Peringatan Keamanan

Ibrutinib was not showed to present a mutagenic potential in bacterial assays, nor clastogenic in chromosome aberration assays in mammalian cells or in bone marrow micronucleus assays in mice. Carcinogenicity or effects on fertility have not been determined.L12228

Ibrutinib

DB09053

small molecule approved

Deskripsi

Ibrutinib is a small molecule that acts as an irreversible potent inhibitor of Burton's tyrosine kinase. It is designated as a targeted covalent drug and presented as a promising activity in B-cell malignancies in clinical trials.A32299 Ibrutinib was developed by Pharmacyclics Inc and was first approved by the FDA in November 2013 for the treatment of mantle cell lymphoma (MCL) under accelerated approval;L12228 however, in April 2023, the drug manufacturer withdrew the accelerated approvals for ibrutinib in the US.L45894

Ibrutinib was approved by the EMA in October 2014 L45884 and by Health Canada in November 2014.L45889 It is currently approved for the treatment of various conditions, such as chronic lymphocytic leukemia (CLL), Waldenström's Macroglobulinemia, and chronic graft versus host disease (cGVHD) in August 2017.L12228 Notably, ibrutinib became the first FDA-approved cGVHD treatment for children in August 2017.L43020

Struktur Molekul 2D

Berat 440.507
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of ibrutinib is of approximately 4-6 hours.[T148]
Volume Distribusi The volume of distribution at steady-state of ibrutinib is in approximately 10,000 L.[T148]
Klirens (Clearance) In patients with normal renal function, the clearance rate is in the range of 112-159 ml/min.[A7663]

Absorpsi

Ibrutinib is rapidly absorbed after oral administration and it presents a Cmax, tmax and AUC of approximately 35 ng/ml, 1-2 hour and 953 mg.h/ml respectively.T148

Metabolisme

Three metabolic pathways have been identified according to the possible metabolites. These pathways are the hydroxylation of the phenyl group (M35), the opening of the piperidine with a reduction of the primary alcohol (M34) and the oxidation to a carboxylic acid and epoxidation of the ethylene followed by a hydrolysis to the formation of dihydrodiol (PCI-45227). The latter metabolite presents also 15 times lower inhibitory activity against BTK. The metabolism of ibrutinib is mainly performed by CYP3A5 and CYP3A4. and in a minor extent it is seen to be performed by CYP2D6.A7663

Rute Eliminasi

The cumulative excretion of ibrutinib in urine is of about 7.8% of the administered dose and most of this excretion is found during the first 24 hours after administration. In feces, the cumulative excretion accounts for 80% of the administered dose and the excretion occurs within 48 hours of the initial administration. The total excretion of ibrutinib during the first 168 hours after initial administration accounts for 88.5% of the administered dose.A7663

Interaksi Makanan

4 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of ibrutinib.
  • 2. Avoid St. John's Wort. This herb induces CYP3A4 and may reduce the serum concentration of ibrutinib.
  • 3. Take at the same time every day.
  • 4. Take with a full glass of water.

Interaksi Obat

1111 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Ibrutinib.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Ibrutinib.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Ibrutinib.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Ibrutinib.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Ibrutinib.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Ibrutinib.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Ibrutinib.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Ibrutinib.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Ibrutinib.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Ibrutinib.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Ibrutinib.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Ibrutinib.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Ibrutinib.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Ibrutinib.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Ibrutinib.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Ibrutinib.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Ibrutinib.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Ibrutinib.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Ibrutinib.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Ibrutinib.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Ibrutinib.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Ibrutinib.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Ibrutinib.
Cladribine Ibrutinib may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Ibrutinib.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Ibrutinib.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Ibrutinib.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Ibrutinib.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Ibrutinib.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Ibrutinib.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Ibrutinib.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Ibrutinib.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Ibrutinib.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Ibrutinib.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Ibrutinib.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Ibrutinib.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Ibrutinib.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Ibrutinib.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Ibrutinib.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Ibrutinib.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Ibrutinib.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Ibrutinib.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Ibrutinib.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Ibrutinib.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Ibrutinib.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Ibrutinib.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Ibrutinib.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Ibrutinib.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Ibrutinib.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Ibrutinib.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Ibrutinib.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Ibrutinib.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Ibrutinib.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Ibrutinib.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Ibrutinib.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Ibrutinib.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Ibrutinib.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Ibrutinib.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Ibrutinib.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Ibrutinib.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Ibrutinib.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Ibrutinib.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Ibrutinib.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Ibrutinib.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Ibrutinib.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Ibrutinib.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Ibrutinib.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Ibrutinib.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Ibrutinib.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Ibrutinib.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Ibrutinib.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Ibrutinib.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Ibrutinib.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Ibrutinib.
Belinostat The risk or severity of adverse effects can be increased when Belinostat is combined with Ibrutinib.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Ibrutinib.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Ibrutinib.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Ibrutinib.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Ibrutinib.
Mepolizumab The risk or severity of adverse effects can be increased when Mepolizumab is combined with Ibrutinib.
Abetimus The risk or severity of adverse effects can be increased when Abetimus is combined with Ibrutinib.
Belatacept The risk or severity of adverse effects can be increased when Belatacept is combined with Ibrutinib.
Bendamustine The risk or severity of adverse effects can be increased when Bendamustine is combined with Ibrutinib.
Pralatrexate The risk or severity of adverse effects can be increased when Pralatrexate is combined with Ibrutinib.
Wortmannin The risk or severity of adverse effects can be increased when Wortmannin is combined with Ibrutinib.
Eribulin The risk or severity of adverse effects can be increased when Eribulin is combined with Ibrutinib.
Belimumab The risk or severity of adverse effects can be increased when Belimumab is combined with Ibrutinib.
Teriflunomide The risk or severity of adverse effects can be increased when Teriflunomide is combined with Ibrutinib.
Carfilzomib The risk or severity of adverse effects can be increased when Carfilzomib is combined with Ibrutinib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Dimethyl fumarate is combined with Ibrutinib.
Obinutuzumab The risk or severity of adverse effects can be increased when Obinutuzumab is combined with Ibrutinib.
Vedolizumab The risk or severity of adverse effects can be increased when Vedolizumab is combined with Ibrutinib.
Blinatumomab The risk or severity of adverse effects can be increased when Blinatumomab is combined with Ibrutinib.
Dinutuximab The risk or severity of adverse effects can be increased when Ibrutinib is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Ibrutinib is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Ibrutinib is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Ibrutinib is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Ibrutinib is combined with Tepoxalin.
Ixekizumab The risk or severity of adverse effects can be increased when Ibrutinib is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Ibrutinib is combined with Ravulizumab.

Target Protein

Tyrosine-protein kinase BTK BTK

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25892147
    Bagcchi S: Ibrutinib in pretreated Waldenstrom's macroglobulinaemia. Lancet Oncol. 2015 May;16(5):e204. doi: 10.1016/S1470-2045(15)70185-3. Epub 2015 Apr 16.
  • PMID: 25802231
    Kim ES, Dhillon S: Ibrutinib: a review of its use in patients with mantle cell lymphoma or chronic lymphocytic leukaemia. Drugs. 2015 May;75(7):769-76. doi: 10.1007/s40265-015-0380-3.
  • PMID: 25488930
    Scheers E, Leclercq L, de Jong J, Bode N, Bockx M, Laenen A, Cuyckens F, Skee D, Murphy J, Sukbuntherng J, Mannens G: Absorption, metabolism, and excretion of oral (1)(4)C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos. 2015 Feb;43(2):289-97. doi: 10.1124/dmd.114.060061. Epub 2014 Dec 8.
  • PMID: 26111359
    Berglof A, Hamasy A, Meinke S, Palma M, Krstic A, Mansson R, Kimby E, Osterborg A, Smith CI: Targets for Ibrutinib Beyond B Cell Malignancies. Scand J Immunol. 2015 Sep;82(3):208-17. doi: 10.1111/sji.12333.
  • PMID: 23188619
    Sellner L, Denzinger S, Dietrich S, Glimm H, Merkel O, Dreger P, Zenz T: What do we do with chronic lymphocytic leukemia with 17p deletion? Curr Hematol Malig Rep. 2013 Mar;8(1):81-90. doi: 10.1007/s11899-012-0143-0.
  • PMID: 24941982
    Davids MS, Brown JR: Ibrutinib: a first in class covalent inhibitor of Bruton's tyrosine kinase. Future Oncol. 2014 May;10(6):957-67. doi: 10.2217/fon.14.51.
  • PMID: 23045577
    Advani RH, Buggy JJ, Sharman JP, Smith SM, Boyd TE, Grant B, Kolibaba KS, Furman RR, Rodriguez S, Chang BY, Sukbuntherng J, Izumi R, Hamdy A, Hedrick E, Fowler NH: Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies. J Clin Oncol. 2013 Jan 1;31(1):88-94. doi: 10.1200/JCO.2012.42.7906. Epub 2012 Oct 8.
  • PMID: 23782158
    Byrd JC, Furman RR, Coutre SE, Flinn IW, Burger JA, Blum KA, Grant B, Sharman JP, Coleman M, Wierda WG, Jones JA, Zhao W, Heerema NA, Johnson AJ, Sukbuntherng J, Chang BY, Clow F, Hedrick E, Buggy JJ, James DF, O'Brien S: Targeting BTK with ibrutinib in relapsed chronic lymphocytic leukemia. N Engl J Med. 2013 Jul 4;369(1):32-42. doi: 10.1056/NEJMoa1215637. Epub 2013 Jun 19.
Menampilkan 8 dari 10 artikel.
Textbook
  • Bronson J., Black A., Dhar M., Ellsworth B. and Merritt R. (2014). Annual reports in medicinal chemistry. Elsevier.

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