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

Cabozantinib-S-Malate Compared With Temozolomide or Dacarbazine in Treating Patients With Metastatic Melanoma of the Eye That Cannot Be Removed by Surgery

Phase 2

Completed

Conditions: Recurrent Uveal Melanoma
Stage IIIA Uveal Melanoma AJCC v7
Stage III Uveal Melanoma AJCC v7
Stage IIIB Uveal Melanoma AJCC v7
Stage IIIC Uveal Melanoma AJCC v7
Stage IV Uveal Melanoma AJCC v7

Interventions: Drug: Cabozantinib S-malate
Drug: Dacarbazine
Other: Laboratory Biomarker Analysis
Drug: Temozolomide

First Posted Date: 2013-04-18

Last Posted Date: 2022-08-04

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 47

Registration Number: NCT01835145

Locations: 🇺🇸
University of Pennsylvania/Abramson Cancer Center, Philadelphia, Pennsylvania, United States
🇺🇸
University of Chicago Comprehensive Cancer Center, Chicago, Illinois, United States
🇺🇸
Kaiser Permanente Washington, Seattle, Washington, United States

and more 225 locations

A Phase III Study of Re-Irradiation in Recurrent Glioblastoma

Phase 3

Withdrawn

Conditions: Recurrent Glioblastoma

Interventions: Drug: TMZ plus concurrent re-irradiation
Drug: Temozolomide

First Posted Date: 2013-04-12

Last Posted Date: 2016-03-16

Lead Sponsor: AHS Cancer Control Alberta

Registration Number: NCT01830101

Locations: 🇨🇦
Cross Cancer Institute, Edmonton, Alberta, Canada

MPACT Study to Compare Effects of Targeted Drugs on Tumor Gene Variations

Phase 2

Completed

Conditions: Advanced Malignant Solid Neoplasm

Interventions: Drug: Temozolomide
Drug: Adavosertib
Drug: Everolimus
Drug: Trametinib
Drug: Veliparib
Drug: Carboplatin

First Posted Date: 2013-04-09

Last Posted Date: 2023-09-29

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 208

Registration Number: NCT01827384

Locations: 🇺🇸
Rutgers Cancer Institute of New Jersey, New Brunswick, New Jersey, United States
🇺🇸
Emory University Hospital/Winship Cancer Institute, Atlanta, Georgia, United States
🇺🇸
National Cancer Institute Developmental Therapeutics Clinic, Bethesda, Maryland, United States

and more 5 locations

Temozolomide With or Without Capecitabine in Treating Patients With Advanced Pancreatic Neuroendocrine Tumors

Phase 2

Active, not recruiting

Conditions: Gastrinoma
Somatostatinoma
Glucagonoma
Recurrent Islet Cell Carcinoma
Insulinoma
Islet Cell Carcinoma
Pancreatic Polypeptide Tumor

Interventions: Drug: temozolomide
Drug: capecitabine

First Posted Date: 2013-04-05

Last Posted Date: 2024-02-07

Lead Sponsor: ECOG-ACRIN Cancer Research Group

Target Recruit Count: 144

Registration Number: NCT01824875

Locations: 🇺🇸
University of Miami Miller School of Medicine-Sylvester Cancer Center, Miami, Florida, United States
🇺🇸
Nevada Cancer Research Foundation CCOP, Las Vegas, Nevada, United States
🇺🇸
Oncology Hematology Care Inc - Western Hills, Cincinnati, Ohio, United States

and more 318 locations

Evaluating the Safety and Pharmacokinetics of ABT-414 for Subjects With Glioblastoma Multiforme

Phase 1

Completed

Conditions: Glioblastoma Multiforme

Interventions: Drug: ABT-414
Drug: Temozolomide
Radiation: Whole Brain Radiation

First Posted Date: 2013-02-28

Last Posted Date: 2017-11-21

Lead Sponsor: AbbVie

Target Recruit Count: 202

Registration Number: NCT01800695

A Phase 1b/2 Study of PLX3397 + Radiation Therapy + Temozolomide in Patients With Newly Diagnosed Glioblastoma

Phase 1

Completed

Conditions: Patients With Newly Diagnosed Glioblastoma

Interventions: Drug: PLX3397
Radiation: Radiation Therapy
Drug: Temozolomide

First Posted Date: 2013-02-13

Last Posted Date: 2020-06-30

Lead Sponsor: Daiichi Sankyo

Target Recruit Count: 65

Registration Number: NCT01790503

Locations: 🇺🇸
Massachusetts General Hospital, Boston, Massachusetts, United States
🇺🇸
James Cancer Hospital/Ohio State University, Columbia, Ohio, United States
🇺🇸
Seattle Cancer Care Alliance, Seattle, Washington, United States

and more 6 locations

Preoperative CRT With Temozolomide Plus Capecitabine in Rectal Cancer

Phase 1

Completed

Conditions: Rectal Cancer

Interventions: Drug: Temozolomide

First Posted Date: 2013-02-01

Last Posted Date: 2021-02-04

Lead Sponsor: Asan Medical Center

Target Recruit Count: 22

Registration Number: NCT01781403

Locations: 🇰🇷
Asan Medical Center, Seoul, Songpa-gu, Korea, Republic of

Disulfiram/Copper Combination In The Treatment of Newly Diagnosed Glioblastoma Multiform

Phase 2

Conditions: Glioblastoma Multiforme

Interventions: Drug: Temozolomide
Drug: Disulfiram
Drug: Copper

First Posted Date: 2013-01-29

Last Posted Date: 2016-10-17

Lead Sponsor: Olympion Medical Center

Target Recruit Count: 32

Registration Number: NCT01777919

Locations: 🇬🇷
Olympion Medical Center, Patras, Greece

Irinotecan Hydrochloride and Temozolomide With Temsirolimus or Dinutuximab in Treating Younger Patients With Refractory or Relapsed Neuroblastoma

Phase 2

Completed

Conditions: Ganglioneuroblastoma
Recurrent Neuroblastoma

Interventions: Drug: Irinotecan Hydrochloride
Biological: Dinutuximab
Other: Laboratory Biomarker Analysis
Drug: Temozolomide
Biological: Sargramostim
Drug: Temsirolimus

First Posted Date: 2013-01-14

Last Posted Date: 2022-10-24

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 73

Registration Number: NCT01767194

Locations: 🇺🇸
Children's Hospital Los Angeles, Los Angeles, California, United States
🇺🇸
Nationwide Children's Hospital, Columbus, Ohio, United States
🇺🇸
Children's Hospital of Philadelphia, Philadelphia, Pennsylvania, United States

and more 154 locations

A Phase III Trial on Adjuvant Temozolomide With or Without Interferon-alpha in Newly Diagnosed High-grade Gliomas

Phase 3

Conditions: Anaplastic Astrocytoma
Glioblastoma
Anaplastic Oligoastrocytoma

Interventions: Drug: Temozolomide
Drug: α-IFN

First Posted Date: 2013-01-10

Last Posted Date: 2018-02-23

Lead Sponsor: Sun Yat-sen University

Target Recruit Count: 300

Registration Number: NCT01765088

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

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