Temozolomide

Generic Name: Temozolomide

Brand Names: Temodar, Temomedac, Temodal, Temozolomide Sun, Temozolomide Accord, Temozolomide Teva

Drug Type: Small Molecule

Chemical Formula: C_₆H_₆N_₆O_₂

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: -

Clinical Trials

Gamma-secretase/Notch Signalling Pathway Inhibitor RO4929097 in Combination With Cisplatin, Vinblastine, and Temozolomide in Treating Patients With Recurrent or Metastatic Melanoma

Phase 1

Completed

Conditions: Stage IV Skin Melanoma
Recurrent Melanoma

Interventions: Drug: Cisplatin
Drug: Gamma-Secretase Inhibitor RO4929097
Other: Laboratory Biomarker Analysis
Other: Pharmacological Study
Drug: Temozolomide
Drug: Vinblastine Sulfate

First Posted Date: 2010-09-08

Last Posted Date: 2019-11-18

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 14

Registration Number: NCT01196416

Locations: 🇺🇸
Memorial Sloan-Kettering Cancer Center, New York, New York, United States

To Evaluate the Safety of Veliparib in Combination With Temozolomide in Subjects With Solid Tumors

Phase 2

Completed

Conditions: Solid Tumor Cancers

Interventions: Drug: veliparib
Drug: Temozolomide

First Posted Date: 2010-09-01

Last Posted Date: 2012-11-21

Lead Sponsor: Abbott

Target Recruit Count: 24

Registration Number: NCT01193140

Locations: 🇺🇸
Site Reference ID/Investigator# 42662, Santa Monica, California, United States
🇺🇸
Site Reference ID/Investigator# 43022, Encinitas, California, United States

Gliadel, XRT, Temodar, Avastin Followed by Avastin, Temodar for Newly Diagnosed Glioblastoma Multiforme (GBM)

Phase 2

Terminated

Conditions: Gliosarcoma
Glioblastoma Multiforme

Interventions: Drug: Gliadel
Radiation: Radiation Therapy
Drug: Avastin
Drug: Temodar

First Posted Date: 2010-08-23

Last Posted Date: 2019-02-15

Lead Sponsor: Duke University

Target Recruit Count: 41

Registration Number: NCT01186406

Locations: 🇺🇸
The Preston Robert Tisch Brain Tumor Center, Durham, North Carolina, United States

Molecularly Determined Treatment of Diffuse Intrinsic Pontine Gliomas (DIPG)

Phase 2

Terminated

Conditions: Diffuse Intrinsic Pontine Glioma

Interventions: Drug: Bevacizumab
Radiation: Radiation
Drug: Erlotinib
Drug: Temozolomide

First Posted Date: 2010-08-16

Last Posted Date: 2019-09-04

Lead Sponsor: Karen D. Wright MD

Target Recruit Count: 53

Registration Number: NCT01182350

Locations: 🇺🇸
Ann & Robert H Lurie Children's Hospital of Chicago, Chicago, Illinois, United States
🇺🇸
Johns Hopkins, Baltimore, Maryland, United States
🇺🇸
Dana-Farber Cancer Institute, Boston, Massachusetts, United States

and more 20 locations

Vitamin D for Treatment of Glioblastoma Multiforme

Phase 1

Conditions: Glioblastoma Multiforme

First Posted Date: 2010-08-13

Last Posted Date: 2011-03-29

Lead Sponsor: Soroka University Medical Center

Target Recruit Count: 20

Registration Number: NCT01181193

Locations: 🇮🇱
Soroka University Medical Center, Beer Sheva, Israel

Bevacizumab in Recurrent Grade II and III Glioma

Phase 2

Completed

Conditions: Central Nervous System Tumors

Interventions: Drug: Temozolomide
Biological: Bevacizumab

First Posted Date: 2010-07-16

Last Posted Date: 2019-02-28

Lead Sponsor: European Organisation for Research and Treatment of Cancer - EORTC

Target Recruit Count: 155

Registration Number: NCT01164189

Locations: 🇧🇪
U.Z. Leuven - Campus Gasthuisberg, Leuven, Belgium
🇦🇹
Medical University Vienna - General Hospital AKH, Vienna, Austria
🇫🇷
CHU Pitie-Salpetriere, Paris, France

and more 36 locations

Bevacizumab and Temozolomide in Treating Older Patients With Newly-Diagnosed Glioblastoma Multiforme or Gliosarcoma

Phase 2

Completed

Conditions: Giant Cell Glioblastoma
Glioblastoma
Gliosarcoma

Interventions: Biological: bevacizumab
Drug: temozolomide
Other: laboratory biomarker analysis
Other: immunohistochemistry staining method
Genetic: microarray analysis
Genetic: DNA methylation analysis

First Posted Date: 2010-06-24

Last Posted Date: 2024-03-04

Lead Sponsor: Jonsson Comprehensive Cancer Center

Target Recruit Count: 50

Registration Number: NCT01149850

Locations: 🇺🇸
University of California, Los Angeles, Los Angeles, California, United States
🇺🇸
Kaiser Foundation Hospital, Los Angeles, California, United States
🇺🇸
Kaiser Permanente at San Diego, San Diego, California, United States

Efficacy and Safety Study of Lomustine/Temozolomide Combination Therapy vs. Standard Therapy for Glioblastoma Patients

Phase 3

Completed

Conditions: Glioblastoma

Interventions: Drug: Temozolomide and lomustine
Drug: Temozolomide

First Posted Date: 2010-06-23

Last Posted Date: 2017-06-14

Lead Sponsor: University Hospital, Bonn

Target Recruit Count: 141

Registration Number: NCT01149109

Locations: 🇩🇪
Depatment of Neurosurgery, Charité, University Hospital Berlin, Berlin, Germany
🇩🇪
Department of Neurology, University Hospital Bonn, Bonn, Germany
🇩🇪
Department of Neurology, University Hospital Bochum, Bochum, Germany

and more 9 locations

Temozolomide or Selumetinib in Treating Patients With Metastatic Melanoma of the Eye

Phase 2

Completed

Conditions: Iris Melanoma
Recurrent Uveal Melanoma
Stage IV Uveal Melanoma
Medium/Large Size Posterior Uveal Melanoma
Ocular Melanoma With Extraocular Extension
Small Size Posterior Uveal Melanoma

Interventions: Drug: Dacarbazine
Other: Laboratory Biomarker Analysis
Other: Quality-of-Life Assessment
Drug: Selumetinib
Drug: Temozolomide

First Posted Date: 2010-06-14

Last Posted Date: 2017-07-26

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 120

Registration Number: NCT01143402

Locations: 🇨🇦
University Health Network-Princess Margaret Hospital, Toronto, Ontario, Canada
🇺🇸
Mount Sinai Medical Center, Miami Beach, Florida, United States
🇺🇸
Emory University/Winship Cancer Institute, Atlanta, Georgia, United States

and more 30 locations

Temsirolimus, Irinotecan Hydrochloride, and Temozolomide in Treating Younger Patients With Relapsed or Refractory Solid Tumors

Phase 1

Completed

Conditions: Unspecified Childhood Solid Tumor, Protocol Specific

Interventions: Drug: temsirolimus
Drug: temozolomide
Drug: irinotecan hydrochloride
Other: laboratory biomarker analysis

First Posted Date: 2010-06-10

Last Posted Date: 2014-04-10

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 72

Registration Number: NCT01141244

Locations: 🇨🇦
Hospital for Sick Children, Toronto, Ontario, Canada
🇺🇸
University of California San Francisco Medical Center-Parnassus, San Francisco, California, United States
🇺🇸
C S Mott Children's Hospital, Ann Arbor, Michigan, United States

and more 22 locations

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