Temozolomide

Generic Name
Temozolomide
Brand Names
Temodar, Temomedac, Temodal, Temozolomide Sun, Temozolomide Accord, Temozolomide Teva
Drug Type
Small Molecule
Chemical Formula
C6H6N6O2
CAS Number
85622-93-1
Unique Ingredient Identifier
YF1K15M17Y
Background

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. 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. 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. Temozomolide as an adjunct to radiotherapy followed by maintenance dosing remains the standard of care for both Glioblastoma and refractory anaplastic astrocytoma.

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.

Indication

Temozolomide is indicated in adult patients for the treatment of newly diagnosed glioblastoma concomitantly with radiotherapy and for use as maintenance treatment thereafter. It is also indicated for the treatment of refractory anaplastic astrocytoma in adult patients or adjuvant therapy for adults with newly diagnosed anaplastic astrocytoma.

Associated Conditions
Advanced Melanoma, High Grade Glioma: Glioblastoma (GBM), Primary Central Nervous System Lymphoma, Refractory Ewing Sarcoma, Refractory Neuroblastoma, Soft Tissue Sarcoma, Advanced Neuroendocrine tumor, Newly diagnosed Anaplastic Astrocytoma (AA), Refractory Anaplastic astrocytoma, Refractory, advanced Mycosis fungoides, Refractory, advanced Sezary Syndrome
Associated Therapies
-

Randomized Trial of ATN-224 and Temozolomide in Advanced Melanoma

Phase 2
Conditions
First Posted Date
2006-10-04
Last Posted Date
2007-12-06
Lead Sponsor
Attenuon
Target Recruit Count
60
Registration Number
NCT00383851
Locations
🇺🇸

Cancer Center of the Carolinas, Greenville, South Carolina, United States

🇺🇸

Hematology and Oncology Specialists, LLC, Metairie, Louisiana, United States

🇺🇸

Center for Cancer and Blood Disorders, Bethesda, Maryland, United States

and more 14 locations

Radiation Boost for Newly Diagnosed Glioblastoma Multiforme

Phase 1
Terminated
Conditions
First Posted Date
2006-09-14
Last Posted Date
2009-09-18
Lead Sponsor
Methodist Healthcare
Target Recruit Count
3
Registration Number
NCT00376103
Locations
🇺🇸

Methodist University Hospital, Memphis, Tennessee, United States

Phase II Study of Temozolomide in Newly Diagnosed Glioblastoma

Phase 2
Terminated
Conditions
Interventions
First Posted Date
2006-08-17
Last Posted Date
2009-01-22
Lead Sponsor
H. Lee Moffitt Cancer Center and Research Institute
Target Recruit Count
1
Registration Number
NCT00365222
Locations
🇺🇸

H. Lee Moffitt Cancer Center & Research Institute, Tampa, Florida, United States

Temozolomide in Patients With Newly Diagnosed Anaplastic Oligodendroglioma and Mixed Oligoastrocytoma

First Posted Date
2006-08-10
Last Posted Date
2017-11-30
Lead Sponsor
Ohio State University Comprehensive Cancer Center
Target Recruit Count
1
Registration Number
NCT00362570
Locations
🇺🇸

Ohio State University, Columbus, Ohio, United States

Carboplatin and Temozolomide (Temodar) for Recurrent and Symptomatic Residual Brain Metastases

First Posted Date
2006-08-10
Last Posted Date
2017-06-01
Lead Sponsor
Ohio State University Comprehensive Cancer Center
Target Recruit Count
17
Registration Number
NCT00362817
Locations
🇺🇸

Ohio State University, Columbus, Ohio, United States

Cisplatin and Temozolomide in Treating Young Patients With Malignant Glioma

First Posted Date
2006-08-07
Last Posted Date
2013-09-17
Lead Sponsor
Children's Cancer and Leukaemia Group
Target Recruit Count
87
Registration Number
NCT00360945
Locations
🇬🇧

Birmingham Children's Hospital, Birmingham, England, United Kingdom

🇬🇧

Royal Aberdeen Children's Hospital, Aberdeen, Scotland, United Kingdom

🇫🇷

Institut Gustave Roussy, Villejuif, France

and more 19 locations

Imatinib Mesylate and Temozolomide in Treating Patients With Malignant Glioma

Phase 1
Completed
Conditions
First Posted Date
2006-07-20
Last Posted Date
2013-03-28
Lead Sponsor
Duke University
Target Recruit Count
65
Registration Number
NCT00354068
Locations
🇺🇸

Duke Cancer Institute, Durham, North Carolina, United States

Randomised Study to Compare the Efficacy of AZD6244 vs TMZ

Phase 2
Completed
Conditions
Interventions
First Posted Date
2006-06-20
Last Posted Date
2014-08-13
Lead Sponsor
AstraZeneca
Target Recruit Count
239
Registration Number
NCT00338130
Locations
🇬🇧

Research Site, Oxford, United Kingdom

Efficacy and Safety of Temodal vs Semustine in Subjects With Recurrent Glioblastoma or Anaplastic Astrocytoma (Study P03644)

Phase 3
Completed
Conditions
Interventions
First Posted Date
2006-06-08
Last Posted Date
2017-05-15
Lead Sponsor
Merck Sharp & Dohme LLC
Target Recruit Count
151
Registration Number
NCT00335075

Phase II Feasibility Study of Dendritic Cell Vaccination for Newly Diagnosed Glioblastoma Multiforme

First Posted Date
2006-05-09
Last Posted Date
2018-10-10
Lead Sponsor
Dartmouth-Hitchcock Medical Center
Target Recruit Count
11
Registration Number
NCT00323115
Locations
🇺🇸

Dartmouth-Hitchcock Medical Center, Lebanon, New Hampshire, United States

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