everolimus Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
immunosuppressants, rapamycin derivatives 1118 159351-69-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • votubia
  • everolimus
  • afinitor
  • certican
  • RAD001
A derivative of sirolimus and an inhibitor of TOR SERINE-THREONINE KINASES. It is used to prevent GRAFT REJECTION in heart and kidney transplant patients by blocking cell proliferation signals. It is also an ANTINEOPLASTIC AGENT.
  • Molecular weight: 958.24
  • Formula: C53H83NO14
  • CLOGP: 7.10
  • LIPINSKI: 3
  • HAC: 15
  • HDO: 3
  • TPSA: 204.66
  • ALOGS: -5.77
  • ROTB: 9

Drug dosage:

DoseUnitRoute
1.50 mg O

Approvals:

DateAgencyCompanyOrphan
Sept. 2, 2011 EMA
March 30, 2009 FDA NOVARTIS

FDA Adverse Event Reporting System

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
Malignant neoplasm progression 4807.51 32.48 1272 13127 16521 3354939
Stomatitis 4405.29 32.48 1094 13305 10758 3360702
Dyspnoea 2293.02 32.48 1162 13237 101772 3269688
Pneumonitis 2226.99 32.48 559 13840 5644 3365816
Pyrexia 2223.40 32.48 1056 13343 80059 3291401
Diarrhoea 1903.21 32.48 1032 13367 103316 3268144
Cough 1833.71 32.48 749 13650 39109 3332351
Fatigue 1713.93 32.48 973 13426 106267 3265193
Death 1681.79 32.48 1089 13310 151235 3220225
Anaemia 1501.67 32.48 714 13685 53619 3317841
General physical health deterioration 1359.21 32.48 504 13895 20085 3351375
Interstitial lung disease 1308.44 32.48 444 13955 13572 3357888
Blood creatinine increased 1272.92 32.48 488 13911 21330 3350130
Pleural effusion 1214.42 32.48 453 13946 18326 3353134
Decreased appetite 1106.34 32.48 533 13866 40957 3330503
Neoplasm malignant 1086.94 32.48 341 14058 8056 3363404
Pneumonia 1072.84 32.48 621 13778 69522 3301938
Oedema peripheral 1018.29 32.48 475 13924 33886 3337574
Neoplasm progression 1003.27 32.48 288 14111 4956 3366504
Metastases to liver 991.10 32.48 269 14130 3727 3367733
C-reactive protein increased 956.83 32.48 318 14081 9065 3362395
Asthenia 923.26 32.48 551 13848 65114 3306346
Rash 907.73 32.48 560 13839 70261 3301199
Lung disorder 868.50 32.48 292 14107 8625 3362835
Hyperglycaemia 864.65 32.48 289 14110 8379 3363081
Nausea 860.71 32.48 684 13715 128961 3242499
Mucosal inflammation 843.51 32.48 278 14121 7705 3363755
Weight decreased 788.96 32.48 420 13979 39691 3331769
Vomiting 778.60 32.48 556 13843 88975 3282485
Haemoglobin decreased 778.27 32.48 380 14019 29914 3341546
Malaise 777.99 32.48 493 13906 64684 3306776
Abdominal pain 727.76 32.48 418 13981 45807 3325653
Metastases to bone 725.84 32.48 199 14200 2862 3368598
Metastases to lung 701.09 32.48 185 14214 2279 3369181
Thrombocytopenia 652.97 32.48 355 14044 34913 3336547
Acute kidney injury 630.09 32.48 391 14008 49292 3322168
Disease progression 614.54 32.48 331 14068 31928 3339532
Ascites 607.61 32.48 227 14172 9150 3362310
Dehydration 606.97 32.48 333 14066 33316 3338144
Gamma-glutamyltransferase increased 602.53 32.48 224 14175 8904 3362556
Kidney transplant rejection 552.83 32.48 141 14258 1502 3369958
Mouth ulceration 550.91 32.48 175 14224 4285 3367175
Renal impairment 550.43 32.48 256 14143 18005 3353455
Platelet count decreased 498.20 32.48 273 14126 27195 3344265
Breast cancer metastatic 489.80 32.48 131 14268 1702 3369758
Epistaxis 480.57 32.48 217 14182 14234 3357226
Renal failure 472.84 32.48 281 14118 32659 3338801
Oral pain 471.88 32.48 150 14249 3678 3367782
Proteinuria 429.70 32.48 147 14252 4559 3366901
Aphthous ulcer 427.46 32.48 114 14285 1463 3369997
Urinary tract infection 417.82 32.48 255 14144 31073 3340387
Lung infiltration 415.52 32.48 138 14261 3900 3367560
Blood glucose increased 413.69 32.48 214 14185 18941 3352519
Cardiac failure 386.99 32.48 208 14191 19897 3351563
Pain 375.22 32.48 331 14068 71226 3300234
Diabetes mellitus 371.19 32.48 172 14227 11961 3359499
Respiratory failure 362.31 32.48 209 14190 22932 3348528
Pericardial effusion 360.74 32.48 138 14261 5923 3365537
Blood alkaline phosphatase increased 358.71 32.48 161 14238 10392 3361068
Concomitant disease progression 353.47 32.48 87 14312 790 3370670
Blood lactate dehydrogenase increased 351.78 32.48 138 14261 6342 3365118
Oedema 337.08 32.48 171 14228 14509 3356951
Transplant rejection 324.49 32.48 98 14301 2013 3369447
Infection 321.24 32.48 200 14199 25202 3346258
Sepsis 319.12 32.48 218 14181 32155 3339305
Pulmonary embolism 311.46 32.48 203 14196 27685 3343775
Metastatic renal cell carcinoma 306.50 32.48 77 14322 766 3370694
Hypertension 294.19 32.48 222 14177 38244 3333216
Febrile neutropenia 290.57 32.48 169 14230 18806 3352654
Neutropenia 289.81 32.48 208 14191 33178 3338282
Aspartate aminotransferase increased 289.25 32.48 175 14224 20938 3350522
Blood cholesterol increased 268.09 32.48 117 14282 7052 3364408
Headache 266.93 32.48 309 14090 91671 3279789
Lymphocyte count decreased 266.59 32.48 100 14299 4059 3367401
Complications of transplanted kidney 260.57 32.48 67 14332 737 3370723
Breast cancer 260.43 32.48 119 14280 7998 3363462
Pruritus 259.79 32.48 224 14175 46609 3324851
Dysgeusia 259.03 32.48 132 14267 11292 3360168
Lymphocele 246.88 32.48 54 14345 272 3371188
Abdominal pain upper 245.88 32.48 168 14231 24748 3346712
Leukopenia 245.03 32.48 142 14257 15681 3355779
Cytomegalovirus infection 244.60 32.48 96 14303 4411 3367049
Second primary malignancy 242.83 32.48 73 14326 1474 3369986
Blood urea increased 239.91 32.48 110 14289 7450 3364010
Acne 238.94 32.48 91 14308 3852 3367608
Pneumocystis jirovecii pneumonia 238.81 32.48 90 14309 3700 3367760
Alanine aminotransferase increased 234.68 32.48 160 14239 23480 3347980
Dyspnoea exertional 233.70 32.48 105 14294 6781 3364679
Blood triglycerides increased 233.23 32.48 93 14306 4457 3367003
Immunosuppressant drug level increased 232.63 32.48 62 14337 792 3370668
Hypertriglyceridaemia 231.66 32.48 72 14327 1632 3369828
Hypokalaemia 230.11 32.48 130 14269 13675 3357785
Peripheral swelling 229.37 32.48 137 14262 15995 3355465
Drug ineffective 227.67 32.48 321 14078 115769 3255691
Metastases to central nervous system 226.03 32.48 81 14318 2882 3368578
Hypoxia 225.58 32.48 114 14285 9577 3361883
Productive cough 222.12 32.48 99 14300 6272 3365188
Hypercholesterolaemia 221.87 32.48 77 14322 2489 3368971
Heart transplant rejection 220.07 32.48 48 14351 238 3371222
Back pain 219.25 32.48 186 14213 37819 3333641
Nephropathy toxic 207.92 32.48 77 14322 3012 3368448
Pulmonary oedema 206.19 32.48 115 14284 11796 3359664
Pain in extremity 205.75 32.48 201 14198 49011 3322449
Osteonecrosis of jaw 205.66 32.48 110 14289 10386 3361074
Liver transplant rejection 203.68 32.48 54 14345 675 3370785
Dysphagia 199.74 32.48 135 14264 19516 3351944
White blood cell count decreased 199.46 32.48 148 14251 24799 3346661
Septic shock 198.35 32.48 113 14286 12071 3359389
Abdominal distension 197.41 32.48 117 14282 13459 3358001
Lymphoedema 197.32 32.48 59 14340 1168 3370292
Multiple organ dysfunction syndrome 193.52 32.48 118 14281 14292 3357168
Constipation 192.57 32.48 158 14241 30654 3340806
Arthralgia 188.93 32.48 212 14187 60649 3310811
Blood pressure increased 184.72 32.48 135 14264 22095 3349365
Chronic kidney disease 181.07 32.48 86 14313 6306 3365154
Chest pain 180.55 32.48 171 14228 40104 3331356
Seizure 180.09 32.48 171 14228 40229 3331231
Pancytopenia 178.73 32.48 124 14275 18696 3352764
Metastases to lymph nodes 178.12 32.48 56 14343 1319 3370141
Urine output decreased 173.44 32.48 64 14335 2477 3368983
Gastrointestinal haemorrhage 171.46 32.48 134 14265 24240 3347220
Hypophagia 170.01 32.48 81 14318 5980 3365480
Metastasis 169.88 32.48 56 14343 1541 3369919
Glomerular filtration rate decreased 169.77 32.48 62 14337 2329 3369131
Deep vein thrombosis 168.94 32.48 126 14273 21263 3350197
Chills 167.88 32.48 127 14272 21895 3349565
Renal cell carcinoma 165.46 32.48 59 14340 2067 3369393
Metastases to peritoneum 162.13 32.48 43 14356 538 3370922
Drug intolerance 159.38 32.48 97 14302 11701 3359759
Haematocrit decreased 158.67 32.48 83 14316 7484 3363976
Lung infection 158.16 32.48 75 14324 5478 3365982
Product use issue 157.98 32.48 108 14291 15893 3355567
Renal tubular necrosis 157.42 32.48 63 14336 3045 3368415
Swelling 156.70 32.48 115 14284 18929 3352531
Inflammation 156.66 32.48 82 14317 7403 3364057
Hepatic lesion 156.30 32.48 46 14353 860 3370600
Therapy cessation 155.93 32.48 66 14333 3683 3367777
Confusional state 154.59 32.48 153 14246 37845 3333615
Erythema 153.85 32.48 135 14264 28675 3342785
Concomitant disease aggravated 153.06 32.48 47 14352 1021 3370439
Bone pain 152.08 32.48 88 14311 9673 3361787
Feeding disorder 151.64 32.48 51 14348 1495 3369965
Hepatic function abnormal 148.31 32.48 91 14308 11136 3360324
Tumour marker increased 147.34 32.48 39 14360 484 3370976
Hypotension 145.94 32.48 168 14231 49346 3322114
Pancreatic neuroendocrine tumour 145.73 32.48 29 14370 82 3371378
Dry skin 144.69 32.48 79 14320 7764 3363696
Hyponatraemia 144.62 32.48 108 14291 18251 3353209
Dizziness 144.30 32.48 208 14191 76304 3295156
Eating disorder 143.07 32.48 57 14342 2722 3368738
Hepatic failure 142.39 32.48 87 14312 10565 3360895
Atelectasis 141.51 32.48 60 14339 3362 3368098
Lymphadenopathy 141.10 32.48 78 14321 7854 3363606
Ejection fraction decreased 139.91 32.48 63 14336 4084 3367376
Cholestasis 136.61 32.48 67 14332 5270 3366190
Palmar-plantar erythrodysaesthesia syndrome 135.10 32.48 71 14328 6461 3364999
Cholangitis 134.14 32.48 47 14352 1562 3369898
Bone marrow failure 133.50 32.48 77 14322 8410 3363050
Immunosuppressant drug level decreased 133.49 32.48 33 14366 305 3371155
Angioedema 132.70 32.48 95 14304 15040 3356420
Skin ulcer 132.43 32.48 66 14333 5374 3366086
Hepatic enzyme increased 129.84 32.48 90 14309 13535 3357925
Generalised oedema 129.53 32.48 57 14342 3498 3367962
Blood pressure systolic increased 128.67 32.48 55 14344 3144 3368316
Lymphangiosis carcinomatosa 127.18 32.48 32 14367 320 3371140
Oropharyngeal pain 126.51 32.48 85 14314 12149 3359311
Neoplasm 125.56 32.48 46 14353 1743 3369717
Thrombotic microangiopathy 123.52 32.48 48 14351 2144 3369316
Urosepsis 122.91 32.48 51 14348 2706 3368754
Pulmonary toxicity 121.73 32.48 42 14357 1332 3370128
Chest discomfort 121.43 32.48 95 14304 17190 3354270
Hyperlipidaemia 121.14 32.48 59 14340 4569 3366891
Melaena 119.44 32.48 68 14331 7244 3364216
Lethargy 118.35 32.48 86 14313 13929 3357531
Hypophosphataemia 116.42 32.48 46 14353 2148 3369312
Liver function test abnormal 115.44 32.48 82 14317 12819 3358641
Blood albumin decreased 115.18 32.48 50 14349 2968 3368492
Intestinal obstruction 114.10 32.48 63 14336 6326 3365134
Rales 112.85 32.48 42 14357 1664 3369796
Impaired healing 111.84 32.48 64 14335 6884 3364576
Lung consolidation 111.74 32.48 36 14363 919 3370541
Jaundice 111.21 32.48 73 14326 10034 3361426
Nephrotic syndrome 110.35 32.48 44 14355 2105 3369355
Metastases to pleura 109.99 32.48 26 14373 195 3371265
Drug level decreased 109.92 32.48 40 14359 1486 3369974
Pyelonephritis 109.54 32.48 45 14354 2327 3369133
Haemoptysis 108.34 32.48 62 14337 6669 3364791
Respiratory distress 108.24 32.48 67 14332 8321 3363139
Crepitations 107.74 32.48 35 14364 918 3370542
Ileus 107.25 32.48 52 14347 3987 3367473
Post transplant lymphoproliferative disorder 106.68 32.48 33 14366 735 3370725
Metastases to spine 105.44 32.48 31 14368 577 3370883
Atrial fibrillation 104.01 32.48 100 14299 23841 3347619
Hypocalcaemia 102.85 32.48 57 14342 5764 3365696
Dysuria 102.34 32.48 58 14341 6124 3365336
Wheezing 102.23 32.48 64 14335 8107 3363353
Fall 102.12 32.48 154 14245 58729 3312731
Hyperkalaemia 101.53 32.48 72 14327 11222 3360238
Red blood cell count decreased 100.90 32.48 58 14341 6290 3365170
Bronchitis 100.84 32.48 80 14319 14765 3356695
Cholelithiasis 100.17 32.48 63 14336 8045 3363415
Renal disorder 100.17 32.48 60 14339 7024 3364436
Pneumothorax 99.58 32.48 50 14349 4134 3367326
Hypercalcaemia 98.88 32.48 48 14351 3689 3367771
Epstein-Barr virus infection 98.57 32.48 38 14361 1660 3369800
Cholecystitis 98.07 32.48 46 14353 3275 3368185
Pulmonary mass 97.33 32.48 41 14358 2259 3369201
Wound dehiscence 95.35 32.48 34 14365 1190 3370270
Musculoskeletal pain 95.16 32.48 72 14327 12394 3359066
Pneumonia bacterial 94.12 32.48 37 14362 1704 3369756
Renal transplant failure 94.08 32.48 23 14376 202 3371258
Neutrophil count decreased 93.52 32.48 66 14333 10207 3361253
Cell marker increased 92.80 32.48 23 14376 215 3371245
Cellulitis 92.40 32.48 71 14328 12504 3358956
Respiratory disorder 90.62 32.48 53 14346 5937 3365523
Cachexia 90.17 32.48 34 14365 1397 3370063
Malignant pleural effusion 90.06 32.48 27 14372 539 3370921
Lymphopenia 89.99 32.48 45 14354 3688 3367772
Herpes zoster 88.02 32.48 66 14333 11206 3360254
Blood potassium decreased 87.90 32.48 53 14346 6277 3365183
Orthopnoea 87.04 32.48 30 14369 948 3370512
Gastroenteritis 86.79 32.48 46 14353 4255 3367205
Small intestinal obstruction 86.07 32.48 42 14357 3265 3368195
Colitis 84.64 32.48 54 14345 7067 3364393
Drug level increased 84.41 32.48 46 14353 4499 3366961
Nasopharyngitis 82.96 32.48 85 14314 21862 3349598
Incisional hernia 82.13 32.48 23 14376 357 3371103
Skin lesion 81.99 32.48 48 14351 5385 3366075
Kidney fibrosis 81.62 32.48 25 14374 538 3370922
Escherichia infection 81.27 32.48 33 14366 1655 3369805
Hydronephrosis 81.14 32.48 36 14363 2251 3369209
Ageusia 80.50 32.48 38 14361 2744 3368716
Electrolyte imbalance 80.08 32.48 38 14361 2776 3368684
Blood creatine phosphokinase increased 79.64 32.48 66 14333 12947 3358513
Acute respiratory distress syndrome 78.38 32.48 48 14351 5846 3365614
Pulmonary fibrosis 77.84 32.48 43 14356 4319 3367141
Haematuria 77.10 32.48 58 14341 9894 3361566
Swollen tongue 76.66 32.48 50 14349 6793 3364667
Abdominal discomfort 76.61 32.48 76 14323 18808 3352652
Bone lesion 76.24 32.48 27 14372 926 3370534
Skin disorder 74.90 32.48 43 14356 4650 3366810
Blood bilirubin increased 74.29 32.48 58 14341 10451 3361009
Muscular weakness 73.67 32.48 77 14322 20264 3351196
Acute respiratory failure 73.35 32.48 42 14357 4520 3366940
Flatulence 72.84 32.48 46 14353 5913 3365547
Hypoalbuminaemia 72.35 32.48 34 14365 2430 3369030
Tumour necrosis 72.05 32.48 20 14379 300 3371160
Pulmonary hypertension 71.55 32.48 47 14352 6463 3364997
Oral herpes 70.88 32.48 32 14367 2085 3369375
Mitral valve incompetence 70.80 32.48 39 14360 3895 3367565
Lymphadenopathy mediastinal 70.69 32.48 22 14377 500 3370960
Blister 70.11 32.48 52 14347 8682 3362778
Performance status decreased 69.57 32.48 27 14372 1201 3370259
Gastritis 68.69 32.48 46 14353 6531 3364929
Lip swelling 68.51 32.48 45 14354 6186 3365274
Alveolitis 68.44 32.48 23 14376 672 3370788
Liver abscess 68.21 32.48 24 14375 807 3370653
Bile duct stenosis 68.03 32.48 20 14379 372 3371088
Faeces discoloured 67.72 32.48 38 14361 3934 3367526
Oxygen saturation decreased 67.69 32.48 54 14345 10037 3361423
Upper respiratory tract infection 67.63 32.48 53 14346 9602 3361858
Weight increased 67.58 32.48 84 14315 26656 3344804
Polyneuropathy 67.27 32.48 32 14367 2350 3369110
Glycosylated haemoglobin increased 66.73 32.48 34 14365 2898 3368562
Insomnia 66.62 32.48 97 14302 35801 3335659
Tachycardia 66.55 32.48 78 14321 23293 3348167
Candida infection 66.43 32.48 37 14362 3775 3367685
Hypoglycaemia 66.33 32.48 62 14337 14256 3357204
Joint swelling 66.16 32.48 67 14332 16990 3354470
Gait disturbance 66.09 32.48 85 14314 27907 3343553
Neuroendocrine tumour 66.09 32.48 17 14382 187 3371273
Body temperature decreased 65.18 32.48 29 14370 1825 3369635
Pseudocirrhosis 65.11 32.48 14 14385 64 3371396
Blood uric acid increased 64.93 32.48 27 14372 1439 3370021
Tricuspid valve incompetence 64.79 32.48 32 14367 2553 3368907
White blood cell count increased 64.46 32.48 58 14341 12702 3358758
Atypical pneumonia 64.28 32.48 23 14376 813 3370647
Escherichia urinary tract infection 64.27 32.48 26 14373 1291 3370169
Bacterial infection 63.99 32.48 35 14364 3447 3368013
Renal cancer 63.65 32.48 27 14372 1513 3369947
Body temperature increased 63.10 32.48 39 14360 4827 3366633
Onychoclasis 62.78 32.48 22 14377 731 3370729
Biliary dilatation 62.73 32.48 20 14379 493 3370967
Pulmonary congestion 62.61 32.48 33 14366 3017 3368443
Dry mouth 62.57 32.48 51 14348 9771 3361689
Cardiomegaly 61.98 32.48 37 14362 4301 3367159
Skin toxicity 61.84 32.48 25 14374 1239 3370221
Hepatocellular injury 61.54 32.48 37 14362 4358 3367102
Left ventricular dysfunction 61.41 32.48 28 14371 1867 3369593
Anuria 61.40 32.48 32 14367 2859 3368601
Therapy change 61.36 32.48 23 14376 929 3370531
Toxicity to various agents 61.04 32.48 108 14291 46946 3324514
Liver disorder 60.79 32.48 51 14348 10172 3361288
Focal segmental glomerulosclerosis 60.67 32.48 19 14380 441 3371019
Dyslipidaemia 60.11 32.48 25 14374 1333 3370127
Hepatic neoplasm 59.69 32.48 21 14378 706 3370754
Blood creatine increased 59.04 32.48 24 14375 1207 3370253
Viral infection 58.22 32.48 40 14359 5922 3365538
Tongue ulceration 58.20 32.48 20 14379 626 3370834
Oliguria 58.03 32.48 28 14371 2122 3369338
Sinus tachycardia 57.94 32.48 37 14362 4848 3366612
Glossodynia 57.86 32.48 28 14371 2136 3369324
Fluid retention 57.60 32.48 45 14354 8113 3363347
Flushing 57.60 32.48 57 14342 14056 3357404
Epilepsy 57.20 32.48 42 14357 6903 3364557
Dysphonia 56.50 32.48 43 14356 7461 3363999
Respiratory tract infection 56.40 32.48 36 14363 4712 3366748
Flank pain 56.37 32.48 27 14372 2013 3369447
Abdominal hernia 56.36 32.48 21 14378 834 3370626
Hepatotoxicity 56.12 32.48 38 14361 5493 3365967
Skin exfoliation 56.03 32.48 44 14355 7993 3363467
Febrile infection 55.99 32.48 16 14383 268 3371192
Dyspepsia 55.98 32.48 52 14347 11860 3359600
Arrhythmia 55.98 32.48 49 14350 10348 3361112
Eastern Cooperative Oncology Group performance status worsened 55.65 32.48 13 14386 92 3371368
Abscess 55.58 32.48 32 14367 3478 3367982
Chronic allograft nephropathy 55.44 32.48 16 14383 278 3371182
Subileus 55.34 32.48 21 14378 878 3370582
Cardiomyopathy 55.19 32.48 36 14363 4890 3366570
Organising pneumonia 55.17 32.48 24 14375 1431 3370029
Karnofsky scale worsened 54.90 32.48 10 14389 14 3371446
General physical condition abnormal 54.26 32.48 22 14377 1099 3370361
Erysipelas 54.25 32.48 23 14376 1287 3370173
Cerebral haemorrhage 54.18 32.48 47 14352 9807 3361653
Bronchopulmonary aspergillosis 53.85 32.48 26 14373 1973 3369487
BK virus infection 53.65 32.48 18 14381 523 3370937
Blood calcium decreased 53.63 32.48 29 14370 2791 3368669
Haematochezia 53.53 32.48 41 14358 7180 3364280
Malnutrition 53.48 32.48 29 14370 2807 3368653
Alopecia 53.43 32.48 63 14336 18923 3352537
Post procedural urine leak 53.39 32.48 11 14388 39 3371421
Neuropathy peripheral 52.74 32.48 59 14340 16748 3354712
Computerised tomogram thorax abnormal 52.35 32.48 14 14385 181 3371279
Renal lymphocele 52.35 32.48 10 14389 21 3371439
Osteonecrosis 52.03 32.48 48 14351 10851 3360609
Oncologic complication 51.84 32.48 13 14386 128 3371332
Ovarian cyst 51.64 32.48 25 14374 1909 3369551
Palpitations 51.53 32.48 62 14337 19021 3352439
Carcinoid crisis 51.43 32.48 10 14389 24 3371436
Gastric haemorrhage 51.39 32.48 30 14369 3346 3368114
Gastrointestinal disorder 51.34 32.48 47 14352 10522 3360938
Protein total decreased 51.24 32.48 22 14377 1270 3370190
Carbohydrate antigen 15-3 increased 51.24 32.48 12 14387 86 3371374
Transaminases increased 51.14 32.48 39 14360 6785 3364675
Face oedema 51.13 32.48 35 14364 5149 3366311
Tongue oedema 50.79 32.48 21 14378 1103 3370357
Feeling abnormal 50.50 32.48 74 14325 27451 3344009
Enteritis 50.23 32.48 23 14376 1548 3369912
Cheilitis 49.96 32.48 21 14378 1150 3370310
Tachypnoea 49.95 32.48 30 14369 3526 3367934
Graft loss 49.58 32.48 15 14384 309 3371151
Pallor 49.56 32.48 36 14363 5819 3365641
Blood pressure decreased 49.41 32.48 52 14347 13784 3357676
Hypothyroidism 49.37 32.48 36 14363 5853 3365607
Oesophagitis 49.29 32.48 29 14370 3282 3368178
Rash pruritic 48.95 32.48 43 14356 9121 3362339
Cardiac failure congestive 48.79 32.48 76 14323 29746 3341714
Nail disorder 48.77 32.48 21 14378 1221 3370239
Myalgia 48.70 32.48 79 14320 31996 3339464
Product use in unapproved indication 48.65 32.48 30 14369 3696 3367764
Thrombosis 48.62 32.48 52 14347 14038 3357422
Swelling face 48.25 32.48 47 14352 11369 3360091
Urinary fistula 47.99 32.48 10 14389 38 3371422
Haemolytic uraemic syndrome 47.99 32.48 20 14379 1072 3370388
Renal tubular atrophy 47.84 32.48 14 14385 256 3371204
Influenza 47.80 32.48 49 14350 12597 3358863
Metastases to kidney 47.42 32.48 12 14387 123 3371337
Pollakiuria 47.36 32.48 34 14365 5396 3366064
Blood chromogranin A increased 47.19 32.48 11 14388 77 3371383
Neutrophil count increased 46.97 32.48 30 14369 3930 3367530
Abdominal pain lower 46.58 32.48 31 14368 4355 3367105
Musculoskeletal chest pain 46.28 32.48 27 14372 3008 3368452
Azotaemia 46.18 32.48 20 14379 1179 3370281
Metastases to adrenals 46.16 32.48 13 14386 206 3371254
Nephropathy 45.93 32.48 21 14378 1409 3370051
Complications of transplanted heart 45.76 32.48 10 14389 50 3371410
Mean cell haemoglobin decreased 45.71 32.48 14 14385 301 3371159
Haematoma 45.62 32.48 38 14361 7501 3363959
Pneumonia aspiration 45.56 32.48 37 14362 7051 3364409
Polyomavirus-associated nephropathy 45.54 32.48 15 14384 411 3371049
Polyuria 45.16 32.48 23 14376 1958 3369502
Haemorrhage 44.68 32.48 59 14340 19862 3351598
Tumour haemorrhage 44.63 32.48 17 14382 718 3370742
Gastroenteritis viral 44.32 32.48 25 14374 2613 3368847
Complications of transplanted liver 44.26 32.48 12 14387 164 3371296
Gastric ulcer 44.13 32.48 31 14368 4754 3366706
Circulatory collapse 44.08 32.48 34 14365 6015 3365445
Blood sodium decreased 44.06 32.48 31 14368 4765 3366695
Acute pulmonary oedema 44.04 32.48 23 14376 2063 3369397
Blood potassium increased 44.00 32.48 29 14370 4007 3367453
Odynophagia 43.88 32.48 20 14379 1332 3370128
Nodule 43.53 32.48 24 14375 2400 3369060
Hepatic steatosis 43.35 32.48 31 14368 4889 3366571
Eyelid oedema 43.26 32.48 27 14372 3398 3368062
Hepatitis C 42.99 32.48 28 14371 3793 3367667
Syncope 42.87 32.48 66 14333 25567 3345893
Sinusitis 42.87 32.48 53 14346 16715 3354745
Metastases to pelvis 42.78 32.48 10 14389 71 3371389
Oral discomfort 42.63 32.48 20 14379 1423 3370037
Toothache 42.58 32.48 25 14374 2818 3368642
Portal hypertension 42.29 32.48 18 14381 1017 3370443
Abnormal behaviour 41.84 32.48 41 14358 9987 3361473
Oral candidiasis 41.84 32.48 24 14375 2590 3368870
Thoracic cavity drainage 41.73 32.48 10 14389 80 3371380
Upper gastrointestinal haemorrhage 41.55 32.48 28 14371 4015 3367445
Mental status changes 41.43 32.48 41 14358 10106 3361354
Metastases to skin 41.29 32.48 12 14387 214 3371246
Ventricular hypokinesia 41.15 32.48 18 14381 1087 3370373
Lower respiratory tract infection 41.15 32.48 34 14365 6635 3364825
Brain natriuretic peptide increased 41.09 32.48 17 14382 894 3370566
Inappropriate schedule of drug administration 40.97 32.48 47 14352 13706 3357754
Blood phosphorus decreased 40.91 32.48 17 14382 904 3370556
Rhinorrhoea 40.91 32.48 36 14363 7653 3363807
Peritonitis 40.88 32.48 30 14369 4925 3366535
Hyperthermia 40.55 32.48 23 14376 2429 3369031
Hyperuricaemia 40.08 32.48 19 14380 1384 3370076
Pseudomonas infection 40.04 32.48 21 14378 1900 3369560
Disorientation 39.82 32.48 40 14359 10039 3361421
Diastolic dysfunction 39.61 32.48 17 14382 980 3370480
Loss of consciousness 39.60 32.48 67 14332 28080 3343380
Speech disorder 39.34 32.48 38 14361 9094 3362366
Paraesthesia 39.32 32.48 66 14333 27482 3343978
Needle issue 39.16 32.48 17 14382 1008 3370452
Red cell distribution width increased 39.04 32.48 15 14384 649 3370811
Angiofibroma 38.77 32.48 7 14392 9 3371451
Type I hypersensitivity 38.59 32.48 14 14385 515 3370945
Lung neoplasm 38.59 32.48 19 14380 1505 3369955
Cell death 38.57 32.48 14 14385 516 3370944
Rectal haemorrhage 38.56 32.48 38 14361 9320 3362140
Acidosis 38.42 32.48 23 14376 2687 3368773
Cardiac arrest 38.39 32.48 65 14334 27254 3344206
Oral disorder 38.26 32.48 20 14379 1797 3369663
Spinal pain 38.01 32.48 18 14381 1308 3370152
Night sweats 37.73 32.48 28 14371 4675 3366785
Klebsiella infection 37.20 32.48 17 14382 1139 3370321
Heart rate decreased 37.01 32.48 29 14370 5249 3366211
Necrosis 36.62 32.48 19 14380 1681 3369779
Fluid intake reduced 36.57 32.48 16 14383 967 3370493
Pharyngitis 36.53 32.48 22 14377 2598 3368862
Cancer pain 36.29 32.48 13 14386 461 3370999
Insulinoma 36.29 32.48 8 14391 42 3371418
Escherichia sepsis 36.23 32.48 16 14383 989 3370471
Ear infection 36.16 32.48 24 14375 3355 3368105
Haematemesis 36.16 32.48 32 14367 6853 3364607
Diabetes mellitus inadequate control 36.13 32.48 23 14376 2996 3368464
Ulcer 36.11 32.48 21 14378 2325 3369135
Breast cancer recurrent 35.89 32.48 14 14385 631 3370829
Papilloedema 35.76 32.48 17 14382 1246 3370214
Hepatic cirrhosis 35.71 32.48 26 14373 4216 3367244
Gingivitis 35.68 32.48 19 14380 1773 3369687
Respiratory rate increased 35.40 32.48 21 14378 2412 3369048
Drug interaction 35.32 32.48 86 14313 46726 3324734
Hepatic artery thrombosis 35.24 32.48 9 14390 96 3371364
Metastases to the mediastinum 35.07 32.48 9 14390 98 3371362
Metastases to meninges 35.04 32.48 13 14386 510 3370950
Gastrointestinal oedema 35.00 32.48 12 14387 373 3371087
Embolism 34.98 32.48 21 14378 2465 3368995
Tubulointerstitial nephritis 34.93 32.48 26 14373 4360 3367100
Hypovolaemia 34.88 32.48 20 14379 2156 3369304
Disseminated intravascular coagulation 34.87 32.48 30 14369 6187 3365273
Bronchiectasis 34.83 32.48 16 14383 1085 3370375
Exposed bone in jaw 34.73 32.48 16 14383 1092 3370368
Cerebrovascular accident 34.65 32.48 72 14327 35216 3336244
Lymphocytic infiltration 34.64 32.48 12 14387 385 3371075
Bile duct obstruction 34.62 32.48 14 14385 694 3370766
Blood creatinine decreased 34.61 32.48 14 14385 695 3370765
Dilatation ventricular 34.58 32.48 16 14383 1103 3370357
Anxiety 34.49 32.48 77 14322 39552 3331908
Renal cancer metastatic 34.39 32.48 11 14388 274 3371186
Iron deficiency anaemia 34.30 32.48 21 14378 2554 3368906
Perinephric collection 34.20 32.48 8 14391 57 3371403
Hypomagnesaemia 34.17 32.48 24 14375 3678 3367782
Cyanosis 34.11 32.48 27 14372 4959 3366501
Haematoma evacuation 34.04 32.48 9 14390 111 3371349
Fluid overload 33.89 32.48 24 14375 3727 3367733
Systemic inflammatory response syndrome 33.79 32.48 17 14382 1410 3370050
Clostridium difficile colitis 33.77 32.48 22 14377 2981 3368479
Intestinal perforation 33.73 32.48 22 14377 2986 3368474
Gait inability 33.72 32.48 32 14367 7493 3363967
Cardiac failure acute 33.61 32.48 18 14381 1699 3369761
Hepatic pain 33.52 32.48 13 14386 577 3370883
Cholecystitis acute 33.41 32.48 18 14381 1719 3369741
Folliculitis 33.34 32.48 15 14384 969 3370491
Nephrostomy 32.85 32.48 8 14391 69 3371391
Dermatitis acneiform 32.83 32.48 17 14382 1498 3369962
Frequent bowel movements 32.78 32.48 19 14380 2091 3369369
Glomerulonephritis 32.57 32.48 14 14385 810 3370650
Metabolic disorder 32.57 32.48 15 14384 1023 3370437

Pharmacologic Action:

SourceCodeDescription
ATC L01XE10 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Protein kinase inhibitors
ATC L04AA18 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000175076 Protein Kinase Inhibitors
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000182137 Cytochrome P450 2D6 Inhibitors
FDA EPC N0000175625 mTOR Inhibitor Immunosuppressant
FDA MoA N0000175624 mTOR Inhibitors
FDA PE N0000175550 Decreased Immunologic Activity
MeSH PA D000970 Antineoplastic Agents
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents
CHEBI has role CHEBI:35705 immunosuppressive agent
CHEBI has role CHEBI:35610 antineoplastic agent

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Tuberous sclerosis syndrome indication 7199000 DOID:13515
Carcinoma of breast indication 254838004 DOID:3459
Angiomyolipoma of kidney indication 254921004 DOID:8411
Hormone receptor positive malignant neoplasm of breast indication 417181009
Renal cell carcinoma indication 702391001 DOID:4450
Prevention of Kidney Transplant Rejection indication
Pancreatic Neuroendocrine Tumor indication
Subependymal Giant Cell Astrocytoma associated with Tuberous Sclerosis indication
Hypercholesterolemia contraindication 13644009
Proteinuria contraindication 29738008 DOID:576
Hyperlipidemia contraindication 55822004 DOID:1168
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Stomatitis contraindication 61170000 DOID:9637
Acute infectious disease contraindication 63171007
Interstitial pneumonia contraindication 64667001 DOID:3082
Diabetes mellitus contraindication 73211009 DOID:9351
Thrombotic thrombocytopenic purpura contraindication 78129009 DOID:10772
Hyperglycemia contraindication 80394007 DOID:4195
Leukopenia contraindication 84828003 DOID:615
Kidney disease contraindication 90708001 DOID:2527
Thrombosis of renal artery contraindication 95579008
Hemolytic uremic syndrome contraindication 111407006 DOID:12554
Malignant lymphoma contraindication 118600007 DOID:0060058
Disease of liver contraindication 235856003 DOID:409
Edema contraindication 267038008
Impaired wound healing contraindication 271618001
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Hypertriglyceridemia contraindication 302870006
Neutropenic disorder contraindication 303011007 DOID:1227
Primary malignant neoplasm contraindication 372087000
Pericardial effusion contraindication 373945007 DOID:118
Ascites contraindication 389026000
Breastfeeding (mother) contraindication 413712001
BK Polyomavirus Reactivation Nephropathy contraindication
Pleural Effusions contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.5 acidic
pKa2 13.7 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.25MG ZORTRESS NOVARTIS N021560 April 20, 2010 RX TABLET ORAL 5665772 Sept. 9, 2019 PROPHYLAXIS OF ALLOGRAFT REJECTION IN ADULT PATIENTS RECEIVING A LIVER TRANSPLANT
0.25MG ZORTRESS NOVARTIS N021560 April 20, 2010 RX TABLET ORAL 5665772 Sept. 9, 2019 PROPHYLAXIS OF ORGAN REJECTION IN ADULT PATIENTS AT LOW-MODERATE IMMUNOLOGIC RISK RECEIVING A RENAL TRANSPLANT
0.5MG ZORTRESS NOVARTIS N021560 April 20, 2010 RX TABLET ORAL 5665772 Sept. 9, 2019 PROPHYLAXIS OF ALLOGRAFT REJECTION IN ADULT PATIENTS RECEIVING A LIVER TRANSPLANT
0.5MG ZORTRESS NOVARTIS N021560 April 20, 2010 RX TABLET ORAL 5665772 Sept. 9, 2019 PROPHYLAXIS OF ORGAN REJECTION IN ADULT PATIENTS AT LOW-MODERATE IMMUNOLOGIC RISK RECEIVING A RENAL TRANSPLANT
0.75MG ZORTRESS NOVARTIS N021560 April 20, 2010 RX TABLET ORAL 5665772 Sept. 9, 2019 PROPHYLAXIS OF ALLOGRAFT REJECTION IN ADULT PATIENTS RECEIVING A LIVER TRANSPLANT
0.75MG ZORTRESS NOVARTIS N021560 April 20, 2010 RX TABLET ORAL 5665772 Sept. 9, 2019 PROPHYLAXIS OF ORGAN REJECTION IN ADULT PATIENTS AT LOW-MODERATE IMMUNOLOGIC RISK RECEIVING A RENAL TRANSPLANT
10MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL 8778962 Feb. 18, 2022 TREATMENT OF PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX (TSC) WHO HAVE SUBEPENDYMAL GIANT CELL ASTROCYTOMA (SEGA) THAT REQUIRES THERAPEUTIC INTERVENTION BUT CANNOT BE CURATIVELY RESECTED.
2.5MG AFINITOR NOVARTIS N022334 July 9, 2010 RX TABLET ORAL 8778962 Feb. 18, 2022 TREATMENT OF PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX (TSC) WHO HAVE SUBEPENDYMAL GIANT CELL ASTROCYTOMA (SEGA) THAT REQUIRES THERAPEUTIC INTERVENTION BUT CANNOT BE CURATIVELY RESECTED.
5MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL 8778962 Feb. 18, 2022 TREATMENT OF PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX (TSC) WHO HAVE SUBEPENDYMAL GIANT CELL ASTROCYTOMA (SEGA) THAT REQUIRES THERAPEUTIC INTERVENTION BUT CANNOT BE CURATIVELY RESECTED.
7.5MG AFINITOR NOVARTIS N022334 March 30, 2012 RX TABLET ORAL 8778962 Feb. 18, 2022 TREATMENT OF PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX (TSC) WHO HAVE SUBEPENDYMAL GIANT CELL ASTROCYTOMA (SEGA) THAT REQUIRES THERAPEUTIC INTERVENTION BUT CANNOT BE CURATIVELY RESECTED.
2MG AFINITOR DISPERZ NOVARTIS PHARM N203985 Aug. 29, 2012 RX TABLET, FOR SUSPENSION ORAL 8778962 Feb. 18, 2022 TREATMENT OF PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX (TSC) WHO HAVE SUBEPENDYMAL GIANT CELL ASTROCYTOMA (SEGA) THAT REQUIRES THERAPEUTIC INTERVENTION BUT CANNOT BE CURATIVELY RESECTED.
3MG AFINITOR DISPERZ NOVARTIS PHARM N203985 Aug. 29, 2012 RX TABLET, FOR SUSPENSION ORAL 8778962 Feb. 18, 2022 TREATMENT OF PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX (TSC) WHO HAVE SUBEPENDYMAL GIANT CELL ASTROCYTOMA (SEGA) THAT REQUIRES THERAPEUTIC INTERVENTION BUT CANNOT BE CURATIVELY RESECTED.
5MG AFINITOR DISPERZ NOVARTIS PHARM N203985 Aug. 29, 2012 RX TABLET, FOR SUSPENSION ORAL 8778962 Feb. 18, 2022 TREATMENT OF PATIENTS WITH TUBEROUS SCLEROSIS COMPLEX (TSC) WHO HAVE SUBEPENDYMAL GIANT CELL ASTROCYTOMA (SEGA) THAT REQUIRES THERAPEUTIC INTERVENTION BUT CANNOT BE CURATIVELY RESECTED.
10MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL 8436010 Feb. 22, 2022 TREATMENT OF ADVANCED HORMONE RECEPTOR POSITIVE, HER2-NEGATIVE BREAST CANCER IN COMBINATION WITH EXEMESTANE AFTER FAILURE OF TREATMENT WITH LETROZOLE OR ANASTROZOLE
2.5MG AFINITOR NOVARTIS N022334 July 9, 2010 RX TABLET ORAL 8436010 Feb. 22, 2022 TREATMENT OF ADVANCED HORMONE RECEPTOR POSITIVE, HER2-NEGATIVE BREAST CANCER IN COMBINATION WITH EXEMESTANE AFTER FAILURE OF TREATMENT WITH LETROZOLE OR ANASTROZOLE
5MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL 8436010 Feb. 22, 2022 TREATMENT OF ADVANCED HORMONE RECEPTOR POSITIVE, HER2-NEGATIVE BREAST CANCER IN COMBINATION WITH EXEMESTANE AFTER FAILURE OF TREATMENT WITH LETROZOLE OR ANASTROZOLE
7.5MG AFINITOR NOVARTIS N022334 March 30, 2012 RX TABLET ORAL 8436010 Feb. 22, 2022 TREATMENT OF ADVANCED HORMONE RECEPTOR POSITIVE, HER2-NEGATIVE BREAST CANCER IN COMBINATION WITH EXEMESTANE AFTER FAILURE OF TREATMENT WITH LETROZOLE OR ANASTROZOLE
10MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL 8410131 Nov. 1, 2025 TREATMENT OF SOLID EXCRETORY SYSTEM TUMORS; ADVANCED RENAL CELL CARCINOMA (RCC), AFTER FAILURE OF TREATMENT WITH SUNITINIB OR SORAFENIB
2.5MG AFINITOR NOVARTIS N022334 July 9, 2010 RX TABLET ORAL 8410131 Nov. 1, 2025 TREATMENT OF SOLID EXCRETORY SYSTEM TUMORS; ADVANCED RENAL CELL CARCINOMA (RCC), AFTER FAILURE OF TREATMENT WITH SUNITINIB OR SORAFENIB
5MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL 8410131 Nov. 1, 2025 TREATMENT OF SOLID EXCRETORY SYSTEM TUMORS; ADVANCED RENAL CELL CARCINOMA (RCC), AFTER FAILURE OF TREATMENT WITH SUNITINIB OR SORAFENIB
7.5MG AFINITOR NOVARTIS N022334 March 30, 2012 RX TABLET ORAL 8410131 Nov. 1, 2025 TREATMENT OF SOLID EXCRETORY SYSTEM TUMORS; ADVANCED RENAL CELL CARCINOMA (RCC), AFTER FAILURE OF TREATMENT WITH SUNITINIB OR SORAFENIB
10MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL 9006224 July 1, 2028 TREATMENT OF PATIENTS WITH PROGESSIVE NEUROENDOCRINE TUMORS OF PANCREATIC ORIGIN (PNET) THAT ARE UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC
2.5MG AFINITOR NOVARTIS N022334 July 9, 2010 RX TABLET ORAL 9006224 July 1, 2028 TREATMENT OF PATIENTS WITH PROGESSIVE NEUROENDOCRINE TUMORS OF PANCREATIC ORIGIN (PNET) THAT ARE UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC
5MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL 9006224 July 1, 2028 TREATMENT OF PATIENTS WITH PROGESSIVE NEUROENDOCRINE TUMORS OF PANCREATIC ORIGIN (PNET) THAT ARE UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC
7.5MG AFINITOR NOVARTIS N022334 March 30, 2012 RX TABLET ORAL 9006224 July 1, 2028 TREATMENT OF PATIENTS WITH PROGESSIVE NEUROENDOCRINE TUMORS OF PANCREATIC ORIGIN (PNET) THAT ARE UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL April 29, 2018 PEDIATRIC EXCLUSIVITY
2.5MG AFINITOR NOVARTIS N022334 July 9, 2010 RX TABLET ORAL April 29, 2018 PEDIATRIC EXCLUSIVITY
5MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL April 29, 2018 PEDIATRIC EXCLUSIVITY
7.5MG AFINITOR NOVARTIS N022334 March 30, 2012 RX TABLET ORAL April 29, 2018 PEDIATRIC EXCLUSIVITY
2MG AFINITOR DISPERZ NOVARTIS PHARM N203985 Aug. 29, 2012 RX TABLET, FOR SUSPENSION ORAL April 29, 2018 PEDIATRIC EXCLUSIVITY
3MG AFINITOR DISPERZ NOVARTIS PHARM N203985 Aug. 29, 2012 RX TABLET, FOR SUSPENSION ORAL April 29, 2018 PEDIATRIC EXCLUSIVITY
5MG AFINITOR DISPERZ NOVARTIS PHARM N203985 Aug. 29, 2012 RX TABLET, FOR SUSPENSION ORAL April 29, 2018 PEDIATRIC EXCLUSIVITY
10MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL May 5, 2018 TREATMENT OF PROGRESSIVE NEUROENDOCRINE TUMORS OF PANCREATIC ORIGIN (PNET) IN PATIENTS WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE
2.5MG AFINITOR NOVARTIS N022334 July 9, 2010 RX TABLET ORAL May 5, 2018 TREATMENT OF PROGRESSIVE NEUROENDOCRINE TUMORS OF PANCREATIC ORIGIN (PNET) IN PATIENTS WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE
5MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL May 5, 2018 TREATMENT OF PROGRESSIVE NEUROENDOCRINE TUMORS OF PANCREATIC ORIGIN (PNET) IN PATIENTS WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE
7.5MG AFINITOR NOVARTIS N022334 March 30, 2012 RX TABLET ORAL May 5, 2018 TREATMENT OF PROGRESSIVE NEUROENDOCRINE TUMORS OF PANCREATIC ORIGIN (PNET) IN PATIENTS WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE
10MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL Nov. 5, 2018 PEDIATRIC EXCLUSIVITY
2.5MG AFINITOR NOVARTIS N022334 July 9, 2010 RX TABLET ORAL Nov. 5, 2018 PEDIATRIC EXCLUSIVITY
5MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL Nov. 5, 2018 PEDIATRIC EXCLUSIVITY
7.5MG AFINITOR NOVARTIS N022334 March 30, 2012 RX TABLET ORAL Nov. 5, 2018 PEDIATRIC EXCLUSIVITY
10MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL Feb. 26, 2019 TREATMENT OF ADULT PATIENTS WITH PROGRESSIVE, WELL DIFFERENTIATED, NON-FUNCTIONAL NEUROENDOCRINE TUMORS (NET) OF GI OR LUNG ORIGIN WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE
2.5MG AFINITOR NOVARTIS N022334 July 9, 2010 RX TABLET ORAL Feb. 26, 2019 TREATMENT OF ADULT PATIENTS WITH PROGRESSIVE, WELL DIFFERENTIATED, NON-FUNCTIONAL NEUROENDOCRINE TUMORS (NET) OF GI OR LUNG ORIGIN WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE
5MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL Feb. 26, 2019 TREATMENT OF ADULT PATIENTS WITH PROGRESSIVE, WELL DIFFERENTIATED, NON-FUNCTIONAL NEUROENDOCRINE TUMORS (NET) OF GI OR LUNG ORIGIN WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE
7.5MG AFINITOR NOVARTIS N022334 March 30, 2012 RX TABLET ORAL Feb. 26, 2019 TREATMENT OF ADULT PATIENTS WITH PROGRESSIVE, WELL DIFFERENTIATED, NON-FUNCTIONAL NEUROENDOCRINE TUMORS (NET) OF GI OR LUNG ORIGIN WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE
10MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL April 26, 2019 TREATMENT OF ADULTS WITH RENAL ANGIOMYOLIPOMA AND TUBEROUS SCLEROSIS COMPLEX (TSC) NOT REQUIRING IMMEDIATE SURGERY
2.5MG AFINITOR NOVARTIS N022334 July 9, 2010 RX TABLET ORAL April 26, 2019 TREATMENT OF ADULTS WITH RENAL ANGIOMYOLIPOMA AND TUBEROUS SCLEROSIS COMPLEX (TSC) NOT REQUIRING IMMEDIATE SURGERY
5MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL April 26, 2019 TREATMENT OF ADULTS WITH RENAL ANGIOMYOLIPOMA AND TUBEROUS SCLEROSIS COMPLEX (TSC) NOT REQUIRING IMMEDIATE SURGERY
7.5MG AFINITOR NOVARTIS N022334 March 30, 2012 RX TABLET ORAL April 26, 2019 TREATMENT OF ADULTS WITH RENAL ANGIOMYOLIPOMA AND TUBEROUS SCLEROSIS COMPLEX (TSC) NOT REQUIRING IMMEDIATE SURGERY
10MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL Oct. 26, 2019 PEDIATRIC EXCLUSIVITY
2.5MG AFINITOR NOVARTIS N022334 July 9, 2010 RX TABLET ORAL Oct. 26, 2019 PEDIATRIC EXCLUSIVITY
5MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL Oct. 26, 2019 PEDIATRIC EXCLUSIVITY
7.5MG AFINITOR NOVARTIS N022334 March 30, 2012 RX TABLET ORAL Oct. 26, 2019 PEDIATRIC EXCLUSIVITY
10MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL Feb. 26, 2023 TREATMENT OF ADULT PATIENTS WITH PROGRESSIVE, WELL-DIFFERENTIATED, NON-FUNCTIONAL, NEUROENDOCRINE TUMORS (NET) OF GASTROINTESTINAL (GI) OR LUNG ORIGIN, (EXCLUDING PANCREATIC) WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE
2.5MG AFINITOR NOVARTIS N022334 July 9, 2010 RX TABLET ORAL Feb. 26, 2023 TREATMENT OF ADULT PATIENTS WITH PROGRESSIVE, WELL-DIFFERENTIATED, NON-FUNCTIONAL, NEUROENDOCRINE TUMORS (NET) OF GASTROINTESTINAL (GI) OR LUNG ORIGIN, (EXCLUDING PANCREATIC) WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE
5MG AFINITOR NOVARTIS N022334 March 30, 2009 RX TABLET ORAL Feb. 26, 2023 TREATMENT OF ADULT PATIENTS WITH PROGRESSIVE, WELL-DIFFERENTIATED, NON-FUNCTIONAL, NEUROENDOCRINE TUMORS (NET) OF GASTROINTESTINAL (GI) OR LUNG ORIGIN, (EXCLUDING PANCREATIC) WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE
7.5MG AFINITOR NOVARTIS N022334 March 30, 2012 RX TABLET ORAL Feb. 26, 2023 TREATMENT OF ADULT PATIENTS WITH PROGRESSIVE, WELL-DIFFERENTIATED, NON-FUNCTIONAL, NEUROENDOCRINE TUMORS (NET) OF GASTROINTESTINAL (GI) OR LUNG ORIGIN, (EXCLUDING PANCREATIC) WITH UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC DISEASE

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Peptidyl-prolyl cis-trans isomerase FKBP1A Enzyme INHIBITOR IC50 8.26 WOMBAT-PK CHEMBL
Serine/threonine-protein kinase mTOR Kinase INHIBITOR IC50 8.70 IUPHAR
Multidrug resistance protein 1 Transporter WOMBAT-PK

External reference:

IDSource
4028636 VUID
N0000178379 NUI
C0541315 UMLSCUI
5889 IUPHAR_LIGAND_ID
D02714 KEGG_DRUG
428127005 SNOMEDCT_US
428698007 SNOMEDCT_US
141704 RXNORM
20447 MMSL
d05626 MMSL
4028636 VANDF
N0000178379 NDFRT
010829 NDDF
N0000191925 NDFRT
9HW64Q8G6G UNII
7863 INN_ID
DB01590 DRUGBANK_ID
CHEMBL1908360 ChEMBL_ID
6442177 PUBCHEM_CID
D000068338 MESH_DESCRIPTOR_UI
CHEBI:68478 CHEBI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Zortress HUMAN PRESCRIPTION DRUG LABEL 1 0078-0414 TABLET 0.50 mg ORAL NDA 19 sections
Zortress HUMAN PRESCRIPTION DRUG LABEL 1 0078-0415 TABLET 0.75 mg ORAL NDA 19 sections
Zortress HUMAN PRESCRIPTION DRUG LABEL 1 0078-0417 TABLET 0.25 mg ORAL NDA 19 sections
Afinitor HUMAN PRESCRIPTION DRUG LABEL 1 0078-0566 TABLET 5 mg ORAL NDA 20 sections
Afinitor HUMAN PRESCRIPTION DRUG LABEL 1 0078-0567 TABLET 10 mg ORAL NDA 20 sections
Afinitor HUMAN PRESCRIPTION DRUG LABEL 1 0078-0594 TABLET 2.50 mg ORAL NDA 20 sections
Afinitor HUMAN PRESCRIPTION DRUG LABEL 1 0078-0620 TABLET 7.50 mg ORAL NDA 20 sections
Afinitor HUMAN PRESCRIPTION DRUG LABEL 1 0078-0626 TABLET, FOR SUSPENSION 2 mg ORAL NDA 20 sections
Afinitor HUMAN PRESCRIPTION DRUG LABEL 1 0078-0627 TABLET, FOR SUSPENSION 3 mg ORAL NDA 20 sections
Afinitor HUMAN PRESCRIPTION DRUG LABEL 1 0078-0628 TABLET, FOR SUSPENSION 5 mg ORAL NDA 20 sections