Peringatan Keamanan

Decitabine has demonstrated mutagenic potential in L5178Y mouse lymphoma cells and an Escherichia coil lac-I transgene within the colonic DNA of mice. Decitabine treatment increased chromosomal rearrangements in fruit fly larvae. In mouse models, decitabine exposure in utero (approximately 7% of the recommended daily dose) resulted in decreased weight and decreased male fertility. Adult male mice administered with between 0.3 and 1% of the recommended daily dose of decitabine three times a week for seven weeks had smaller testes with abnormal histology, decreased sperm count, and decreased fertility.L14962

There is no known antidote for decitabine overdose. Patients experiencing an overdose are at an increased risk of severe adverse effects such as myelosuppression, including prolonged and severe neutropenia and thrombocytopenia. Symptomatic and supportive measures are recommended.L14962

Decitabine

DB01262

small molecule approved investigational

Deskripsi

Myelodysplastic syndromes (MDS) are a heterogeneous group of hematopoietic neoplasms with variable underlying etiology and presentation, including neutropenia and thrombocytopenia. Further mutations leading to increased proliferation of cancerous cells can eventually lead to secondary acute myeloid leukemia, which has a poor prognosis.A215082, A215092 Among treatment options, nucleoside analogues such as decitabine and azacitidine integrate into cellular DNA and inhibit the action of DNA methyltransferases, leading to global hypomethylation and related downstream therapeutic benefits.A2263, A2264, A2265, A215317, L14962

Decitabine was developed by MGI Pharma/SuperGen Inc. and was approved by the FDA for the treatment of MDS on February 5, 2006. It was first marketed under the name Dacogen®.L14962 It is also available as an oral combination product together with the cytidine deaminase inhibitor cedazuridine.

Struktur Molekul 2D

Berat 228.2053
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Decitabine has a half-life of 0.62 hours (49% CV) when administered intravenously at 15 mg/m<sup>2</sup> for three hours every eight hours over three days, and a half-life of 0.54 hours (43% CV) at 20 mg/m<sup>2</sup> for one hour once daily over five days.[L14962]
Volume Distribusi Decitabine as an apparent volume of distribution of 4.59 ± 1.42 L/kg.[A2264]
Klirens (Clearance) Decitabine has a clearance of 125 L/hr/m<sup>2</sup> (53% CV) when administered intravenously at 15 mg/m<sup>2</sup> for three hours every eight hours over three days, and a clearance of 210 L/hr/m<sup>2</sup> (47% CV) at 20 mg/m<sup>2</sup> for one hour once daily over five days.[L14962]

Absorpsi

Decitabine administered intravenously at 15 mg/m2 for three hours every eight hours over three days resulted in a Cmax of 73.8 ng/mL (66% coefficient of variation, CV), an AUC0-? of 163 ng\*h/mL (62% CV), and a cumulative AUC of 1332 ng\*h/mL (95% CI of 1010-1730).L14962 Similarly, decitabine at 20 mg/m2 for one hour once daily over five days resulted in a Cmax of 147 ng/mL (49% CV), an AUC0-? of 115 ng\*h/mL (43% CV), and a cumulative AUC of 570 ng\*h/mL (95% CI of 470-700).L14962

Metabolisme

Decitabine is phosphorylated inside cells by the sequential action of deoxycytidine kinase, nucleotide monophosphate kinase, and nucleotide diphosphate kinase, prior to being incorporated into newly synthesized DNA by DNA polymerase.A2263, A2266, A2267, A215317 Decitabine not incorporated into cellular DNA undergoes deamination by cytidine deaminase followed by additional degradation prior to excretion.A2263, A2266, A215317

Rute Eliminasi

Less than 1% of administered decitabine is excreted in the urine.A2264

Interaksi Obat

526 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Decitabine.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Decitabine.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Decitabine.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Decitabine.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Decitabine.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Decitabine.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Decitabine.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Decitabine.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Decitabine.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Decitabine.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Decitabine.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Decitabine.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Decitabine.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Decitabine.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Decitabine.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Decitabine.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Decitabine.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Decitabine.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Decitabine.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Decitabine.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Decitabine.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Decitabine.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Decitabine.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Decitabine.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Decitabine.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Decitabine.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Decitabine.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Decitabine.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Decitabine.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Decitabine.
Cladribine Decitabine may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Decitabine.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Decitabine.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Decitabine.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Decitabine.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Decitabine.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Decitabine.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Decitabine.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Decitabine.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Decitabine.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Decitabine.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Decitabine.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Decitabine.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Decitabine.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Decitabine.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Decitabine.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Decitabine.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Decitabine.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Decitabine.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Decitabine.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Decitabine.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Decitabine.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Decitabine.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Decitabine.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Decitabine.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Decitabine.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Decitabine.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Decitabine.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Decitabine.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Decitabine.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Decitabine.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Decitabine.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Decitabine.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Decitabine.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Decitabine.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Decitabine.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Decitabine.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Decitabine.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Decitabine.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Decitabine.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Decitabine.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Decitabine.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Decitabine.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Decitabine.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Decitabine.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Decitabine.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Decitabine.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Decitabine.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Decitabine.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Decitabine.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Decitabine.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Decitabine.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Decitabine.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Decitabine.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Decitabine.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Decitabine.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Decitabine.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Decitabine.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Decitabine.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Decitabine.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Decitabine.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Decitabine.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Decitabine.
Doxorubicin The risk or severity of adverse effects can be increased when Doxorubicin is combined with Decitabine.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Decitabine.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Decitabine.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Decitabine.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Decitabine.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Decitabine.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Decitabine.

Target Protein

DNA
DNA (cytosine-5)-methyltransferase 1 DNMT1
DNA (cytosine-5)-methyltransferase 3A DNMT3A
DNA (cytosine-5)-methyltransferase 3B DNMT3B
Histone deacetylase HDAC1

Referensi & Sumber

Synthesis reference: Julian Paul Henschke, Xiaoheng Zhang, Jianbo Yu, Kun Hu, Lijun Mei, "Synthesis of Decitabine." U.S. Patent US20100087637, issued April 08, 2010.
Artikel (PubMed)
  • PMID: 17925555
    Appleton K, Mackay HJ, Judson I, Plumb JA, McCormick C, Strathdee G, Lee C, Barrett S, Reade S, Jadayel D, Tang A, Bellenger K, Mackay L, Setanoians A, Schatzlein A, Twelves C, Kaye SB, Brown R: Phase I and pharmacodynamic trial of the DNA methyltransferase inhibitor decitabine and carboplatin in solid tumors. J Clin Oncol. 2007 Oct 10;25(29):4603-9.
  • PMID: 17881052
    Wijermans PW, Ruter B, Baer MR, Slack JL, Saba HI, Lubbert M: Efficacy of decitabine in the treatment of patients with chronic myelomonocytic leukemia (CMML). Leuk Res. 2008 Apr;32(4):587-91. Epub 2007 Sep 18.
  • PMID: 20072836
    Daskalakis M, Blagitko-Dorfs N, Hackanson B: Decitabine. Recent Results Cancer Res. 2010;184:131-57. doi: 10.1007/978-3-642-01222-8_10.
  • PMID: 16015501
    Saba HI, Wijermans PW: Decitabine in myelodysplastic syndromes. Semin Hematol. 2005 Jul;42(3 Suppl 2):S23-31.
  • PMID: 18398832
    Jabbour E, Issa JP, Garcia-Manero G, Kantarjian H: Evolution of decitabine development: accomplishments, ongoing investigations, and future strategies. Cancer. 2008 Jun;112(11):2341-51. doi: 10.1002/cncr.23463.
  • PMID: 18425818
    Stresemann C, Lyko F: Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine. Int J Cancer. 2008 Jul 1;123(1):8-13. doi: 10.1002/ijc.23607.
  • PMID: 17023173
    Oki Y, Aoki E, Issa JP: Decitabine--bedside to bench. Crit Rev Oncol Hematol. 2007 Feb;61(2):140-52. Epub 2006 Oct 4.
  • PMID: 29455551
    Seelan RS, Mukhopadhyay P, Pisano MM, Greene RM: Effects of 5-Aza-2'-deoxycytidine (decitabine) on gene expression. Drug Metab Rev. 2018 May;50(2):193-207. doi: 10.1080/03602532.2018.1437446. Epub 2018 Feb 18.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 46 • International brands: 0
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