Nilotinib

DB04868

small molecule approved investigational

Deskripsi

Nilotinib, also known as AMN107, is a tyrosine kinase inhibitor under investigation as a possible treatment for chronic myelogenous leukemia (CML). A Phase I clinical trial in 2006 showed that this drug was relatively safe and offered significant therapeutic benefits in cases of CML which were found to be resistant to treatment with imatinib (Gleevec), another tyrosine kinase inhibitor used as a first-line treatment for CML.

Struktur Molekul 2D

Berat 529.5158
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 15 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Orally available

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Farmakogenomik

1 Varian
UGT1A1 (rs8175347)

Patients who carry this polymorphism in UGT1A1 are at a higer risk of developing hyperbilirubinemia when treated with nilotinib.

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of nilotinib, causing increased serum levels of nilotinib.
  • 2. Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of nilotinib.
  • 3. Take on an empty stomach. Food increases the AUC of nilotinib. Separate nilotinib administration from meals by at least one hour before and two hours after eating.

Interaksi Obat

1691 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Nilotinib.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Nilotinib.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Nilotinib.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Nilotinib.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Nilotinib.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Nilotinib.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Nilotinib.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Nilotinib.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Nilotinib.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Nilotinib.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Nilotinib.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Nilotinib.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Nilotinib.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Nilotinib.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Nilotinib.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Nilotinib.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Nilotinib.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Nilotinib.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Nilotinib.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Nilotinib.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Nilotinib.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Nilotinib.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Nilotinib.
Cladribine The excretion of Cladribine can be decreased when combined with Nilotinib.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Nilotinib.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Nilotinib.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Nilotinib.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Nilotinib.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Nilotinib.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Nilotinib.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Nilotinib.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Nilotinib.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Nilotinib.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Nilotinib.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Nilotinib.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Nilotinib.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Nilotinib.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Nilotinib.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Nilotinib.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Nilotinib.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Nilotinib.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Nilotinib.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Nilotinib.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Nilotinib.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Nilotinib.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Nilotinib.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Nilotinib.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Nilotinib.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Nilotinib.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Nilotinib.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Nilotinib.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Nilotinib.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Nilotinib.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Nilotinib.
Thalidomide The metabolism of Thalidomide can be decreased when combined with Nilotinib.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Nilotinib.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Nilotinib.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Nilotinib.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Nilotinib.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Nilotinib.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Nilotinib.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Nilotinib.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Nilotinib.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Nilotinib.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Nilotinib.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Nilotinib.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Nilotinib.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Nilotinib.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Nilotinib.
Pirfenidone The risk or severity of adverse effects can be increased when Nilotinib is combined with Pirfenidone.
Interferon alfa The risk or severity of adverse effects can be increased when Nilotinib is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Nilotinib is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Nilotinib is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Nilotinib is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Nilotinib is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Nilotinib is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Nilotinib is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Nilotinib is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Nilotinib is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Nilotinib is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Nilotinib is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Nilotinib is combined with Teriflunomide.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Nilotinib is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Nilotinib is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Nilotinib is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Nilotinib is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Nilotinib is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Nilotinib is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Nilotinib is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Nilotinib is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Nilotinib is combined with Tepoxalin.
Ixekizumab The risk or severity of adverse effects can be increased when Nilotinib is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Nilotinib is combined with Ravulizumab.
Pirarubicin The risk or severity of adverse effects can be increased when Nilotinib is combined with Pirarubicin.
Peficitinib The risk or severity of adverse effects can be increased when Nilotinib is combined with Peficitinib.
Brodalumab The risk or severity of adverse effects can be increased when Nilotinib is combined with Brodalumab.
Sirukumab The risk or severity of adverse effects can be increased when Nilotinib is combined with Sirukumab.
Guselkumab The risk or severity of adverse effects can be increased when Nilotinib is combined with Guselkumab.
Ocrelizumab The risk or severity of adverse effects can be increased when Nilotinib is combined with Ocrelizumab.
Triptolide The risk or severity of adverse effects can be increased when Nilotinib is combined with Triptolide.

Target Protein

Tyrosine-protein kinase ABL1 ABL1
Mast/stem cell growth factor receptor Kit KIT

Referensi & Sumber

Synthesis reference: Yanling WANG, Jie LI, Vinod Kumar KANSAL, Jirang ZHU, Revital LIFSHITZ-LIRON, Dhirenkumar N. MISTRY, Sanjay L. VASOYA, Sundaraselvan ARIYAMUTHU, Gideon PILARSKI, Xungui HE, "NILOTINIB INTERMEDIATES AND PREPARATION THEREOF." U.S. Patent US20100016590, issued January 21, 2010.
Artikel (PubMed)
  • PMID: 16775235
    Kantarjian H, Giles F, Wunderle L, Bhalla K, O'Brien S, Wassmann B, Tanaka C, Manley P, Rae P, Mietlowski W, Bochinski K, Hochhaus A, Griffin JD, Hoelzer D, Albitar M, Dugan M, Cortes J, Alland L, Ottmann OG: Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL. N Engl J Med. 2006 Jun 15;354(24):2542-51.
  • PMID: 17929114
    Maekawa T, Ashihara E, Kimura S: The Bcr-Abl tyrosine kinase inhibitor imatinib and promising new agents against Philadelphia chromosome-positive leukemias. Int J Clin Oncol. 2007 Oct;12(5):327-40. Epub 2007 Oct 22.
  • PMID: 17890849
    Breccia M, Cannella L, Nanni M, Stefanizzi C, Alimena G: Nilotinib can override dasatinib resistance in chronic myeloid leukemia patients with secondary resistance to imatinib first-line therapy. Acta Haematol. 2007;118(3):162-4. Epub 2007 Sep 20.
  • PMID: 17715389
    Kantarjian HM, Giles F, Gattermann N, Bhalla K, Alimena G, Palandri F, Ossenkoppele GJ, Nicolini FE, O'Brien SG, Litzow M, Bhatia R, Cervantes F, Haque A, Shou Y, Resta DJ, Weitzman A, Hochhaus A, le Coutre P: Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is effective in patients with Philadelphia chromosome-positive chronic myelogenous leukemia in chronic phase following imatinib resistance and intolerance. Blood. 2007 Nov 15;110(10):3540-6. Epub 2007 Aug 22.
  • PMID: 17642017
    Jabbour E, Cortes J, Giles F, O'Brien S, Kantarijan H: Drug evaluation: Nilotinib - a novel Bcr-Abl tyrosine kinase inhibitor for the treatment of chronic myelocytic leukemia and beyond. IDrugs. 2007 Jul;10(7):468-79.

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