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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
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Study of IV Edotecarin Vs Temozolomide or Carmustine (BCNU) or Lomustine (CCNU) in Patients With Glioblastoma Multiforme

Phase 3
Completed
Conditions
Glioblastoma
First Posted Date
2003-09-16
Last Posted Date
2008-04-01
Lead Sponsor
Pfizer
Target Recruit Count
118
Registration Number
NCT00068952
Locations

Pfizer Investigational Site

Temozolomide and Radiation Therapy in Treating Patients With Stage IV Malignant Melanoma With Measurable and Unresectable Cancer of the Central Nervous System

Phase 2
Terminated
Conditions
Melanoma (Skin)
Metastatic Cancer
Interventions
Drug: temozolomide
Radiation: radiation therapy
First Posted Date
2003-09-11
Last Posted Date
2016-12-15
Lead Sponsor
Alliance for Clinical Trials in Oncology
Target Recruit Count
41
Registration Number
NCT00068666
Locations
🇺🇸

John Stoddard Cancer Center at Iowa Methodist Medical Center, Des Moines, Iowa, United States

🇺🇸

Mayo Clinic Scottsdale, Scottsdale, Arizona, United States

🇺🇸

Mercy Capitol Hospital, Des Moines, Iowa, United States

and more 42 locations

Temozolomide in Treating Adults With Newly Diagnosed Primary Malignant Glioblastoma Multiforme

Phase 2
Completed
Conditions
Brain and Central Nervous System Tumors
First Posted Date
2003-08-20
Last Posted Date
2013-06-20
Lead Sponsor
Duke University
Target Recruit Count
50
Registration Number
NCT00003464
Locations
🇺🇸

Duke Comprehensive Cancer Center, Durham, North Carolina, United States

Temozolomide Plus PEG-Interferon Alfa-2B in Treating Patients With Advanced Solid Tumors

Phase 1
Completed
Conditions
Unspecified Adult Solid Tumor, Protocol Specific
First Posted Date
2003-07-30
Last Posted Date
2018-03-30
Lead Sponsor
Dartmouth-Hitchcock Medical Center
Registration Number
NCT00014261
Locations
🇺🇸

Norris Cotton Cancer Center, Lebanon, New Hampshire, United States

Temozolomide in Treating Patients With Recurrent or Progressive Malignant Glioma

Phase 2
Conditions
Brain and Central Nervous System Tumors
First Posted Date
2003-07-18
Last Posted Date
2014-01-06
Lead Sponsor
Herbert Irving Comprehensive Cancer Center
Registration Number
NCT00004204
Locations
🇺🇸

Cleveland Clinic Taussig Cancer Center, Cleveland, Ohio, United States

🇺🇸

Nalitt Institute for Cancer And Blood Related Diseases, Staten Island, New York, United States

🇺🇸

Stanford University Medical Center, Stanford, California, United States

and more 7 locations

Irinotecan Followed by Radiation Therapy and Temozolomide in Treating Children With Newly Diagnosed Brain Tumor

Phase 2
Completed
Conditions
Brain and Central Nervous System Tumors
First Posted Date
2003-05-08
Last Posted Date
2011-10-04
Lead Sponsor
St. Jude Children's Research Hospital
Target Recruit Count
53
Registration Number
NCT00004068
Locations
🇺🇸

Saint Jude Children's Research Hospital, Memphis, Tennessee, United States

Temozolomide in Treating Patients With Relapsed or Progressive Small Cell Lung Cancer

Phase 2
Completed
Conditions
Lung Cancer
Interventions
First Posted Date
2003-01-27
Last Posted Date
2013-07-11
Lead Sponsor
Fox Chase Cancer Center
Target Recruit Count
7
Registration Number
NCT00022711
Locations
🇺🇸

Kimball Medical Center, Lakewood, New Jersey, United States

🇺🇸

Fox Chase Cancer Center at Virtua Memorial Hospital Burlington County, Mount Holly, New Jersey, United States

🇺🇸

South Jersey Regional Cancer Center, Millville, New Jersey, United States

and more 14 locations

Temozolomide Compared to Procarbazine, Lomustine, and Vincristine in Treating Patients With Recurrent Malignant Glioma

Phase 3
Completed
Conditions
Brain and Central Nervous System Tumors
First Posted Date
2003-01-27
Last Posted Date
2013-12-18
Lead Sponsor
Institute of Cancer Research, United Kingdom
Target Recruit Count
500
Registration Number
NCT00052455
Locations
🇬🇧

Medical Research Council Clinical Trials Unit, London, England, United Kingdom

Temozolomide in Treating Patients With Leptomeningeal Metastases From a Solid Tumor or Lymphoma

Phase 2
Terminated
Conditions
Brain Tumors
Central Nervous System Tumors
Leptomeningeal Metastases
Interventions
First Posted Date
2003-01-27
Last Posted Date
2013-05-14
Lead Sponsor
Dartmouth-Hitchcock Medical Center
Target Recruit Count
12
Registration Number
NCT00005812
Locations
🇺🇸

Norris Cotton Cancer Center, Lebanon, New Hampshire, United States

Combination Chemotherapy Following Radiation Therapy in Treating Patients With Malignant Glioma

Phase 1
Completed
Conditions
Brain and Central Nervous System Tumors
First Posted Date
2003-01-27
Last Posted Date
2013-04-04
Lead Sponsor
Memorial Sloan Kettering Cancer Center
Registration Number
NCT00005637
Locations
🇺🇸

Memorial Sloan-Kettering Cancer Center, New York, New York, United States

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