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Temozolomide

drug
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Also known as CCRG-81045M&B 39831M&B-39831M-39831MethazolastoneMk-7365NSC-362856SCH 52365SCH-52365TemodalTemodarTemomedacTemozolomidaTemozolomide accordTemozolomide hexalTemozolomide sandozTemozolomide sunTemozolomide tevaSID26719845

Summary

Temozolomide (CHEMBL810) is an approved small-molecule antineoplastic agent (ATC L01AX03); indicated across 84 conditions including central nervous system cancer and glioblastoma.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01AX03
  • Indications: 84 conditions
  • Clinical trials: 853
  • Chemistry: 194.15 Da · C6H6N6O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL810
NameTemozolomide
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID5394
ChEBICHEBI:72564
ATCL01AX03
Molecular formulaC6H6N6O2
Molecular weight194.15
InChIKeyBPEGJWRSRHCHSN-UHFFFAOYSA-N

SMILES: CN1C(=O)N2C=NC(=C2N=N1)C(=O)N

IUPAC name: 3-methyl-4-oxoimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide

ChEBI definition: An imidazotetrazine that is 3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine which is substituted at positions 3, 4, and 8 by methyl, oxo, and carboxamide groups, respectively. A prodrug for MTIC (5-(3-methyltriaz-1-en-1-yl)-1H-imidazole-4-carboxamide, formed by spontaneous hydrolysis of temozolomide in the body), it is used as an oral alkylating agent for the treatment of newly diagnosed malignant glioblastoma multiforme (concomitantly with radiotherapy) and malignant melanoma.

Pharmacological roles (ChEBI): antineoplastic agent, prodrug, alkylating agent.

Also known as: CCRG-81045, M&B 39831, M&B-39831, M-39831, Methazolastone, Mk-7365, NSC-362856, SCH 52365, SCH-52365, Temodal, Temodar, Temomedac

Patent coverage: 24,379 distinct patent families (97,713 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Polyadenylate-binding protein 1, Menin/Histone-lysine N-methyltransferase MLL.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
MEN15Potency10000nMCHEMBL_ACT_4589423

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

84 indications (9 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
central nervous system cancer4MONDO:0002714EFO:0000326
glioblastoma4MONDO:0018177EFO:0000519
neoplasm4MONDO:0005070EFO:0000616
glioma4MONDO:0021042EFO:0005543
melanoma3MONDO:0005105EFO:0000756
brain neoplasm3MONDO:0021211EFO:0003833
cutaneous melanoma3MONDO:0005012EFO:0000389
non-small cell lung carcinoma3MONDO:0005233EFO:0003060
neuroblastoma3MONDO:0005072EFO:0000621
Ewing sarcoma3MONDO:0012817EFO:0000174
astrocytoma (excluding glioblastoma)3MONDO:0019781EFO:0000272
metastatic melanoma3MONDO:0005191EFO:0002617
gliosarcoma3MONDO:0016681EFO:1001465
oligoastrocytoma3MONDO:0016702EFO:0000630
oligodendroglioma3MONDO:0016695EFO:0000632
anaplastic astrocytoma3MONDO:0016684EFO:0002499
anaplastic oligodendroglioma3MONDO:0016696EFO:0002501
optic nerve glioma3MONDO:0003235EFO:0009254
ganglioneuroblastoma3MONDO:0005035EFO:0000502
diffuse intrinsic pontine glioma3MONDO:0006033EFO:1000026
central nervous system neoplasm3MONDO:0006130EFO:1000158
brain cancer3MONDO:0001657MONDO:0001657
paraganglioma3MONDO:0000448EFO:1000453
leukemia2MONDO:0005059EFO:0000565
small cell lung carcinoma2MONDO:0008433EFO:0000702
lymphoma2MONDO:0005062EFO:0000574
sarcoma2MONDO:0005089EFO:0000691
medulloblastoma2MONDO:0007959EFO:0002939
acute myeloid leukemia2MONDO:0018874EFO:0000222
rectal cancer2MONDO:0006519EFO:1000657
brain disorder2MONDO:0005560EFO:0005774
hepatocellular carcinoma2MONDO:0007256EFO:0000182
myelodysplastic syndrome2MONDO:0018881EFO:0000198
alveolar rhabdomyosarcoma2MONDO:0009994EFO:0000248
embryonal rhabdomyosarcoma2MONDO:0009993EFO:0000437
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
rhabdomyosarcoma2MONDO:0005212EFO:0002918
spinal cord neoplasm2MONDO:0021234EFO:0003828
pancreatic neuroendocrine tumor2MONDO:0019954EFO:1000045
pineoblastoma2MONDO:0016722EFO:1000475
neuroendocrine neoplasm2MONDO:0019496EFO:1001901
hereditary breast ovarian cancer syndrome2MONDO:0003582Orphanet:145
colorectal neoplasm2MONDO:0005335EFO:0004142
pancreatic endocrine carcinoma2MONDO:0005893EFO:0007416
pituitary gland adenoma2MONDO:0006373EFO:1000478
soft tissue sarcoma2MONDO:0018078EFO:1001968
neuroendocrine carcinoma2MONDO:0002120MONDO:0002120
brainstem cancer2MONDO:0002912MONDO:0002914
breast neoplasm2MONDO:0021100MONDO:0007254
ovarian cancer2MONDO:0008170MONDO:0008170
lung neoplasm2MONDO:0021117MONDO:0008903
carcinoid tumor2MONDO:0005369MONDO:0024503
colorectal adenocarcinoma2MONDO:0005008EFO:0000365
lung neuroendocrine neoplasm2MONDO:0005454EFO:0005220
skin neoplasm2MONDO:0002531MONDO:0002898
retinoblastoma2MONDO:0008380MONDO:0008380
gastrointestinal stromal tumor2MONDO:0011719MONDO:0011719
neurofibromatosis type 12MONDO:0018975MONDO:0018975
adrenal gland pheochromocytoma2MONDO:0004974EFO:0000239
non-Hodgkin lymphoma2MONDO:0018908EFO:0005952
leiomyosarcoma2MONDO:0005058EFO:0000564
ocular melanoma2MONDO:0006325EFO:1000403
uveal melanoma2MONDO:0006486EFO:1000616
ependymoma1MONDO:0016698EFO:1000028
prostate adenocarcinoma1MONDO:0005082EFO:0000673
cytomegalovirus infection1MONDO:0005132EFO:0001062
aseptic meningitis1MONDO:0006662EFO:1000823
fallopian tube neoplasm1MONDO:0021092MONDO:0002158
Wilms tumor1MONDO:0006058MONDO:0006058
metastatic prostate carcinoma1MONDO:0004956EFO:0000196
desmoplastic small round cell tumor0MONDO:0019373EFO:1000895

13 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 853.

Phase distribution

PhaseTrials
PHASE2395
PHASE1181
PHASE1/PHASE2141
PHASE369
Not specified26
EARLY_PHASE119
PHASE2/PHASE318
PHASE44

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02496988PHASE4NOT_YET_RECRUITINGEffect of Cytokine-induced Killer Cells for Advanced Malignant Gliomas
NCT00686725PHASE4COMPLETEDStandard Temodal (Temozolomide) Regimen Versus Standard Regimen Plus Early Postsurgery Temodal for Newly Diagnosed Glioblastoma Multiforme (Study P05572)
NCT02343081PHASE4COMPLETEDBioequivalence Study of Temozolomide in Patients With Primary Tumors of the Central Nervous System
NCT06625047PHASE4COMPLETEDComparing Telehealth and In-person Assessments in Glioma Patients Receiving Oral Chemotherapy
NCT00626990PHASE3ACTIVE_NOT_RECRUITINGPhase III Trial of Anaplastic Glioma Without 1p/19q Loss of Heterozygosity (LOH)
NCT00978458PHASE3ACTIVE_NOT_RECRUITINGRadiation Therapy With or Without Temozolomide in Treating Patients With Low-Grade Glioma
NCT01649830PHASE3RECRUITINGEfficacy of Post-radiation Adjuvant Temozolomide Chemotherapy in Residue Low-grade Glioma
NCT02152982PHASE2/PHASE3ACTIVE_NOT_RECRUITINGTemozolomide With or Without Veliparib in Treating Patients With Newly Diagnosed Glioblastoma Multiforme
NCT02685605PHASE3ACTIVE_NOT_RECRUITINGIntraoperative Radiotherapy in Newly Diagnosed Glioblastoma Multiforme
NCT03970447PHASE2/PHASE3RECRUITINGA Trial to Evaluate Multiple Regimens in Newly Diagnosed and Recurrent Glioblastoma
NCT04164199PHASE3ACTIVE_NOT_RECRUITINGStudy of Tislelizumab, Pamiparib, and Other Investigational Agents in Participants With Advanced Malignancies
NCT04221035PHASE3RECRUITINGHigh-Risk Neuroblastoma Study 2 of SIOP-Europa-Neuroblastoma (SIOPEN)
NCT04316039PHASE2/PHASE3RECRUITINGRadiotherapy Versus Radiotherapy Combined With Temozolomide in High-risk Low-grade Gliomas After Surgery
NCT05095376PHASE3ACTIVE_NOT_RECRUITINGTesting the Addition of the Chemotherapy Drug Lomustine (Gleostine) to the Usual Treatment (Temozolomide and Radiation Therapy) for Newly Diagnosed MGMT Methylated Glioblastoma
NCT05271240PHASE3RECRUITINGRepeated Superselective Intraarterial Cerebral Infusion (SIACI) of Bevacizumab With Temozolomide and Radiation Compared to Temozolomide and Radiation Alone in Newly Diagnosed GBM
NCT05432791PHASE2/PHASE3ACTIVE_NOT_RECRUITINGTesting Olaparib and Temozolomide Versus the Usual Treatment for Uterine Leiomyosarcoma After Chemotherapy Has Stopped Working
NCT05439278PHASE3RECRUITINGConventional Versus Hypofractionated Radiotherapy With Temozolomide in Elderly Glioblastoma
NCT05685004PHASE2/PHASE3ACTIVE_NOT_RECRUITINGStudy of Neoantigen-specific Adoptive T Cell Therapy for Newly Diagnosed MGMT Negative Glioblastoma Multiforme (GBM)
NCT05902169PHASE3RECRUITINGSonocloud-9 in Association With Carboplatin Versus Standard-of-Care Chemotherapies (CCNU or TMZ) in Recurrent GBM
NCT06105619PHASE2/PHASE3ACTIVE_NOT_RECRUITINGA Study of PLB1001 Enteric Capsules in the Treatment of sGBM/IDH Mutant Glioblastoma Patients With the ZM Fusion Gene (FUGEN).
NCT06172296PHASE3RECRUITINGDinutuximab With Chemotherapy, Surgery and Stem Cell Transplantation for the Treatment of Children With Newly Diagnosed High Risk Neuroblastoma
NCT06346067PHASE3ACTIVE_NOT_RECRUITINGA Study to Assess Naporafenib (ERAS-254) Administered With Trametinib in Patients With NRAS-mutant Melanoma (SEACRAFT-2)
NCT06388733PHASE3RECRUITINGA Study Comparing Niraparib With Temozolomide in Adult Participants With Newly-diagnosed, MGMT Unmethylated Glioblastoma
NCT06419946PHASE3RECRUITINGLomustine in Addition to Standard of Care in Patients With MGMT Methylated Glioblastoma
NCT06448286PHASE3NOT_YET_RECRUITINGPH Weighted Chemical Exchange Saturation Transfer MRI-Based Surgical Resection to Improve Survival in Patients With Glioblastoma
NCT06490536PHASE3RECRUITINGThe Sagittarius Trial
NCT06556563PHASE3RECRUITINGEF-41/KEYNOTE D58: Phase 3 Study of Optune Concomitant With Temozolomide Plus Pembrolizumab in Newly Diagnosed Glioblastoma
NCT06743126PHASE3RECRUITINGSUPRAME-ACTengine® IMA203 vs. Investigator’s Choice of Treatment in Previously Treated, Unresectable or Metastatic Cutaneous Melanoma
NCT07104032PHASE3RECRUITINGIGNITE: Study of Tirabrutinib vs Rituximab/Temozolomide for Relapsed/Refractory Primary Central Nervous System Lymphoma (PCNSL)
NCT07195591PHASE3RECRUITINGBeginning Radiation Immediately With GammaTile at GBM Excision Versus Standard of Care
NCT07215910PHASE3NOT_YET_RECRUITINGTesting Addition of an Anti-cancer Drug, Vorasidenib to Temozolomide, After Radiation for Advanced Brain Cancer
NCT07375563PHASE3RECRUITINGChemoimmunotherapy Combined With Autologous NK Cell Therapy for Pediatric Patients With Refractory and Relapsed High-Risk Neuroblastoma and Ganglioneuroblastoma
NCT07452458PHASE3NOT_YET_RECRUITINGTemporally-Modulated Pulsed Radiation Therapy Versus Standard Radiation Therapy for the Treatment of Newly Diagnosed, IDH Wildtype, MGMT-Unmethylated Glioblastoma
NCT07549321PHASE2/PHASE3RECRUITINGA Safety and Efficacy Study of hu14 in High-Risk Neuroblastoma Patients
NCT07605364PHASE2/PHASE3NOT_YET_RECRUITINGTesting the Addition of an Anti-Cancer Drug, Mycophenolate Mofetil, to the Usual Treatment (Radiation Therapy and Temozolomide) for Advanced Brain Cancer
NCT00006353PHASE3COMPLETEDRadiation Therapy With or Without Temozolomide in Treating Patients With Newly Diagnosed Glioblastoma Multiforme
NCT00020839PHASE3TERMINATEDTemozolomide With or Without Radiation Therapy to the Brain in Treating Patients With Stage IV Melanoma That Is Metastatic to the Brain
NCT00052455PHASE3COMPLETEDTemozolomide Compared to Procarbazine, Lomustine, and Vincristine in Treating Patients With Recurrent Malignant Glioma
NCT00068952PHASE3COMPLETEDStudy of IV Edotecarin Vs Temozolomide or Carmustine (BCNU) or Lomustine (CCNU) in Patients With Glioblastoma Multiforme
NCT00091572PHASE3COMPLETEDTemozolomide Versus Dacarbazine in Stage IV Metastatic Melanoma (Study P03267)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 8 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 16

This page pulls from 16 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclinical_trialsefogtopdb_interactiongtopdb_ligandmeshmondopatent_compoundpharmgkbpharmgkb_guidelinepubchemuniprot