drug · small molecule

GLEEVEC

updated 3mo ago

by $NVS NOVARTIS AG🔗 ChEMBL

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Small molecule drug with a maximum clinical stage of Approval (across all indications), with an approval for chronic myelogenous leukemia and 55 investigational indications.

targets

Bcr/Abl fusion proteinMast/stem cell growth factor receptor KitPlatelet-derived growth factor receptor betaTyrosine-protein kinase ABL1

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Trials studying GLEEVEC

phase2KQB198 in Combination With Imatinib in Participants With Advanced/Metastatic GIST in 1st Line Setting (SynerGIST-1st Line)recruitingn=46
phase4Study to Allow Access to Imatinib for Patients Who Are on Imatinib Treatment in a Novartis-sponsored Study and Are Benefiting From the Treatment as Judged by the Investigatorcompletedn=250
phase1A Study of Ziftomenib in Combination With Imatinib in Patients With Advanced Gastrointestinal Stromal Tumors (GIST)recruitingn=157
phase2Efficacy and Safety of Nilotinib in Patients With a Chronic Disease of the Graft Against the Hostcompletedn=65
phase1A Dose Calibration Study Comparing IkT-001Pro to Imatinib Mesylate 400mgcompletedn=64
phase2Imatinib Mesylate in Combination With Pembrolizumab in Patients With Melanomaunknownn=22

News(2)

How Reimagined Research Endeavors Intersect With Dignified End-of-Life Care: With D. Ross Camidge, MD, PhD; and Charles D. Blanke, MD, FACP, FASCO
Drs Camidge and Blanke discuss Dr Blanke's career path from pioneering targeted cancer therapies to becoming a leading advocate for medical aid in dying.
onclive · 3mo ago
Dr Mauro on the Significance of Alternative TKI Formulations in CML
Michael Mauro, MD, details the FDA approval of the small-molecule formulation of dasatinib and other alternate TKI formulations in chronic myeloid leukemia.
onclive · 3mo ago

brand

GLEEVEC

trade names

Gleevec, Glivec, Imatinib accord, Imatinib actavis, Imatinib koanaa, Imatinib medac

generic

IMATINIB MESYLATE

MOA

12.1 Mechanism of Action Imatinib mesylate is a protein-tyrosine kinase inhibitor that inhibits the BCR-ABL tyrosine kinase, the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in CML. Imatinib inhibits proliferation and induces apoptosis in BCR-ABL positive cell lines as well as fresh leukemic cells from Philadelphia chromosome positive chronic myeloid leukemia. Imatinib inhibits colony formation in assays using ex vivo peripheral blood and bone marrow samples from CML patients. In vivo, imatinib inhibits tumor growth of BCR-ABL transfected murine myeloid cells as well as BCR-ABL positive leukemia lines derived from CML patients in blast crisis. Imatinib is also an inhibitor of the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-Kit, and inhibits PDGF- and SCF-mediated cellular events. In vitro, imatinib inhibits proliferation and induces apoptosis in GIST cells, which express an activating c-Kit mutation.

indication

1 INDICATIONS AND USAGE Gleevec is a kinase inhibitor indicated for the treatment of: Newly diagnosed adult and pediatric patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase. ( 1.1 ) Patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in blast crisis (BC), accelerated phase (AP), or in chronic phase (CP) after failure of interferon-alpha therapy. ( 1.2 ) Adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL). ( 1.3 ) Pediatric patients with newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in combination with chemotherapy. ( 1.4 ) Adult patients with myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with platelet-derived growth factor receptor (PDGFR) gene re-arrangements. ( 1.5 ) Adult patients with aggressive systemic mastocytosis (ASM) without the D816V c-Kit mutation or with c-Kit mutational status unknown. ( 1.6 ) Adult patients with hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL) who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or fluorescence in situ hybridization [FISH] demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unknown. ( 1.7 ) Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans (DFSP). ( 1.8 ) Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST). ( 1.9 ) Adjuvant treatment of adult patients following resection of Kit (CD117) positive GIST. ( 1.10 ) 1.1 Newly Diagnosed Philadelphia Positive Chronic Myeloid Leukemia (Ph+ CML) Newly diagnosed adult and pediatric patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase. 1.2 Ph+ CML in Blast Crisis (BC), Accelerated Phase (AP) or Chronic Phase (CP) After Interf

Data sources

ClinicalTrials.gov · OpenTargets

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News(2)

How Reimagined Research Endeavors Intersect With Dignified End-of-Life Care: With D. Ross Camidge, MD, PhD; and Charles D. Blanke, MD, FACP, FASCO

Drs Camidge and Blanke discuss Dr Blanke's career path from pioneering targeted cancer therapies to becoming a leading advocate for medical aid in dying.

onclive · 3mo ago

Dr Mauro on the Significance of Alternative TKI Formulations in CML

Michael Mauro, MD, details the FDA approval of the small-molecule formulation of dasatinib and other alternate TKI formulations in chronic myeloid leukemia.

onclive · 3mo ago

GLEEVEC

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Trials studying GLEEVEC

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GLEEVEC

🐶 often sniffed alongside

targets

all catalysts(0)

Trials studying GLEEVEC

News(2)

Report a data issue

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