Identification

Name
Dasatinib
Accession Number
DB01254
Type
Small Molecule
Groups
Approved, Investigational
Description

Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML). The main targets of Dasatinib, are BCRABL, SRC, Ephrins and GFR.

Structure
Thumb
Synonyms
  • anh. dasatinib
  • Anhydrous dasatinib
  • BMS dasatinib
  • Dasatinib
  • Dasatinib (anh.)
  • dasatinib (anhydrous)
  • Dasatinib anhydrous
  • Dasatinibum
  • N-(2-CHLORO-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide
External IDs
BMS-354825
Product Ingredients
IngredientUNIICASInChI Key
Dasatinib monohydrateRBZ1571X5H863127-77-9XHXFZZNHDVTMLI-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SprycelTablet, film coated100 mgOralBristol Myers Squibb Pharma Eeig2006-11-20Not applicableEu
SprycelTablet100 mgOralBristol Myers Squibb2009-05-04Not applicableCanada
SprycelTablet20 mgOralBristol Myers Squibb2007-04-13Not applicableCanada
SprycelTablet100 mg/1OralE.R. Squibb & Sons, L.L.C.2008-05-30Not applicableUs
SprycelTablet, film coated50 mgOralBristol Myers Squibb Pharma Eeig2006-11-20Not applicableEu
SprycelTablet70 mg/1OralE.R. Squibb & Sons, L.L.C.2006-06-27Not applicableUs
SprycelTablet, film coated70 mgOralBristol Myers Squibb Pharma Eeig2006-11-20Not applicableEu
SprycelTablet, film coated70 mgOralBristol Myers Squibb Pharma Eeig2006-11-20Not applicableEu
SprycelTablet70 mg/1OralPhysicians Total Care, Inc.2007-02-12Not applicableUs
SprycelTablet140 mgOralBristol Myers Squibb2011-03-29Not applicableCanada
Categories
UNII
X78UG0A0RN
CAS number
302962-49-8
Weight
Average: 488.006
Monoisotopic: 487.155721508
Chemical Formula
C22H26ClN7O2S
InChI Key
ZBNZXTGUTAYRHI-UHFFFAOYSA-N
InChI
InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
IUPAC Name
N-(2-chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide
SMILES
CC1=NC(NC2=NC=C(S2)C(=O)NC2=C(C)C=CC=C2Cl)=CC(=N1)N1CCN(CCO)CC1

Pharmacology

Indication

For the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy.

Associated Conditions
Pharmacodynamics

Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor

Mechanism of action

Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.

TargetActionsOrganism
ATyrosine-protein kinase ABL1
multitarget
Human
AProto-oncogene tyrosine-protein kinase Src
multitarget
Human
AEphrin type-A receptor 2
antagonist
Human
ATyrosine-protein kinase Lck
multitarget
Human
ATyrosine-protein kinase Yes
inhibitor
Human
UMast/stem cell growth factor receptor Kit
antagonist
Human
UPlatelet-derived growth factor receptor beta
antagonist
Human
USignal transducer and activator of transcription 5B
inhibitor
Human
UAbelson tyrosine-protein kinase 2
multitarget
Human
UTyrosine-protein kinase Fyn
multitarget
Human
UTyrosine-protein kinase BTKNot AvailableHuman
UNuclear receptor subfamily 4 group A member 3Not AvailableHuman
UBreakpoint cluster region proteinNot AvailableHuman
UTyrosine-protein kinase CSKNot AvailableHuman
UEphrin type-A receptor 5Not AvailableHuman
UEphrin type-B receptor 4Not AvailableHuman
UTyrosine-protein kinase FgrNot AvailableHuman
UTyrosine-protein kinase FRKNot AvailableHuman
UHeat shock cognate 71 kDa proteinNot AvailableHuman
UTyrosine-protein kinase LynNot AvailableHuman
UMitogen-activated protein kinase kinase kinase MLTNot AvailableHuman
UMitogen-activated protein kinase 14Not AvailableHuman
UAmidophosphoribosyltransferaseNot AvailableHuman
Absorption
Not Available
Volume of distribution
  • 2505 L
Protein binding

96%

Metabolism

Dasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4

Route of elimination

Dasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4. Elimination is primarily via the feces.

Half life

The overall mean terminal half-life of dasatinib is 3-5 hours.

Clearance
Not Available
Toxicity

Acute overdose in animals was associated with cardiotoxicity.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Dasatinib Inhibition of BCR-ABLDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
AbciximabThe risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Abciximab.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Dasatinib.
AbirateroneThe serum concentration of Dasatinib can be increased when it is combined with Abiraterone.
AcenocoumarolThe risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Acenocoumarol.
AcetaminophenAcetaminophen may increase the hepatotoxic activities of Dasatinib.
AcetazolamideThe metabolism of Dasatinib can be decreased when combined with Acetazolamide.
Acetyl sulfisoxazoleThe metabolism of Dasatinib can be decreased when combined with Acetyl sulfisoxazole.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Dasatinib.
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Dasatinib.
Acetylsalicylic acidThe risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Acetylsalicylic acid.
Food Interactions
Not Available

References

Synthesis Reference
US6596746
General References
  1. Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC: 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor. J Med Chem. 2006 Nov 16;49(23):6819-32. [PubMed:17154512]
  2. Talpaz M, Shah NP, Kantarjian H, Donato N, Nicoll J, Paquette R, Cortes J, O'Brien S, Nicaise C, Bleickardt E, Blackwood-Chirchir MA, Iyer V, Chen TT, Huang F, Decillis AP, Sawyers CL: Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N Engl J Med. 2006 Jun 15;354(24):2531-41. [PubMed:16775234]
External Links
Human Metabolome Database
HMDB0015384
KEGG Drug
D03658
PubChem Compound
3062316
PubChem Substance
46505143
ChemSpider
2323020
BindingDB
13216
ChEBI
49375
ChEMBL
CHEMBL1421
Therapeutic Targets Database
DAP000004
PharmGKB
PA162372878
HET
1N1
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Dasatinib
ATC Codes
L01XE06 — Dasatinib
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
PDB Entries
2gqg / 2y6o / 2zva / 3g5d / 3k54 / 3lfa / 3oct / 3oht / 3qlg / 3sxr
show 9 more
FDA label
Download (237 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedBasic ScienceEndometrial Cancers1
0TerminatedBasic ScienceHepatic Metastases / Metastatic Colon Cancer / Mucinous Adenocarcinoma of the Colon / Mucinous Adenocarcinoma of the Rectum / Recurrent Colon Cancer / Recurrent Rectal Cancer / Signet Ring Adenocarcinoma of the Colon / Signet Ring Adenocarcinoma of the Rectum / Stage IV Rectal Cancer1
1Active Not RecruitingTreatmentAdvanced Cancers1
1Active Not RecruitingTreatmentB Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Childhood Acute Lymphoblastic Leukemia / Refractory Adult Acute Lymphoblastic Leukemia / Refractory Childhood Acute Lymphoblastic Leukemia1
1Active Not RecruitingTreatmentCancer, Advanced1
1Active Not RecruitingTreatmentChronic Myeloid Leukemia (CML)1
1Active Not RecruitingTreatmentDiffuse Intrinsic Pontine Glioma (DIPG) / High-Grade Gliomas1
1Active Not RecruitingTreatmentEndometrial Adenocarcinomas / Endometrial Adenosquamous Carcinoma / Endometrial Clear Cell Adenocarcinoma / Endometrial Mucinous Adenocarcinoma / Endometrial Serous Adenocarcinoma / Endometrial Squamous Cell Carcinoma / Endometrial Transitional Cell Carcinoma / Endometrial Undifferentiated Carcinoma / Endometrioid Adenocarcinoma / Recurrent Uterine Corpus Carcinoma / Stage III Uterine Corpus Cancer / Stage III Uterine Corpus Cancer AJCC v7 / Stage IIIA Uterine Corpus Cancer / Stage IIIA Uterine Corpus Cancer AJCC v7 / Stage IIIB Uterine Corpus Cancer / Stage IIIB Uterine Corpus Cancer AJCC v7 / Stage IIIC Uterine Corpus Cancer / Stage IIIC Uterine Corpus Cancer AJCC v7 / Stage IV Uterine Corpus Cancer / Stage IV Uterine Corpus Cancer AJCC v7 / Stage IVA Uterine Corpus Cancer / Stage IVA Uterine Corpus Cancer AJCC v7 / Stage IVB Uterine Corpus Cancer / Stage IVB Uterine Corpus Cancer AJCC v7 / Uterine Carcinosarcoma1
1Active Not RecruitingTreatmentLeukemias1
1Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Lung Cancers1
1Active Not RecruitingTreatmentMalignant Pleural Mesothelioma (MPM)1
1Active Not RecruitingTreatmentPancreatic Adenocarcinoma Metastatic / Recurrent Pancreatic Carcinoma / Stage III Pancreatic Cancer / Stage III Pancreatic Cancer AJCC v6 and v7 / Stage IV Pancreatic Cancer / Stage IV Pancreatic Cancer AJCC v6 and v71
1CompletedNot AvailablePharmacokinetic Study in Healthy Participants1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedSupportive CareHealthy Volunteers1
1CompletedTreatmentAccelerated Phase Chronic Myelogenous Leukemia / Blastic Phase Chronic Myelogenous Leukemia / Childhood Chronic Myelogenous Leukemia / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Meningeal Chronic Myelogenous Leukemia / Recurrent Childhood Acute Lymphoblastic Leukemia / Relapsing Chronic Myelogenous Leukemia / Unspecified Childhood Solid Tumor, Protocol Specific1
1CompletedTreatmentAcute Lymphoblastic Leukaemias (ALL) / Leukemias1
1CompletedTreatmentAcute Myelogenous Leukaemia (AML) / Myelodysplastic Syndrome1
1CompletedTreatmentAdult Acute Lymphoblastic Leukemia in Remission / Adult B Acute Lymphoblastic Leukemia / Adult Hepatocellular Carcinoma / Adult Nasal Type Extranodal NK/T-Cell Lymphoma / Adult Solid Neoplasm / Adult T Acute Lymphoblastic Leukemia / Advanced Adult Hepatocellular Carcinoma / Anaplastic Large Cell Lymphoma / Angioimmunoblastic T-Cell Lymphoma / Chronic Lymphocytic Leukaemia (CLL) / Chronic Lymphocytic Leukemia (CLL) - Refractory / Cutaneous B-Cell Non-Hodgkin Lymphoma / Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue / Hepatosplenic T-Cell Lymphoma / Intraocular Lymphoma / Localized Non-Resectable Adult Liver Carcinoma / Localized Resectable Adult Liver Carcinoma / Lymphomatous Involvement of Non-Cutaneous Extranodal Site / Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma / Nodal Marginal Zone Lymphoma / Progressive Hairy Cell Leukemia Initial Treatment / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Burkitt Lymphoma / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Adult Diffuse Mixed Cell Lymphoma / Recurrent Adult Diffuse Small Cleaved Cell Lymphoma / Recurrent Adult Grade III Lymphomatoid Granulomatosis / Recurrent Adult Hodgkin's Lymphoma / Recurrent Adult Immunoblastic Lymphoma / Recurrent Adult Liver Carcinoma / Recurrent Adult Lymphoblastic Lymphoma / Recurrent Adult T-Cell Leukemia/Lymphoma / Recurrent Cutaneous T-Cell Non-Hodgkin Lymphoma / Recurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Mantle Cell Lymphoma / Recurrent Marginal Zone Lymphoma / Recurrent Mycosis Fungoides and Sezary Syndrome / Recurrent Small Lymphocytic Lymphoma / Refractory Hairy Cell Leukemia / Small Intestinal Lymphoma / Splenic Marginal Zone Lymphoma / Stage II Small Lymphocytic Lymphoma / Stage III Adult Burkitt Lymphoma / Stage III Adult Diffuse Large Cell Lymphoma / Stage III Adult Diffuse Mixed Cell Lymphoma / Stage III Adult Diffuse Small Cleaved Cell Lymphoma / Stage III Adult Hodgkin Lymphoma / Stage III Adult Immunoblastic Lymphoma / Stage III Adult Lymphoblastic Lymphoma / Stage III Adult T-Cell Leukemia/Lymphoma / Stage III Chronic Lymphocytic Leukemia / Stage III Cutaneous T-Cell Non-Hodgkin Lymphoma / Stage III Grade 1 Follicular Lymphoma / Stage III Grade 2 Follicular Lymphoma / Stage III Grade 3 Follicular Lymphoma / Stage III Mantle Cell Lymphoma / Stage III Marginal Zone Lymphoma / Stage III Small Lymphocytic Lymphoma / Stage IIIA Mycosis Fungoides and Sezary Syndrome / Stage IIIB Mycosis Fungoides and Sezary Syndrome / Stage IV Adult Burkitt Lymphoma / Stage IV Adult Diffuse Large Cell Lymphoma / Stage IV Adult Diffuse Mixed Cell Lymphoma / Stage IV Adult Diffuse Small Cleaved Cell Lymphoma / Stage IV Adult Hodgkin Lymphoma / Stage IV Adult Immunoblastic Lymphoma / Stage IV Adult Lymphoblastic Lymphoma / Stage IV Adult T-Cell Leukemia/Lymphoma / Stage IV Chronic Lymphocytic Leukemia / Stage IV Cutaneous T-Cell Non-Hodgkin Lymphoma / Stage IV Grade 1 Follicular Lymphoma / Stage IV Grade 2 Follicular Lymphoma / Stage IV Grade 3 Follicular Lymphoma / Stage IV Mantle Cell Lymphoma / Stage IV Marginal Zone Lymphoma / Stage IV Small Lymphocytic Lymphoma / Stage IVA Mycosis Fungoides and Sezary Syndrome / Stage IVB Mycosis Fungoides and Sezary Syndrome / T-Cell Large Granular Lymphocyte Leukemia / Testicular Lymphoma / Untreated Adult Acute Lymphoblastic Leukemia / Untreated Hairy Cell Leukemia / Waldenström's Macroglobulinemia (WM)1
1CompletedTreatmentAdvanced Breast Cancer1
1CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Malignant Peritoneal Neoplasm1
1CompletedTreatmentCancer, Advanced1
1CompletedTreatmentCancer, Advanced / Tumors, Solid1
1CompletedTreatmentColorectal Cancers1
1CompletedTreatmentDiffuse Intrinsic Pontine Glioma (DIPG)1
1CompletedTreatmentGastrointestinal Stromal Tumors / Stage III Soft Tissue Sarcoma / Stage IV Soft Tissue Sarcoma1
1CompletedTreatmentGlioblastomas / Gliosarcoma1
1CompletedTreatmentHead and Neck Carcinoma / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedTreatmentLeukemia, Lymphoblastic, Acute, Philadelphia-Positive / Leukemia, Myeloid, Chronic-Phase1
1CompletedTreatmentLeukemias4
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedTreatmentMalignant Solid Tumours1
1CompletedTreatmentMetastatic Colorectal Cancers / Tumors, Solid1
1CompletedTreatmentMultiple Myeloma (MM)1
1CompletedTreatmentNeoplasms1
1CompletedTreatmentTumors1
1CompletedTreatmentTumors, Solid3
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
1Not Yet RecruitingTreatmentB-cell Acute Lymphoblastic Leukemia / Chronic Myeloid Leukemia (CML) in Lymphoid Blast Crisis / Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia Ph+ ALL1
1RecruitingBasic ScienceIdiopathic Pulmonary Fibrosis (IPF)1
1RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL)1
1RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Leukemia Acute Myeloid Leukemia (AML) / Untreated Adult Acute Myeloid Leukemia1
1RecruitingTreatmentAcute Lymphoblastic Leukemia With Failed Remission / Acute Lymphoblastic Leukemia, in Relapse1
1RecruitingTreatmentC-KIT Mutation / Relapsed AML / T(8;21)1
1RecruitingTreatmentChronic Myeloid Leukemia Accelerated Phase (CML-AP, Ph+) / Chronic Myeloid Leukemia Blast Crisis (CML-BC, Ph+) / Ph+ Acute Lymphoblastic Leukemia (Ph+ALL) / Ph- Acute Lymphoblastic Leukemia (Ph-ALL)1
1RecruitingTreatmentChronic Chronic myelogenous leukemia / Philadelphia Chromosome-positive Acute Lymphoblastic Leukemia1
1RecruitingTreatmentTumors, Solid1
1TerminatedTreatmentAccelerated Phase Chronic Myelogenous Leukemia / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Phase Chronic Myelogenous Leukemia / Relapsing Chronic Myelogenous Leukemia1
1TerminatedTreatmentAdenocarcinoma of the Pancreas / Refractory Solid Tumors1
1TerminatedTreatmentBrain Diseases / CNS Disease / Glioblastomas1
1TerminatedTreatmentChronic Chronic myelogenous leukemia / Leukemia, Lymphoblastic, Acute, Philadelphia-Positive1
1TerminatedTreatmentMultiple Myeloma (MM)1
1TerminatedTreatmentTumors1
1TerminatedTreatmentChronic Chronic myelogenous leukemia1
1WithdrawnTreatmentAcute Lymphoblastic Leukaemias (ALL)1
1WithdrawnTreatmentChronic Lymphocytic Leukaemia (CLL)1
1WithdrawnTreatmentHealthy Volunteers1
1WithdrawnTreatmentLeukemia Acute Myeloid Leukemia (AML)1
1WithdrawnTreatmentProstate Cancer1
1, 2Active Not RecruitingTreatmentBone Metastases / Cancer, Breast1
1, 2Active Not RecruitingTreatmentBrain and Central Nervous System Tumors1
1, 2Active Not RecruitingTreatmentBrain and Central Nervous System Tumors / Cancer of the Ovary / Childhood Germ Cell Tumor / Extragonadal Germ Cell Tumor / Liver Cancer / Malignant Lymphomas / Neuroblastomas / Renal Cancers / Sarcomas / Testicular germ cell tumour / Unspecified Childhood Solid Tumor, Protocol Specific1
1, 2Active Not RecruitingTreatmentCancer, Breast / Metastatic Breast Cancer (MBC)1
1, 2Active Not RecruitingTreatmentLeukemias1
1, 2Active Not RecruitingTreatmentNon-Hodgkin's Lymphoma (NHL)1
1, 2CompletedTreatmentAcute, secondary Myeloid Leukemia / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Del(5q) / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(15;17)(q22;q12) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Recurrent Adult Acute Myeloid Leukemia / Untreated Adult Acute Myeloid Leukemia1
1, 2CompletedTreatmentCancer, Breast1
1, 2CompletedTreatmentChronic Myeloid Leukemia (CML)1
1, 2CompletedTreatmentLeukemia Acute Myeloid Leukemia (AML)1
1, 2CompletedTreatmentLeukemias1
1, 2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Lung Cancers1
1, 2CompletedTreatmentMetastatic Breast Cancer (MBC)1
1, 2CompletedTreatmentMetastatic Hormone Refractory Prostate Cancer1
1, 2CompletedTreatmentMetastatic Melanoma1
1, 2CompletedTreatmentChronic Chronic myelogenous leukemia / Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia1
1, 2CompletedTreatmentScleroderma1
1, 2CompletedTreatmentChronic Chronic myelogenous leukemia1
1, 2RecruitingTreatmentChronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Myelogenous Leukemia, BCR-ABL1 Positive in Remission / Leukemias / Minimal Residual Disease / Philadelphia Chromosome Positive, BCR-ABL1 Positive Chronic Myelogenous Leukemia1
1, 2RecruitingTreatmentChronic Myelogenous Leukemia, Ph1-Positive1
1, 2RecruitingTreatmentEGFR Gene Mutations / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2RecruitingTreatmentLeukemia, Lymphocytic / Lymphoma, Hodgkins / Multiple Myeloma (MM) / Myelodysplastic Syndrome / Myeloid Leukemias / Non-Hodgkin's Lymphoma (NHL)1
1, 2RecruitingTreatmentLymphoma, Hodgkins / Multiple / Multiple Myeloma (MM) / Mycosis Fungoides (MF) / Non-Hodgkin's Lymphoma (NHL)1
1, 2RecruitingTreatmentRhabdomyosarcoma- Alveolar / Rhabdomyosarcoma-Embryonal / Rhabdomyosarcomas1
1, 2TerminatedTreatmentCancer, Breast1
1, 2TerminatedTreatmentGlioblastomas1
1, 2TerminatedTreatmentHead and Neck Carcinoma1
1, 2Unknown StatusTreatmentChronic Lymphocytic Leukaemia (CLL)1
1, 2Unknown StatusTreatmentChronic Lymphocytic Leukaemia (CLL) / Leukemias1
2Active Not RecruitingNot AvailableChronic Phase of Chronic Myeloid Leukemia1
2Active Not RecruitingOtherChronic Phase Chronic Myeloid Leukemia1
2Active Not RecruitingPreventionCancer, Breast1
2Active Not RecruitingSupportive CareMultiple Indications Cancer1
2Active Not RecruitingTreatmentAcinar Cell Adenocarcinoma of the Pancreas / Duct Cell Adenocarcinoma of the Pancreas / Recurrent Pancreatic Cancer / Stage IA Pancreatic Cancer / Stage IB Pancreatic Cancer / Stage IIA Pancreatic Cancer / Stage IIB Pancreatic Cancer / Stage III Pancreatic Cancer1
2Active Not RecruitingTreatmentAcute Lymphoblastic Leukaemia Recurrent / Acute Lymphoblastic Leukaemias (ALL) / BCR-ABL1 Fusion Protein Expression / Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Leukemias / Philadelphia Chromosome Positive / T(9;22)1
2Active Not RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Adult Acute Lymphoblastic Leukemia in Remission / Adult B Acute Lymphoblastic Leukemia / Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 / Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 / Adult L1 Acute Lymphoblastic Leukemia / Adult L2 Acute Lymphoblastic Leukemia / Adult T Acute Lymphoblastic Leukemia / Recurrent Adult Acute Lymphoblastic Leukemia / Untreated Adult Acute Lymphoblastic Leukemia1
2Active Not RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 / Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 / Untreated Adult Acute Lymphoblastic Leukemia1
2Active Not RecruitingTreatmentAcute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome / Acute, secondary Myeloid Leukemia / Adult Acute Myeloid Leukemia With Inv(16)(p13.1q22); CBFB-MYH11 / Adult Acute Myeloid Leukemia With t(16;16)(p13.1;q22); CBFB-MYH11 / Adult Acute Myeloid Leukemia With t(8;21)(q22;q22); RUNX1-RUNX1T1 / Adult Acute Myeloid Leukemia With t(8;21); (q22; q22.1); RUNX1-RUNX1T1 / Core Binding Factor Acute Myeloid Leukemia / Leukemia Acute Myeloid Leukemia (AML) / Therapy-Related Acute Myeloid Leukemia / Untreated Adult Acute Myeloid Leukemia1
2Active Not RecruitingTreatmentAdult Acute Lymphoblastic Leukemia in Remission / Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 / Blastic Phase / Blastic Phase Chronic Myelogenous Leukemia / Childhood Acute Lymphoblastic Leukemia in Remission / Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 / Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Phase Chronic Myelogenous Leukemia / Chronic Phase of Disease / Philadelphia Chromosome Positive Adult Precursor Acute Lymphoblastic Leukemia / Philadelphia Chromosome Positive Childhood Precursor Acute Lymphoblastic Leukemia / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Childhood Acute Lymphoblastic Leukemia / Recurrent Disease / Relapsing Chronic Myelogenous Leukemia1
2Active Not RecruitingTreatmentAdult Giant Cell Glioblastoma / Adult Glioblastoma / Adult Gliosarcoma / Recurrent Adult Brain Neoplasm1
2Active Not RecruitingTreatmentAlveolar Soft Part Sarcoma (ASPS) / Chondrosarcomas / Chordomas / Epithelioid Sarcoma / Ewing's Sarcoma (ES) / Gastrointestinal Stromal Tumors (GISTs) / Giant Cell Tumors of Bone / Hemangiopericytoma / Malignant Peripheral Nerve Sheath Tumour (MPNST) / Rhabdomyosarcomas1
2Active Not RecruitingTreatmentChronic Myelogenous Leukemia, BCR-ABL1 Positive / Chronic Phase of Disease1
2Active Not RecruitingTreatmentChronic Myeloid Leukemia (CML)1
2Active Not RecruitingTreatmentChronic Phase Chronic Myeloid Leukemia1
2Active Not RecruitingTreatmentEndometrial Clear Cell Adenocarcinoma / Estrogen Receptor Negative / Ovarian Clear Cell Cystadenocarcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Recurrent Uterine Corpus Carcinoma1
2Active Not RecruitingTreatmentGastrointestinal Stromal Tumors1
2Active Not RecruitingTreatmentGlioblastoma Multiforme (GBM)1
2Active Not RecruitingTreatmentHormone-Resistant Prostate Cancer / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
2Active Not RecruitingTreatmentLeukemia, Lymphoblastic, Acute, Philadelphia-Positive1
2Active Not RecruitingTreatmentLeukemias2
2Active Not RecruitingTreatmentMelanoma (Skin)1
2Active Not RecruitingTreatmentMetastatic Cancers1
2Active Not RecruitingTreatmentMetastatic Melanoma1
2Active Not RecruitingTreatmentPancreatic Cancer Metastatic1
2Active Not RecruitingTreatmentPediatric Leukemia1
2Active Not RecruitingTreatmentProstate Cancer1
2Active Not RecruitingTreatmentChronic Chronic myelogenous leukemia1
2CompletedSupportive CareAcute Myelogenous Leukaemia (AML)1
2CompletedTreatmentAcute Lymphoblastic Leukaemias (ALL)3
2CompletedTreatmentAdenocarcinoma of Colon / Adenocarcinoma of Rectum / Metastatic Disease1
2CompletedTreatmentAdenocarcinoma of the Pancreas / Recurrent Pancreatic Cancer / Stage IV Pancreatic Cancer1
2CompletedTreatmentAdenocarcinoma of the Prostate / Hormone-Refractory Prostate Cancer / Hormone-Resistant Prostate Cancer / Prostate Cancer / Recurrent Prostate Cancer1
2CompletedTreatmentAdvanced Breast Cancer2
2CompletedTreatmentAgnogenic Myeloid Metaplasia / Hypereosinophilic Syndromes / Leukemia Acute Myeloid Leukemia (AML) / Leukemia, Myelomonocytic, Chronic / Myelodysplastic Syndromes / Polycythemia Vera (PV) / Urticaria Pigmentosa1
2CompletedTreatmentBlast Crisis / Chronic Myeloid Leukemia (CML)1
2CompletedTreatmentCancer, Breast1
2CompletedTreatmentCancer, Breast / Metastasis2
2CompletedTreatmentCholangiocarcinomas1
2CompletedTreatmentChronic Lymphocytic Leukaemia (CLL)1
2CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Chronic Lymphocytic Leukemia (CLL) - Refractory / Stage I Chronic Lymphocytic Leukemia / Stage II Chronic Lymphocytic Leukemia / Stage III Chronic Lymphocytic Leukemia / Stage IV Chronic Lymphocytic Leukemia1
2CompletedTreatmentChronic Myelogenous Leukemia, BCR/ABL Positive1
2CompletedTreatmentChronic Myeloid Leukemia (CML)3
2CompletedTreatmentChronic Myeloid Leukemia (CML) / Leukemia, Lymphoblastic, Acute, Philadelphia-Positive1
2CompletedTreatmentChronic Myeloid Leukemia (CML) / Leukemia, Lymphocytic, Acute, L21
2CompletedTreatmentChronic Myeloid Leukemia (CML) / Philadelphia-Positive Myeloid Leukemia2
2CompletedTreatmentExtensive Stage Small Cell Lung Cancer / Limited Stage Small Cell Lung Cancer / Refractory Small cell lung cancer1
2CompletedTreatmentHigh-grade Salivary Gland Mucoepidermoid Carcinoma / Low-grade Salivary Gland Mucoepidermoid Carcinoma / Malignant Salivary Gland Neoplasm / Recurrent Salivary Gland Cancer / Recurrent Salivary Gland Carcinoma / Salivary Gland Acinic Cell Tumor / Salivary Gland Adenocarcinoma / Salivary Gland Adenoid Cystic Carcinoma / Salivary Gland Anaplastic Carcinoma / Salivary Gland Malignant Mixed Cell Type Tumor / Salivary Gland Poorly Differentiated Carcinoma / Salivary Gland Squamous Cell Carcinoma / Stage IV Major Salivary Gland Cancer AJCC v7 / Stage IV Salivary Gland Cancer1
2CompletedTreatmentHormone Refractory Prostate Cancer / Hormone-Resistant Prostate Cancer / Recurrent Prostate Cancer1
2CompletedTreatmentLeukemia, Myeloid, Chronic-Phase1
2CompletedTreatmentLeukemias2
2CompletedTreatmentLeukemias / Malignant Lymphomas1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Non-Small Cell Lung Cancer Recurrent / Stage IIIb Non-small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer1
2CompletedTreatmentLung Cancers1
2CompletedTreatmentMalignant Neoplasm of Pancreas1
2CompletedTreatmentMesothelioma, Malignant1
2CompletedTreatmentMetastatic Breast Cancer (MBC)1
2CompletedTreatmentMetastatic Colon Cancer / Recurrent Colon Cancer / Recurrent Rectal Cancer / Stage IV Rectal Cancer1
2CompletedTreatmentMetastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma / Recurrent Metastatic Squamous Neck Cancer With Occult Primary / Recurrent Salivary Gland Cancer / Recurrent Squamous Cell Carcinoma of the Hypopharynx / Recurrent Squamous Cell Carcinoma of the Larynx / Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity / Recurrent Squamous Cell Carcinoma of the Nasopharynx / Recurrent Squamous Cell Carcinoma of the Oropharynx / Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Recurrent Verrucous Carcinoma of the Larynx / Recurrent Verrucous Carcinoma of the Oral Cavity / Salivary Gland Squamous Cell Carcinoma / Stage IV Squamous Cell Carcinoma of the Hypopharynx / Stage IV Squamous Cell Carcinoma of the Nasopharynx / Stage IVA Salivary Gland Cancer / Stage IVA Squamous Cell Carcinoma of the Larynx / Stage IVA Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IVA Squamous Cell Carcinoma of the Oropharynx / Stage IVA Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IVA Verrucous Carcinoma of the Larynx / Stage IVA Verrucous Carcinoma of the Oral Cavity / Stage IVB Salivary Gland Cancer / Stage IVB Squamous Cell Carcinoma of the Larynx / Stage IVB Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IVB Squamous Cell Carcinoma of the Oropharynx / Stage IVB Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IVB Verrucous Carcinoma of the Larynx / Stage IVB Verrucous Carcinoma of the Oral Cavity / Stage IVC Salivary Gland Cancer / Stage IVC Squamous Cell Carcinoma of the Larynx / Stage IVC Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IVC Squamous Cell Carcinoma of the Oropharynx / Stage IVC Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IVC Verrucous Carcinoma of the Larynx / Stage IVC Verrucous Carcinoma of the Oral Cavity / Tongue Cancer1
2CompletedTreatmentPhiladelphia Positive Acute Lymphoblastic Leukemia1
2CompletedTreatmentPolycythemia Vera (PV)1
2CompletedTreatmentProstate Cancer1
2CompletedTreatmentRecurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma1
2CompletedTreatmentRecurrent Melanoma / Stage IIIA Melanoma / Stage IIIB Melanoma / Stage IIIc Melanoma / Stage IV Melanoma1
2CompletedTreatmentRecurrent Skin Cancer / Squamous Cell Carcinoma of the Skin / Stage 0 Chronic Lymphocytic Leukemia / Stage I Chronic Lymphocytic Leukemia1
2CompletedTreatmentRelapsed, Refractory or Plateau Phase Multiple Myeloma1
2CompletedTreatmentChronic Chronic myelogenous leukemia1
2Enrolling by InvitationTreatmentAcute,Leukemia, Lymphoid1
2Not Yet RecruitingTreatmentChronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Minimal Residual Disease1
2Not Yet RecruitingTreatmentChronic Chronic myelogenous leukemia1
2RecruitingNot AvailableChronic Myeloid Leukemia (CML)1
2RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL)1
2RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Acute Myelogenous Leukaemia (AML) / Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome / Chronic Myelomonocytic Leukemia / Myelodysplastic Syndrome / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Acute Myeloid Leukemia / Refractory Adult Acute Lymphoblastic Leukemia1
2RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / B Acute Lymphoblastic Leukemia / B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 / B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 / B Acute Lymphoblastic Leukemia, Philadelphia Chromosome Negative / Philadelphia Chromosome Positive / Recurrent Adult Acute Lymphoblastic Leukemia / Refractory Adult Acute Lymphoblastic Leukemia / Untreated Adult Acute Lymphoblastic Leukemia1
2RecruitingTreatmentAcute Lymphocytic Leukemia (ALL) / Adult Lymphoblastic Lymphoma1
2RecruitingTreatmentAdult Acute Lymphoblastic Leukemia / Adult Lymphoblastic Lymphoma / CD20 Positive / Philadelphia Chromosome Positive1
2RecruitingTreatmentAdvanced Malignant Neoplasm / Advanced Malignant Solid Neoplasm / Bladder Carcinoma / Carcinoma, Breast / Carcinoma, Colorectal / Carcinoma, Pancreatic / Cervical Carcinoma / Colon Carcinoma / Endometrial Carcinoma / Gastric Carcinoma / Gliomas / Head and Neck Carcinoma / Liver and Intrahepatic Bile Duct Carcinoma / Lung, Carcinoma / Malignant Lymphomas / Malignant Uterine Neoplasm / Melanoma / Oesophageal Carcinoma / Ovarian Carcinoma / Plasma Cell Myeloma / Prostate Cancer / Rectal Carcinoma / Recurrent Bladder Carcinoma / Recurrent Breast Carcinoma / Recurrent Cervical Carcinoma / Recurrent Colon Carcinoma / Recurrent Colorectal Carcinoma / Recurrent Esophageal Carcinoma / Recurrent Gastric Carcinoma / Recurrent Gliomas / Recurrent Head and Neck Carcinoma / Recurrent Liver Carcinoma / Recurrent Lung Carcinoma / Recurrent Lymphoma / Recurrent Malignant Solid Neoplasm / Recurrent Melanoma / Recurrent Ovarian Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Plasma Cell Myeloma / Recurrent Prostate Carcinoma / Recurrent Rectal Carcinoma / Recurrent Skin Carcinoma / Recurrent Solid Neoplasm / Recurrent Thyroid Gland Carcinoma / Recurrent Uterine Corpus Carcinoma / Refractory Lymphomas / Refractory Malignant Neoplasm / Refractory Malignant Solid Neoplasm / Refractory Plasma Cell Myeloma / Renal Carcinoma / Skin Carcinoma / Solid Neoplasms / Thyroid Gland Carcinoma / Uterine Corpus Cancer1
2RecruitingTreatmentAdvanced Solid Tumors / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)2
2RecruitingTreatmentCML, Relapsed1
2RecruitingTreatmentCancer, Advanced1
2RecruitingTreatmentChronic Kidney Disease (CKD)1
2RecruitingTreatmentChronic Myeloid Leukemia (CML)2
2RecruitingTreatmentChronic Chronic myelogenous leukemia / Chronic Myeloid Leukemia (CML) / Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Leukemias1
2RecruitingTreatmentChronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive1
2RecruitingTreatmentDiffuse Intrinsic Pontine Glioma (DIPG)1
2RecruitingTreatmentGliomas1
2RecruitingTreatmentLeukemias1
2RecruitingTreatmentNeoplasms, Breast / Triple Negative Breast Neoplasms1
2RecruitingTreatmentNeuroblastomas1
2RecruitingTreatmentPinealoblastoma1
2RecruitingTreatmentProstate Cancer1
2RecruitingTreatmentRecurrent Neuroblastoma1
2RecruitingTreatmentRefractory Pediatric AML / Refractory Pediatric Solid Tumors / Relapsed Pediatric AML / Relapsed Pediatric Solid Tumors1
2RecruitingTreatmentChronic Chronic myelogenous leukemia1
2TerminatedTreatmentAdult Primary Hepatocellular Carcinoma / Advanced Adult Primary Liver Cancer / Recurrent Adult Primary Liver Cancer1
2TerminatedTreatmentCancer, Breast2
2TerminatedTreatmentChronic Lymphocytic Leukaemia (CLL) / Small Lymphocytic Lymphoma (SLL)1
2TerminatedTreatmentChronic Myeloid Leukemia (CML)2
2TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
2TerminatedTreatmentLung Cancers1
2TerminatedTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL)1
2TerminatedTreatmentMalignant Neoplasm of Pancreas1
2TerminatedTreatmentMelanoma1
2TerminatedTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
2TerminatedTreatmentPlasma Cell Myeloma1
2TerminatedTreatmentProstate Cancer2
2TerminatedTreatmentSquamous Cell Carcinoma of Lung1
2TerminatedTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
2Unknown StatusTreatmentCancer, Breast / Metastatic Cancers1
2Unknown StatusTreatmentChronic Lymphocytic Leukaemia (CLL)1
2Unknown StatusTreatmentChronic Myeloid Leukemia (CML)1
2Unknown StatusTreatmentLeukemias1
2Unknown StatusTreatmentMyelogenous Leukemia, Chronic, Chronic Phase1
2Unknown StatusTreatmentSystemic Mastocytosis1
2WithdrawnTreatmentBrain Diseases / CNS Disease / Glioblastomas1
2WithdrawnTreatmentCancer, Breast1
2, 3CompletedTreatmentAdult B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 / Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 / Untreated Adult Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia1
2, 3RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Acute Lymphoblastic Lymphoma1
2, 3RecruitingTreatmentLeukaemia, Lymphoblastic / Leukemia, Acute / Leukemia, B-Cell / Leukemias1
2, 3WithdrawnTreatmentAcute Lymphoblastic Leukaemias (ALL) / Chronic Myeloid Leukemia (CML)1
3Active Not RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL)1
3CompletedTreatmentChronic Myeloid Leukemia (CML)1
3CompletedTreatmentLeukemia, Lymphoblastic, Acute, Philadelphia-Positive / Myeloid Leukemia, Chronic, Accelerated Phase1
3CompletedTreatmentMyeloid Leukemia, Chronic, Chronic Phase1
3CompletedTreatmentMyeloid Leukemia, Chronic, Chronic-Phase1
3CompletedTreatmentProstatic Neoplasms1
3RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / B Acute Lymphoblastic Leukemia / Central Nervous System Leukemia / Cognitive Side Effects of Cancer Therapy / Neurotoxicity Syndrome / Osteonecrosis / Pain / Ph-Like Acute Lymphoblastic Leukemia / Testicular Leukemia / Therapy-Related Toxicity / Untreated Adult Acute Lymphoblastic Leukemia / Untreated Childhood Acute Lymphoblastic Leukemia1
3RecruitingTreatmentAcute Lymphoblastic Leukemia, Pediatric1
3RecruitingTreatmentChronic Myeloid Leukemia (CML)2
3RecruitingTreatmentChronic Myeloid Leukemia - Chronic Phase1
3RecruitingTreatmentLeukemia Acute Myeloid Leukemia (AML)1
3TerminatedTreatmentLeukemias1
4CompletedTreatmentChronic Phase Chronic Myeloid Leukemia1
4Not Yet RecruitingTreatmentPh+ Acute Lymphoblastic Leukemia1
4RecruitingTreatmentChronic Chronic myelogenous leukemia1
Not AvailableActive Not RecruitingDiagnosticAdvanced Solid Tumors / Cancers1
Not AvailableActive Not RecruitingTreatmentRecurrent Childhood Brain Tumor1
Not AvailableApproved for MarketingNot AvailableLeukemias1
Not AvailableAvailableNot AvailableChronic Myeloid Leukemia (CML)1
Not AvailableCompletedNot AvailableChronic Myeloid Leukemia (CML)1
Not AvailableCompletedNot AvailableLeukemia, Myelogenous, Chronic, BCR-ABL Positive1
Not AvailableCompletedNot AvailableLeukemia, Myeloid, Chronic-Phase (CML-CP)1
Not AvailableCompletedNot AvailableLeukemias / Lung Cancer Small Cell Lung Cancer (SCLC)1
Not AvailableCompletedNot AvailableLiver Diseases1
Not AvailableCompletedTreatmentMyelodysplastic Syndromes1
Not AvailableCompletedTreatmentTransitional Cell Carcinoma of the Bladder1
Not AvailableNot Yet RecruitingNot AvailableAcute Lymphoblastic Leukaemias (ALL)1
Not AvailableRecruitingNot AvailableAcute Lymphoblastic Leukaemias (ALL)1
Not AvailableRecruitingTreatmentGastrointestinal Stromal Tumors1
Not AvailableRecruitingTreatmentHematopoietic Stem Cell Transplant (HSCT)1
Not AvailableRecruitingTreatmentLeukemia Acute Myeloid Leukemia (AML)1
Not AvailableWithdrawnNot AvailableLeukemia, Myelogenous, Chronic, BCR-ABL Positive1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Bristol-Myers Squibb Co.
  • E.R. Squibb and Sons LLC
  • Physicians Total Care Inc.
Dosage forms
FormRouteStrength
TabletOral100 mg
TabletOral100 mg/1
TabletOral140 mg/1
TabletOral140 mg
TabletOral20 mg
TabletOral20 mg/1
TabletOral50 mg
TabletOral50 mg/1
TabletOral70 mg/1
TabletOral70 mg
TabletOral80 mg/1
TabletOral80 mg
Tablet, film coatedOral100 mg
Tablet, film coatedOral140 mg
Tablet, film coatedOral20 mg
Tablet, film coatedOral50 mg
Tablet, film coatedOral70 mg
Tablet, film coatedOral80 mg
Prices
Unit descriptionCostUnit
Sprycel 100 mg tablet278.24USD tablet
Sprycel 50 mg tablet139.12USD tablet
Sprycel 70 mg tablet139.12USD tablet
Sprycel 20 mg tablet69.56USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2366932No2009-08-252020-04-12Canada
US6596746No2000-06-282020-06-28Us
US7125875No2000-04-132020-04-13Us
US7153856No2000-04-282020-04-28Us
US7491725No2006-03-282026-03-28Us
US8680103No2005-02-042025-02-04Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)280-286 °CNot Available
logP1.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0128 mg/mLALOGPS
logP2.77ALOGPS
logP3.82ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)8.49ChemAxon
pKa (Strongest Basic)7.22ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area106.51 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity133.08 m3·mol-1ChemAxon
Polarizability51.58 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9852
Blood Brain Barrier-0.507
Caco-2 permeable-0.5638
P-glycoprotein substrateSubstrate0.6562
P-glycoprotein inhibitor IInhibitor0.5371
P-glycoprotein inhibitor IIInhibitor0.5425
Renal organic cation transporterNon-inhibitor0.7288
CYP450 2C9 substrateNon-substrate0.7061
CYP450 2D6 substrateNon-substrate0.8152
CYP450 3A4 substrateSubstrate0.5704
CYP450 1A2 substrateNon-inhibitor0.5612
CYP450 2C9 inhibitorInhibitor0.8008
CYP450 2D6 inhibitorNon-inhibitor0.8358
CYP450 2C19 inhibitorInhibitor0.574
CYP450 3A4 inhibitorInhibitor0.7295
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8343
Ames testNon AMES toxic0.7185
CarcinogenicityNon-carcinogens0.7308
BiodegradationNot ready biodegradable0.9863
Rat acute toxicity2.4772 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8538
hERG inhibition (predictor II)Inhibitor0.718
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000m-0390000000-8a413cb9e53d14cbe10a
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-0011900000-4dac51b915117532ebe0

Taxonomy

Description
This compound belongs to the class of organic compounds known as aromatic anilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with an aromatic group. They have the general structure RNC(=O)R', where R= benzene, and R = aryl group.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Anilides
Direct Parent
Aromatic anilides
Alternative Parents
N-arylpiperazines / Thiazolecarboxamides / 2-heteroaryl carboxamides / Dialkylarylamines / 2,5-disubstituted thiazoles / Toluenes / Aminopyrimidines and derivatives / Chlorobenzenes / N-alkylpiperazines / 2-amino-1,3-thiazoles
show 14 more
Substituents
Aromatic anilide / N-arylpiperazine / 2-heteroaryl carboxamide / Thiazolecarboxamide / Thiazolecarboxylic acid or derivatives / Dialkylarylamine / Halobenzene / 2,5-disubstituted 1,3-thiazole / Chlorobenzene / Aminopyrimidine
show 36 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
tertiary amino compound, N-arylpiperazine, N-(2-hydroxyethyl)piperazine, aminopyrimidine, monocarboxylic acid amide, organochlorine compound, 1,3-thiazole, secondary amino compound (CHEBI:49375)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Multitarget
General Function
Syntaxin binding
Specific Function
Non-receptor tyrosine-protein kinase that plays a role in many key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility a...
Gene Name
ABL1
Uniprot ID
P00519
Uniprot Name
Tyrosine-protein kinase ABL1
Molecular Weight
122871.435 Da
References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  2. Piccaluga PP, Paolini S, Martinelli G: Tyrosine kinase inhibitors for the treatment of Philadelphia chromosome-positive adult acute lymphoblastic leukemia. Cancer. 2007 Sep 15;110(6):1178-86. [PubMed:17701954]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Multitarget
General Function
Sh3/sh2 adaptor activity
Specific Function
Non-receptor protein tyrosine kinase which is activated following engagement of many different classes of cellular receptors including immune response receptors, integrins and other adhesion recept...
Gene Name
SRC
Uniprot ID
P12931
Uniprot Name
Proto-oncogene tyrosine-protein kinase Src
Molecular Weight
59834.295 Da
References
  1. Kamath AV, Wang J, Lee FY, Marathe PH: Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL. Cancer Chemother Pharmacol. 2008 Mar;61(3):365-76. Epub 2007 Apr 11. [PubMed:17429625]
  2. Serrels A, Macpherson IR, Evans TR, Lee FY, Clark EA, Sansom OJ, Ashton GH, Frame MC, Brunton VG: Identification of potential biomarkers for measuring inhibition of Src kinase activity in colon cancer cells following treatment with dasatinib. Mol Cancer Ther. 2006 Dec;5(12):3014-22. Epub 2006 Dec 5. [PubMed:17148760]
  3. Quintas-Cardama A, Kantarjian H, Cortes J: Targeting ABL and SRC kinases in chronic myeloid leukemia: experience with dasatinib. Future Oncol. 2006 Dec;2(6):655-65. [PubMed:17155893]
  4. Schittenhelm MM, Shiraga S, Schroeder A, Corbin AS, Griffith D, Lee FY, Bokemeyer C, Deininger MW, Druker BJ, Heinrich MC: 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. Cancer Res. 2006 Jan 1;66(1):473-81. [PubMed:16397263]
  5. Nam S, Kim D, Cheng JQ, Zhang S, Lee JH, Buettner R, Mirosevich J, Lee FY, Jove R: Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. Cancer Res. 2005 Oct 15;65(20):9185-9. [PubMed:16230377]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Details
3. Ephrin type-A receptor 2
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Transmembrane receptor protein tyrosine kinase activity
Specific Function
Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. Th...
Gene Name
EPHA2
Uniprot ID
P29317
Uniprot Name
Ephrin type-A receptor 2
Molecular Weight
108265.585 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Multitarget
General Function
Sh2 domain binding
Specific Function
Non-receptor tyrosine-protein kinase that plays an essential role in the selection and maturation of developing T-cells in the thymus and in the function of mature T-cells. Plays a key role in T-ce...
Gene Name
LCK
Uniprot ID
P06239
Uniprot Name
Tyrosine-protein kinase Lck
Molecular Weight
58000.15 Da
References
  1. Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC: 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor. J Med Chem. 2006 Nov 16;49(23):6819-32. [PubMed:17154512]
  2. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Receptor binding
Specific Function
Non-receptor protein tyrosine kinase that is involved in the regulation of cell growth and survival, apoptosis, cell-cell adhesion, cytoskeleton remodeling, and differentiation. Stimulation by rece...
Gene Name
YES1
Uniprot ID
P07947
Uniprot Name
Tyrosine-protein kinase Yes
Molecular Weight
60800.78 Da
References
  1. Trevino JG, Summy JM, Lesslie DP, Parikh NU, Hong DS, Lee FY, Donato NJ, Abbruzzese JL, Baker CH, Gallick GE: Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model. Am J Pathol. 2006 Mar;168(3):962-72. [PubMed:16507911]
  2. Margutti S, Laufer SA: Are MAP kinases drug targets? Yes, but difficult ones. ChemMedChem. 2007 Aug;2(8):1116-40. [PubMed:17541990]
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Transmembrane receptor protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell main...
Gene Name
KIT
Uniprot ID
P10721
Uniprot Name
Mast/stem cell growth factor receptor Kit
Molecular Weight
109863.655 Da
References
  1. Schittenhelm MM, Shiraga S, Schroeder A, Corbin AS, Griffith D, Lee FY, Bokemeyer C, Deininger MW, Druker BJ, Heinrich MC: 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. Cancer Res. 2006 Jan 1;66(1):473-81. [PubMed:16397263]
  2. Shah NP, Lee FY, Luo R, Jiang Y, Donker M, Akin C: Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis. Blood. 2006 Jul 1;108(1):286-91. Epub 2006 Jan 24. [PubMed:16434489]
  3. Dizdar O, Dede DS, Bulut N, Altundag K: Dasatinib may also inhibit c-Kit in triple negative breast cancer cell lines. Breast Cancer Res Treat. 2008 Jan;107(2):303. Epub 2007 Mar 10. [PubMed:17351742]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Vascular endothelial growth factor binding
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic...
Gene Name
PDGFRB
Uniprot ID
P09619
Uniprot Name
Platelet-derived growth factor receptor beta
Molecular Weight
123966.895 Da
References
  1. Zhang Z, Meier KE: New assignments for multitasking signal transduction inhibitors. Mol Pharmacol. 2006 May;69(5):1510-2. Epub 2006 Feb 23. [PubMed:16497876]
  2. Chen Z, Lee FY, Bhalla KN, Wu J: Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib). Mol Pharmacol. 2006 May;69(5):1527-33. Epub 2006 Jan 25. [PubMed:16436588]
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transcription factor activity, sequence-specific dna binding
Specific Function
Carries out a dual function: signal transduction and activation of transcription. Mediates cellular responses to the cytokine KITLG/SCF and other growth factors. Binds to the GAS element and activa...
Gene Name
STAT5B
Uniprot ID
P51692
Uniprot Name
Signal transducer and activator of transcription 5B
Molecular Weight
89865.35 Da
References
  1. Fiskus W, Pranpat M, Balasis M, Bali P, Estrella V, Kumaraswamy S, Rao R, Rocha K, Herger B, Lee F, Richon V, Bhalla K: Cotreatment with vorinostat (suberoylanilide hydroxamic acid) enhances activity of dasatinib (BMS-354825) against imatinib mesylate-sensitive or imatinib mesylate-resistant chronic myelogenous leukemia cells. Clin Cancer Res. 2006 Oct 1;12(19):5869-78. [PubMed:17020995]
  2. Nam S, Williams A, Vultur A, List A, Bhalla K, Smith D, Lee FY, Jove R: Dasatinib (BMS-354825) inhibits Stat5 signaling associated with apoptosis in chronic myelogenous leukemia cells. Mol Cancer Ther. 2007 Apr;6(4):1400-5. [PubMed:17431118]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Multitarget
General Function
Receptor binding
Specific Function
Non-receptor tyrosine-protein kinase that plays an ABL1-overlapping role in key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, ce...
Gene Name
ABL2
Uniprot ID
P42684
Uniprot Name
Abelson tyrosine-protein kinase 2
Molecular Weight
128341.935 Da
References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  2. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Multitarget
General Function
Protein tyrosine kinase activity
Specific Function
Non-receptor tyrosine-protein kinase that plays a role in many biological processes including regulation of cell growth and survival, cell adhesion, integrin-mediated signaling, cytoskeletal remode...
Gene Name
FYN
Uniprot ID
P06241
Uniprot Name
Tyrosine-protein kinase Fyn
Molecular Weight
60761.49 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Protein tyrosine kinase activity
Specific Function
Non-receptor tyrosine kinase indispensable for B lymphocyte development, differentiation and signaling. Binding of antigen to the B-cell antigen receptor (BCR) triggers signaling that ultimately le...
Gene Name
BTK
Uniprot ID
Q06187
Uniprot Name
Tyrosine-protein kinase BTK
Molecular Weight
76280.71 Da
References
  1. Hantschel O, Rix U, Schmidt U, Burckstummer T, Kneidinger M, Schutze G, Colinge J, Bennett KL, Ellmeier W, Valent P, Superti-Furga G: The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13283-8. Epub 2007 Aug 7. [PubMed:17684099]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transcriptional activator that binds to regulatory elements in promoter regions in a cell- and response element (target)-specific manner. Induces gene expression by binding as monomers to the NR4A1 response element (NBRE) 5'-AAAAGGTCA-3' site and as homodimers to the Nur response element (NurRE) site in the promoter of their regulated target genes (By similarity). Plays a role in the regulation of proliferation, survival and differentiation of many different cell types and also in metabolism and inflammation. Mediates proliferation of vascular smooth muscle, myeloid progenitor cell and type B pancreatic cells; promotes mitogen-induced vascular smooth muscle cell proliferation through transactivation of SKP2 promoter by binding a NBRE site (By similarity). Upon PDGF stimulation, stimulates vascular smooth muscle cell proliferation by regulating CCND1 and CCND2 expression. In islets, induces type B pancreatic cell proliferation through up-regulation of genes that activate cell cycle, as well as genes that cause degradation of the CDKN1A (By similarity). Negatively regulates myeloid progenitor cell proliferation by repressing RUNX1 in a NBRE site-independent manner. During inner ear, plays a role as a key mediator of the proliferative growth phase of semicircular canal development (By similarity). Mediates also survival of neuron and smooth muscle cells; mediates CREB-induced neuronal survival, and during hippocampus development, plays a critical role in pyramidal cell survival and axonal guidance. Is required for S phase entry of the cell cycle and survival of smooth muscle cells by inducing CCND1, resulting in RB1 phosphorylation. Binds to NBRE motif in CCND1 promoter, resulting in the activation of the promoter and CCND1 transcription (By similarity). Plays also a role in inflammation; upon TNF stimulation, mediates monocyte adhesion by inducing the expression of VCAM1 and ICAM1 by binding to the NBRE consensus site (By similarity) (PubMed:20558821). In mast cells activated by Fc-epsilon receptor cross-linking, promotes the synthesis and release of cytokines but impairs events leading to degranulation (By similarity). Plays also a role in metabolism; by modulating feeding behavior; and by playing a role in energy balance by inhibiting the glucocorticoid-induced orexigenic neuropeptides AGRP expression, at least in part by forming a complex with activated NR3C1 on the AGRP- glucocorticoid response element (GRE), and thus weakening the DNA binding activity of NR3C1. Upon catecholamines stimulation, regulates gene expression that controls oxidative metabolism in skeletal muscle (By similarity). Plays a role in glucose transport by regulating translocation of the SLC2A4 glucose transporter to the cell surface (PubMed:24022864). Finally, during gastrulation plays a crucial role in the formation of anterior mesoderm by controlling cell migration. Inhibits adipogenesis (By similarity). Also participates in cardiac hypertrophy by activating PARP1 (By similarity).
Specific Function
Core promoter sequence-specific dna binding
Gene Name
NR4A3
Uniprot ID
Q92570
Uniprot Name
Nuclear receptor subfamily 4 group A member 3
Molecular Weight
68229.025 Da
References
  1. Hantschel O, Rix U, Schmidt U, Burckstummer T, Kneidinger M, Schutze G, Colinge J, Bennett KL, Ellmeier W, Valent P, Superti-Furga G: The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13283-8. Epub 2007 Aug 7. [PubMed:17684099]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Rho guanyl-nucleotide exchange factor activity
Specific Function
GTPase-activating protein for RAC1 and CDC42. Promotes the exchange of RAC or CDC42-bound GDP by GTP, thereby activating them. Displays serine/threonine kinase activity.
Gene Name
BCR
Uniprot ID
P11274
Uniprot Name
Breakpoint cluster region protein
Molecular Weight
142818.07 Da
References
  1. Shah NP, Tran C, Lee FY, Chen P, Norris D, Sawyers CL: Overriding imatinib resistance with a novel ABL kinase inhibitor. Science. 2004 Jul 16;305(5682):399-401. [PubMed:15256671]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Receptor binding
Specific Function
Non-receptor tyrosine-protein kinase that plays an important role in the regulation of cell growth, differentiation, migration and immune response. Phosphorylates tyrosine residues located in the C...
Gene Name
CSK
Uniprot ID
P41240
Uniprot Name
Tyrosine-protein kinase CSK
Molecular Weight
50703.975 Da
References
  1. Kneidinger M, Schmidt U, Rix U, Gleixner KV, Vales A, Baumgartner C, Lupinek C, Weghofer M, Bennett KL, Herrmann H, Schebesta A, Thomas WR, Vrtala S, Valenta R, Lee FY, Ellmeier W, Superti-Furga G, Valent P: The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils. Blood. 2008 Mar 15;111(6):3097-107. doi: 10.1182/blood-2007-08-104372. Epub 2008 Jan 7. [PubMed:18180381]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transmembrane-ephrin receptor activity
Specific Function
Receptor tyrosine kinase which binds promiscuously GPI-anchored ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The ...
Gene Name
EPHA5
Uniprot ID
P54756
Uniprot Name
Ephrin type-A receptor 5
Molecular Weight
114802.31 Da
References
  1. Kneidinger M, Schmidt U, Rix U, Gleixner KV, Vales A, Baumgartner C, Lupinek C, Weghofer M, Bennett KL, Herrmann H, Schebesta A, Thomas WR, Vrtala S, Valenta R, Lee FY, Ellmeier W, Superti-Furga G, Valent P: The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils. Blood. 2008 Mar 15;111(6):3097-107. doi: 10.1182/blood-2007-08-104372. Epub 2008 Jan 7. [PubMed:18180381]
Details
16. Ephrin type-B receptor 4
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transmembrane receptor protein tyrosine kinase activity
Specific Function
Receptor tyrosine kinase which binds promiscuously transmembrane ephrin-B family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The...
Gene Name
EPHB4
Uniprot ID
P54760
Uniprot Name
Ephrin type-B receptor 4
Molecular Weight
108269.26 Da
References
  1. Kneidinger M, Schmidt U, Rix U, Gleixner KV, Vales A, Baumgartner C, Lupinek C, Weghofer M, Bennett KL, Herrmann H, Schebesta A, Thomas WR, Vrtala S, Valenta R, Lee FY, Ellmeier W, Superti-Furga G, Valent P: The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils. Blood. 2008 Mar 15;111(6):3097-107. doi: 10.1182/blood-2007-08-104372. Epub 2008 Jan 7. [PubMed:18180381]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Protein tyrosine kinase activity
Specific Function
Non-receptor tyrosine-protein kinase that transmits signals from cell surface receptors devoid of kinase activity and contributes to the regulation of immune responses, including neutrophil, monocy...
Gene Name
FGR
Uniprot ID
P09769
Uniprot Name
Tyrosine-protein kinase Fgr
Molecular Weight
59478.11 Da
References
  1. Kneidinger M, Schmidt U, Rix U, Gleixner KV, Vales A, Baumgartner C, Lupinek C, Weghofer M, Bennett KL, Herrmann H, Schebesta A, Thomas WR, Vrtala S, Valenta R, Lee FY, Ellmeier W, Superti-Furga G, Valent P: The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils. Blood. 2008 Mar 15;111(6):3097-107. doi: 10.1182/blood-2007-08-104372. Epub 2008 Jan 7. [PubMed:18180381]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Receptor binding
Specific Function
Non-receptor tyrosine-protein kinase that negatively regulates cell proliferation. Positively regulates PTEN protein stability through phosphorylation of PTEN on 'Tyr-336', which in turn prevents i...
Gene Name
FRK
Uniprot ID
P42685
Uniprot Name
Tyrosine-protein kinase FRK
Molecular Weight
58253.61 Da
References
  1. Kneidinger M, Schmidt U, Rix U, Gleixner KV, Vales A, Baumgartner C, Lupinek C, Weghofer M, Bennett KL, Herrmann H, Schebesta A, Thomas WR, Vrtala S, Valenta R, Lee FY, Ellmeier W, Superti-Furga G, Valent P: The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils. Blood. 2008 Mar 15;111(6):3097-107. doi: 10.1182/blood-2007-08-104372. Epub 2008 Jan 7. [PubMed:18180381]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Unfolded protein binding
Specific Function
Acts as a repressor of transcriptional activation. Inhibits the transcriptional coactivator activity of CITED1 on Smad-mediated transcription. Chaperone. Component of the PRP19-CDC5L complex that f...
Gene Name
HSPA8
Uniprot ID
P11142
Uniprot Name
Heat shock cognate 71 kDa protein
Molecular Weight
70897.565 Da
References
  1. Kneidinger M, Schmidt U, Rix U, Gleixner KV, Vales A, Baumgartner C, Lupinek C, Weghofer M, Bennett KL, Herrmann H, Schebesta A, Thomas WR, Vrtala S, Valenta R, Lee FY, Ellmeier W, Superti-Furga G, Valent P: The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils. Blood. 2008 Mar 15;111(6):3097-107. doi: 10.1182/blood-2007-08-104372. Epub 2008 Jan 7. [PubMed:18180381]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Receptor signaling protein tyrosine kinase activity
Specific Function
Non-receptor tyrosine-protein kinase that transmits signals from cell surface receptors and plays an important role in the regulation of innate and adaptive immune responses, hematopoiesis, respons...
Gene Name
LYN
Uniprot ID
P07948
Uniprot Name
Tyrosine-protein kinase Lyn
Molecular Weight
58573.595 Da
References
  1. Kneidinger M, Schmidt U, Rix U, Gleixner KV, Vales A, Baumgartner C, Lupinek C, Weghofer M, Bennett KL, Herrmann H, Schebesta A, Thomas WR, Vrtala S, Valenta R, Lee FY, Ellmeier W, Superti-Furga G, Valent P: The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils. Blood. 2008 Mar 15;111(6):3097-107. doi: 10.1182/blood-2007-08-104372. Epub 2008 Jan 7. [PubMed:18180381]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Protein serine/threonine kinase activity
Specific Function
Stress-activated component of a protein kinase signal transduction cascade. Regulates the JNK and p38 pathways. Pro-apoptotic. Role in regulation of S and G2 cell cycle checkpoint by direct phospho...
Gene Name
ZAK
Uniprot ID
Q9NYL2
Uniprot Name
Mitogen-activated protein kinase kinase kinase MLT
Molecular Weight
91154.315 Da
References
  1. Kneidinger M, Schmidt U, Rix U, Gleixner KV, Vales A, Baumgartner C, Lupinek C, Weghofer M, Bennett KL, Herrmann H, Schebesta A, Thomas WR, Vrtala S, Valenta R, Lee FY, Ellmeier W, Superti-Furga G, Valent P: The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils. Blood. 2008 Mar 15;111(6):3097-107. doi: 10.1182/blood-2007-08-104372. Epub 2008 Jan 7. [PubMed:18180381]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Protein serine/threonine kinase activity
Specific Function
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK14 is one of the four p38 MAPKs which play an important role in the cascades of cellu...
Gene Name
MAPK14
Uniprot ID
Q16539
Uniprot Name
Mitogen-activated protein kinase 14
Molecular Weight
41292.885 Da
References
  1. Kneidinger M, Schmidt U, Rix U, Gleixner KV, Vales A, Baumgartner C, Lupinek C, Weghofer M, Bennett KL, Herrmann H, Schebesta A, Thomas WR, Vrtala S, Valenta R, Lee FY, Ellmeier W, Superti-Furga G, Valent P: The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils. Blood. 2008 Mar 15;111(6):3097-107. doi: 10.1182/blood-2007-08-104372. Epub 2008 Jan 7. [PubMed:18180381]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Metal ion binding
Specific Function
Not Available
Gene Name
PPAT
Uniprot ID
Q06203
Uniprot Name
Amidophosphoribosyltransferase
Molecular Weight
57398.52 Da
References
  1. Kneidinger M, Schmidt U, Rix U, Gleixner KV, Vales A, Baumgartner C, Lupinek C, Weghofer M, Bennett KL, Herrmann H, Schebesta A, Thomas WR, Vrtala S, Valenta R, Lee FY, Ellmeier W, Superti-Furga G, Valent P: The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils. Blood. 2008 Mar 15;111(6):3097-107. doi: 10.1182/blood-2007-08-104372. Epub 2008 Jan 7. [PubMed:18180381]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976]
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d 24-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976]
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976]
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1B1
Uniprot ID
Q16678
Uniprot Name
Cytochrome P450 1B1
Molecular Weight
60845.33 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976]
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976]
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Trimethylamine monooxygenase activity
Specific Function
Involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. It N-oxygenates primary aliphatic alkylamines as well as secondary and tertiary amines. Plays an impor...
Gene Name
FMO3
Uniprot ID
P31513
Uniprot Name
Dimethylaniline monooxygenase [N-oxide-forming] 3
Molecular Weight
60032.975 Da
References
  1. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Dohse M, Scharenberg C, Shukla S, Robey RW, Volkmann T, Deeken JF, Brendel C, Ambudkar SV, Neubauer A, Bates SE: Comparison of ATP-binding cassette transporter interactions with the tyrosine kinase inhibitors imatinib, nilotinib, and dasatinib. Drug Metab Dispos. 2010 Aug;38(8):1371-80. doi: 10.1124/dmd.109.031302. Epub 2010 Apr 27. [PubMed:20423956]
  2. Hegedus C, Ozvegy-Laczka C, Apati A, Magocsi M, Nemet K, Orfi L, Keri G, Katona M, Takats Z, Varadi A, Szakacs G, Sarkadi B: Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol. 2009 Oct;158(4):1153-64. doi: 10.1111/j.1476-5381.2009.00383.x. Epub 2009 Sep 28. [PubMed:19785662]
  3. Giannoudis A, Davies A, Lucas CM, Harris RJ, Pirmohamed M, Clark RE: Effective dasatinib uptake may occur without human organic cation transporter 1 (hOCT1): implications for the treatment of imatinib-resistant chronic myeloid leukemia. Blood. 2008 Oct 15;112(8):3348-54. doi: 10.1182/blood-2007-10-116236. Epub 2008 Jul 31. [PubMed:18669873]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Dohse M, Scharenberg C, Shukla S, Robey RW, Volkmann T, Deeken JF, Brendel C, Ambudkar SV, Neubauer A, Bates SE: Comparison of ATP-binding cassette transporter interactions with the tyrosine kinase inhibitors imatinib, nilotinib, and dasatinib. Drug Metab Dispos. 2010 Aug;38(8):1371-80. doi: 10.1124/dmd.109.031302. Epub 2010 Apr 27. [PubMed:20423956]
  2. Hegedus C, Ozvegy-Laczka C, Apati A, Magocsi M, Nemet K, Orfi L, Keri G, Katona M, Takats Z, Varadi A, Szakacs G, Sarkadi B: Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol. 2009 Oct;158(4):1153-64. doi: 10.1111/j.1476-5381.2009.00383.x. Epub 2009 Sep 28. [PubMed:19785662]

Drug created on May 08, 2007 18:32 / Updated on October 16, 2018 08:36