanamycin: Clinical
Cancer Research, Vol. 10, Iss. 23, 12-1-2004, Pages:
8077-8084,
Abstract:
PDF:
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PubMed: PM:15585643
KAUR, Gurmeet, Belotti, Dorina et al,
Antiangiogenic Properties of
17-(Dimethylaminoethylamino)-17-Demethoxygeldanamycin: An Orally
Bioavailable Heat Shock Protein 90 Modulator
11: Clinical Cancer Research, Vol. 10, Iss. 14, 7-15-2004, Pages:
4813-4821,
Abstract:
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MIMNAUGH, Edward G., Xu, Wanping et al,
Simultaneous inhibition of hsp 90 and the proteasome promotes
protein ubiquitination, causes endoplasmic reticulum-derived
cytosolic vacuolization, and enhances antitumor activity
9: Molecular Cancer Therapeutics, Vol. 3, Iss. 5, 5-1-2004, Pages:
551-566,
Abstract:
PDF:
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PubMed: PM:15141013
VILENCHIK, Maria, Solit, David et al, Targeting
Wide-Range Oncogenic Transformation via PU24FCl, a Specific
Inhibitor of Tumor Hsp90
5: Chemistry & Biology, Vol. 11, Iss. 6, 2004, Pages:
787-797,
Full Text:
PubMed: PM:15217612
DEBIEC-RYCHTER, Maria, Cools, Jan et al, Mechanisms
of resistance to imatinib mesylate in gastrointestinal stromal
tumors and activity of the PKC412 inhibitor against
imatinib-resistant mutants: Gastroenterology, Vol. 128, Iss. 2,
2005, Pages: 270-279,
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GROWNEY, Joseph D., Clark, Jennifer J. et al,
Activation mutations of human c-KIT resistant to imatinib mesylate
are sensitive to the tyrosine kinase inhibitor PKC412: Blood, Vol.
106, Iss. 2, 7-15-2005, Pages: 721-724,
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mesylate (IM) in patients (pts) with gastrointestinal stromal tumor
(GIST) refractory to IM. (Poster Discussion: Abstract # 3016): Proc
Am Soc Clin Oncol, Iss. 2005, 5-15-2005,
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GEORGE, Prince, Bali, Purva et al, Cotreatment with
17-Allylamino-Demethoxygeldanamycin and FLT-3 Kinase Inhibitor
PKC412 Is Highly Effective against Human Acute Myelogenous Leukemia
Cells with Mutant FLT-3
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RAD001 and other mTOR inhibitors
VAN OOSTEROM, A., Reichardt, J. et al, A phase I/II
trial of the oral mTOR-inhibitor Everolimus (E) and Imatinib
Mesylate (IM) in patients (pts) with gastrointestinal stromal tumor
(GIST) refractory to IM: Study update (Poster: Abstract # 9033):
Proc Am Soc Clin Oncol, 5-14-2005,
2005 ASCO
Abstract and presentation
VAN OOSTEROM, A. T.,