Nilotinib in the form of the hydrochloride monohydrate salt, is a tyrosine kinase inhibitor approved for the treatment of chronic myelogenous leukemia

Chronic myelogenous leukemia

Chronic myelogenous leukemia , also known as chronic granulocytic leukemia , is a cancer of the white blood cells. It is a form of leukemia characterized by the increased and unregulated growth of predominantly myeloid cells in the bone marrow and the accumulation of these cells in the blood...

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Uses

It was approved as Tasigna in the USA and the EU for drug-resistant chronic myelogenous leukemia

Chronic myelogenous leukemia

Chronic myelogenous leukemia , also known as chronic granulocytic leukemia , is a cancer of the white blood cells. It is a form of leukemia characterized by the increased and unregulated growth of predominantly myeloid cells in the bone marrow and the accumulation of these cells in the blood...

 (CML). In June 2006, a Phase I clinical trial

Clinical trial

Clinical trials are a set of procedures in medical research and drug development that are conducted to allow safety and efficacy data to be collected for health interventions...

 found nilotinib has a relatively favorable safety profile and shows activity in cases of CML resistant to treatment with imatinib

Imatinib

Imatinib is a drug used to treat certain types of cancer. It is currently marketed by Novartis as Gleevec or Glivec as its mesylate salt, imatinib mesilate . It is used in treating chronic myelogenous leukemia , gastrointestinal stromal tumors and some other diseases...

 (Gleevec), another tyrosine kinase inhibitor currently used as a first-line treatment. In that study 92% of patients (already resistant or unresponsive to imatinib) achieved a normal white blood cell counts after five months of treatment.
The drug carries a black box warning for possible heart complications.

Pharmacology

Nilotinib inhibits the kinases BCR-ABL, KIT

CD117

Mast/stem cell growth factor receptor also known as proto-oncogene c-Kit or tyrosine-protein kinase Kit or CD117 is a protein that in humans is encoded by the KIT gene...

, LCK

Lck

Lck is a protein that is found inside specialized cells of the immune system called lymphocytes. Lck is a tyrosine kinase, which phosphorylates tyrosine residues of certain proteins involved in the intracellular signaling pathways of these lymphocytes...

, EPHA3

EPHA3

EPH receptor A3 is a protein that in humans is encoded by the EPHA3 gene.-Interactions:EPH receptor A3 has been shown to interact with EFNB2 and EFNA5.-Further reading:...

, EPHA8

EPHA8

Ephrin type-A receptor 8 is a protein that in humans is encoded by the EPHA8 gene.-Further reading:...

, DDR1

DDR1

For the older type of computer memory, see DDR SDRAM.Discoidin domain receptor family, member 1, also known as DDR1 or CD167a , is a human gene.-Further reading:...

, DDR2

DDR2

DDR2 may refer to:* DDR2 SDRAM, the computer memory technology* Dance Dance Revolution 2ndMix, the video game* DDR2 , a human gene...

, PDGFRB

PDGFRB

Beta-type platelet-derived growth factor receptor is a protein that in humans is encoded by the PDGFRB gene.-Interactions:PDGFRB has been shown to interact with PTPN11, NCK1, Grb2, Caveolin 1, PDGFRA, Sodium-hydrogen antiporter 3 regulator 1, RAS p21 protein activator 1, CRK, SHC1 and...

, MAPK11

MAPK11

Mitogen-activated protein kinase 11 is an enzyme that in humans is encoded by the MAPK11 gene.-Interactions:MAPK11 has been shown to interact with HDAC3 and Promyelocytic leukemia protein.-Further reading:...

 and ZAK

ZAK

Sterile alpha motif and leucine zipper containing kinase AZK, also known as ZAK, is a human gene.- Further reading :...

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