temozolomide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
2589 85622-93-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • temomedac
  • SCH 52365
  • temozolomide
  • methazolastone
  • temodal
  • temozolamide
Temozolomide is not directly active but undergoes rapid nonenzymatic conversion at physiologic pH to the reactive compound 5-(3-methyltriazen1-yl)-imidazole-4-carboxamide (MTIC). The cytotoxicity of MTIC is thought to be primarily due to alkylation of DNA.
  • Molecular weight: 194.15
  • Formula: C6H6N6O2
  • CLOGP: -0.81
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 1
  • TPSA: 105.94
  • ALOGS: -1.58
  • ROTB: 1
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 5.60 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 25.46 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 96 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.50 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3.60 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.50 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 3 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.873 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.782 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 25.763 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 11.169 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 92.800 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 93.640 % High 1
herg hERG pIC50 3.632 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 5.728 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.034 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 83.140 % High 1
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,CAMK2D,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,GRK2,MAP3K21,MAPK7,PDK1,PIK3CD,PRKDC,SIK2,TEK 18
kinase-selectivity-class GRK2 1
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 1.233 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 5.728 High 1
mh-clint Mouse hepatocyte intrinsic clearance 25.763 High 1
mppb Mouse plasma protein binding (% unbound) 88.520 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 3.214 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 87.470 % High 1
rat-kpuu-brain Rat brain Kpuu 0.673 % High 1
rh-clint Rat hepatocyte intrinsic clearance 9.594 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 98.860 % High 1
rppb Rat plasma protein binding (% unbound) 76.890 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 1028.016 uM High 1

Approvals:

DateAgencyCompanyOrphan
July 26, 2007 PMDA Schering-Plough K.K.
Aug. 11, 1999 FDA MERCK SHARP DOHME
Jan. 26, 1999 EMA MERCK SHARP & DOHME B.V.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Disease progression 1002.14 23.03 574 22533 156041 90449299
Thrombocytopenia 874.36 23.03 584 22523 208141 90397199
Malignant neoplasm progression 653.98 23.03 381 22726 106489 90498851
Product use in unapproved indication 562.75 23.03 550 22557 335686 90269654
Pancytopenia 407.32 23.03 296 22811 119967 90485373
Tumour pseudoprogression 376.15 23.03 75 23032 646 90604694
Hypermutation 362.89 23.03 52 23055 18 90605322
Death 313.61 23.03 476 22631 456075 90149265
Neoplasm progression 302.12 23.03 170 22937 44316 90561024
Neutropenia 256.71 23.03 301 22806 224603 90380737
Off label use 253.29 23.03 731 22376 1101521 89503819
Bone marrow failure 245.87 23.03 133 22974 32088 90573252
Lymphopenia 236.93 23.03 116 22991 22765 90582575
Seizure 236.42 23.03 240 22867 152389 90452951
Myelosuppression 213.90 23.03 146 22961 53445 90551895
Platelet count decreased 198.73 23.03 208 22899 136761 90468579
Metastases to liver 187.20 23.03 107 23000 28700 90576640
Febrile neutropenia 172.33 23.03 207 22900 158142 90447198
Haematotoxicity 168.14 23.03 76 23031 12459 90592881
Vasogenic cerebral oedema 157.21 23.03 41 23066 1249 90604091
Therapy partial responder 157.10 23.03 87 23020 21956 90583384
Disease recurrence 151.20 23.03 103 23004 37550 90567790
Aplastic anaemia 130.58 23.03 65 23042 13204 90592136
Eastern Cooperative Oncology Group performance status worsened 123.19 23.03 37 23070 1902 90603438
Leukopenia 113.33 23.03 134 22973 100576 90504764
Brain oedema 111.38 23.03 64 23043 17321 90588019
Hospice care 105.85 23.03 51 23056 9653 90595687
Joint swelling 101.28 23.03 7 23100 503293 90102047
Glioblastoma multiforme 91.49 23.03 25 23082 913 90604427
Herpes simplex encephalitis 84.57 23.03 20 23087 403 90604937
Radiation necrosis 80.13 23.03 21 23086 652 90604688
Metastases to central nervous system 77.65 23.03 51 23056 17491 90587849
Glioblastoma 77.61 23.03 22 23085 921 90604419
Nausea 75.63 23.03 512 22595 1109804 89495536
Pulmonary embolism 75.01 23.03 126 22981 130694 90474646
Diffuse large B-cell lymphoma recurrent 72.66 23.03 29 23078 3497 90601843
Hemiparesis 72.27 23.03 62 23045 31757 90573583
Infusion related reaction 70.51 23.03 11 23096 416769 90188571
Metastases to peritoneum 68.06 23.03 29 23078 4126 90601214
Glossodynia 66.09 23.03 4 23103 321775 90283565
Neurological symptom 65.77 23.03 33 23074 6814 90598526
Recurrent cancer 64.12 23.03 24 23083 2435 90602905
Brain neoplasm 63.67 23.03 29 23078 4835 90600505
Wound 61.52 23.03 4 23103 302976 90302364
Eastern Cooperative Oncology Group performance status improved 59.24 23.03 9 23098 9 90605331
Arthralgia 59.11 23.03 67 23040 778455 89826885
Angina bullosa haemorrhagica 58.46 23.03 12 23095 121 90605219
Ascites 56.12 23.03 65 23042 47675 90557665
Sinusitis 55.92 23.03 10 23097 343078 90262262
Abdominal discomfort 52.75 23.03 28 23079 477300 90128040
Neoplasm recurrence 50.92 23.03 22 23085 3237 90602103
Malignant glioma 50.48 23.03 8 23099 13 90605327
Sepsis 50.45 23.03 129 22978 179685 90425655
Disseminated cryptococcosis 50.26 23.03 15 23092 754 90604586
Swelling 50.23 23.03 22 23085 419036 90186304
Central nervous system necrosis 49.82 23.03 11 23096 161 90605179
Maternal exposure during pregnancy 49.76 23.03 15 23092 360048 90245292
Asthma 49.74 23.03 3 23104 242157 90363183
Musculoskeletal stiffness 49.74 23.03 8 23099 296524 90308816
Metastases to lymph nodes 49.35 23.03 33 23074 11656 90593684
Peripheral swelling 49.03 23.03 22 23085 413084 90192256
Pneumocystis jirovecii pneumonia 48.84 23.03 42 23065 21574 90583766
Metastasis 48.65 23.03 26 23081 6111 90599229
Vomiting 47.88 23.03 354 22753 787939 89817401
Mental status changes 47.84 23.03 58 23049 44621 90560719
Brain neoplasm malignant 47.10 23.03 16 23091 1225 90604115
White blood cell count decreased 46.99 23.03 120 22987 166989 90438351
Pain 46.73 23.03 117 22990 996224 89609116
Magnetic resonance imaging head abnormal 45.74 23.03 19 23088 2537 90602803
Drug resistance 45.43 23.03 47 23060 30402 90574938
Agranulocytosis 45.12 23.03 50 23057 34952 90570388
Drug hypersensitivity 44.55 23.03 32 23075 463577 90141763
Hydrocephalus 43.26 23.03 24 23083 6070 90599270
Blood cholesterol increased 41.47 23.03 3 23104 208009 90397331
Gliosarcoma 41.22 23.03 6 23101 3 90605337
Platelet transfusion 40.78 23.03 14 23093 1106 90604234
Ganglioneuroma 40.74 23.03 9 23098 132 90605208
Muscle swelling 40.50 23.03 12 23095 588 90604752
Acute myeloid leukaemia 40.45 23.03 37 23070 20603 90584737
Crystal nephropathy 40.41 23.03 14 23093 1137 90604203
Corneal toxicity 40.10 23.03 8 23099 69 90605271
Dehydration 39.38 23.03 124 22983 194323 90411017
Facial asymmetry 39.16 23.03 13 23094 927 90604413
Petechiae 38.47 23.03 32 23075 15709 90589631
Blister 38.29 23.03 9 23098 254989 90350351
Product administered to patient of inappropriate age 37.69 23.03 20 23087 4633 90600707
DNA mismatch repair protein gene mutation 36.37 23.03 5 23102 0 90605340
Enterocutaneous fistula 36.13 23.03 14 23093 1560 90603780
Jaw operation 36.10 23.03 12 23095 859 90604481
Deep vein thrombosis 35.90 23.03 75 23032 91545 90513795
Rhabdoid tumour 35.78 23.03 7 23100 54 90605286
Discomfort 35.14 23.03 13 23094 274322 90331018
Optic neuropathy 35.04 23.03 16 23091 2682 90602658
Migraine 34.60 23.03 4 23103 190388 90414952
Hepatic enzyme increased 34.51 23.03 25 23082 360711 90244629
Anaemia 34.30 23.03 179 22928 352623 90252717
Nasopharyngitis 34.25 23.03 32 23075 407072 90198268
Early satiety 34.03 23.03 13 23094 1394 90603946
Therapy change 33.95 23.03 23 23084 8299 90597041
Metastases to bone 33.85 23.03 37 23070 25468 90579872
Lymphocyte count decreased 33.52 23.03 43 23064 35007 90570333
Weight increased 32.70 23.03 35 23072 417892 90187448
Asthenia 32.49 23.03 240 22867 533511 90071829
Drug ineffective 32.35 23.03 513 22594 1383785 89221555
Therapy cessation 32.27 23.03 43 23064 36318 90569022
Sialoadenitis 31.72 23.03 14 23093 2168 90603172
Anxiety 31.59 23.03 20 23087 309752 90295588
Hypersensitivity 31.40 23.03 42 23065 454635 90150705
Neutrophil count abnormal 31.35 23.03 17 23090 4111 90601229
Vulval disorder 31.02 23.03 12 23095 1332 90604008
Renal-limited thrombotic microangiopathy 30.95 23.03 8 23099 235 90605105
Type 2 diabetes mellitus 30.85 23.03 7 23100 203237 90402103
Glioma 30.56 23.03 9 23098 432 90604908
Metastases to lung 30.04 23.03 28 23079 15963 90589377
Lethargy 29.95 23.03 56 23051 63083 90542257
Cerebral haemorrhage 29.38 23.03 40 23067 34482 90570858
Primary progressive aphasia 29.10 23.03 4 23103 0 90605340
Metastatic malignant melanoma 28.82 23.03 12 23095 1612 90603728
Mobility decreased 28.72 23.03 14 23093 250720 90354620
Diffuse large B-cell lymphoma 28.55 23.03 21 23086 8624 90596716
Impaired healing 28.51 23.03 12 23095 234187 90371153
Blood disorder 28.18 23.03 20 23087 7770 90597570
Penetrating aortic ulcer 27.95 23.03 5 23102 22 90605318
Constipation 27.74 23.03 143 22964 280252 90325088
Disorientation 27.29 23.03 44 23063 44070 90561270
Depression 27.25 23.03 22 23085 300579 90304761
Psoriasis 27.11 23.03 3 23104 147751 90457589
Arthritis 26.97 23.03 5 23102 167310 90438030
Gastrooesophageal reflux disease 26.75 23.03 5 23102 166332 90439008
White blood cell count abnormal 26.54 23.03 19 23088 7485 90597855
Malaise 26.47 23.03 70 23037 585916 90019424
Oesophagitis 26.41 23.03 27 23080 17222 90588118
Medulloblastoma recurrent 26.06 23.03 6 23101 107 90605233
Mucosal inflammation 25.95 23.03 50 23057 57575 90547765
Intracranial tumour haemorrhage 25.87 23.03 7 23100 246 90605094
Gastroenteropancreatic neuroendocrine tumour disease 25.74 23.03 5 23102 37 90605303
Myelodysplastic syndrome 25.47 23.03 29 23078 20874 90584466
Needle issue 25.41 23.03 24 23083 13910 90591430
Coagulation time prolonged 25.07 23.03 11 23096 1679 90603661
Alopecia 24.01 23.03 57 23050 495014 90110326
Neutrophil count decreased 23.98 23.03 55 23052 71477 90533863
Drug clearance decreased 23.85 23.03 11 23096 1887 90603453
Drug intolerance 23.79 23.03 49 23058 447542 90157798
Dyspnoea 23.72 23.03 130 22977 880825 89724515
Metastases to bone marrow 23.57 23.03 8 23099 611 90604729
Lung infiltration 23.54 23.03 24 23083 15258 90590082
Condition aggravated 23.37 23.03 76 23031 595469 90009871
Tumour necrosis 23.32 23.03 9 23098 992 90604348
Acute hepatitis B 23.26 23.03 7 23100 362 90604978
Gastritis fungal 23.25 23.03 6 23101 175 90605165
Cryptococcosis 23.21 23.03 10 23097 1461 90603879
Pneumonia fungal 23.04 23.03 17 23090 7014 90598326

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Disease progression 1120.76 18.33 794 22889 142862 42454790
Product use in unapproved indication 674.57 18.33 658 23025 183798 42413854
Malignant neoplasm progression 358.45 18.33 367 23316 108033 42489619
Tumour pseudoprogression 344.15 18.33 86 23597 964 42596688
Thrombocytopenia 307.09 18.33 448 23235 189831 42407821
Neoplasm progression 275.92 18.33 182 23501 28818 42568834
Hypermutation 257.90 18.33 42 23641 18 42597634
Seizure 239.37 18.33 314 23369 120247 42477405
Lymphopenia 238.94 18.33 149 23534 21414 42576238
Death 203.34 18.33 647 23036 470538 42127114
Nausea 179.29 18.33 554 23129 396245 42201407
Myelosuppression 142.50 18.33 142 23541 40319 42557333
Recurrent cancer 134.45 18.33 46 23637 1627 42596025
Disease recurrence 130.92 18.33 118 23565 29560 42568092
Off label use 125.58 18.33 689 22994 637646 41960006
Vanishing bile duct syndrome 121.87 18.33 44 23639 1827 42595825
Glioblastoma 109.66 18.33 38 23645 1397 42596255
Vomiting 104.92 18.33 376 23307 289347 42308305
Cholestatic liver injury 89.73 18.33 43 23640 3666 42593986
Metastases to liver 88.39 18.33 73 23610 16253 42581399
Hemiparesis 84.42 18.33 73 23610 17303 42580349
Brain operation 82.23 18.33 24 23659 499 42597153
Brain oedema 82.18 18.33 70 23613 16257 42581395
Hospice care 79.84 18.33 53 23630 8460 42589192
Constipation 74.06 18.33 228 23455 162063 42435589
Therapy partial responder 73.66 18.33 72 23611 19949 42577703
Radiation necrosis 73.43 18.33 19 23664 247 42597405
Eastern Cooperative Oncology Group performance status worsened 70.79 18.33 27 23656 1309 42596343
Malignant glioma 68.33 18.33 13 23670 32 42597620
Aphasia 66.01 18.33 74 23609 24009 42573643
Haematotoxicity 65.55 18.33 52 23631 10933 42586719
Fatigue 62.83 18.33 435 23248 435206 42162446
Metastases to lung 61.66 18.33 51 23632 11373 42586279
Product use issue 61.09 18.33 133 23550 76618 42521034
Hydrocephalus 59.82 18.33 39 23644 6039 42591613
Neoplasm recurrence 58.16 18.33 29 23654 2695 42594957
Drug ineffective 54.04 18.33 560 23123 629637 41968015
Intracranial tumour haemorrhage 52.49 18.33 16 23667 388 42597264
Neutropenia 52.04 18.33 234 23449 199197 42398455
Diaphragmatic spasm 50.79 18.33 12 23671 104 42597548
Product administered to patient of inappropriate age 50.44 18.33 32 23651 4729 42592923
Brain neoplasm 48.14 18.33 28 23655 3540 42594112
Glioblastoma multiforme 47.36 18.33 18 23665 864 42596788
Pancytopenia 45.16 18.33 156 23527 117587 42480065
Diabetes insipidus 44.51 18.33 27 23656 3686 42593966
Arthralgia 44.13 18.33 30 23653 205208 42392444
Metastases to lymph nodes 43.73 18.33 32 23651 5966 42591686
Metastases to peritoneum 43.40 18.33 23 23660 2426 42595226
Pancreatic neuroendocrine tumour metastatic 43.39 18.33 11 23672 131 42597521
Faecal volume decreased 43.06 18.33 12 23671 210 42597442
Metastases to meninges 42.23 18.33 21 23662 1940 42595712
Pulmonary embolism 40.36 18.33 152 23531 119460 42478192
Dyspnoea 38.74 18.33 122 23561 442499 42155153
Platelet count decreased 37.15 18.33 164 23519 138417 42459235
Bone marrow failure 36.78 18.33 66 23617 33027 42564625
Metastasis 36.35 18.33 26 23657 4679 42592973
Brain tumour operation 35.91 18.33 6 23677 4 42597648
Metastases to central nervous system 35.78 18.33 36 23647 10319 42587333
Hepatic lesion 35.10 18.33 25 23658 4469 42593183
Myocardial infarction 34.29 18.33 13 23670 123996 42473656
Therapy cessation 34.00 18.33 49 23634 20401 42577251
Herpes simplex encephalitis 32.58 18.33 11 23672 373 42597279
Deep vein thrombosis 32.17 18.33 105 23578 76852 42520800
Intussusception 31.99 18.33 13 23670 746 42596906
Confusional state 31.91 18.33 180 23503 167417 42430235
Drug interaction 31.56 18.33 63 23620 266936 42330716
Magnetic resonance imaging head abnormal 31.45 18.33 16 23667 1551 42596101
Nasopharyngitis 30.54 18.33 5 23678 83991 42513661
Lymphocyte count decreased 30.31 18.33 55 23628 27754 42569898
Biliary obstruction 30.02 18.33 20 23663 3209 42594443
Astrocytoma 29.81 18.33 9 23674 211 42597441
Brain neoplasm malignant 29.30 18.33 13 23670 928 42596724
Radiation injury 28.88 18.33 11 23672 531 42597121
Epilepsy 28.83 18.33 52 23631 26119 42571533
Product dose omission issue 28.82 18.33 26 23657 154339 42443313
Acquired gene mutation 28.46 18.33 15 23668 1565 42596087
Parathyroid tumour malignant 28.12 18.33 7 23676 77 42597575
Atrial fibrillation 27.91 18.33 22 23661 139571 42458081
Bone marrow disorder 27.89 18.33 16 23667 1970 42595682
Tumour haemorrhage 27.87 18.33 20 23663 3618 42594034
Oligodendroglioma 27.47 18.33 6 23677 35 42597617
Metastases to bone 26.87 18.33 37 23646 14772 42582880
Swelling of eyelid 26.87 18.33 16 23667 2112 42595540
Nephrogenic diabetes insipidus 25.70 18.33 14 23669 1560 42596092
Cardiac failure congestive 25.34 18.33 8 23675 85594 42512058
Cardiac failure 25.19 18.33 14 23669 106842 42490810
COVID-19 24.83 18.33 17 23666 115931 42481721
Hyperkalaemia 24.76 18.33 7 23676 80451 42517201
Rosacea 24.67 18.33 13 23670 1355 42596297
Pneumocystis jirovecii pneumonia 23.96 18.33 47 23636 25134 42572518
Acute kidney injury 23.88 18.33 114 23569 367223 42230429
Rhabdomyolysis 23.62 18.33 7 23676 78012 42519640
Medulloblastoma 23.55 18.33 6 23677 73 42597579
Hippocampal sclerosis 23.48 18.33 7 23676 157 42597495
Skin warm 22.73 18.33 16 23667 2807 42594845
Gait disturbance 22.57 18.33 111 23572 97889 42499763
Drug resistance 22.43 18.33 55 23628 34193 42563459
Paraparesis 22.14 18.33 14 23669 2057 42595595
Influenza 21.94 18.33 4 23679 62171 42535481
Anaplastic astrocytoma 21.75 18.33 6 23677 101 42597551
Metastases to spinal cord 21.74 18.33 5 23678 38 42597614
Xanthoma 21.12 18.33 6 23677 113 42597539
Neurological decompensation 20.62 18.33 17 23666 3772 42593880
Chest discomfort 20.59 18.33 5 23678 63611 42534041
Pruritus 20.23 18.33 47 23636 188724 42408928
Alexia 20.20 18.33 4 23679 13 42597639
Central nervous system necrosis 20.08 18.33 7 23676 262 42597390
Asthma 19.97 18.33 5 23678 62309 42535343
Blood pressure diastolic increased 19.84 18.33 21 23662 6384 42591268
Therapy non-responder 19.82 18.33 70 23613 53289 42544363
Feeling abnormal 19.82 18.33 7 23676 69779 42527873
Aplastic anaemia 19.61 18.33 29 23654 12355 42585297
Myxoid liposarcoma 19.56 18.33 4 23679 16 42597636
Therapy change 19.47 18.33 17 23666 4078 42593574
Hospitalisation 19.16 18.33 87 23596 74243 42523409
Glioma 19.07 18.33 8 23675 498 42597154
Generalised tonic-clonic seizure 19.04 18.33 44 23639 26335 42571317
Ataxia 19.00 18.33 33 23650 16092 42581560
Condition aggravated 18.68 18.33 78 23605 260676 42336976
Paraganglion neoplasm malignant 18.67 18.33 4 23679 21 42597631
Hypotension 18.50 18.33 77 23606 257554 42340098
Chronic obstructive pulmonary disease 18.49 18.33 6 23677 63108 42534544

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Disease progression 2036.57 18.22 1210 39692 242824 110305573
Product use in unapproved indication 1085.94 18.22 1061 39841 446316 110102081
Thrombocytopenia 1055.78 18.22 936 39966 347949 110200448
Malignant neoplasm progression 866.80 18.22 627 40275 173940 110374457
Tumour pseudoprogression 613.82 18.22 138 40764 1478 110546919
Hypermutation 565.09 18.22 86 40816 34 110548363
Neoplasm progression 553.60 18.22 327 40575 64268 110484129
Death 497.81 18.22 909 39993 697960 109850437
Lymphopenia 474.11 18.22 251 40651 39919 110508478
Seizure 370.19 18.22 432 40470 220753 110327644
Disease recurrence 318.56 18.22 226 40676 60558 110487839
Pancytopenia 297.90 18.22 377 40525 209236 110339161
Off label use 287.27 18.22 1202 39700 1498983 109049414
Neutropenia 258.90 18.22 482 40420 374138 110174259
Myelosuppression 258.22 18.22 240 40662 94100 110454297
Therapy partial responder 254.54 18.22 163 40739 36898 110511499
Metastases to liver 253.91 18.22 160 40742 35226 110513171
Bone marrow failure 218.69 18.22 177 40725 57671 110490726
Haematotoxicity 210.54 18.22 118 40784 20964 110527433
Eastern Cooperative Oncology Group performance status worsened 197.33 18.22 64 40838 2905 110545492
Glioblastoma 185.99 18.22 56 40846 1984 110546413
Platelet count decreased 176.13 18.22 310 40592 230133 110318264
Nausea 167.98 18.22 898 40004 1234792 109313605
Recurrent cancer 161.31 18.22 57 40845 3366 110545031
Hospice care 158.67 18.22 82 40820 12391 110536006
Brain oedema 154.54 18.22 112 40790 30986 110517411
Vasogenic cerebral oedema 147.33 18.22 48 40854 2210 110546187
Febrile neutropenia 145.40 18.22 345 40557 316422 110231975
Product administered to patient of inappropriate age 117.34 18.22 58 40844 7978 110540419
Radiation necrosis 116.11 18.22 32 40870 822 110547575
Joint swelling 115.63 18.22 14 40888 442831 110105566
Hemiparesis 114.88 18.22 109 40793 43794 110504603
Metastases to peritoneum 114.40 18.22 51 40851 5559 110542838
Herpes simplex encephalitis 111.83 18.22 31 40871 814 110547583
Arthralgia 110.23 18.22 77 40825 779555 109768842
Aplastic anaemia 106.12 18.22 81 40821 24227 110524170
Hydrocephalus 106.11 18.22 59 40843 10316 110538081
Infusion related reaction 104.73 18.22 10 40892 381152 110167245
Malignant glioma 101.01 18.22 19 40883 74 110548323
Drug ineffective 100.84 18.22 928 39974 1519612 109028785
Metastases to central nervous system 99.53 18.22 76 40826 22741 110525656
Leukopenia 99.45 18.22 189 40713 148602 110399795
Glioblastoma multiforme 98.54 18.22 32 40870 1458 110546939
Metastases to lymph nodes 95.54 18.22 63 40839 14969 110533428
Vomiting 94.27 18.22 617 40285 910058 109638339
Vanishing bile duct syndrome 91.93 18.22 37 40865 3131 110545266
Constipation 91.81 18.22 316 40586 357470 110190927
Arthropathy 89.35 18.22 4 40898 287518 110260879
Metastasis 87.25 18.22 48 40854 8219 110540178
Pulmonary embolism 86.04 18.22 222 40680 214252 110334145
Neoplasm recurrence 83.10 18.22 40 40862 5192 110543205
Metastases to lung 79.67 18.22 67 40835 22996 110525401
Lymphocyte count decreased 78.06 18.22 101 40801 57142 110491255
Intracranial tumour haemorrhage 77.81 18.22 22 40880 622 110547775
Contraindicated product administered 75.38 18.22 4 40898 248263 110300134
Magnetic resonance imaging head abnormal 71.64 18.22 32 40870 3503 110544894
Therapeutic product effect decreased 70.98 18.22 5 40897 244311 110304086
Pneumocystis jirovecii pneumonia 70.51 18.22 83 40819 42652 110505745
Asthma 70.25 18.22 6 40896 250285 110298112
Wheezing 69.28 18.22 7 40895 255223 110293174
Wound 67.52 18.22 5 40897 234432 110313965
Brain neoplasm 67.45 18.22 37 40865 6300 110542097
Glossodynia 66.10 18.22 4 40898 222000 110326397
Musculoskeletal stiffness 65.74 18.22 12 40890 279810 110268587
Abdominal discomfort 65.33 18.22 32 40870 393826 110154571
Nasopharyngitis 63.97 18.22 33 40869 394328 110154069
Pain 63.05 18.22 165 40737 954790 109593607
Central nervous system necrosis 61.93 18.22 17 40885 430 110547967
Brain operation 61.82 18.22 20 40882 900 110547497
Metastases to bone 60.37 18.22 66 40836 31306 110517091
Diabetes insipidus 58.15 18.22 34 40868 6536 110541861
Dyspnoea 57.69 18.22 213 40689 1106659 109441738
Cholestatic liver injury 57.05 18.22 35 40867 7341 110541056
Eastern Cooperative Oncology Group performance status improved 55.89 18.22 9 40893 9 110548388
Sinusitis 55.78 18.22 20 40882 296668 110251729
Agranulocytosis 54.94 18.22 89 40813 61671 110486726
Diaphragmatic spasm 54.85 18.22 12 40890 112 110548285
Glioma 54.40 18.22 18 40884 870 110547527
Drug resistance 53.95 18.22 84 40818 56290 110492107
Maternal exposure during pregnancy 53.65 18.22 14 40888 254869 110293528
Aphasia 52.45 18.22 85 40817 58912 110489485
Platelet transfusion 52.10 18.22 24 40878 2822 110545575
Metastases to meninges 52.00 18.22 29 40873 5099 110543298
Therapy cessation 51.79 18.22 73 40829 44784 110503613
Brain neoplasm malignant 51.27 18.22 21 40881 1859 110546538
Inflammation 50.66 18.22 6 40896 193232 110355165
Hepatic lesion 50.13 18.22 34 40868 8459 110539938
Medulloblastoma recurrent 49.03 18.22 12 40890 190 110548207
Fatigue 48.23 18.22 672 40230 1215286 109333111
White blood cell count decreased 47.36 18.22 189 40713 229201 110319196
Petechiae 46.52 18.22 50 40852 23267 110525130
Swelling 46.49 18.22 37 40865 351004 110197393
Deep vein thrombosis 46.30 18.22 135 40767 139752 110408645
Brain tumour operation 45.84 18.22 10 40892 92 110548305
Blood cholesterol increased 45.44 18.22 7 40895 184778 110363619
Injury 45.26 18.22 6 40896 177259 110371138
Folliculitis 44.46 18.22 5 40897 167648 110380749
Acute myeloid leukaemia 43.96 18.22 62 40840 38048 110510349
Mental status changes 42.79 18.22 90 40812 76032 110472365
Arthritis 42.01 18.22 6 40896 167580 110380817
Neurological symptom 41.29 18.22 39 40863 15569 110532828
Astrocytoma 41.23 18.22 11 40891 249 110548148
Hepatic enzyme increased 41.03 18.22 35 40867 320857 110227540
Faecal volume decreased 40.18 18.22 12 40890 413 110547984
Malaise 39.89 18.22 122 40780 671697 109876700
Hypersensitivity 39.56 18.22 55 40847 403943 110144454
Gliosarcoma 38.99 18.22 6 40896 3 110548394
Peritumoural oedema 38.88 18.22 7 40895 20 110548377
Type 2 diabetes mellitus 38.72 18.22 9 40893 177223 110371174
Therapy change 38.62 18.22 31 40871 9966 110538431
Tumour haemorrhage 38.32 18.22 24 40878 5221 110543176
Mobility decreased 38.28 18.22 20 40882 237402 110310995
Angina bullosa haemorrhagica 38.24 18.22 10 40892 209 110548188
Pancreatic neuroendocrine tumour metastatic 37.80 18.22 10 40892 219 110548178
Acquired gene mutation 37.62 18.22 19 40883 2735 110545662
Oligodendroglioma 36.86 18.22 9 40893 141 110548256
Diffuse large B-cell lymphoma recurrent 36.66 18.22 25 40877 6274 110542123
Metastatic malignant melanoma 36.54 18.22 20 40882 3389 110545008
Drug hypersensitivity 35.93 18.22 71 40831 454019 110094378
Blister 35.42 18.22 20 40882 227356 110321041
Psoriasis 35.12 18.22 5 40897 139988 110408409
Migraine 35.04 18.22 10 40892 171642 110376755
Anxiety 34.77 18.22 46 40856 345032 110203365
Corneal toxicity 34.66 18.22 8 40894 97 110548300
C-reactive protein abnormal 34.06 18.22 4 40898 129691 110418706
Nephrogenic diabetes insipidus 33.78 18.22 17 40885 2428 110545969
Pain in extremity 33.74 18.22 82 40820 487036 110061361
Weight increased 33.73 18.22 65 40837 419579 110128818
Alanine aminotransferase increased 33.67 18.22 146 40756 183627 110364770
Condition aggravated 33.41 18.22 149 40753 734687 109813710
Radiation injury 33.30 18.22 13 40889 1015 110547382
Cerebral haemorrhage 33.30 18.22 74 40828 64894 110483503
Dehydration 32.87 18.22 196 40706 279315 110269082
Depression 32.28 18.22 42 40860 317293 110231104
Jaw operation 32.10 18.22 12 40890 832 110547565
Ganglioneuroma 31.72 18.22 8 40894 144 110548253
Product dose omission issue 31.30 18.22 44 40858 321738 110226659
Incoherent 30.36 18.22 25 40877 8333 110540064
Needle issue 30.01 18.22 35 40867 17805 110530592
Peripheral swelling 29.58 18.22 66 40836 403968 110144429
Neuroblastoma recurrent 29.34 18.22 10 40892 530 110547867
Discomfort 29.21 18.22 22 40880 214685 110333712
Crystal nephropathy 28.90 18.22 14 40888 1842 110546555
Sleep disorder 28.81 18.22 19 40883 198625 110349772
DNA mismatch repair protein gene mutation 28.70 18.22 5 40897 11 110548386
Gene mutation 28.40 18.22 17 40885 3412 110544985
Myocardial infarction 28.37 18.22 18 40884 192065 110356332
Optic neuropathy 28.34 18.22 19 40883 4639 110543758
Impaired healing 28.28 18.22 19 40883 196698 110351699
Tumour necrosis 28.09 18.22 15 40887 2421 110545976
Primary progressive aphasia 27.61 18.22 4 40898 0 110548397
Dizziness 27.44 18.22 149 40753 698044 109850353
Product dispensing error 27.38 18.22 32 40870 16313 110532084
Febrile bone marrow aplasia 27.29 18.22 33 40869 17432 110530965
Body temperature decreased 27.26 18.22 49 40853 36886 110511511
Facial asymmetry 27.01 18.22 11 40891 959 110547438
Cardiac failure congestive 27.00 18.22 11 40891 150989 110397408
Sepsis 26.82 18.22 210 40692 327136 110221261
Sialoadenitis 26.78 18.22 15 40887 2658 110545739
Anaplastic astrocytoma 26.78 18.22 7 40895 146 110548251
Road traffic accident 26.56 18.22 4 40898 107394 110441003
Muscle spasms 26.10 18.22 39 40863 278118 110270279
Parathyroid tumour malignant 26.05 18.22 7 40895 163 110548234
Drug reaction with eosinophilia and systemic symptoms 25.98 18.22 78 40824 82017 110466380
Myelodysplastic syndrome 25.49 18.22 48 40854 37436 110510961
Renal-limited thrombotic microangiopathy 25.34 18.22 9 40893 539 110547858
Blood pressure diastolic increased 25.34 18.22 33 40869 18774 110529623
Dry mouth 25.31 18.22 22 40880 199926 110348471
Bone marrow disorder 25.15 18.22 17 40885 4206 110544191
Lung disorder 25.07 18.22 18 40884 180029 110368368
Ataxia 24.90 18.22 42 40860 30066 110518331
Craniotomy 24.35 18.22 9 40893 605 110547792
Hippocampal sclerosis 24.30 18.22 7 40895 212 110548185
Vulval disorder 24.22 18.22 10 40892 903 110547494
Cholestasis 24.02 18.22 65 40837 64453 110483944
Drug intolerance 23.96 18.22 74 40828 406438 110141959
Sciatica 23.89 18.22 3 40899 92396 110456001
Penetrating aortic ulcer 23.77 18.22 5 40897 38 110548359
Asthenia 23.73 18.22 372 40530 688627 109859770
Neutrophil count decreased 23.63 18.22 98 40804 120843 110427554
Nasal congestion 23.54 18.22 4 40898 98278 110450119
Haemorrhage intracranial 23.42 18.22 40 40862 28929 110519468
Musculoskeletal pain 23.34 18.22 20 40882 183003 110365394
Cardiac failure 23.32 18.22 21 40881 187605 110360792
Hyperhidrosis 23.24 18.22 21 40881 187277 110361120
Suicide attempt 23.08 18.22 5 40897 103389 110445008
Myalgia 23.05 18.22 29 40873 222352 110326045
Electrocardiogram QT prolonged 22.89 18.22 6 40896 108954 110439443
Rhabdomyolysis 22.81 18.22 8 40894 120393 110428004
Muscle swelling 22.56 18.22 10 40892 1075 110547322
Gastrooesophageal reflux disease 22.54 18.22 20 40882 179956 110368441
Hyperkalaemia 22.54 18.22 11 40891 135785 110412612
Hyperglycaemia 22.50 18.22 76 40826 85014 110463383
Prescribed overdose 22.27 18.22 3 40899 87578 110460819
Influenza 22.15 18.22 18 40884 169083 110379314
Osteoporosis 22.12 18.22 3 40899 87149 110461248
Meningitis bacterial 22.02 18.22 14 40888 3125 110545272
Pruritus 21.81 18.22 126 40776 581434 109966963
Neurological decompensation 21.74 18.22 19 40883 6864 110541533
Exposure during pregnancy 21.71 18.22 18 40884 167406 110380991
Radiation interaction 21.34 18.22 5 40897 65 110548332
Cognitive disorder 21.26 18.22 76 40826 87435 110460962
Chronic obstructive pulmonary disease 21.12 18.22 7 40895 109151 110439246
Hepatocellular injury 20.87 18.22 53 40849 50589 110497808
Gastroenteropancreatic neuroendocrine tumour disease 20.68 18.22 5 40897 75 110548322
Neck pain 20.40 18.22 10 40892 123120 110425277
Ascites 20.37 18.22 78 40824 92730 110455667
Disorientation 20.37 18.22 65 40837 70606 110477791
Swelling of eyelid 20.28 18.22 18 40884 6635 110541762
Bronchitis 20.21 18.22 17 40885 157015 110391382
Suicidal ideation 20.06 18.22 5 40897 93932 110454465
Diffuse large B-cell lymphoma 20.04 18.22 27 40875 15871 110532526
Intracranial pressure increased 19.98 18.22 22 40880 10513 110537884
Atrial fibrillation 19.84 18.22 34 40868 229608 110318789
Encephalomalacia 19.46 18.22 10 40892 1492 110546905
Alexia 19.43 18.22 4 40898 27 110548370
Monocyte count decreased 19.42 18.22 14 40888 3837 110544560
Xanthoma 19.27 18.22 6 40896 238 110548159
Anaemia 19.05 18.22 296 40606 546790 110001607
Hepatic cytolysis 19.04 18.22 54 40848 54999 110493398
Metastases to spinal cord 19.01 18.22 6 40896 249 110548148
Acute myocardial infarction 18.81 18.22 4 40898 83773 110464624
COVID-19 18.78 18.22 39 40863 245021 110303376
Myxoid liposarcoma 18.73 18.22 4 40898 33 110548364
Cerebrospinal fluid leakage 18.70 18.22 11 40891 2137 110546260
Breast necrosis 18.27 18.22 5 40897 125 110548272

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01AX03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
ALKYLATING AGENTS
Other alkylating agents
FDA MoA N0000000236 Alkylating Activity
FDA EPC N0000175558 Alkylating Drug
MeSH PA D000477 Alkylating Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D018906 Antineoplastic Agents, Alkylating
CHEBI has role CHEBI:22333 alkylating agent
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:50266 prodrug

Related Drugs by ATC class:

L01AX Other alkylating agents 3 drugs
dacarbazinemitobronitolpipobroman

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Astrocytoma, anaplastic indication 55353007 DOID:3078
Glioma, malignant indication 74532006
Ewing's sarcoma indication 76909002 DOID:3369
Glioblastoma multiforme of brain indication 276828006 DOID:3073
Metastatic malignant melanoma off-label use 443493003
Pancreatic Neuroendocrine Tumor off-label use 717919005
Lymphocytopenia contraindication 48813009 DOID:614
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Myelodysplastic syndrome contraindication 109995007
Pancytopenia contraindication 127034005 DOID:12450
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Aplastic anemia contraindication 306058006 DOID:12449
Bone marrow depression contraindication 307762000
Breastfeeding (mother) contraindication 413712001
Pneumocystosis jiroveci pneumonia contraindication 415125002 DOID:11339




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.94 acidic
pKa2 1.16 Basic
pKa3 0.53 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
4021173 VUID
N0000148622 NUI
D06067 KEGG_DRUG
4021173 VANDF
C0076080 UMLSCUI
CHEBI:72564 CHEBI
CHEMBL810 ChEMBL_ID
DB00853 DRUGBANK_ID
D000077204 MESH_DESCRIPTOR_UI
5394 PUBCHEM_CID
7301 IUPHAR_LIGAND_ID
6027 INN_ID
YF1K15M17Y UNII
37776 RXNORM
172754 MMSL
8290 MMSL
d04451 MMSL
007794 NDDF
116099008 SNOMEDCT_US
387009002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1366 CAPSULE 100 mg ORAL NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1366 CAPSULE 100 mg ORAL NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1381 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2.50 mg INTRAVENOUS NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1381 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2.50 mg INTRAVENOUS NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1417 CAPSULE 250 mg ORAL NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1417 CAPSULE 250 mg ORAL NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1425 CAPSULE 140 mg ORAL NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1425 CAPSULE 140 mg ORAL NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1430 CAPSULE 180 mg ORAL NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1430 CAPSULE 180 mg ORAL NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1519 CAPSULE 20 mg ORAL NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-1519 CAPSULE 20 mg ORAL NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-3004 CAPSULE 5 mg ORAL NDA 34 sections
TEMODAR HUMAN PRESCRIPTION DRUG LABEL 1 0085-3004 CAPSULE 5 mg ORAL NDA 34 sections
Temozolomide HUMAN PRESCRIPTION DRUG LABEL 1 0527-1777 CAPSULE 5 mg ORAL ANDA 28 sections
Temozolomide HUMAN PRESCRIPTION DRUG LABEL 1 0527-1778 CAPSULE 20 mg ORAL ANDA 28 sections
Temozolomide HUMAN PRESCRIPTION DRUG LABEL 1 0527-1779 CAPSULE 100 mg ORAL ANDA 28 sections
Temozolomide HUMAN PRESCRIPTION DRUG LABEL 1 0527-1780 CAPSULE 140 mg ORAL ANDA 28 sections
Temozolomide HUMAN PRESCRIPTION DRUG LABEL 1 0527-1781 CAPSULE 180 mg ORAL ANDA 28 sections
Temozolomide HUMAN PRESCRIPTION DRUG LABEL 1 0527-1782 CAPSULE 250 mg ORAL ANDA 28 sections
TEMOZOLOMIDE Human Prescription Drug Label 1 16571-816 CAPSULE 5 mg ORAL ANDA 27 sections
TEMOZOLOMIDE Human Prescription Drug Label 1 16571-817 CAPSULE 20 mg ORAL ANDA 27 sections
TEMOZOLOMIDE Human Prescription Drug Label 1 16571-818 CAPSULE 100 mg ORAL ANDA 27 sections
TEMOZOLOMIDE Human Prescription Drug Label 1 16571-819 CAPSULE 140 mg ORAL ANDA 27 sections
TEMOZOLOMIDE Human Prescription Drug Label 1 16571-820 CAPSULE 180 mg ORAL ANDA 27 sections
TEMOZOLOMIDE Human Prescription Drug Label 1 16571-821 CAPSULE 250 mg ORAL ANDA 27 sections
Temozolomide HUMAN PRESCRIPTION DRUG LABEL 1 16729-048 CAPSULE 5 mg ORAL ANDA 30 sections
Temozolomide HUMAN PRESCRIPTION DRUG LABEL 1 16729-049 CAPSULE 20 mg ORAL ANDA 30 sections
Temozolomide HUMAN PRESCRIPTION DRUG LABEL 1 16729-050 CAPSULE 100 mg ORAL ANDA 30 sections
Temozolomide HUMAN PRESCRIPTION DRUG LABEL 1 16729-051 CAPSULE 250 mg ORAL ANDA 30 sections