Temozolomide
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1999
- First approval year
- 1999
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Temozolomide
- Molecular weight
- 194.15
- Structure (SMILES)
- Cn1nnc2c(C(N)=O)ncn2c1=O
- temodal
- Temodal
- temodar
- Temodar
- temomedac
- Temomedac
- temozolomide
- Temozolomide
- temozolomide accord
- Temozolomide accord
- temozolomide hexal
- Temozolomide hexal
- temozolomide sandoz
- Temozolomide sandoz
- temozolomide sun
- Temozolomide sun
- temozolomide teva
- Temozolomide teva
- 3 4 dihydro 3 methyl 4 oxoimidazo 5 1 d as tetrazine 8 carboxamide
- 3,4-Dihydro-3-methyl-4-oxoimidazo[5,1-d]-as-tetrazine-8-carboxamide
- abemaciclib temozolomide
- ccrg 81045
- CCRG-81045
- m 39831
- m b 39831
- M-39831
- M&B 39831
- M&B-39831
- methazolastone
- Methazolastone
- mk 7365
- Mk-7365
- nsc 362856
- NSC-362856
- sch 52365
- SCH 52365
- SCH-52365
- Temodal
- temodar
- Temodar
- Temodar (Temozolomide)
- Temodar® (temozolomide)
- temozolomida
And 46 more, listed on the interactive page.
- ATC classification codes
- L01AX03
Sources for recorded values
- CAS registry numbers
- 85622-93-1
- ChEMBL ID
- CHEMBL810
- InChIKey
- BPEGJWRSRHCHSN-UHFFFAOYSA-N
- PubChem compound IDs
- 5394
- RxNorm IDs (RxCUI)
- 37776
- FDA ingredient codes (UNII)
- YF1K15M17Y
- Applicant
- MERCK SHARP DOHME
- Approval date
- 11 Aug 1999
- Application number
- NDA021029
- Status
- Authorised
- Status date
- 26 Jan 1999
- Authorisation date
- 26 Jan 1999
- Approved indications
- Temodal hard capsules is indicated for the treatment of: adult patients with newly diagnosed glioblastoma multiforme concomitantly with radiotherapy and subsequently as monotherapy treatment; children from the age of three years, adolescents and adult patients with malignant glioma, such as glioblastoma multiforme or anaplastic astrocytoma, showing recurrence or progression after standard therapy.
- Product number
- EMEA/H/C/000229
- Authorisation holder
- Merck Sharp & Dohme B.V.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 4
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Glioma
European medicines record
- Patents
- 0
- Designations
- 5
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- temozolomide
- Type
- Synthetic organic
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Parenteral
Mechanisms of action
- Mechanism
- DNA inhibitor
- Action type
- Inhibitor
- Target
- DNA
- Condition
- Sarcoma, Ewing
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000174
- Subject identifier
- D012512
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000196
- Subject identifier
- D011471
- Condition
- Myelodysplastic Syndromes
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000198
- Subject identifier
- D009190
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Pheochromocytoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000239
- Subject identifier
- D010673
- Condition
- Rhabdomyosarcoma, Alveolar
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000248
- Subject identifier
- D018232
- Condition
- Astrocytoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000272
- Subject identifier
- D001254
- Condition
- Glioma
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000326
- Subject identifier
- D005910
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000365
- Subject identifier
- D015179
- Condition
- Melanoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000389
- Subject identifier
- D008545
- Condition
- Rhabdomyosarcoma, Embryonal
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000437
- Subject identifier
- D018233
- Condition
- Ganglioneuroblastoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000502
- Subject identifier
- D018305
- Condition
- Glioblastoma
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Leiomyosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000564
- Subject identifier
- D007890
- Condition
- Leukemia
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Lymphoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Neuroblastoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000621
- Subject identifier
- D009447
- Condition
- Oligodendroglioma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000630
- Subject identifier
- D009837
- Condition
- Oligodendroglioma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000632
- Subject identifier
- D009837
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000673
- Subject identifier
- D011471
- Condition
- Sarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000691
- Subject identifier
- D012509
- Condition
- Small Cell Lung Carcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000702
- Subject identifier
- D055752
- Condition
- Melanoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
And 59 more, listed on the interactive page.
- Condition identifier
- EFO_0000174
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000182
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000222
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000239
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000272
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000389
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000519
- Condition identifier
- EFO_0000564
- Condition identifier
- EFO_0000565
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000574
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000621
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000630
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000632
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000658
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000702
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 3
- Condition identifier
- EFO_0002499
- Highest recorded phase
- 3
- Condition identifier
- EFO_0002501
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002617
- Highest recorded phase
- 3
- Condition identifier
- EFO_0002939
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Condition identifier
- EFO_0003833
- Highest recorded phase
- 3
- Condition identifier
- EFO_0005220
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005543
And 141 more, listed on the interactive page.
Warnings
- Warning
- Black Box Warning
Open Targets warnings
- Warning
- Black Box Warning
- Country
- United States
- Event
- alanine aminotransferase increased
- Reports
- 155
- Reporting signal score
- 92.8449
- Event
- aplastic anaemia
- Reports
- 63
- Reporting signal score
- 140.222
- Event
- bone marrow failure
- Reports
- 169
- Reporting signal score
- 263.458
- Event
- brain oedema
- Reports
- 100
- Reporting signal score
- 226.786
- Event
- convulsion
- Reports
- 151
- Reporting signal score
- 104.573
- Event
- deep vein thrombosis
- Reports
- 150
- Reporting signal score
- 93.4563
- Event
- desmoplastic small round cell tumour
- Reports
- 18
- Reporting signal score
- 93.7117
- Event
- disease progression
- Reports
- 481
- Reporting signal score
- 709.192
- Event
- disease recurrence
- Reports
- 113
- Reporting signal score
- 148.99
- Event
- febrile bone marrow aplasia
- Reports
- 50
- Reporting signal score
- 94.1678
- Event
- febrile neutropenia
- Reports
- 245
- Reporting signal score
- 261.918
- Event
- glioblastoma
- Reports
- 67
- Reporting signal score
- 246.422
- Event
- glioblastoma multiforme
- Reports
- 46
- Reporting signal score
- 184.302
- Event
- haematotoxicity
- Reports
- 119
- Reporting signal score
- 252.486
- Event
- hemiparesis
- Reports
- 79
- Reporting signal score
- 97.5772
- Event
- hospice care
- Reports
- 57
- Reporting signal score
- 116.533
- Event
- hypermutation
- Reports
- 45
- Reporting signal score
- 249.897
- Event
- leukopenia
- Reports
- 162
- Reporting signal score
- 135.351
- Event
- lymphopenia
- Reports
- 189
- Reporting signal score
- 382.673
- Event
- malignant neoplasm progression
- Reports
- 289
- Reporting signal score
- 389.409
- Event
- metastases to liver
- Reports
- 76
- Reporting signal score
- 118.853
- Event
- myelosuppression
- Reports
- 100
- Reporting signal score
- 180.777
- Event
- nausea
- Reports
- 577
- Reporting signal score
- 104.271
- Event
- neoplasm progression
- Reports
- 132
- Reporting signal score
- 191.271
- Event
- neutropenia
- Reports
- 333
- Reporting signal score
- 231.089
And 7 more, listed on the interactive page.
- NCT00003062
- NCT00005037
- NCT00006877
- NCT00022711
- NCT00080938
- NCT00238251
- NCT00385398
- NCT00740636
- NCT02133677
- NCT03830918
- NCT00003176
- NCT00003304
- NCT00003464
- NCT00003465
- NCT00003466
- NCT00003567
- NCT00003731
- NCT00004068
- NCT00004113
- NCT00004200
- NCT00004204
- NCT00004259
- NCT00005637
- NCT00005951
- NCT00005954
And 628 more, listed on the interactive page.
- Dose
- 75 mg/m2
- Route
- Oral, intravenous
- How often
- Once daily during concomitant phase for 42 to 49 days, then once daily on days 1-5 of 28-day cycle for 6 cycles, with potential escalation for maintenance phase
- Administer during concomitant radiotherapy phase in combination with focal radiotherapy
- Obtain complete blood counts weekly during treatment
- Hydrogen bond acceptors
- 7
- Hydrogen bond donors
- 1
- Polar surface area
- 108.17
- Calculated partition coefficient (ALogP)
- -2.08
- Calculated partition coefficient (XLogP)
- -1.1
- Prodrug
- Yes
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 1
- Heavy atoms
- 14
- Molecular formula
- C6H6N6O2
- Monoisotopic mass
- 194.05522346
- Natural product
- Yes
- 0085-1366
- 0085-1381
- 0085-1417
- 0085-1425
- 0085-1430
- 0085-1519
- 0085-3004
- 16571-816
- 16571-817
- 16571-818
- 16571-819
- 16571-820
- 16571-821
- 16729-048
- 16729-049
- 16729-050
- 16729-051
- 16729-129
- 16729-130
- 31722-411
- 31722-412
- 31722-413
- 31722-414
- 31722-415
- 31722-416
And 46 more, listed on the interactive page.
- Recorded assays
- 3,798
- Active assays
- 70
- Confirmatory
- Other
- Screening
- Antineoplastic Agents, Alkylating
These details could not be displayed.
Related records
Trials (930)
- 131I-Omburtamab, in Recurrent Medulloblastoma and Ependymoma
- 18F-DOPA-PET in Finding Tumors in Patients With Newly Diagnosed Gliomas Undergoing Radiation Therapy
- 18F-DOPA-PET/MRI Scan in Imaging Elderly Patients With Newly Diagnosed Grade IV Malignant Glioma or Glioblastoma During Planning for a Short Course of Proton Beam Radiation Therapy
- 5 Fraction Stereotactic Radiosurgery With Temozolomide for Glioblastoma Multiforme
- 5FU/LV, Irinotecan, Temozolomide and Bevacizumab for MGMT Silenced, Microsatellite Stable Metastatic Colorectal Cancer.
- 5G-PEARL: Paxalisib in Malignant Brain Tumours
- 5G-RUBY: Avutometinib and Defactinib in Malignant Brain Tumours
- 6-TG, Capecitabine and Celecoxib Plus TMZ or CCNU for Anaplastic Glioma Patients
- 9-ING-41 in Pediatric Patients With Refractory Malignancies.
- A Clinical Study on the Efficacy and Safety of Methotrexate (MTX) or Thiotepa (for MTX Intolerance) or Temozolomide (TMZ) Combined With Orelabrutinib and Selinexor in Relapsed/Refractory Primary or Secondary Central Nervous System Lymphoma（SELINA）
- A Clinical Trial Evaluating the Efficacy of Valganciclovir in Glioblastoma Patients
- A Clinical Trial on Whole-brain Radiotherapy With Temozolomide Concurrent Chemotherapy or Avoidance of Hippocampus for Patients of Brain Metastases
- A Clinical Trial Testing the Safety of the Investigational Drug Pumitamig (BNT327) and How Well it Works in Patients With Recurrent Glioblastoma
- A Comparison of Continuous Bevacizumab (Avastin) Treatment or Placebo in Addition to Lomustine Followed by Standard of Care After Disease Progression in Participants With Glioblastoma
- A Dose Per Fraction Escalation Trial of Hypofractionated IMRT With Temozolomide for Newly Diagnosed Glioblastoma
- A Large-scale Research for Immunotherapy of Glioblastoma With Autologous Heat Shock Protein gp96
- A Longitudinal Assessment of Tumor Evolution in Patients With Brain Cancer
- A Master Protocol (LY900023) That Includes Several Clinical Trials of Drugs for Children and Young Adults With Cancer
- A Multi-Arm, Platform Trial For Relapsed Neuroblastoma
- A Phase 0/1 Study of BDTX-1535 in Recurrent High-Grade Glioma (rHGG) and Newly Diagnosed Glioblastoma (nGBM) Participants With EGFR Alterations or Fusions
Approved for (9)
- Adult glioblastoma
- Cancer
- Central nervous system cancer
- Glioblastoma
- Glioma
- Low grade glioma
- Malignant glioma
- Mixed glioma
- Neoplasm
In development for (77)
- Acute myeloid leukemia Phase 2
- Adrenal gland pheochromocytoma Phase 2
- Adult brainstem glioma Phase 2
- Alveolar rhabdomyosarcoma Phase 2
- Anaplastic astrocytoma Phase 3
- Anaplastic oligodendroglioma Phase 3
- Aseptic meningitis Phase 1
- Astrocytoma (excluding glioblastoma) Phase 3
- Biliary tract cancer Phase 2
- Brain cancer Phase 3
- Brain disorder Phase 2
- Brain neoplasm Phase 3
- Breast cancer Phase 2
- Central nervous system neoplasm Phase 3
- Childhood brain stem neoplasm Phase 2
- Choroid plexus neoplasm Phase 3
- Colorectal adenocarcinoma Phase 2
- Colorectal cancer Phase 2
- Colorectal neoplasm Phase 2
- Cutaneous melanoma Phase 3