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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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PPX and Concurrent Radiation for Newly Diagnosed Glioblastoma Without MGMT Methylation

Phase 2
Completed
Conditions
Glioblastoma Multiforme
Interventions
Drug: PPX (CT2103)
Drug: Temozolomide
First Posted Date
2011-07-26
Last Posted Date
2020-02-17
Lead Sponsor
Brown University
Target Recruit Count
63
Registration Number
NCT01402063
Locations
🇺🇸

Thomas Jefferson University Cancer Center, Philadelphia, Pennsylvania, United States

🇺🇸

UT Southwestern Cancer Center, Dallas, Texas, United States

🇺🇸

University of Washington, Seattle, Washington, United States

and more 6 locations

Olaparib and Temozolomide in Treating Patients With Relapsed Glioblastoma

Phase 1
Completed
Conditions
Brain and Central Nervous System Tumors
First Posted Date
2011-07-11
Last Posted Date
2018-02-05
Lead Sponsor
Cancer Research UK
Target Recruit Count
34
Registration Number
NCT01390571
Locations
🇬🇧

Bristol Haematology and Oncology Centre, Bristol, England, United Kingdom

🇬🇧

Royal Marsden Hospital, Sutton, England, United Kingdom

🇬🇧

Christie Hospital, Manchester, England, United Kingdom

and more 4 locations

Conventional Adjuvant Temozolomide With Dose Intensive Temozolomide in Patients With Newly Diagnosed Glioblastoma

Phase 3
Completed
Conditions
Glioblastoma
Interventions
First Posted Date
2011-06-02
Last Posted Date
2016-02-25
Lead Sponsor
King Faisal Specialist Hospital & Research Center
Target Recruit Count
1153
Registration Number
NCT01364064

Comparison of Different Methods to Test MGMT Status in Glioblastoma Patients

Completed
Conditions
Glioblastoma
Interventions
Drug: Temozolomide
Radiation: Radiation Therapy
First Posted Date
2011-05-02
Last Posted Date
2016-01-29
Lead Sponsor
Center Eugene Marquis
Target Recruit Count
300
Registration Number
NCT01345370
Locations
🇫🇷

CHU de Bordeaux, Bordeaux, Aquitaine, France

🇫🇷

Center Eugene Marquis, Rennes, Brittany, France

🇫🇷

CHU de Poitiers, Poitiers, Poitou-Charentes, France

and more 7 locations

Magnetic Resonance Spectroscopy Imaging in Predicting Response to Vorinostat and Temozolomide in Patients With Recurrent or Progressive Glioblastoma

Not Applicable
Completed
Conditions
Adult Glioblastoma
Depression
Recurrent Adult Brain Tumor
Interventions
Drug: vorinostat
Drug: temozolomide
Procedure: magnetic resonance spectroscopic imaging
Other: survey administration
First Posted Date
2011-04-27
Last Posted Date
2018-01-29
Lead Sponsor
National Cancer Institute (NCI)
Target Recruit Count
12
Registration Number
NCT01342757
Locations
🇺🇸

Emory University, Atlanta, Georgia, United States

Individualized Temozolomide in Treating Patients With Stage IV Melanoma That Cannot Be Removed By Surgery

Phase 2
Completed
Conditions
Stage IV Melanoma
Recurrent Melanoma
Interventions
Drug: temozolomide
Other: flow cytometry
Other: staining method
Procedure: biopsy
Other: laboratory biomarker analysis
First Posted Date
2011-04-04
Last Posted Date
2020-10-22
Lead Sponsor
Mayo Clinic
Target Recruit Count
25
Registration Number
NCT01328535
Locations
🇺🇸

Mayo Clinic, Rochester, Minnesota, United States

Cyclophosphamide, Doxorubicin, Vincristine w/ Irinotecan and Temozolomide in Ewings Sarcoma

Phase 2
Terminated
Conditions
Bone Cancer
Ewing's Sarcoma
Interventions
First Posted Date
2011-03-14
Last Posted Date
2017-11-24
Lead Sponsor
Stanford University
Target Recruit Count
3
Registration Number
NCT01313884
Locations
🇺🇸

Stanford University School of Medicine, Stanford, California, United States

Study of the Safety and Efficacy of MK-4827 Given With Temozolomide in Participants With Advanced Cancer (MK-4827-014 AM1)

Phase 1
Completed
Conditions
Recurrence of Solid Tumor
Glioblastoma Multiforme
Melanoma
Interventions
Drug: MK-4827
Drug: Temozolomide
First Posted Date
2011-02-11
Last Posted Date
2012-08-15
Lead Sponsor
Merck Sharp & Dohme LLC
Target Recruit Count
19
Registration Number
NCT01294735

A Safety Study in Participants With Advanced Solid Tumors

First Posted Date
2011-01-27
Last Posted Date
2019-01-10
Lead Sponsor
Eli Lilly and Company
Target Recruit Count
234
Registration Number
NCT01284335
Locations
🇺🇸

For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Yakima, Washington, United States

BG & TMZ Therapy of Glioblastoma Multiforme

Phase 1
Completed
Conditions
Glioblastoma Multiforme
Interventions
Biological: MGMTP140K-encoding retroviral vector
Drug: O6-benzylguanine
Drug: temozolomide
Other: laboratory biomarker analysis
Procedure: autologous hematopoietic stem cell transplantation
Procedure: in vitro-treated peripheral blood stem cell transplantation
Radiation: radiation therapy
First Posted Date
2011-01-04
Last Posted Date
2023-03-02
Lead Sponsor
Stanton Gerson MD
Target Recruit Count
10
Registration Number
NCT01269424
Locations
🇺🇸

University Hospitals Cleveland Medical Center, Case Comprehensive Cancer Center, Cleveland, Ohio, United States

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