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

Phase 3 Study of ANP Therapy vs. TMZ for Optic Pathway Glioma

Phase 3

Withdrawn

Conditions: Optic Nerve Glioma

Interventions: Drug: ANP Therapy
Drug: Temozolomide

First Posted Date: 2010-12-15

Last Posted Date: 2017-07-26

Lead Sponsor: Burzynski Research Institute

Registration Number: NCT01260103

Temozolomide in Elderly Patients With KPS < 70

Phase 2

Completed

Conditions: Primary Brain Tumor
Glioblastoma

Interventions: Drug: Temozolomide

First Posted Date: 2010-11-17

Last Posted Date: 2010-11-17

Lead Sponsor: Assistance Publique - Hôpitaux de Paris

Target Recruit Count: 70

Registration Number: NCT01242566

Locations: 🇫🇷
Pitie salpetriere hospital, Paris, France

The Addition of Temozolomide to Conditioning for Autologous Transplantation in Relapsed & Refractory CNS Lymphoma

Phase 2

Terminated

Conditions: B-Cell Lymphoma Originating in the CNS

Interventions: Drug: Temozolomide

First Posted Date: 2010-11-08

Last Posted Date: 2018-11-20

Lead Sponsor: Cedars-Sinai Medical Center

Target Recruit Count: 11

Registration Number: NCT01235793

Locations: 🇺🇸
Cedars Sinai Medical Center, Los Angeles, California, United States

Vorinostat, Temozolomide, or Bevacizumab in Combination With Radiation Therapy Followed by Bevacizumab and Temozolomide in Young Patients With Newly Diagnosed High-Grade Glioma

Phase 2

Completed

Conditions: Brain Stem Glioma
Childhood Spinal Cord Neoplasm
Cerebral Astrocytoma
Childhood Cerebellar Anaplastic Astrocytoma
Childhood Cerebral Anaplastic Astrocytoma

Interventions: Biological: Bevacizumab
Drug: Temozolomide
Drug: Vorinostat

First Posted Date: 2010-11-07

Last Posted Date: 2024-02-20

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 101

Registration Number: NCT01236560

Locations: 🇺🇸
Mattel Children's Hospital UCLA, Los Angeles, California, United States
🇺🇸
Naval Medical Center - Portsmouth, Portsmouth, Virginia, United States
🇺🇸
Children's Oncology Group, Philadelphia, Pennsylvania, United States

and more 129 locations

Vaccine Therapy, Temozolomide, and Radiation Therapy in Treating Patients With Newly Diagnosed Glioblastoma Multiforme

Phase 1

Completed

Conditions: Brain and Central Nervous System Tumors

First Posted Date: 2010-10-18

Last Posted Date: 2015-10-14

Lead Sponsor: Cancer Research UK

Target Recruit Count: 45

Registration Number: NCT01222221

Locations: 🇬🇧
Addenbrooke's Hospital, Cambridge, England, United Kingdom
🇬🇧
Beatson West of Scotland Cancer Centre, Glasgow, Scotland, United Kingdom
🇬🇧
Western General Hospital, Edinburgh, United Kingdom

and more 4 locations

A Study Combining LY2157299 With Temozolomide-based Radiochemotherapy in Patients With Newly Diagnosed Malignant Glioma

Phase 1

Completed

Conditions: Glioma

Interventions: Drug: LY2157299
Drug: Radiation
Drug: Temozolomide

First Posted Date: 2010-10-13

Last Posted Date: 2017-02-16

Lead Sponsor: Eli Lilly and Company

Target Recruit Count: 75

Registration Number: NCT01220271

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., Madrid, Spain

Temozolomide and Bevacizumab in Treating Patients With Metastatic Melanoma of the Eye

Phase 2

Conditions: Intraocular Melanoma

First Posted Date: 2010-10-08

Last Posted Date: 2013-08-26

Lead Sponsor: Institut Curie

Target Recruit Count: 35

Registration Number: NCT01217398

Locations: 🇫🇷
Institut Curie Hopital, Paris, France

Temozolomide and Irinotecan Hydrochloride With or Without Bevacizumab in Treating Young Patients With Recurrent or Refractory Medulloblastoma or CNS Primitive Neuroectodermal Tumors

Phase 2

Completed

Conditions: Pineoblastoma
Recurrent Medulloblastoma
Refractory Peripheral Primitive Neuroectodermal Tumor
Recurrent Primitive Neuroectodermal Tumor
Refractory Medulloblastoma
Central Nervous System Neoplasm

Interventions: Biological: Bevacizumab
Drug: Irinotecan Hydrochloride
Drug: Temozolomide

First Posted Date: 2010-10-08

Last Posted Date: 2021-07-23

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 108

Registration Number: NCT01217437

Locations: 🇺🇸
Baylor College of Medicine/Dan L Duncan Comprehensive Cancer Center, Houston, Texas, United States
🇺🇸
Loma Linda University Medical Center, Loma Linda, California, United States
🇺🇸
University of Illinois, Chicago, Illinois, United States

and more 155 locations