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

Clinical Trials

Combination Chemotherapy, Monoclonal Antibody, and Radiation Therapy in Treating Patients With Primary Central Nervous System Lymphoma

Phase 1

Completed

Conditions: Brain and Central Nervous System Tumors
Lymphoma

Interventions: Drug: rituximab
Drug: methotrexate
Drug: temozolomide 150 mg/m^2
Drug: temozolomide 200 mg/m^2
Drug: temozolomide 100 mg/m^2
Radiation: radiation therapy
Drug: post-radiation therapy temozolomide

First Posted Date: 2003-09-11

Last Posted Date: 2018-02-07

Lead Sponsor: Radiation Therapy Oncology Group

Target Recruit Count: 60

Registration Number: NCT00068250

Locations: 🇺🇸
Providence Milwaukie Hospital, Milwaukie, Oregon, United States
🇺🇸
Baptist Cancer Institute - Jacksonville, Jacksonville, Florida, United States
🇺🇸
Flagler Cancer Center, Saint Augustine, Florida, United States

and more 23 locations

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

Gene Therapy and Chemotherapy in Treating Patients With Advanced Solid Tumors or Non-Hodgkin's Lymphoma

Phase 1

Terminated

Conditions: Brain and Central Nervous System Tumors
Lymphoma
Unspecified Adult Solid Tumor, Protocol Specific

First Posted Date: 2003-01-27

Last Posted Date: 2010-06-11

Lead Sponsor: Case Comprehensive Cancer Center

Target Recruit Count: 8

Registration Number: NCT00003567

Locations: 🇺🇸
Ireland Cancer Center at University Hospitals Case Medical Center, Case Comprehensive Cancer Center, Cleveland, Ohio, United States

Temozolomide and Vinorelbine in Treating Patients With Recurrent Brain Metastases

Phase 1

Completed

Conditions: Metastatic Cancer

Interventions: Drug: temozolomide
Drug: vinorelbine tartrate

First Posted Date: 2003-01-27

Last Posted Date: 2016-01-18

Lead Sponsor: Memorial Sloan Kettering Cancer Center

Target Recruit Count: 49

Registration Number: NCT00026494

Locations: 🇺🇸
Memorial Sloan-Kettering Cancer Center, New York, New York, United States
🇺🇸
Robert H. Lurie Comprehensive Cancer Center at Northwestern University, Chicago, Illinois, United States

Temozolomide Plus Lomustine Followed by Radiation Therapy in Treating Patients With High-Grade Malignant Glioma

Phase 1

Completed

Conditions: Brain Tumor
Central Nervous System Tumor

Interventions: Drug: lomustine
Drug: temozolomide

First Posted Date: 2003-01-27

Last Posted Date: 2014-02-13

Lead Sponsor: Children's Oncology Group

Target Recruit Count: 32

Registration Number: NCT00006024

Locations: 🇺🇸
Children's Hospital of Columbus, Columbus, Ohio, United States
🇺🇸
Cleveland Clinic Taussig Cancer Center, Cleveland, Ohio, United States
🇨🇭
Swiss Pediatric Oncology Group Lausanne, Lausanne, Switzerland

and more 231 locations

Radiation Therapy Plus Thalidomide and Temozolomide in Treating Patients With Newly Diagnosed Brain Metastases

Phase 2

Completed

Conditions: Brain and Central Nervous System Tumors
Unspecified Adult Solid Tumor, Protocol Specific

First Posted Date: 2003-01-27

Last Posted Date: 2021-09-09

Lead Sponsor: Wake Forest University Health Sciences

Registration Number: NCT00049361

Locations: 🇺🇸
CCOP - Central Illinois, Decatur, Illinois, United States
🇺🇸
CCOP - Upstate Carolina, Spartanburg, South Carolina, United States
🇺🇸
CCOP - Southeast Cancer Control Consortium, Goldsboro, North Carolina, United States

and more 2 locations

Drug Development Updates

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