Peringatan Keamanan

The most common non-hematologic adverse reactions (? 20%) were hypertension, rash, abdominal pain, fatigue, headache, dry skin, constipation, arthralgia, nausea, and pyrexia. Hematologic adverse reactions included thrombocytopenia, anemia, neutropenia, lymphopenia, and leukopenia.

Ponatinib

DB08901

small molecule approved investigational

Deskripsi

Ponatinib is a novel Bcr-Abl tyrosine kinase inhibitor that is especially effective against the T315I mutation for the treatment of chronic myeloid leukemia. FDA approved on December 14, 2012.

Struktur Molekul 2D

Berat 532.5595
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) After oral administration of 45 mg ponatinib once daily for 28 days in cancer patients, the terminal elimination half-life is 24 hours (range of 12 - 66 hours).
Volume Distribusi After oral administration of 45 mg ponatinib once daily for 28 days in cancer patients, the steady state volume of distribution is 1223 L. Ponatinib is a weak substrate for P-gp and ABCG2.
Klirens (Clearance) -

Absorpsi

The absolute bioavailability of ponatinib is unknown. Peak concentrations of ponatinib are observed within 6 hours after Iclusig oral administration. Food does not affect absorption of food. The aqueous solubility of ponatinib is pH dependent, with higher pH resulting in lower solubility. When 45 mg of ponatinib is given to cancer patients, the pharmacokinetic parameters are as follows: Cmax = 73 ng/mL; AUC = 1253 ng•hr/mL;

Metabolisme

At least 64% of a ponatinib dose undergoes phase I and phase II metabolism. CYP3A4 and to a lesser extent CYP2C8, CYP2D6 and CYP3A5 are involved in the phase I metabolism of ponatinib in vitro. Ponatinib is also metabolized by esterases and/or amidases.

Rute Eliminasi

Ponatinib is mainly eliminated via feces. Following a single oral dose of 14C-labeled ponatinib, approximately 87% of the radioactive dose is recovered in the feces and approximately 5% in the urine.

Interaksi Makanan

3 Data
  • 1. Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of ponatinib and may reduce its serum concentration.
  • 2. Exercise caution with grapefruit products. If coadministration of ponatinib and grapefruit is necessary, reduce the dose of ponatinib.
  • 3. Take with or without food.

Interaksi Obat

1338 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Ponatinib.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Ponatinib.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Ponatinib.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Ponatinib.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Ponatinib.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Ponatinib.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Ponatinib.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Ponatinib.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Ponatinib.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Ponatinib.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Ponatinib.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Ponatinib.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Ponatinib.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Ponatinib.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Ponatinib.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Ponatinib.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Ponatinib.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Ponatinib.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Ponatinib.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Ponatinib.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Ponatinib.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Ponatinib.
Cladribine The excretion of Cladribine can be decreased when combined with Ponatinib.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Ponatinib.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Ponatinib.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Ponatinib.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Ponatinib.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Ponatinib.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Ponatinib.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Ponatinib.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Ponatinib.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Ponatinib.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Ponatinib.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Ponatinib.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Ponatinib.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Ponatinib.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Ponatinib.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Ponatinib.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Ponatinib.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Ponatinib.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Ponatinib.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Ponatinib.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Ponatinib.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Ponatinib.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Ponatinib.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Ponatinib.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Ponatinib.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Ponatinib.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Ponatinib.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Ponatinib.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Ponatinib.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Ponatinib.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Ponatinib.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Ponatinib.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Ponatinib.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Ponatinib.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Ponatinib.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Ponatinib.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Ponatinib.
Thalidomide The metabolism of Ponatinib can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Ponatinib.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Ponatinib.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Ponatinib.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Ponatinib.
Trilostane The risk or severity of adverse effects can be increased when Trilostane is combined with Ponatinib.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Ponatinib.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Ponatinib.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Ponatinib.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Ponatinib.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Ponatinib.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Ponatinib.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Ponatinib.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Ponatinib.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Ponatinib.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Ponatinib.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Ponatinib.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Ponatinib.
Thiotepa The risk or severity of adverse effects can be increased when Thiotepa is combined with Ponatinib.
Aldosterone The risk or severity of adverse effects can be increased when Aldosterone is combined with Ponatinib.
Ixabepilone The risk or severity of adverse effects can be increased when Ixabepilone is combined with Ponatinib.
Pirfenidone The metabolism of Ponatinib can be decreased when combined with Pirfenidone.
Belinostat The risk or severity of adverse effects can be increased when Belinostat is combined with Ponatinib.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Ponatinib.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Ponatinib.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Ponatinib.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Ponatinib.
Mepolizumab The risk or severity of adverse effects can be increased when Mepolizumab is combined with Ponatinib.
Abetimus The risk or severity of adverse effects can be increased when Abetimus is combined with Ponatinib.
Belatacept The risk or severity of adverse effects can be increased when Belatacept is combined with Ponatinib.
Pralatrexate The risk or severity of adverse effects can be increased when Pralatrexate is combined with Ponatinib.
Wortmannin The risk or severity of adverse effects can be increased when Wortmannin is combined with Ponatinib.
Eribulin The risk or severity of adverse effects can be increased when Eribulin is combined with Ponatinib.
Ruxolitinib The risk or severity of adverse effects can be increased when Ruxolitinib is combined with Ponatinib.
Belimumab The risk or severity of adverse effects can be increased when Belimumab is combined with Ponatinib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Ponatinib is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Ponatinib is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Ponatinib is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Ponatinib is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Ponatinib is combined with Dinutuximab.
Vilanterol The risk or severity of adverse effects can be increased when Ponatinib is combined with Vilanterol.

Target Protein

Tyrosine-protein kinase ABL1 ABL1
Breakpoint cluster region protein BCR
Mast/stem cell growth factor receptor Kit KIT
Proto-oncogene tyrosine-protein kinase receptor Ret RET
Angiopoietin-1 receptor TEK
Receptor-type tyrosine-protein kinase FLT3 FLT3
Fibroblast growth factor receptor 1 FGFR1
Fibroblast growth factor receptor 2 FGFR2
Fibroblast growth factor receptor 3 FGFR3
Fibroblast growth factor receptor 4 FGFR4
Tyrosine-protein kinase Lck LCK
Proto-oncogene tyrosine-protein kinase Src SRC
Tyrosine-protein kinase Lyn LYN
Vascular endothelial growth factor receptor 2 KDR
Platelet-derived growth factor receptor alpha PDGFRA

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23226582
    Reddy EP, Aggarwal AK: The ins and outs of bcr-abl inhibition. Genes Cancer. 2012 May;3(5-6):447-54. doi: 10.1177/1947601912462126.

Contoh Produk & Brand

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