IMATINIB

Details

Stereochemistry	ACHIRAL
Molecular Formula	C29H31N7O
Molecular Weight	493.6027
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1CCN(CC2=CC=C(C=C2)C(=O)NC3=CC(NC4=NC(=CC=N4)C5=CC=CN=C5)=C(C)C=C3)CC1

InChI

InChIKey=KTUFNOKKBVMGRW-UHFFFAOYSA-N

InChI=1S/C29H31N7O/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34)

HIDE SMILES / InChI

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021588s047lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/mesh/2009892

Imatinib (GLEEVEC®) is a tyrosine kinase inhibitor and antineoplastic agent that inhibits the BCR-ABL tyrosine kinase, the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in chronic myeloid leukaemia (CML). It inhibits proliferation and induces apoptosis in BCR-ABL positive cell lines as well as fresh leukemic cells from Philadelphia chromosome positive CML. Imatinib (GLEEVEC®) inhibits colony formation in assays using ex vivo peripheral blood and bone marrow samples from CML patients. It 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 (GLEEVEC®) inhibits proliferation and induces apoptosis in gastrointestinal stromal tumor (GIST) cells, which express an activating c-kit mutation.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Bcr/Abl fusion protein 16 Target ID: CHEMBL2096618 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021588s047lbl.pdf	Inhibitor 8228	0.025 µM [IC50]
Platelet-derived growth factor receptor alpha 30 Target ID: CHEMBL2007 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021588s047lbl.pdf	Inhibitor 8228	0.1 µM [IC50]
Stem cell growth factor receptor 52 Target ID: CHEMBL1936 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021588s047lbl.pdf	Inhibitor 8228	0.1 µM [IC50]
Platelet-derived growth factor receptor beta 55 Target ID: CHEMBL1913 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021588s047lbl.pdf	Inhibitor 8228	39.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Philadelphia chromosome positive chronic myeloid leukemia 3 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021588s047lbl.pdf	Primary	Approved 8360	GLEEVEC Approved Use 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 PDGFR (platelet-derived growth factor receptor) 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 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 in chronic phase. 1.2 Ph+ CML in Blast Crisis (BC), Accelerated Phase (AP) or Chronic Phase (CP) After Interferon-alpha (IFN) Therapy Patients with Philadelphia chromosome positive chronic myeloid leukemia in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy. 1.3 Adult patients with Ph+ Acute Lymphoblastic Leukemia (ALL) Adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia. 1.4 Pediatric patients with Ph+ Acute Lymphoblastic Leukemia (ALL) Pediatric patients with newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in combination with chemotherapy. 1.5 Myelodysplastic/Myeloproliferative Diseases (MDS/MPD) Adult patients with myelodysplastic/myeloproliferative diseases associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements. 1.6 Aggressive Systemic Mastocytosis (ASM) Adult patients with aggressive systemic mastocytosis without the D816V c-Kit mutation or with c-Kit mutational status unknown. 1.7 Hypereosinophilic Syndrome (HES) and/or Chronic Eosinophilic Leukemia (CEL) Adult patients with hypereosinophilic syndrome and/or chronic eosinophilic leukemia who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or FISH demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unknown. 1.8 Dermatofibrosarcoma Protuberans (DFSP) Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans. 1.9 Kit+ Gastrointestinal Stromal Tumors (GIST) Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors. 1.10 Adjuvant Treatment of GIST Adjuvant treatment of adult patients following complete gross resection of Kit (CD117) positive GIST. Launch Date 9.8945283E11
Philadelphia chromosome positive acute lymphoblastic leukemia 7 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021588s047lbl.pdf	Primary	Approved 8360	GLEEVEC Approved Use 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 PDGFR (platelet-derived growth factor receptor) 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 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 in chronic phase. 1.2 Ph+ CML in Blast Crisis (BC), Accelerated Phase (AP) or Chronic Phase (CP) After Interferon-alpha (IFN) Therapy Patients with Philadelphia chromosome positive chronic myeloid leukemia in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy. 1.3 Adult patients with Ph+ Acute Lymphoblastic Leukemia (ALL) Adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia. 1.4 Pediatric patients with Ph+ Acute Lymphoblastic Leukemia (ALL) Pediatric patients with newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in combination with chemotherapy. 1.5 Myelodysplastic/Myeloproliferative Diseases (MDS/MPD) Adult patients with myelodysplastic/myeloproliferative diseases associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements. 1.6 Aggressive Systemic Mastocytosis (ASM) Adult patients with aggressive systemic mastocytosis without the D816V c-Kit mutation or with c-Kit mutational status unknown. 1.7 Hypereosinophilic Syndrome (HES) and/or Chronic Eosinophilic Leukemia (CEL) Adult patients with hypereosinophilic syndrome and/or chronic eosinophilic leukemia who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or FISH demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unknown. 1.8 Dermatofibrosarcoma Protuberans (DFSP) Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans. 1.9 Kit+ Gastrointestinal Stromal Tumors (GIST) Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors. 1.10 Adjuvant Treatment of GIST Adjuvant treatment of adult patients following complete gross resection of Kit (CD117) positive GIST. Launch Date 9.8945283E11
Myelodysplastic/myeloproliferative diseases associated with PDGFR 3 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021588s047lbl.pdf	Primary	Approved 8360	GLEEVEC Approved Use 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 PDGFR (platelet-derived growth factor receptor) 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 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 in chronic phase. 1.2 Ph+ CML in Blast Crisis (BC), Accelerated Phase (AP) or Chronic Phase (CP) After Interferon-alpha (IFN) Therapy Patients with Philadelphia chromosome positive chronic myeloid leukemia in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy. 1.3 Adult patients with Ph+ Acute Lymphoblastic Leukemia (ALL) Adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia. 1.4 Pediatric patients with Ph+ Acute Lymphoblastic Leukemia (ALL) Pediatric patients with newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in combination with chemotherapy. 1.5 Myelodysplastic/Myeloproliferative Diseases (MDS/MPD) Adult patients with myelodysplastic/myeloproliferative diseases associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements. 1.6 Aggressive Systemic Mastocytosis (ASM) Adult patients with aggressive systemic mastocytosis without the D816V c-Kit mutation or with c-Kit mutational status unknown. 1.7 Hypereosinophilic Syndrome (HES) and/or Chronic Eosinophilic Leukemia (CEL) Adult patients with hypereosinophilic syndrome and/or chronic eosinophilic leukemia who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or FISH demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unknown. 1.8 Dermatofibrosarcoma Protuberans (DFSP) Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans. 1.9 Kit+ Gastrointestinal Stromal Tumors (GIST) Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors. 1.10 Adjuvant Treatment of GIST Adjuvant treatment of adult patients following complete gross resection of Kit (CD117) positive GIST. Launch Date 9.8945283E11
Aggressive systemic mastocytosis (D816V c-Kit mutation status negative/c-Kit mutational status unknown) 3 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021588s047lbl.pdf	Primary	Approved 8360	GLEEVEC Approved Use 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 PDGFR (platelet-derived growth factor receptor) 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 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 in chronic phase. 1.2 Ph+ CML in Blast Crisis (BC), Accelerated Phase (AP) or Chronic Phase (CP) After Interferon-alpha (IFN) Therapy Patients with Philadelphia chromosome positive chronic myeloid leukemia in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy. 1.3 Adult patients with Ph+ Acute Lymphoblastic Leukemia (ALL) Adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia. 1.4 Pediatric patients with Ph+ Acute Lymphoblastic Leukemia (ALL) Pediatric patients with newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in combination with chemotherapy. 1.5 Myelodysplastic/Myeloproliferative Diseases (MDS/MPD) Adult patients with myelodysplastic/myeloproliferative diseases associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements. 1.6 Aggressive Systemic Mastocytosis (ASM) Adult patients with aggressive systemic mastocytosis without the D816V c-Kit mutation or with c-Kit mutational status unknown. 1.7 Hypereosinophilic Syndrome (HES) and/or Chronic Eosinophilic Leukemia (CEL) Adult patients with hypereosinophilic syndrome and/or chronic eosinophilic leukemia who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or FISH demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unknown. 1.8 Dermatofibrosarcoma Protuberans (DFSP) Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans. 1.9 Kit+ Gastrointestinal Stromal Tumors (GIST) Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors. 1.10 Adjuvant Treatment of GIST Adjuvant treatment of adult patients following complete gross resection of Kit (CD117) positive GIST. Launch Date 9.8945283E11
Hypereosinophilic syndrome 3 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021588s047lbl.pdf	Primary	Approved 8360	GLEEVEC Approved Use 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 PDGFR (platelet-derived growth factor receptor) 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 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 in chronic phase. 1.2 Ph+ CML in Blast Crisis (BC), Accelerated Phase (AP) or Chronic Phase (CP) After Interferon-alpha (IFN) Therapy Patients with Philadelphia chromosome positive chronic myeloid leukemia in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy. 1.3 Adult patients with Ph+ Acute Lymphoblastic Leukemia (ALL) Adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia. 1.4 Pediatric patients with Ph+ Acute Lymphoblastic Leukemia (ALL) Pediatric patients with newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in combination with chemotherapy. 1.5 Myelodysplastic/Myeloproliferative Diseases (MDS/MPD) Adult patients with myelodysplastic/myeloproliferative diseases associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements. 1.6 Aggressive Systemic Mastocytosis (ASM) Adult patients with aggressive systemic mastocytosis without the D816V c-Kit mutation or with c-Kit mutational status unknown. 1.7 Hypereosinophilic Syndrome (HES) and/or Chronic Eosinophilic Leukemia (CEL) Adult patients with hypereosinophilic syndrome and/or chronic eosinophilic leukemia who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or FISH demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unknown. 1.8 Dermatofibrosarcoma Protuberans (DFSP) Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans. 1.9 Kit+ Gastrointestinal Stromal Tumors (GIST) Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors. 1.10 Adjuvant Treatment of GIST Adjuvant treatment of adult patients following complete gross resection of Kit (CD117) positive GIST. Launch Date 9.8945283E11

C_max

Value	Dose	Analyte	Population
1.74 mg/L EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/15796158	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	IMATINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
4478 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	500 mg 2 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1907.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3508.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	600 mg 1 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1907.5 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/16122278	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.82 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.75 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	500 mg 2 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.71 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CGP-74588 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.18 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	500 mg 2 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CGP-74588 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
19.9 mg × h/L EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/15796158	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	IMATINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
174.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	500 mg 2 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
38.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
89.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	600 mg 1 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
38.8 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/16122278	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
63.7 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
97.3 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	500 mg 2 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
10.1 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CGP-74588 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
19.7 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	500 mg 2 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CGP-74588 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
15.8 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/15796158	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	IMATINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
17 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	500 mg 2 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
14.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
15.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	600 mg 1 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
83.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
23.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	500 mg 2 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
50.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	600 mg 2 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CGP-74588 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
10.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/18359865	500 mg 2 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CGP-74588 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Analyte	Population
4% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	500 mg 2 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	400 mg 1 times / day steady-state, oral dose: 400 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14990650	600 mg 1 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5% EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/16122278	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	IMATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
500 mg 2 times / day steady, oral MTD Dose: 500 mg, 2 times / day Route: oral Route: steady Dose: 500 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	unhealthy, 53.3 years (range: 29.8–69.9 years) n = 35 Health Status: unhealthy Condition: malignant glioma Age Group: 53.3 years (range: 29.8–69.9 years) Sex: M+F Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	Sources: https://pubmed.ncbi.nlm.nih.gov/18359865
400 mg 2 times / day steady, oral Dose: 400 mg, 2 times / day Route: oral Route: steady Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	unhealthy, 53.3 years (range: 29.8–69.9 years) n = 35 Health Status: unhealthy Condition: malignant glioma Age Group: 53.3 years (range: 29.8–69.9 years) Sex: M+F Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	DLT: Transaminases increased... Dose limiting toxicities: Transaminases increased (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/18359865
600 mg 2 times / day steady, oral Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	unhealthy, 53.3 years (range: 29.8–69.9 years) n = 35 Health Status: unhealthy Condition: malignant glioma Age Group: 53.3 years (range: 29.8–69.9 years) Sex: M+F Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	DLT: Neutropenia, Hypocalcemia... Dose limiting toxicities: Neutropenia (grade 3, 2 patients) Hypocalcemia (grade 4, 2 patients) Hypophosphatemia (grade 4, 2 patients) Hypokalemia (grade 3, 2 patients) Nausea (grade 3, 2 patients) Emesis (grade 3, 2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/18359865

AEs

AE	Significance	Dose	Population
Transaminases increased	grade 3, 1 patient DLT	400 mg 2 times / day steady, oral Dose: 400 mg, 2 times / day Route: oral Route: steady Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	unhealthy, 53.3 years (range: 29.8–69.9 years) n = 35 Health Status: unhealthy Condition: malignant glioma Age Group: 53.3 years (range: 29.8–69.9 years) Sex: M+F Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/18359865
Emesis	grade 3, 2 patients DLT	600 mg 2 times / day steady, oral Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	unhealthy, 53.3 years (range: 29.8–69.9 years) n = 35 Health Status: unhealthy Condition: malignant glioma Age Group: 53.3 years (range: 29.8–69.9 years) Sex: M+F Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/18359865
Hypokalemia	grade 3, 2 patients DLT	600 mg 2 times / day steady, oral Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	unhealthy, 53.3 years (range: 29.8–69.9 years) n = 35 Health Status: unhealthy Condition: malignant glioma Age Group: 53.3 years (range: 29.8–69.9 years) Sex: M+F Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/18359865
Nausea	grade 3, 2 patients DLT	600 mg 2 times / day steady, oral Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	unhealthy, 53.3 years (range: 29.8–69.9 years) n = 35 Health Status: unhealthy Condition: malignant glioma Age Group: 53.3 years (range: 29.8–69.9 years) Sex: M+F Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/18359865
Neutropenia	grade 3, 2 patients DLT	600 mg 2 times / day steady, oral Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	unhealthy, 53.3 years (range: 29.8–69.9 years) n = 35 Health Status: unhealthy Condition: malignant glioma Age Group: 53.3 years (range: 29.8–69.9 years) Sex: M+F Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/18359865
Hypocalcemia	grade 4, 2 patients DLT	600 mg 2 times / day steady, oral Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	unhealthy, 53.3 years (range: 29.8–69.9 years) n = 35 Health Status: unhealthy Condition: malignant glioma Age Group: 53.3 years (range: 29.8–69.9 years) Sex: M+F Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/18359865
Hypophosphatemia	grade 4, 2 patients DLT	600 mg 2 times / day steady, oral Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18359865	unhealthy, 53.3 years (range: 29.8–69.9 years) n = 35 Health Status: unhealthy Condition: malignant glioma Age Group: 53.3 years (range: 29.8–69.9 years) Sex: M+F Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/18359865

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709	substrate 1010 inhibitor 1752	substrate 1193 inhibitor 1837	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A4/5 273 CYP1A2 1509 CYP2A6 704 CYP2C19 1463 CYP2B6 799 CYP2E1 876 CYP4A9/11 37	CYP3A5 391 CYP1A2 1032 CYP2C8 688 CYP2C19 985

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP2B6 985	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	no
CYP2E1 964	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	no
CYP4A9/11 37	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	no
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	yes [IC50 120 uM]
CYP2A6 736	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	yes [IC50 230 uM]
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	yes [IC50 410 uM]
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	yes [Ki 27 uM]
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	yes [Ki 7.5 uM]
CYP3A4/5 330	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	yes [Ki 8 uM]	yes (co-administration study) Comment: imatinib increased cmax of simvastatin by 2x, auc by 3.5x Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1709	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	major	yes (co-administration study) Comment: ketoconazole increased cmax of imatinib by 26%, auc by 40% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf
CYP1A2 1032	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	minor
CYP2C19 985	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	minor
CYP2C8 688	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	minor
CYP2C9 1010	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	minor
CYP2D6 1193	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	minor
CYP3A5 391	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/21-335_Gleevec_biopharmr_P1.pdf	minor

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 Sources: https://pubmed.ncbi.nlm.nih.gov/23196655/

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:45783	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:45783
ChemicalBook	CB7370890	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB7370890
MolPort	MolPort-000-883-342	https://www.molport.com/shop/molecule-link/MolPort-000-883-342
Selleck Chemicals	Imatinib(STI571)	http://www.selleckchem.com/products/Imatinib(STI571).html
ZINC	ZINC000019632618	http://zinc15.docking.org/substances/ZINC000019632618
eMolecules	876446	https://www.emolecules.com/cgi-bin/more?vid=876446

PubMed

Title	Date	PubMed
Acute generalized exanthematous pustulosis associated with STI571 in a patient with chronic myeloid leukemia.	2001	11549802
Sarcoma.	2001	11524551
Effect of a selective Abl tyrosine kinase inhibitor, STI571, on in vitro growth of BCR-ABL-positive acute lymphoblastic leukemia cells.	2001 Apr	11368361
Recent advances in the molecular and cellular biology of chronic myeloid leukaemia: lessons to be learned from the laboratory.	2001 Apr	11328274
Leukemia cells fall on their swords.	2001 Apr	11286930
PDGF signal transduction inhibition ameliorates experimental mesangial proliferative glomerulonephritis.	2001 Apr	11260393
Comparison of effects of the tyrosine kinase inhibitors AG957, AG490, and STI571 on BCR-ABL--expressing cells, demonstrating synergy between AG490 and STI571.	2001 Apr 1	11264165
In vitro cytotoxic effects of a tyrosine kinase inhibitor STI571 in combination with commonly used antileukemic agents.	2001 Apr 1	11264164
ST1571, a tyrosine kinase inhibitor for the treatment of chronic myelogenous leukemia: validating the promise of molecularly targeted therapy.	2001 Aug	11587372
STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein: biological and clinical implications.	2001 Aug 16	11526490
Chronic myelogenous leukemia.	2001 Aug 22-29	11509034
Cutaneous reactions to STI571.	2001 Aug 23	11529225
Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification.	2001 Aug 3	11423618
Mechanisms of resistance imatinib (STI571) in preclinical models and in leukemia patients.	2001 Feb	11512149
Mechanisms of resistance to imatinib (STI571) and prospects for combination with conventional chemotherapeutic agents.	2001 Feb	11512148
Induction of apoptosis in chronic myelogenous leukemia cells through nuclear entrapment of BCR-ABL tyrosine kinase.	2001 Feb	11175855
PDGF receptor inhibition prevents cardiac allograft arteriosclerosis in cholesterol-fed rabbits.	2001 Feb-Mar	11266838
The biology and treatment of chronic myelogenous leukemia.	2001 Jan	11271979
Perspectives on the future of chronic myeloid leukemia treatment.	2001 Jul	11526600
Implications of imatinib mesylate for hematopoietic stem cell transplantation.	2001 Jul	11526599
Interferon-alfa-based treatment of chronic myeloid leukemia and implications of signal transduction inhibition.	2001 Jul	11526598
Molecular studies in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors.	2001 Jul	11526597
Signal transduction inhibition: results from phase I clinical trials in chronic myeloid leukemia.	2001 Jul	11526596
The role of Bcr-Abl in chronic myeloid leukemia and stem cell biology.	2001 Jul	11526595
Implications of signal transduction inhibition for the treatment of chronic myeloid leukemia.	2001 Jul	11526594
Cancer treatment. New drugs, new hope.	2001 Jul	11511447
Clinical trials referral resource. ST1571.	2001 Jul	11499689
Chronic myelogenous leukaemia--new therapeutic principles.	2001 Jul	11454136
Approval heralds new generation of kinase inhibitors?	2001 Jul	11433254
Anti-cancer drug success emerges from molecular biology origins.	2001 Jul	11431023
After 30 years of laboratory work, a quick approval for STI571.	2001 Jul 4	11438558
STI571 revolution: can the newer targeted drugs measure up?	2001 Jul 4	11438556
Current treatment approaches for chronic myelogenous leukemia.	2001 Jul-Aug	11504279
ABL-specific tyrosine kinase inhibitor, STI571 in vitro, affects Ph-positive acute lymphoblastic leukemia and chronic myelogenous leukemia in blastic crisis.	2001 Jun	11417489
Quick success for cancer kinase treatment.	2001 Jun	11385473
Cancer research. Why some leukemia cells resist STI-571.	2001 Jun 22	11423629
Sensitivity to the abl inhibitor STI571 in fresh leukaemic cells obtained from chronic myelogenous leukaemia patients in different stages of disease.	2001 Mar	11298594
Synergistic activity of the new ABL-specific tyrosine kinase inhibitor STI571 and chemotherapeutic drugs on BCR-ABL-positive chronic myelogenous leukemia cells.	2001 Mar	11237055
Novel therapies for chronic myelogenous leukemia.	2001 May	11376866
STI571: a gene product-targeted therapy for leukemia.	2001 May	11296132
Tyrosine kinase inhibitor STI571 potentiates the pharmacologic activity of retinoic acid in acute promyelocytic leukemia cells: effects on the degradation of RARalpha and PML-RARalpha.	2001 May 15	11342454
Cancer's mechanics. Targeting errant cells.	2001 May 21	11383095
New hope for cancer.	2001 May 28	11393038
Progenitor cells from patients with advanced phase chronic myeloid leukaemia respond to STI571 in vitro and in vivo.	2001 Nov	11597734
[Chronic myelogenous leukemia].	2001 Sep	11579630
Treatment of leukemia relapse after allogeneic hematopoietic stem cell transplantation by donor lymphocyte infusion and STI-571.	2001 Sep	11532632
Inhibition of tyrosine kinase activity induces caspase-dependent apoptosis in anaplastic large cell lymphoma with NPM-ALK (p80) fusion protein.	2001 Sep	11532349
Cancer in the crosshairs.	2001 Sep	11524965
Roots of clinical resistance to STI-571 cancer therapy.	2001 Sep 21	11569495
Involvement of Jak2 tyrosine phosphorylation in Bcr-Abl transformation.	2001 Sep 27	11593427

Patents

Sample Use Guides

In Vivo Use Guide

The prescribed dose should be administered orally, with a meal and a large glass of water. Doses of 400 mg or 600 mg should be administered once daily, whereas a dose of 800 mg should be administered as 400 mg twice a day. Treatment may be continued as long as there is no evidence of progressive disease or unacceptable toxicity.

Route of Administration: Oral

In Vitro Use Guide

Imatinib (CGP 57148) was tested for growth inhibition of EGF-dependent BALB/MK cells, the H-ras-transformed T24 bladder carcinoma line, and IL-3-dependent growth of FDC-Pl cells. The compound showed only weak antiproliferative activity against these cell lines, with IC50 values of 12.7 uM, 9.4 uM, and 29.2 uM, respectively. However, when tested on v-abl-transformed PB-3c cells, incubation with CGP 57148 resulted in potent growth inhibition even in the presence of exogenous IL-3 (IC50 values, 0.11 uM without IL-3 and 0.9 uM with IL-3). Similar results were obtained using v-sis-transformed BALB/c 3T3 cells, which grow in response to autocrine PDGF production (IC50, 0.33 uM).

Name

Type

Language

IMATINIB

Official Name

English

Imatinib [WHO-DD]

Common Name

English

NSC-743414

Code

English

GLAMOX

Brand Name

English

NSC-759854

Code

English

IMATINIB [VANDF]

Common Name

English

IMATINIB [MI]

Common Name

English

imatinib [INN]

Common Name

English

BENZAMIDE, 4-((4-METHYL-1-PIPERAZINYL)METHYL)-N-(4-METHYL-3-((4-(3-PYRIDINYL)-2-PYRIMIDINYL)AMINOPHENYL)-

Common Name

English

IMATINIB [EMA EPAR]

Common Name

English

Classification Tree Code System Code

WHO-ATC

L01XE01