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 2 Study of the Poly(ADP-Ribose) Polymerase Inhibitor E7016 in Combination With Temozolomide in Subjects With Wild Type BRAF Stage IV or Unresectable Stage III Melanoma

Phase 2

Terminated

Conditions: Unresectable Stage III Melanoma
Wild Type BRAF Stage IV Melanoma

Interventions: Drug: TMZ
Drug: E7016

First Posted Date: 2012-05-24

Last Posted Date: 2016-07-28

Lead Sponsor: Eisai Inc.

Target Recruit Count: 8

Registration Number: NCT01605162

Study of MLN8237 in Combination With Irinotecan and Temozolomide

Phase 1

Completed

Conditions: Neuroblastoma

Interventions: Drug: MLN8237
Drug: Irinotecan
Drug: Temozolomide

First Posted Date: 2012-05-18

Last Posted Date: 2019-07-31

Lead Sponsor: New Approaches to Neuroblastoma Therapy Consortium

Target Recruit Count: 54

Registration Number: NCT01601535

Locations: 🇺🇸
Children's Healthcare of Atlanta, Atlanta, Georgia, United States
🇺🇸
Children's Hospital Los Angeles, Los Angeles, California, United States
🇺🇸
Childrens Hospital Boston, Dana-Farber Cancer Institute., Boston, Massachusetts, United States

and more 10 locations

Study of Vismodegib in Combination With Temozolomide Versus Temozolomide Alone in Patients With Medulloblastomas With an Activation of the Sonic Hedgehog Pathway

Phase 1

Terminated

Conditions: Activation of the Sonic Hedgehog (SHH) Pathway
Histologically Confirmed Medulloblastoma

Interventions: Drug: Temozolomide
Drug: vismodegib

First Posted Date: 2012-05-17

Last Posted Date: 2019-05-21

Lead Sponsor: Centre Leon Berard

Target Recruit Count: 24

Registration Number: NCT01601184

Locations: 🇫🇷
Institut de Cancérologie de l'Ouest - René Gauducheau, St Herblain, Loire Atlantique, France
🇫🇷
Institut Bergonié, Bordeaux, France
🇫🇷
Institut Claudius Régaud (iuct-oncopole), Toulouse, Haute-Garonne, France

and more 12 locations

Doxycycline, Temozolomide and Ipilimumab in Melanoma

Phase 1

Terminated

Conditions: Melanoma

Interventions: Drug: Doxycycline
Drug: Ipilimumab
Drug: Temozolomide

First Posted Date: 2012-05-02

Last Posted Date: 2020-09-02

Lead Sponsor: M.D. Anderson Cancer Center

Target Recruit Count: 12

Registration Number: NCT01590082

Locations: 🇺🇸
University of Texas MD Anderson Cancer Center, Houston, Texas, United States

Temozolomide Plus Vorinostat in Relapse/Refractory Acute Myeloid Leukemia (AML)

Phase 2

Completed

Conditions: Acute Myeloid Leukemia With 11q23-abnormality in Relapse

Interventions: Drug: Temozolomide
Drug: Vorinostat

First Posted Date: 2012-03-09

Last Posted Date: 2018-08-09

Lead Sponsor: Steven E. Coutre

Target Recruit Count: 23

Registration Number: NCT01550224

Locations: 🇺🇸
Stanford University Medical Center, Stanford, California, United States

Metformin in Children With Relapsed or Refractory Solid Tumors

Phase 1

Completed

Conditions: Primary Brain Tumors
Solid Tumors

Interventions: Drug: Vincristine
Drug: Irinotecan
Drug: Temozolomide
Drug: Metformin

First Posted Date: 2012-02-07

Last Posted Date: 2023-01-13

Lead Sponsor: H. Lee Moffitt Cancer Center and Research Institute

Target Recruit Count: 26

Registration Number: NCT01528046

Locations: 🇺🇸
Primary Children's Medical Center/Utah, Salt Lake City, Utah, United States
🇺🇸
Nemours Children's Clinic, Jacksonville, Florida, United States
🇺🇸
University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, United States

and more 11 locations

Capecitabine, Temozolomide, and Bevacizumab for Metastatic or Unresectable Pancreatic Neuroendocrine Tumors

Phase 2

Completed

Conditions: Gastrinoma
Pancreatic Polypeptide Tumor
Recurrent Islet Cell Carcinoma
Glucagonoma
Insulinoma
Recurrent Pancreatic Cancer
Somatostatinoma
Stage IV Pancreatic Cancer
Stage III Pancreatic Cancer

Interventions: Drug: Capecitabine
Drug: Temozolomide
Biological: Bevacizumab

First Posted Date: 2012-02-02

Last Posted Date: 2024-02-06

Lead Sponsor: Shaheen Shagufta

Target Recruit Count: 20

Registration Number: NCT01525082

Locations: 🇺🇸
Stanford University Medical Center, Stanford, California, United States

Cilengitide and Metronomic Temozolomide for Relapsed or Refractory High Grade Gliomas or Diffuse Intrinsic Pontine Gliomas in Children and Adolescents

Phase 2

Terminated

Conditions: Gliomas

Interventions: Drug: Cilengitide
Drug: Temozolomide

First Posted Date: 2012-01-25

Last Posted Date: 2015-07-21

Lead Sponsor: Martin-Luther-Universität Halle-Wittenberg

Target Recruit Count: 28

Registration Number: NCT01517776

Locations: 🇩🇪
University Children´s Hospital, Halle, Saxonia-Anhalt, Germany

Veliparib, Radiation Therapy, and Temozolomide in Treating Younger Patients With Newly Diagnosed Diffuse Pontine Gliomas

Phase 1

Completed

Conditions: Fibrillary Astrocytoma
Untreated Childhood Anaplastic Astrocytoma
Anaplastic Astrocytoma
Giant Cell Glioblastoma
Glioblastoma
Gliosarcoma
Untreated Childhood Fibrillary Astrocytoma
Untreated Childhood Gliosarcoma
Childhood Mixed Glioma
Untreated Childhood Brain Stem Glioma

Interventions: Radiation: 3-Dimensional Conformal Radiation Therapy
Radiation: Intensity-Modulated Radiation Therapy
Other: Laboratory Biomarker Analysis
Other: Pharmacological Study
Drug: Temozolomide
Drug: Veliparib

First Posted Date: 2012-01-23

Last Posted Date: 2019-08-13

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 66

Registration Number: NCT01514201

Locations: 🇺🇸
Lurie Children's Hospital-Chicago, Chicago, Illinois, United States
🇺🇸
Children's National Medical Center, Washington, District of Columbia, United States
🇺🇸
National Institutes of Health Clinical Center, Bethesda, Maryland, United States

and more 9 locations

Study Evaluating Efficacy And Tolerability Of Veliparib in Combination With Temozolomide (TMZ) or In Combination With Carboplatin and Paclitaxel Versus Placebo in Participants With Breast Cancer Gene (BRCA)1 and BRCA2 Mutation and Metastatic Breast Cancer

Phase 2

Completed

Conditions: Metastatic Breast Cancer

Interventions: Drug: Placebo
Drug: Veliparib
Drug: Carboplatin
Drug: Temozolomide
Drug: Paclitaxel

First Posted Date: 2012-01-10

Last Posted Date: 2021-10-25

Lead Sponsor: AbbVie

Target Recruit Count: 294

Registration Number: NCT01506609

Locations: 🇨🇦
Sunnybrook Health Sciences Ctr /ID# 77373, Toronto, Ontario, Canada
🇺🇸
The Angeles Clinic and Researc /ID# 60743, Los Angeles, California, United States
🇺🇸
University of Pennsylvania /ID# 60753, Philadelphia, Pennsylvania, United States

and more 117 locations

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