Peringatan Keamanan

The primary dose-limiting toxicity of temozolomide is myelosuppression, which can occur with any dose but is more severe at higher doses. Patients taking high doses experienced adverse reactions, including severe and prolonged myelosuppression, infections, and death. One patient who took 2000 mg/day for five days experienced pancytopenia, pyrexia, and multi-organ failure, which resulted in death. Patients experiencing an overdose should have complete blood counts monitored and provided with supportive care as necessary.L32033

Temozolomide

DB00853

small molecule approved investigational

Deskripsi

Refractory anaplastic astrocytoma (WHO grade III) and Glioblastoma multiforme (WHO grade IV) are primary malignant brain tumours with poor prognosis and limited treatment options. Despite considerable genetic heterogeneity, these tumours often have impaired DNA repair systems, rendering them initially sensitive to alkylating agents, although they invariably develop resistance to these agents over time.A229848, A229858, L32033 Temozolomide is an imidazotetrazine prodrug that is stable at acidic pH but undergoes spontaneous nonenzymatic hydrolysis at neutral or slightly basic pH; these properties allow for both oral and intravenous administration.A229853, A229888, A229923, L32033 Following initial hydrolysis, further reactions liberate a highly reactive methyl diazonium cation capable of methylating various residues on adenosine and guanine bases leading to DNA lesions and eventual apoptosis.A229853, A229923 Temozomolide as an adjunct to radiotherapy followed by maintenance dosing remains the standard of care for both Glioblastoma and refractory anaplastic astrocytoma.L32033

Temozolomide was granted FDA approval on August 11, 1999, as an oral capsule and subsequently on February 27, 2009, as an intravenous injection. It is currently marketed under the trademark TEMODAR® by Merck.L32033

Struktur Molekul 2D

Berat 194.1508
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Temozolomide has a mean elimination half-life of 1.8 hours.[L32033]
Volume Distribusi Temozolomide has a mean apparent volume of distribution (%CV) of 0.4 (13%) L/kg.[L32033]
Klirens (Clearance) Temozolomide has a clearance of approximately 5.5 L/hr/m<sup>2</sup>.[L32033]

Absorpsi

Temozolomide is rapidly and completely absorbed in the gastrointestinal tract and is stable at both acidic and neutral pH. Therefore, temozolomide may be administered both orally and intravenously with a median Tmax of one hour. Following a single oral dose of 150 mg/m2, temozolomide and its active MTIC metabolite had Cmax values of 7.5 ?g/mL and 282 ng/mL and AUC values of 23.4 ?g\*hr/mL and 864 ng\*hr/mL, respectively. Similarly, following a single 90-minute IV infusion of 150 mg/m2, temozolide and its active MTIC metabolite had Cmax values of 7.3 ?g/mL and 276 ng/mL and AUC values of 24.6 ?g\*hr/mL and 891 ng\*hr/mL, respectively. Temozolomide kinetics are linear over the range of 75-250 mg/m2/day. The median Tmax is 1 hourL32033 Oral temozolomide absorption is affected by food. Administration following a high-fat breakfast of 587 calories caused the mean Cmax and AUC to decrease by 32% and 9%, respectively, and the median Tmax to increase by 2-fold (from 1-2.25 hours).L32033

Metabolisme

After absorption, temozolomide undergoes nonenzymatic chemical conversion to the active metabolite 5-(3-methyltriazen-1-yl) imidazole-4-carboxamide (MTIC) plus carbon dioxide and to a temozolomide acid metabolite, which occurs at physiological pH but is enhanced with increasing alkalinity.A229853, A229888, A229923 MTIC subsequently reacts with water to produce 5-aminoimidazole-4-carboxamide (AIC) and a highly reactive methyl diazonium cation, the active alkylating species.A229853, A229888, A229923 The cytochrome P450 system plays only a minor role in temozolomide metabolism. Relative to the AUC of temozolomide, the exposure to MTIC and AIC is 2.4% and 23%, respectively.L32033

Rute Eliminasi

Roughly 38% of administered temozolomide can be recovered over seven days, with 38% in the urine and only 0.8% in the feces. The recovered material comprises mainly metabolites: unidentified polar metabolites (17%), AIC (12%), and the temozolomide acid metabolite (2.3%). Only 6% of the recovered dose represents unchanged temozolomide.L32033

Interaksi Makanan

2 Data
  • 1. Take at the same time every day.
  • 2. Take on an empty stomach. Food reduces the absorption of temozolomide and taking it on an empty stomach may reduce temozolomide associated nausea and vomiting.

Interaksi Obat

1168 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Temozolomide.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Temozolomide.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Temozolomide.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Temozolomide.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Temozolomide.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Temozolomide.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Temozolomide.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Temozolomide.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Temozolomide.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Temozolomide.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Temozolomide.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Temozolomide.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Temozolomide.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Temozolomide.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Temozolomide.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Temozolomide.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Temozolomide.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Temozolomide.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Temozolomide.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Temozolomide.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Temozolomide.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Temozolomide.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Temozolomide.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Temozolomide.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Temozolomide.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Temozolomide.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Temozolomide.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Temozolomide.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Temozolomide.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Temozolomide.
Cladribine Temozolomide may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Temozolomide.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Temozolomide.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Temozolomide.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Temozolomide.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Temozolomide.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Temozolomide.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Temozolomide.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Temozolomide.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Temozolomide.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Temozolomide.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Temozolomide.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Temozolomide.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Temozolomide.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Temozolomide.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Temozolomide.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Temozolomide.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Temozolomide.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Temozolomide.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Temozolomide.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Temozolomide.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Temozolomide.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Temozolomide.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Temozolomide.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Temozolomide.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Temozolomide.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Temozolomide.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Temozolomide.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Temozolomide.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Temozolomide.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Temozolomide.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Temozolomide.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Temozolomide.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Temozolomide.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Temozolomide.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Temozolomide.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Temozolomide.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Temozolomide.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Temozolomide.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Temozolomide.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Temozolomide.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Temozolomide.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Temozolomide.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Temozolomide.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Temozolomide.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Temozolomide.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Temozolomide.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Temozolomide.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Temozolomide.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Temozolomide.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Temozolomide is combined with Penicillamine.
Prednisolone The risk or severity of adverse effects can be increased when Temozolomide is combined with Prednisolone.
Mechlorethamine The risk or severity of adverse effects can be increased when Temozolomide is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Temozolomide is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Temozolomide is combined with Carboplatin.
Methylprednisolone The risk or severity of adverse effects can be increased when Temozolomide is combined with Methylprednisolone.
Dactinomycin The risk or severity of adverse effects can be increased when Temozolomide is combined with Dactinomycin.
Cytarabine The risk or severity of adverse effects can be increased when Temozolomide is combined with Cytarabine.
Azathioprine The risk or severity of adverse effects can be increased when Temozolomide is combined with Azathioprine.
Doxorubicin The risk or severity of adverse effects can be increased when Temozolomide is combined with Doxorubicin.
Hydroxyurea The risk or severity of adverse effects can be increased when Temozolomide is combined with Hydroxyurea.
Mycophenolic acid The risk or severity of adverse effects can be increased when Temozolomide is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Temozolomide is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Temozolomide is combined with Mercaptopurine.
Thalidomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Temozolomide is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Temozolomide is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Temozolomide is combined with Flucytosine.
Capecitabine The risk or severity of adverse effects can be increased when Temozolomide is combined with Capecitabine.

Target Protein

DNA

Referensi & Sumber

Synthesis reference: Shen-Chun Kuo, "Synthesis of temozolomide and analogs." U.S. Patent US20020133006, issued September 19, 2002.
Artikel (PubMed)
  • PMID: 20564393
    Neyns B, Tosoni A, Hwu WJ, Reardon DA: Dose-dense temozolomide regimens: antitumor activity, toxicity, and immunomodulatory effects. Cancer. 2010 Jun 15;116(12):2868-77. doi: 10.1002/cncr.25035.
  • PMID: 18772354
    Wick W, Platten M, Weller M: New (alternative) temozolomide regimens for the treatment of glioma. Neuro Oncol. 2009 Feb;11(1):69-79. doi: 10.1215/15228517-2008-078. Epub 2008 Sep 4.
  • PMID: 19543728
    Villano JL, Seery TE, Bressler LR: Temozolomide in malignant gliomas: current use and future targets. Cancer Chemother Pharmacol. 2009 Sep;64(4):647-55. doi: 10.1007/s00280-009-1050-5. Epub 2009 Jun 19.
  • PMID: 20455691
    Meije Y, Lizasoain M, Garcia-Reyne A, Martinez P, Rodriguez V, Lopez-Medrano F, Juan RS, Lalueza A, Aguado JM: Emergence of cytomegalovirus disease in patients receiving temozolomide: report of two cases and literature review. Clin Infect Dis. 2010 Jun 15;50(12):e73-6. doi: 10.1086/653011.
  • PMID: 19435405
    Trinh VA, Patel SP, Hwu WJ: The safety of temozolomide in the treatment of malignancies. Expert Opin Drug Saf. 2009 Jul;8(4):493-9. doi: 10.1517/14740330902918281 .
  • PMID: 10866347
    Yung WK: Temozolomide in malignant gliomas. Semin Oncol. 2000 Jun;27(3 Suppl 6):27-34.
  • PMID: 10914698
    Friedman HS, Kerby T, Calvert H: Temozolomide and treatment of malignant glioma. Clin Cancer Res. 2000 Jul;6(7):2585-97.
  • PMID: 16925485
    Mutter N, Stupp R: Temozolomide: a milestone in neuro-oncology and beyond? Expert Rev Anticancer Ther. 2006 Aug;6(8):1187-204.
Menampilkan 8 dari 16 artikel.

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