Vorinostat

DB02546

small molecule approved investigational

Deskripsi

Vorinostat (rINN) or suberoylanilide hydroxamic acid (SAHA), is a drug currently under investigation for the treatment of cutaneous T cell lymphoma (CTCL), a type of skin cancer, to be used when the disease persists, gets worse, or comes back during or after treatment with other medicines. It is the first in a new class of agents known as histone deacetylase inhibitors. A recent study suggested that vorinostat also possesses some activity against recurrent glioblastoma multiforme, resulting in a median overall survival of 5.7 months (compared to 4 - 4.4 months in earlier studies). Further brain tumor trials are planned using combinations of vorinostat with other drugs.

Struktur Molekul 2D

Berat 264.3202
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 2 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

The major pathways of vorinostat metabolism involve glucuronidation and hydrolysis followed by ?-oxidation. Human serum levels of two metabolites, O-glucuronide of vorinostat and 4-anilino-4-oxobutanoic acid were measured. Both metabolites are pharmacologically inactive. Compared to vorinostat, the mean steady state serum exposures in humans of the O-glucuronide of vorinostat and 4-anilino-4-oxobutanoic acid were 4-fold and 13-fold higher, respectively. In vitro studies using human liver microsomes indicate negligible biotransformation by cytochromes P450 (CYP).

Rute Eliminasi

In vitro studies using human liver microsomes indicate negligible biotransformation by cytochromes P450 (CYP). Vorinostat is eliminated predominantly through metabolism with less than 1% of the dose recovered as unchanged drug in urine, indicating that renal excretion does not play a role in the elimination of vorinostat. However, renal excretion does not play a role in the elimination of vorinostat.

Interaksi Makanan

1 Data
  • 1. Take with food.

Interaksi Obat

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

Target Protein

Histone deacetylase 1 HDAC1
Histone deacetylase 2 HDAC2
Histone deacetylase 3 HDAC3
Histone deacetylase 6 HDAC6
Histone deacetylase 8 HDAC8
Acetoin utilization protein acuC1
Histone deacetylase HDAC1

Referensi & Sumber

Synthesis reference: Vinayak G. Gore, Madhukar S. Patil, Rahul A. Bhalerao, Hemant M. Mande, Sandeep G. Mekde, "PROCESS FOR THE PREPARATION OF VORINOSTAT." U.S. Patent US20110263712, issued October 27, 2011.
Artikel (PubMed)
  • PMID: 16928817
    Munshi A, Tanaka T, Hobbs ML, Tucker SL, Richon VM, Meyn RE: Vorinostat, a histone deacetylase inhibitor, enhances the response of human tumor cells to ionizing radiation through prolongation of gamma-H2AX foci. Mol Cancer Ther. 2006 Aug;5(8):1967-74.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Zolinza
    Capsule • 100 mg/1 • Oral • US • Approved
  • Zolinza
    Capsule • 100 mg • Oral • Canada • Approved

Sekuens Gen/Protein (FASTA)

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