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Nilotinib


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
Pregnancy cat.	?
Legal status
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]

Additional recommended knowledge

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. 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

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Antimetabolites	Folic acid: (Aminopterin, Methotrexate, Pemetrexed, Raltitrexed). Purine:(Cladribine, Clofarabine, Fludarabine, Mercaptopurine, Pentostatin, Thioguanine). Pyrimidine:(Capecitabine, Cytarabine, Fluorouracil, Floxuridine, Gemcitabine)
Spindle poison/mitotic inhibitor	Taxane: (Docetaxel, Paclitaxel). Vinca: (Vinblastine, Vincristine, Vindesine, Vinorelbine).
Cytotoxic/antitumor antibiotics	Anthracycline family: (Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone, Valrubicin) - streptomyces (Actinomycin, Bleomycin, Mitomycin, Plicamycin) - Hydroxyurea
Topoisomerase inhibitors	Camptotheca: (Camptothecin, Topotecan, Irinotecan), Podophyllum:(Etoposide, Teniposide)
CI monoclonal antibodies	Receptor tyrosine kinase (Cetuximab, Panitumumab, Trastuzumab) - CD20 (Rituximab, Tositumomab) - other (Alemtuzumab, Bevacizumab, Gemtuzumab)
Photosensitizers	Aminolevulinic acid, Methyl aminolevulinate, Porfimer sodium, Verteporfin
Tyrosine kinase inhibitors	Dasatinib, Erlotinib, Gefitinib, Imatinib, Lapatinib, Nilotinib, Sorafenib, Sunitinib
Other	retinoids (Alitretinoin, Tretinoin) - Altretamine, Amsacrine, Anagrelide, Arsenic trioxide, Asparaginase (Pegaspargase), Bexarotene, Bortezomib, Denileukin diftitox, Estramustine, Ixabepilone, Masoprocol, Mitotane

Categories: Chemotherapeutic agents | Orphan drugs | Tyrosine kinase inhibitors

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Nilotinib". A list of authors is available in Wikipedia.

Nilotinib

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