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

A Phase I Trial of High-Dose Ascorbate in Glioblastoma Multiforme

Phase 1

Completed

Conditions: Glioblastoma Multiforme
GBM
Glioblastoma

Interventions: Drug: Ascorbate
Drug: Temozolomide
Radiation: Radiation therapy

First Posted Date: 2012-12-19

Last Posted Date: 2024-12-20

Lead Sponsor: Joseph J. Cullen, MD, FACS

Target Recruit Count: 13

Registration Number: NCT01752491

Locations: 🇺🇸
Holden Comprehensive Cancer Center at the University of Iowa, Iowa City, Iowa, United States

Bevacizumab Beyond Progression (BBP)

Phase 2

Completed

Conditions: Glioblastoma
Grade 4 Malignant Glioma
Malignant Glioma
Gliosarcoma

Interventions: Radiation: Radiation Therapy
Drug: Temozolomide
Drug: Bevacizumab

First Posted Date: 2012-12-04

Last Posted Date: 2021-01-26

Lead Sponsor: Duke University

Target Recruit Count: 68

Registration Number: NCT01740258

Locations: 🇺🇸
Duke Cancer Center, Durham, North Carolina, United States

Phase II Trial of Chemotherapy With Temodar With Topotecan for CNS Metastasis of Solid Tumors

Phase 2

Withdrawn

Conditions: Brain Metastases
Central Nervous System (CNS) Metastases

Interventions: Drug: Topotecan
Drug: Temozolomide

First Posted Date: 2012-11-29

Last Posted Date: 2017-09-19

Lead Sponsor: The Methodist Hospital Research Institute

Registration Number: NCT01736800

Locations: 🇺🇸
Houston Methodist Hospital, Houston, Texas, United States
🇺🇸
Methodist Neurological Institute - Department of Neurosurgery, Houston, Texas, United States

Temozolomide, Nedaplatin, Vincristine, and Radiotherapy as First-line Treatment in Newly Diagnosed Primary CNS Lymphoma

Phase 2

Conditions: Central Nervous System Tumors

Interventions: Radiation: Radiotherapy
Drug: nedaplatin
Drug: vincristine
Drug: Temozolomide

First Posted Date: 2012-11-28

Last Posted Date: 2013-03-12

Lead Sponsor: Rongjie Tao

Target Recruit Count: 16

Registration Number: NCT01735747

Locations: 🇨🇳
Neurosurgery, Shandong Cancer Hospital and Institute, Jinan, Shandong, China

A Phase II Study of Oral LDE225 in Patients With Hedge-Hog (Hh)-Pathway Activated Relapsed Medulloblastoma (MB)

Phase 2

Completed

Conditions: Medulloblastoma

Interventions: Drug: LDE225
Drug: TMZ

First Posted Date: 2012-10-16

Last Posted Date: 2017-08-11

Lead Sponsor: Novartis Pharmaceuticals

Target Recruit Count: 22

Registration Number: NCT01708174

Locations: 🇺🇸
Children's Hospital of Pittsburgh Dept of Oncology, Pittsburgh, Pennsylvania, United States
🇺🇸
Dana Farber Cancer Institute SC-7, Boston, Massachusetts, United States
🇬🇧
Novartis Investigative Site, Leeds, United Kingdom

and more 6 locations

Study of Pembrolizumab (MK-3475) Versus Chemotherapy in Participants With Advanced Melanoma (MK-3475-002/P08719/KEYNOTE-002)

Phase 2

Completed

Conditions: Malignant Melanoma

Interventions: Drug: Carboplatin
Biological: Pembrolizumab
Drug: Paclitaxel
Drug: Dacarbazine
Drug: Temozolomide

First Posted Date: 2012-10-11

Last Posted Date: 2020-05-18

Lead Sponsor: Merck Sharp & Dohme LLC

Target Recruit Count: 540

Registration Number: NCT01704287

Phase-1 Study of Folinic Acid to Modulate MGMT Gene in Glioblastoma

Phase 1

Terminated

Conditions: Grade IV Astrocytoma
Glioblastoma

Interventions: Drug: Temozolomide
Drug: folinic acid at pharmacological dose is the escalated drug
Radiation: High voltage radiation therapy (linear accelerator)

First Posted Date: 2012-10-04

Last Posted Date: 2023-02-21

Lead Sponsor: Institut Cancerologie de l'Ouest

Target Recruit Count: 24

Registration Number: NCT01700569

Locations: 🇫🇷
Institut de Cacerologie de l'ouest - site Paul Papin, Angers, France
🇫🇷
CHU de Lyon, Bron, France
🇫🇷
ICO site Gauducheau, Nantes, France

and more 1 locations

Efficacy and Safety of TMZ Plus CDDP in the Patients With Recurrent Malignant Gliomas

Phase 2

Conditions: Malignant Gliomas

Interventions: Drug: TMZ
Drug: TMZ plus CDDP

First Posted Date: 2012-08-22

Last Posted Date: 2012-08-22

Lead Sponsor: Peking Union Medical College Hospital

Target Recruit Count: 120

Registration Number: NCT01670890

Locations: 🇨🇳
Tianjin medical university general university, Tianjin, Tianjin, China
🇨🇳
Beijing Tiantan Hospital Affiliated to Capital Medial University, Beijing, Beijing, China
🇨🇳
Peking Union Medical College Hospital, Beijing, Beijing, China

Efficacy of Post-radiation Adjuvant Temozolomide Chemotherapy in Residue Low-grade Glioma

Phase 3

Recruiting

Conditions: Astrocytoma
Oligodendroastrocytoma
Oligodendroglioma

Interventions: Radiation: Radiotherapy
Drug: Temozolomide

First Posted Date: 2012-07-25

Last Posted Date: 2020-05-28

Lead Sponsor: Sun Yat-sen University

Target Recruit Count: 290

Registration Number: NCT01649830

Locations: 🇨🇳
Sun Yat-sen University Cancer Center, Guangzhou, Guangdong, China

Temozolomide With or Without Veliparib in Treating Patients With Relapsed or Refractory Small Cell Lung Cancer

Phase 2

Completed

Conditions: Recurrent Small Cell Lung Carcinoma

Interventions: Other: Laboratory Biomarker Analysis
Drug: Temozolomide
Other: Placebo
Drug: Veliparib

First Posted Date: 2012-07-11

Last Posted Date: 2019-11-19

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 97

Registration Number: NCT01638546

Locations: 🇺🇸
Johns Hopkins University/Sidney Kimmel Cancer Center, Baltimore, Maryland, United States
🇺🇸
M D Anderson Cancer Center, Houston, Texas, United States
🇺🇸
Virginia Commonwealth University/Massey Cancer Center, Richmond, Virginia, United States

and more 7 locations

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