Nilotinib

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Nilotinib
Systematic (IUPAC) name
4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl) phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino] benzamide
Identifiers
CAS number	641571-10-0(base)
ATC code	?
PubChem	644241
Chemical data
Formula	C₂₈H₂₂F₃N₇O
Mol. mass	529.516 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Licence data	EU, US
Pregnancy cat.	?
Legal status	POM(UK) ℞-only(US)
Routes	Oral

Nilotinib, in the form of the hydrochloride monohydrate salt, is a tyrosine kinase inhibitor approved as Tasigna in the USA and the EU for drug-resistant chronic myelogenous leukemia (CML)^[1]. In June 2006, a Phase I clinical trial found nilotinib, also known by its clinical code AMN107, has a relatively favorable safety profile and shows activity in cases of CML resistant to treatment with imatinib (Gleevec), another tyrosine kinase inhibitor currently used as a first-line treatment.^[2] In that study 92% of patients (already resistant or unresponsive to Gleevec) achieved a normal white blood cell counts after 5 month of treatment. ^[3]

The drug will carry a black box warning for possible heart complications. ^[4]

[edit] References

^ Novartis 29/10/2007 Press Release.
^ Kantarjian H et al. (2006). "Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL". N Engl J Med 354 (24): 2542–51. doi:10.1056/NEJMoa055104. PMID 16775235.
^ http://cws.huginonline.com/N/134323/PR/200606/1056533_5.html Patients with treatment-resistant leukemia achieve high responses to Tasigna (nilotinib) in first published clinical trial results - Novartis 14/06/2006 Press Release.
^ http://www.fda.gov/bbs/topics/NEWS/2007/NEW01734.html FDA Approves Tasigna for Treatment of Philadelphia Chromosome Positive Chronic Myeloid Leukemia - FDA 31/10/2007 Press Release

v • d • e Chemotherapeutic agents/Antineoplastic agents (L01)

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Cytotoxic/antitumor antibiotics	Anthracycline family: (Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone, Pixantrone, Valrubicin) streptomyces (Actinomycin, Bleomycin, Mitomycin, Plicamycin) - Hydroxyurea

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Photosensitizers	Aminolevulinic acid, Methyl aminolevulinate, Porfimer sodium, Verteporfin

Tyrosine kinase inhibitors	Axitinib, Bosutinib, Cediranib, Dasatinib, Erlotinib, Gefitinib, Imatinib, Lapatinib, Lestaurtinib, Nilotinib, Semaxanib, Sorafenib, Sunitinib, Vandetanib

Cyclin-dependent kinase inhibitor	Seliciclib

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