sirolimus ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
immunosuppressants, rapamycin derivatives 2446 53123-88-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sirolimus
  • rapamycin
  • rapammune
  • rapamune
  • supralimus
  • rapalimus
  • AY22989
  • AY-22989
A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties. Limited data describing efficacy in patients with COVID-19 is available. However, its efficacy and safety in the treatment of COVID-19 was not established.
  • Molecular weight: 914.19
  • Formula: C51H79NO13
  • CLOGP: 7.04
  • LIPINSKI: 3
  • HAC: 14
  • HDO: 3
  • TPSA: 195.43
  • ALOGS: -5.72
  • ROTB: 6

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
3 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 2 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.15 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 15 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Sept. 15, 1999 FDA PF PRISM CV
July 4, 2014 PMDA NOBELPHARMA CO., LTD
March 13, 2001 EMA Pfizer Europe MA EEIG

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
Transplant dysfunction 2119.59 18.08 445 18051 4427 63466099
Transplant rejection 2050.09 18.08 501 17995 10279 63460247
Ovarian cyst 1445.06 18.08 412 18084 15533 63454993
Acne 1295.14 18.08 413 18083 22880 63447646
Alopecia 345.40 18.08 456 18040 337080 63133446
Epstein-Barr virus infection 266.66 18.08 97 18399 7953 63462573
Sleep disorder due to general medical condition, insomnia type 246.55 18.08 166 18330 52051 63418475
Liver function test abnormal 236.68 18.08 157 18339 48024 63422502
Product use in unapproved indication 222.37 18.08 267 18229 178813 63291713
Post transplant lymphoproliferative disorder 209.99 18.08 72 18424 4959 63465567
Off label use 208.75 18.08 543 17953 673919 62796607
Thrombotic microangiopathy 203.69 18.08 86 18410 10475 63460051
Kidney transplant rejection 201.43 18.08 67 18429 4204 63466322
Kidney fibrosis 145.19 18.08 43 18453 1838 63468688
Immunosuppressant drug level increased 132.34 18.08 47 18449 3591 63466935
Pneumonia 119.91 18.08 347 18149 456420 63014106
Polyomavirus-associated nephropathy 115.87 18.08 36 18460 1812 63468714
Smooth muscle cell neoplasm 114.50 18.08 30 18466 811 63469715
Graft versus host disease in gastrointestinal tract 99.71 18.08 37 18459 3204 63467322
Chronic allograft nephropathy 99.26 18.08 26 18470 702 63469824
Graft versus host disease 94.68 18.08 44 18452 6719 63463807
Graft versus host disease in skin 92.45 18.08 34 18462 2871 63467655
Epstein-Barr virus associated lymphoproliferative disorder 90.45 18.08 30 18466 1864 63468662
Cytomegalovirus infection 90.25 18.08 63 18433 20889 63449637
Human herpesvirus 6 infection 88.20 18.08 33 18463 2924 63467602
Hypertriglyceridaemia 82.31 18.08 39 18457 6220 63464306
Acute graft versus host disease 81.85 18.08 35 18461 4393 63466133
Liver transplant rejection 77.71 18.08 25 18471 1410 63469116
Condition aggravated 77.46 18.08 275 18221 401942 63068584
Arthralgia 76.96 18.08 35 18461 569675 62900851
Product use issue 76.38 18.08 186 18310 220334 63250192
Alveolar proteinosis 74.48 18.08 18 18478 347 63470179
JC virus infection 68.96 18.08 25 18471 2026 63468500
Drug level increased 68.11 18.08 55 18441 22681 63447845
MELAS syndrome 67.69 18.08 14 18482 127 63470399
Posterior reversible encephalopathy syndrome 67.43 18.08 49 18447 17296 63453230
Cryptosporidiosis infection 61.36 18.08 15 18481 304 63470222
BK virus infection 60.87 18.08 26 18470 3253 63467273
Infusion related reaction 59.14 18.08 3 18493 245518 63225008
Adenovirus infection 58.74 18.08 26 18470 3545 63466981
Fatigue 57.87 18.08 107 18389 887921 62582605
Rash 56.96 18.08 48 18448 560823 62909703
Heart transplant rejection 56.06 18.08 16 18480 599 63469927
Hypersensitivity 53.99 18.08 10 18486 292675 63177851
Renal graft infection 53.87 18.08 13 18483 249 63470277
Arthropathy 53.16 18.08 4 18492 234788 63235738
Joint swelling 51.05 18.08 16 18480 327650 63142876
Skin squamous cell carcinoma metastatic 49.81 18.08 8 18488 12 63470514
Incorrect route of product administration 49.69 18.08 50 18446 27402 63443124
Loss of personal independence in daily activities 49.58 18.08 96 18400 97194 63373332
Chronic graft versus host disease 49.15 18.08 22 18474 3080 63467446
Pseudomonas infection 48.94 18.08 34 18462 11179 63459347
Blood creatinine increased 48.88 18.08 90 18406 87754 63382772
Renal impairment 48.51 18.08 90 18406 88265 63382261
Rheumatoid arthritis 48.26 18.08 173 18323 253646 63216880
Multiple organ dysfunction syndrome 47.63 18.08 70 18426 56682 63413844
Drug interaction 46.86 18.08 160 18336 228971 63241555
Nephropathy toxic 46.75 18.08 31 18465 9448 63461078
Pneumocystis jirovecii pneumonia 46.64 18.08 39 18457 16875 63453651
Dizziness 45.85 18.08 35 18461 429890 63040636
Drug ineffective for unapproved indication 45.77 18.08 53 18443 34010 63436516
Plasmablastic lymphoma 45.62 18.08 11 18485 210 63470316
Morphoea 45.36 18.08 12 18484 337 63470189
Fall 44.36 18.08 30 18466 392304 63078222
Cytomegalovirus infection reactivation 44.01 18.08 22 18474 3941 63466585
Lymphocele 43.29 18.08 14 18482 803 63469723
Septic shock 43.19 18.08 73 18423 66556 63403970
Drug level below therapeutic 42.52 18.08 23 18473 4843 63465683
Mouth ulceration 42.12 18.08 50 18446 32934 63437592
Hypogammaglobulinaemia 41.71 18.08 26 18470 7129 63463397
Respiratory failure 40.75 18.08 91 18405 101767 63368759
Complications of transplanted kidney 40.57 18.08 18 18478 2468 63468058
Avian influenza 39.57 18.08 8 18488 64 63470462
Pancreas transplant rejection 38.82 18.08 9 18487 144 63470382
Proteinuria 38.62 18.08 37 18459 19108 63451418
Globulins decreased 38.57 18.08 10 18486 259 63470267
Neurofibrosarcoma 38.20 18.08 9 18487 155 63470371
Immunosuppressant drug level decreased 37.15 18.08 13 18483 950 63469576
Abdominal discomfort 36.98 18.08 24 18472 320861 63149665
Swelling 36.96 18.08 17 18479 275361 63195165
Polyomavirus viraemia 36.55 18.08 12 18484 722 63469804
Pneumonitis 36.36 18.08 48 18448 35174 63435352
Lymphopenia 36.17 18.08 35 18461 18292 63452234
Sinusitis 35.40 18.08 11 18485 226642 63243884
Focal segmental glomerulosclerosis 35.27 18.08 14 18482 1454 63469072
Therapeutic product effect decreased 34.76 18.08 7 18489 193180 63277346
Pneumothorax 33.89 18.08 32 18464 16229 63454297
Dysplasia 33.76 18.08 12 18484 918 63469608
Drug hypersensitivity 33.46 18.08 25 18471 310662 63159864
Somnolence 33.15 18.08 6 18490 178679 63291847
Chronic graft versus host disease in skin 32.29 18.08 11 18485 742 63469784
Hepatitis E 32.03 18.08 13 18483 1431 63469095
Adjusted calcium decreased 31.85 18.08 8 18488 182 63470344
Pain in extremity 31.62 18.08 30 18466 331456 63139070
Constipation 31.58 18.08 13 18483 224930 63245596
Trichodysplasia spinulosa 31.03 18.08 10 18486 567 63469959
Transplant failure 30.86 18.08 13 18483 1572 63468954
Bacillary angiomatosis 30.80 18.08 7 18489 102 63470424
Jejunal perforation 30.55 18.08 7 18489 106 63470420
Alopecia scarring 30.43 18.08 7 18489 108 63470418
Babesiosis 30.36 18.08 8 18488 221 63470305
Feeling abnormal 29.75 18.08 4 18492 148388 63322138
Dyspnoea 29.35 18.08 97 18399 661216 62809310
Trichostasis spinulosa 29.31 18.08 5 18491 13 63470513
Acute graft versus host disease in skin 29.28 18.08 16 18480 3436 63467090
Bronchiolitis obliterans syndrome 28.96 18.08 7 18489 135 63470391
Overdose 28.62 18.08 86 18410 114992 63355534
Renal-limited thrombotic microangiopathy 28.48 18.08 6 18490 60 63470466
Klebsiella infection 28.39 18.08 22 18474 8544 63461982
Endocarditis Q fever 28.30 18.08 5 18491 17 63470509
Weight increased 28.05 18.08 21 18475 260771 63209755
Graft thrombosis 27.92 18.08 7 18489 158 63470368
Skin graft rejection 27.87 18.08 5 18491 19 63470507
Insomnia 27.78 18.08 14 18482 215238 63255288
Blastomycosis 27.64 18.08 8 18488 315 63470211
Haemodialysis 27.54 18.08 22 18474 8925 63461601
Escherichia bacteraemia 27.53 18.08 16 18480 3867 63466659
Back pain 27.49 18.08 22 18474 264123 63206403
Blister 27.25 18.08 3 18493 129811 63340715
Jarisch-Herxheimer reaction 26.42 18.08 8 18488 369 63470157
Fibrosarcoma 26.33 18.08 4 18492 3 63470523
Squamous cell carcinoma 26.09 18.08 21 18475 8611 63461915
Hypoalbuminaemia 26.08 18.08 24 18472 11781 63458745
Maternal exposure during pregnancy 25.96 18.08 16 18480 220046 63250480
Hepatic fibrosis 25.76 18.08 15 18481 3637 63466889
Renal failure 25.64 18.08 84 18412 117568 63352958
Lower respiratory tract infection 25.52 18.08 4 18492 132303 63338223
Muscle spasms 25.43 18.08 7 18489 156143 63314383
Musculoskeletal stiffness 25.38 18.08 11 18485 184607 63285919
Wound 25.34 18.08 8 18488 163255 63307271
Rhinovirus infection 25.25 18.08 16 18480 4513 63466013
Haemolytic uraemic syndrome 25.18 18.08 13 18483 2490 63468036
Gait disturbance 25.04 18.08 11 18485 183167 63287359
Pulmonary haemorrhage 25.02 18.08 19 18477 7162 63463364
Scleroderma 24.87 18.08 17 18479 5445 63465081
Injection site pain 24.86 18.08 4 18492 129796 63340730
Hypoaesthesia 24.84 18.08 9 18487 168384 63302142
Pruritus 24.81 18.08 42 18454 361411 63109115
Drug level fluctuating 24.75 18.08 8 18488 458 63470068
Obliterative bronchiolitis 24.36 18.08 12 18484 2083 63468443
Drug effective for unapproved indication 24.21 18.08 14 18482 3350 63467176
Anxiety 24.06 18.08 17 18479 217524 63253002
Renal tubular necrosis 24.04 18.08 23 18473 11855 63458671
Human polyomavirus infection 23.11 18.08 7 18489 323 63470203
Viraemia 23.00 18.08 10 18486 1306 63469220
Discomfort 22.96 18.08 10 18486 167364 63303162
Acute kidney injury 22.87 18.08 143 18353 263272 63207254
Lung transplant rejection 22.83 18.08 9 18487 918 63469608
Headache 22.83 18.08 101 18395 633140 62837386
Product dose omission issue 22.57 18.08 21 18475 234292 63236234
Pulmonary alveolar haemorrhage 22.37 18.08 15 18481 4653 63465873
Moyamoya disease 22.06 18.08 5 18491 72 63470454
Bacterial colitis 22.06 18.08 5 18491 72 63470454
Enterovirus infection 22.05 18.08 9 18487 1005 63469521
Hepatic angiosarcoma 21.94 18.08 4 18492 17 63470509
Pterygium 21.84 18.08 6 18490 195 63470331
Pleural effusion 21.62 18.08 68 18428 93142 63377384
Acute hepatitis C 21.51 18.08 5 18491 81 63470445
Nausea 21.22 18.08 154 18342 854317 62616209
Chest pain 21.22 18.08 19 18477 215940 63254586
Interstitial lung disease 21.13 18.08 52 18444 61856 63408670
Urticaria 21.07 18.08 11 18485 165791 63304735
Cat scratch disease 20.99 18.08 6 18490 226 63470300
Aspergillus infection 20.95 18.08 18 18478 8075 63462451
Salivary gland mass 20.86 18.08 5 18491 93 63470433
Bacterial translocation 20.59 18.08 6 18490 242 63470284
Malaise 20.55 18.08 58 18438 415896 63054630
Mobility decreased 20.55 18.08 5 18491 121154 63349372
Pulmonary artery atresia 20.51 18.08 4 18492 26 63470500
Kussmaul respiration 20.45 18.08 6 18490 248 63470278
Haemophagocytic lymphohistiocytosis 20.42 18.08 20 18476 10607 63459919
Therapy partial responder 20.37 18.08 20 18476 10638 63459888
Human herpesvirus 8 infection 20.36 18.08 6 18490 252 63470274
Diabetes mellitus 20.25 18.08 48 18448 55762 63414764
Urinary tract infection pseudomonal 20.02 18.08 8 18488 845 63469681
Drug ineffective 19.98 18.08 420 18076 1044345 62426181
Thymus enlargement 19.65 18.08 5 18491 120 63470406
Syncope 19.61 18.08 5 18491 117380 63353146
Visceral leishmaniasis 19.44 18.08 7 18489 556 63469970
Renal transplant 19.38 18.08 9 18487 1371 63469155
Disseminated mycobacterium avium complex infection 19.27 18.08 5 18491 130 63470396
Cardiac murmur functional 18.99 18.08 4 18492 40 63470486
Magnetic resonance imaging head abnormal 18.95 18.08 10 18486 2003 63468523
Varicella zoster virus infection 18.85 18.08 11 18485 2678 63467848
Intussusception 18.81 18.08 7 18489 611 63469915
Microangiopathic haemolytic anaemia 18.75 18.08 7 18489 616 63469910
Epstein-Barr viraemia 18.72 18.08 8 18488 1002 63469524
Biopsy kidney abnormal 18.64 18.08 4 18492 44 63470482
Chronic kidney disease 18.64 18.08 41 18455 45357 63425169
Graft ischaemia 18.56 18.08 4 18492 45 63470481
Disease recurrence 18.54 18.08 31 18465 27999 63442527
Q fever 18.52 18.08 5 18491 152 63470374
Asthma 18.50 18.08 7 18489 127554 63342972
Craniocerebral injury 18.32 18.08 11 18485 2821 63467705
Acinetobacter infection 18.20 18.08 9 18487 1574 63468952
Wheezing 18.18 18.08 3 18493 95592 63374934
Viral oesophagitis 18.13 18.08 3 18493 6 63470520

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
Transplant rejection 464.54 14.32 187 19979 10124 34926641
Off label use 350.33 14.32 753 19413 418771 34517994
Product use in unapproved indication 348.77 14.32 382 19784 117117 34819648
Kidney transplant rejection 310.32 14.32 128 20038 7369 34929396
Cytomegalovirus infection 167.64 14.32 131 20035 26004 34910761
Adenovirus infection 159.19 14.32 72 20094 5185 34931580
Immunosuppressant drug level increased 152.51 14.32 73 20093 5982 34930783
Post transplant lymphoproliferative disorder 150.27 14.32 74 20092 6454 34930311
Liver transplant rejection 140.57 14.32 51 20115 2068 34934697
Thrombotic microangiopathy 139.52 14.32 83 20083 10547 34926218
Transplant failure 138.01 14.32 58 20108 3495 34933270
Epstein-Barr virus infection 130.96 14.32 71 20095 7557 34929208
Acute graft versus host disease 112.95 14.32 61 20105 6442 34930323
BK virus infection 102.95 14.32 55 20111 5683 34931082
Product use issue 101.77 14.32 152 20014 63064 34873701
Nephropathy toxic 100.54 14.32 72 20094 12516 34924249
Cytomegalovirus viraemia 100.07 14.32 59 20107 7371 34929394
Cytomegalovirus infection reactivation 94.48 14.32 50 20116 5068 34931697
Graft versus host disease in skin 88.85 14.32 44 20122 3881 34932884
Squamous cell carcinoma 85.64 14.32 63 20103 11412 34925353
Chronic graft versus host disease 81.51 14.32 43 20123 4330 34932435
Squamous cell carcinoma of skin 79.54 14.32 59 20107 10822 34925943
Polyomavirus-associated nephropathy 77.95 14.32 40 20126 3804 34932961
Lymphocele 76.56 14.32 29 20137 1328 34935437
Blood creatinine increased 72.00 14.32 165 20001 94811 34841954
Complications of transplanted kidney 68.43 14.32 39 20127 4570 34932195
Nocardiosis 68.43 14.32 37 20129 3914 34932851
Chronic allograft nephropathy 67.81 14.32 26 20140 1231 34935534
Skin squamous cell carcinoma recurrent 65.24 14.32 13 20153 42 34936723
Graft versus host disease in gastrointestinal tract 65.21 14.32 35 20131 3648 34933117
Smooth muscle cell neoplasm 64.28 14.32 16 20150 169 34936596
Proteinuria 62.77 14.32 65 20101 18577 34918188
Graft versus host disease in liver 60.23 14.32 24 20142 1260 34935505
Heart transplant rejection 57.71 14.32 23 20143 1208 34935557
Renal impairment 57.57 14.32 151 20015 94362 34842403
Transplant dysfunction 54.97 14.32 28 20138 2621 34934144
Acute graft versus host disease in skin 54.01 14.32 35 20131 5166 34931599
Propionibacterium infection 53.90 14.32 15 20151 251 34936514
Meningitis viral 53.40 14.32 20 20146 887 34935878
Multiple organ dysfunction syndrome 52.54 14.32 128 20038 76438 34860327
Skin squamous cell carcinoma metastatic 51.71 14.32 11 20155 53 34936712
Pneumonia cytomegaloviral 51.22 14.32 28 20138 3026 34933739
Kidney fibrosis 50.50 14.32 25 20141 2203 34934562
Epidermodysplasia verruciformis 49.93 14.32 14 20152 241 34936524
Diarrhoea haemorrhagic 47.92 14.32 36 20130 6728 34930037
Brain abscess 47.90 14.32 27 20139 3098 34933667
Bronchopulmonary aspergillosis 47.35 14.32 50 20116 14609 34922156
Pneumatosis intestinalis 47.25 14.32 29 20137 3894 34932871
Scleroderma 45.91 14.32 21 20145 1551 34935214
Fatigue 45.46 14.32 91 20075 370562 34566203
Dizziness 45.15 14.32 36 20130 218485 34718280
Constipation 42.67 14.32 13 20153 136969 34799796
Herpes zoster meningoencephalitis 42.38 14.32 13 20153 310 34936455
Interstitial lung disease 41.47 14.32 106 20060 65176 34871589
Acute graft versus host disease in intestine 40.43 14.32 23 20143 2685 34934080
Hypotension 40.42 14.32 41 20125 221608 34715157
Diaphragmatic hernia 40.29 14.32 12 20154 258 34936507
Abdominal wall abscess 39.77 14.32 14 20152 519 34936246
Cow pox 39.22 14.32 8 20158 30 34936735
Impaired healing 38.72 14.32 46 20120 15288 34921477
Retinal scar 38.36 14.32 12 20154 306 34936459
Human herpesvirus 8 infection 38.14 14.32 16 20150 959 34935806
Graft versus host disease 37.65 14.32 38 20128 10531 34926234
Staphylococcal mediastinitis 35.99 14.32 8 20158 49 34936716
Escherichia infection 35.70 14.32 33 20133 8212 34928553
Pleocytosis 35.54 14.32 13 20153 539 34936226
Renal tubular atrophy 35.31 14.32 16 20150 1156 34935609
Cytomegalovirus chorioretinitis 34.46 14.32 23 20143 3566 34933199
Hyperlipidaemia 34.10 14.32 42 20124 14487 34922278
Central nervous system lymphoma 34.06 14.32 15 20151 1013 34935752
Hepatic cancer recurrent 34.05 14.32 11 20155 312 34936453
Malacoplakia 33.96 14.32 12 20154 450 34936315
Mouth ulceration 33.89 14.32 38 20128 11872 34924893
Drug ineffective for unapproved indication 33.86 14.32 54 20112 23661 34913104
Transitional cell carcinoma 33.78 14.32 19 20147 2170 34934595
Pericardial effusion 33.64 14.32 55 20111 24607 34912158
Nephrogenic diabetes insipidus 33.48 14.32 16 20150 1305 34935460
Haemolytic uraemic syndrome 33.01 14.32 19 20147 2267 34934498
Venoocclusive liver disease 32.79 14.32 31 20135 7935 34928830
Protothecosis 32.69 14.32 7 20159 35 34936730
Human herpesvirus 6 infection 31.95 14.32 18 20148 2063 34934702
Renal tubular necrosis 31.56 14.32 42 20124 15638 34921127
Gastroenteritis norovirus 31.29 14.32 16 20150 1510 34935255
Drug interaction 31.21 14.32 230 19936 225716 34711049
Acute graft versus host disease in liver 30.90 14.32 16 20150 1550 34935215
Tularaemia 30.69 14.32 8 20158 103 34936662
Metastases to lung 30.47 14.32 32 20134 9288 34927477
Bradycardia 30.00 14.32 4 20162 75414 34861351
Anxiety 29.95 14.32 10 20156 99418 34837347
Hypogammaglobulinaemia 29.74 14.32 29 20137 7711 34929054
Focal segmental glomerulosclerosis 29.70 14.32 17 20149 2008 34934757
Scedosporium infection 29.64 14.32 13 20153 869 34935896
Alveolar proteinosis 29.63 14.32 11 20155 476 34936289
Malignant fibrous histiocytoma 29.28 14.32 9 20157 216 34936549
Pruritus 28.53 14.32 24 20142 141957 34794808
Right ventricular diastolic collapse 28.47 14.32 7 20159 70 34936695
Drug level increased 28.42 14.32 48 20118 22048 34914717
Chronic graft versus host disease in skin 28.40 14.32 13 20153 961 34935804
Nausea 28.31 14.32 101 20065 339807 34596958
Drug effective for unapproved indication 28.22 14.32 18 20148 2584 34934181
Hydronephrosis 27.72 14.32 32 20134 10314 34926451
Epstein-Barr viraemia 27.61 14.32 14 20152 1298 34935467
Drug level decreased 27.57 14.32 28 20138 7818 34928947
Pharyngitis 27.27 14.32 28 20138 7916 34928849
Varicella 27.09 14.32 15 20151 1662 34935103
Renal-limited thrombotic microangiopathy 26.79 14.32 7 20159 91 34936674
Chronic graft versus host disease in liver 26.58 14.32 10 20156 449 34936316
Complications of transplanted heart 26.28 14.32 9 20157 307 34936458
Fall 25.49 14.32 49 20117 202836 34733929
Diffuse large B-cell lymphoma 25.34 14.32 26 20140 7344 34929421
Renal tubular injury 25.20 14.32 12 20154 971 34935794
Back pain 25.19 14.32 20 20146 121769 34814996
Arthralgia 25.11 14.32 37 20129 170004 34766761
Philadelphia positive chronic myeloid leukaemia 24.67 14.32 7 20159 126 34936639
Lung transplant rejection 24.45 14.32 11 20155 781 34935984
Venoocclusive disease 24.27 14.32 17 20149 2850 34933915
Drug resistance 24.13 14.32 49 20117 25878 34910887
Depression 24.07 14.32 13 20153 97085 34839680
Muscle spasms 23.55 14.32 7 20159 74994 34861771
Ileal ulcer 23.51 14.32 10 20156 620 34936145
Enteritis 23.20 14.32 26 20140 8116 34928649
Syncope 23.03 14.32 12 20154 91439 34845326
Ophthalmic herpes zoster 23.02 14.32 11 20155 897 34935868
Insomnia 22.86 14.32 16 20150 103891 34832874
Obliterative bronchiolitis 22.44 14.32 12 20154 1241 34935524
Disseminated varicella zoster virus infection 22.31 14.32 8 20158 313 34936452
Somnolence 22.05 14.32 19 20147 111097 34825668
Aspergillus infection 21.91 14.32 31 20135 12223 34924542
Basal cell carcinoma 21.78 14.32 40 20126 19618 34917147
Neuroendocrine carcinoma of the skin 21.33 14.32 10 20156 781 34935984
Inappropriate schedule of product administration 21.10 14.32 5 20161 62291 34874474
Mycobacterium chelonae infection 21.05 14.32 10 20156 805 34935960
Posterior reversible encephalopathy syndrome 20.55 14.32 27 20139 9927 34926838
Hyperhidrosis 20.48 14.32 9 20157 75683 34861082
Hepatitis B 20.38 14.32 21 20145 5962 34930803
Ureteric stenosis 20.33 14.32 11 20155 1165 34935600
Wound dehiscence 19.92 14.32 16 20150 3295 34933470
Viraemia 19.80 14.32 11 20155 1227 34935538
Encephalitis eastern equine 19.38 14.32 3 20163 0 34936765
Rash 19.30 14.32 65 20101 222687 34714078
Periorbital infection 19.25 14.32 6 20160 151 34936614
Spirochaetal infection 19.21 14.32 4 20162 17 34936748
Toxoplasmosis 19.17 14.32 11 20155 1305 34935460
Splenic neoplasm malignancy unspecified 19.03 14.32 4 20162 18 34936747
Nail discolouration 19.00 14.32 10 20156 1001 34935764
Escherichia urinary tract infection 18.96 14.32 16 20150 3530 34933235
Histology abnormal 18.94 14.32 7 20159 299 34936466
Alveolitis 18.84 14.32 12 20154 1718 34935047
Cytomegalovirus oesophagitis 18.78 14.32 8 20158 498 34936267
Atypical haemolytic uraemic syndrome 18.53 14.32 7 20159 318 34936447
Lip haemorrhage 18.52 14.32 9 20157 761 34936004
Varicella zoster virus infection 18.37 14.32 12 20154 1794 34934971
Perinephric collection 18.35 14.32 6 20160 177 34936588
Acne 18.33 14.32 27 20139 11039 34925726
Livedo reticularis 18.26 14.32 13 20153 2236 34934529
Dyspnoea 18.23 14.32 135 20031 376647 34560118
Kaposi sarcoma inflammatory cytokine syndrome 18.21 14.32 4 20162 23 34936742
Pulmonary toxicity 18.15 14.32 20 20146 6127 34930638
Joint swelling 18.07 14.32 6 20160 59884 34876881
Cytomegalovirus colitis 17.92 14.32 14 20152 2770 34933995
Aphthous ulcer 17.86 14.32 18 20148 4977 34931788
Normocytic anaemia 17.78 14.32 13 20153 2331 34934434
Osmotic demyelination syndrome 17.63 14.32 9 20157 846 34935919
Parvovirus B19 infection 17.63 14.32 9 20157 846 34935919
Pericarditis constrictive 17.63 14.32 7 20159 364 34936401
Hypertriglyceridaemia 17.57 14.32 23 20143 8425 34928340
Pneumonia pseudomonal 17.57 14.32 16 20150 3906 34932859
Inferior vena cava stenosis 17.53 14.32 4 20162 28 34936737
Pneumonitis 17.49 14.32 51 20115 33827 34902938
Pseudomonas infection 17.40 14.32 28 20138 12354 34924411
Pain in extremity 17.27 14.32 29 20137 126484 34810281
Cerebellar stroke 17.21 14.32 6 20160 216 34936549
SARS-CoV-2 RNA 17.18 14.32 4 20162 31 34936734
Bacterial sepsis 17.12 14.32 18 20148 5232 34931533
Candida infection 17.10 14.32 34 20132 17681 34919084
Alternaria infection 17.07 14.32 7 20159 396 34936369
Macroglossia 16.94 14.32 7 20159 404 34936361
Septic shock 16.84 14.32 84 20082 71750 34865015
Skin erosion 16.81 14.32 12 20154 2073 34934692
Staphylococcal infection 16.61 14.32 49 20117 32711 34904054
Chronic obstructive pulmonary disease 16.42 14.32 4 20162 48914 34887851
Overdose 16.38 14.32 17 20149 91042 34845723
Reticulocyte count decreased 16.32 14.32 8 20158 690 34936075
Peritoneal hernia 16.08 14.32 3 20163 6 34936759
Product administered to patient of inappropriate age 15.87 14.32 14 20152 3277 34933488
Haemorrhagic pneumonia 15.85 14.32 5 20161 131 34936634
Human polyomavirus infection 15.83 14.32 8 20158 736 34936029
Blood pressure decreased 15.82 14.32 5 20161 51510 34885255
Stomatitis 15.62 14.32 57 20109 42457 34894308
Herpes virus infection 15.56 14.32 13 20153 2829 34933936
Red blood cell burr cells present 15.53 14.32 4 20162 49 34936716
Confusional state 15.45 14.32 38 20128 144122 34792643
Musculoskeletal stiffness 15.31 14.32 4 20162 46676 34890089
Paraesthesia 15.31 14.32 9 20157 64163 34872602
Anuria 15.31 14.32 24 20142 10361 34926404
Osteomyelitis chronic 15.24 14.32 6 20160 305 34936460
Ovarian cyst 15.22 14.32 3 20163 9 34936756
Urinary tract infection neonatal 15.22 14.32 3 20163 9 34936756
Cryptococcosis 15.22 14.32 12 20154 2407 34934358
Enterobacter infection 15.17 14.32 12 20154 2418 34934347
Hepatic neoplasm 15.07 14.32 11 20155 1966 34934799
Fusarium infection 15.06 14.32 9 20157 1151 34935614
Viral haemorrhagic cystitis 14.92 14.32 9 20157 1171 34935594
Necrotising retinitis 14.90 14.32 8 20158 834 34935931
Myocarditis toxoplasmal 14.78 14.32 4 20162 60 34936705
Metastatic malignant melanoma 14.69 14.32 11 20155 2044 34934721
Wheezing 14.67 14.32 3 20163 41399 34895366
Pelvic fluid collection 14.67 14.32 5 20161 168 34936597
Rabies 14.55 14.32 3 20163 12 34936753
Urticaria 14.53 14.32 9 20157 62368 34874397
Anogenital warts 14.43 14.32 7 20159 590 34936175
Immunosuppressant drug level decreased 14.41 14.32 9 20157 1245 34935520

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
Transplant rejection 2160.01 14.69 641 33384 18796 79691567
Transplant dysfunction 1899.21 14.69 470 33555 6751 79703612
Ovarian cyst 1338.39 14.69 402 33623 12253 79698110
Acne 1141.26 14.69 431 33594 26759 79683604
Product use in unapproved indication 577.48 14.69 618 33407 249741 79460622
Off label use 527.21 14.69 1176 32849 906039 78804324
Alopecia 357.92 14.69 466 33559 230889 79479474
Kidney transplant rejection 353.43 14.69 141 33884 10105 79700258
Epstein-Barr virus infection 335.56 14.69 150 33875 14266 79696097
Post transplant lymphoproliferative disorder 324.70 14.69 137 33888 11327 79699036
Thrombotic microangiopathy 299.14 14.69 154 33871 20015 79690348
Adenovirus infection 259.57 14.69 107 33918 8340 79702023
Acute graft versus host disease 243.69 14.69 108 33917 10059 79700304
Cytomegalovirus infection 235.17 14.69 173 33852 42471 79667892
Immunosuppressant drug level increased 229.66 14.69 100 33925 8927 79701436
Sleep disorder due to general medical condition, insomnia type 220.79 14.69 168 33857 43388 79666975
Product use issue 193.52 14.69 332 33693 209490 79500873
BK virus infection 174.67 14.69 82 33943 8722 79701641
Polyomavirus-associated nephropathy 171.94 14.69 71 33954 5556 79704807
Liver function test abnormal 161.97 14.69 167 33858 64308 79646055
Cytomegalovirus infection reactivation 160.14 14.69 77 33948 8639 79701724
Graft versus host disease in skin 153.57 14.69 67 33958 6006 79704357
Transplant failure 146.70 14.69 60 33965 4581 79705782
Nephropathy toxic 145.60 14.69 97 33928 20322 79690041
Chronic allograft nephropathy 145.35 14.69 46 33979 1665 79708698
Graft versus host disease in gastrointestinal tract 144.26 14.69 65 33960 6291 79704072
Chronic graft versus host disease 130.96 14.69 62 33963 6719 79703644
Graft versus host disease 130.94 14.69 81 33944 14945 79695418
Smooth muscle cell neoplasm 129.98 14.69 37 33988 925 79709438
Liver transplant rejection 127.13 14.69 49 33976 3199 79707164
Human herpesvirus 6 infection 115.81 14.69 53 33972 5317 79705046
Squamous cell carcinoma 106.07 14.69 72 33953 15550 79694813
Arthralgia 103.16 14.69 58 33967 571745 79138618
Blood creatinine increased 96.72 14.69 208 33817 154849 79555514
Multiple organ dysfunction syndrome 96.22 14.69 179 33846 120067 79590296
Renal impairment 93.12 14.69 207 33818 157576 79552787
Acute graft versus host disease in skin 92.44 14.69 51 33974 7607 79702756
Nocardiosis 86.01 14.69 44 33981 5635 79704728
Cytomegalovirus viraemia 84.45 14.69 58 33967 12763 79697600
Skin squamous cell carcinoma metastatic 84.34 14.69 16 34009 55 79710308
Fatigue 83.40 14.69 170 33855 929557 78780806
Alveolar proteinosis 83.04 14.69 25 34000 764 79709599
Dizziness 81.92 14.69 63 33962 526378 79183985
Complications of transplanted kidney 81.28 14.69 44 33981 6322 79704041
Proteinuria 77.66 14.69 82 33943 32420 79677943
Pneumonia 77.60 14.69 514 33511 659732 79050631
Epstein-Barr virus associated lymphoproliferative disorder 76.61 14.69 35 33990 3497 79706866
Drug level increased 75.76 14.69 89 33936 39562 79670801
Lymphocele 75.34 14.69 28 33997 1653 79708710
Fall 75.03 14.69 59 33966 487570 79222793
Joint swelling 74.67 14.69 16 34009 288630 79421733
Heart transplant rejection 74.51 14.69 27 33998 1483 79708880
Drug interaction 71.50 14.69 358 33667 414825 79295538
Mouth ulceration 71.40 14.69 85 33940 38309 79672054
Squamous cell carcinoma of skin 70.78 14.69 54 33971 13979 79696384
Kidney fibrosis 70.35 14.69 33 33992 3502 79706861
Chronic graft versus host disease in skin 66.11 14.69 25 34000 1549 79708814
Posterior reversible encephalopathy syndrome 65.82 14.69 68 33957 26213 79684150
Infusion related reaction 65.50 14.69 10 34015 230227 79480136
Rash 65.35 14.69 91 33934 578267 79132096
Bronchopulmonary aspergillosis 63.78 14.69 62 33963 22232 79688131
Constipation 63.18 14.69 21 34004 283029 79427334
Human herpesvirus 8 infection 60.89 14.69 22 34003 1198 79709165
Drug ineffective for unapproved indication 60.71 14.69 91 33934 51147 79659216
Hypertriglyceridaemia 59.85 14.69 47 33978 12693 79697670
JC virus infection 58.57 14.69 30 33995 3851 79706512
Epidermodysplasia verruciformis 57.64 14.69 16 34009 364 79709999
Acute graft versus host disease in intestine 57.43 14.69 30 33995 4011 79706352
Pneumatosis intestinalis 57.04 14.69 35 33990 6362 79704001
MELAS syndrome 56.95 14.69 14 34011 194 79710169
Skin squamous cell carcinoma recurrent 56.88 14.69 11 34014 43 79710320
Interstitial lung disease 56.83 14.69 139 33886 112461 79597902
Plasmablastic lymphoma 56.76 14.69 17 34008 510 79709853
Nausea 56.67 14.69 214 33811 956982 78753381
Hypersensitivity 55.88 14.69 21 34004 262218 79448145
Propionibacterium infection 55.31 14.69 15 34010 312 79710051
Renal tubular atrophy 55.28 14.69 23 34002 1833 79708530
Pruritus 54.32 14.69 53 33972 394595 79315768
Back pain 53.12 14.69 32 33993 304148 79406215
Pseudomonas infection 52.19 14.69 54 33971 20849 79689514
Pain in extremity 51.28 14.69 48 33977 364490 79345873
Septic shock 51.09 14.69 141 33884 122660 79587703
Focal segmental glomerulosclerosis 51.07 14.69 26 33999 3295 79707068
Haemolytic uraemic syndrome 49.26 14.69 28 33997 4421 79705942
Syncope 48.37 14.69 9 34016 179440 79530923
Somnolence 47.88 14.69 21 34004 238960 79471403
Renal tubular necrosis 47.49 14.69 56 33969 24983 79685380
Cryptosporidiosis infection 47.06 14.69 16 34009 727 79709636
Therapeutic product effect decreased 46.87 14.69 7 34018 163856 79546507
Pneumocystis jirovecii pneumonia 46.25 14.69 63 33962 32445 79677918
Arthropathy 45.41 14.69 10 34015 177101 79533262
Dyspnoea 45.40 14.69 200 33825 856825 78853538
Transitional cell carcinoma 45.32 14.69 22 34003 2519 79707844
Anxiety 45.01 14.69 25 34000 248487 79461876
Pericardial effusion 44.93 14.69 75 33950 46162 79664201
Respiratory failure 44.75 14.69 174 33851 180737 79529626
Renal-limited thrombotic microangiopathy 44.70 14.69 11 34014 153 79710210
Staphylococcal mediastinitis 44.09 14.69 9 34016 49 79710314
Meningitis viral 44.06 14.69 20 34005 1968 79708395
Varicella zoster virus infection 44.00 14.69 26 33999 4415 79705948
Pneumonia cytomegaloviral 43.83 14.69 27 33998 4942 79705421
Aspergillus infection 43.40 14.69 47 33978 19114 79691249
Condition aggravated 43.28 14.69 363 33662 500761 79209602
Hypotension 42.37 14.69 77 33948 440240 79270123
Varicella 42.33 14.69 22 34003 2910 79707453
Epstein-Barr viraemia 42.08 14.69 20 34005 2185 79708178
Pancreas transplant rejection 41.67 14.69 12 34013 313 79710050
Cow pox 41.63 14.69 8 34017 30 79710333
Drug effective for unapproved indication 41.55 14.69 28 33997 5973 79704390
Brain abscess 41.46 14.69 26 33999 4910 79705453
Scleroderma 41.27 14.69 27 33998 5483 79704880
Drug level decreased 41.09 14.69 40 33985 14362 79696001
Hyperlipidaemia 40.86 14.69 53 33972 26040 79684323
Escherichia infection 40.47 14.69 44 33981 17973 79692390
Drug hypersensitivity 40.12 14.69 41 33984 298875 79411488
Graft versus host disease in liver 40.00 14.69 18 34007 1736 79708627
Klebsiella infection 39.95 14.69 41 33984 15679 79694684
Venoocclusive liver disease 39.94 14.69 36 33989 11735 79698628
Insomnia 39.79 14.69 28 33997 245142 79465221
Sinusitis 39.44 14.69 17 34008 195484 79514879
Diaphragmatic hernia 39.30 14.69 12 34013 385 79709978
Urticaria 39.16 14.69 15 34010 185186 79525177
Herpes zoster meningoencephalitis 39.02 14.69 14 34011 747 79709616
Musculoskeletal stiffness 39.00 14.69 13 34012 174995 79535368
Muscle spasms 38.90 14.69 13 34012 174717 79535646
Maternal exposure during pregnancy 38.66 14.69 6 34019 136532 79573831
Venoocclusive disease 38.19 14.69 24 34001 4549 79705814
Malignant fibrous histiocytoma 37.38 14.69 10 34015 197 79710166
Haemodialysis 36.74 14.69 42 33983 18126 79692237
Drug resistance 36.46 14.69 65 33960 42148 79668215
Diarrhoea haemorrhagic 36.35 14.69 36 33989 13198 79697165
Injection site pain 36.10 14.69 6 34019 129832 79580531
Asthma 35.92 14.69 7 34018 135088 79575275
Mobility decreased 35.44 14.69 5 34020 122170 79588193
Acute graft versus host disease in liver 35.25 14.69 17 34008 1918 79708445
Diffuse large B-cell lymphoma 35.15 14.69 34 33991 12115 79698248
Blood triglycerides increased 34.93 14.69 44 33981 20996 79689367
Immunosuppressant drug level decreased 34.69 14.69 17 34008 1987 79708376
Drug ineffective 34.43 14.69 649 33376 1080264 78630099
Viraemia 34.33 14.69 19 34006 2850 79707513
Avian influenza 34.32 14.69 8 34017 87 79710276
Retinal scar 34.27 14.69 11 34014 417 79709946
Hyperhidrosis 34.20 14.69 11 34014 151481 79558882
Pneumonitis 33.80 14.69 78 33947 60782 79649581
Malacoplakia 33.74 14.69 12 34013 624 79709739
Wheezing 33.32 14.69 5 34020 116659 79593704
Chronic graft versus host disease in liver 33.19 14.69 12 34013 655 79709708
Rheumatoid arthritis 33.17 14.69 176 33849 208294 79502069
Tularaemia 32.94 14.69 8 34017 105 79710258
Gastroenteritis norovirus 32.92 14.69 19 34006 3087 79707276
Abdominal wall abscess 32.80 14.69 14 34011 1189 79709174
Protothecosis 32.79 14.69 7 34018 49 79710314
Lung transplant rejection 32.66 14.69 15 34010 1516 79708847
Dyspepsia 32.60 14.69 4 34021 108683 79601680
Malaise 32.58 14.69 104 33921 489765 79220598
Central nervous system lymphoma 32.55 14.69 17 34008 2272 79708091
Neurofibrosarcoma 32.00 14.69 9 34016 215 79710148
Weight increased 31.90 14.69 43 33982 277343 79433020
Drug level below therapeutic 31.43 14.69 29 33996 9741 79700622
Nephrogenic diabetes insipidus 30.78 14.69 16 34009 2118 79708245
Glossodynia 30.52 14.69 4 34021 103333 79607030
Cytomegalovirus colitis 30.39 14.69 21 34004 4664 79705699
Bradycardia 30.32 14.69 10 34015 135547 79574816
Confusional state 30.22 14.69 56 33969 317941 79392422
Blister 30.11 14.69 7 34018 119469 79590894
Depression 29.92 14.69 29 33996 216761 79493602
Contusion 29.90 14.69 13 34012 148763 79561600
Swelling 29.90 14.69 29 33996 216682 79493681
Morphoea 29.74 14.69 10 34015 439 79709924
Renal tubular injury 29.67 14.69 14 34011 1505 79708858
Inappropriate schedule of product administration 29.64 14.69 10 34015 133618 79576745
Right ventricular diastolic collapse 29.64 14.69 7 34018 81 79710282
Cytomegalovirus chorioretinitis 29.63 14.69 22 34003 5468 79704895
Reticulocyte count decreased 29.51 14.69 12 34013 902 79709461
Pulmonary alveolar haemorrhage 29.33 14.69 30 33995 11427 79698936
Globulins decreased 29.28 14.69 10 34015 461 79709902
Feeling abnormal 28.83 14.69 16 34009 159183 79551180
Alopecia scarring 28.41 14.69 7 34018 98 79710265
Gait disturbance 28.36 14.69 28 33997 207478 79502885
Drug intolerance 28.34 14.69 43 33982 264076 79446287
Rhinovirus infection 28.33 14.69 25 34000 7928 79702435
Loss of personal independence in daily activities 28.12 14.69 102 33923 102478 79607885
Polyomavirus viraemia 28.12 14.69 14 34011 1693 79708670
Obliterative bronchiolitis 28.11 14.69 17 34008 3011 79707352
Hypogammaglobulinaemia 28.00 14.69 31 33994 12920 79697443
Incorrect route of product administration 27.91 14.69 52 33973 34877 79675486
Musculoskeletal pain 27.86 14.69 5 34020 102349 79608014
Trichodysplasia spinulosa 27.65 14.69 11 34014 781 79709582
Adjusted calcium decreased 27.48 14.69 8 34017 217 79710146
Trichostasis spinulosa 27.40 14.69 5 34020 13 79710350
Human polyomavirus infection 27.31 14.69 12 34013 1094 79709269
Pleocytosis 27.30 14.69 13 34012 1426 79708937
PIK3CA related overgrowth spectrum 27.04 14.69 4 34021 0 79710363
Wound 27.01 14.69 8 34017 116171 79594192
Headache 26.98 14.69 166 33859 653606 79056757
Scedosporium infection 26.97 14.69 13 34012 1465 79708898
Abdominal pain upper 26.44 14.69 34 33991 223785 79486578
Bacillary angiomatosis 26.37 14.69 8 34017 251 79710112
Pleural effusion 26.15 14.69 127 33898 145135 79565228
Hypoaesthesia 25.92 14.69 23 34002 179329 79531034
Bacterial sepsis 25.73 14.69 24 34001 8174 79702189
Neuroendocrine carcinoma of the skin 25.34 14.69 12 34013 1300 79709063
Anaphylactic reaction 25.32 14.69 3 34022 83740 79626623
Therapy partial responder 25.17 14.69 34 33991 17363 79693000
Blastomycosis 25.15 14.69 10 34015 709 79709654
Mucormycosis 25.06 14.69 24 34001 8445 79701918
Paraesthesia 25.02 14.69 23 34002 176300 79534063
Stem cell transplant 24.97 14.69 17 34008 3687 79706676
Loss of consciousness 24.92 14.69 21 34004 167922 79542441
Arthritis 24.79 14.69 9 34016 114871 79595492
Stomatitis 24.78 14.69 126 33899 146631 79563732
Philadelphia positive chronic myeloid leukaemia 24.70 14.69 7 34018 172 79710191
Biopsy kidney abnormal 24.40 14.69 7 34018 180 79710183
Acute kidney injury 24.40 14.69 333 33692 519071 79191292
Drug level fluctuating 24.37 14.69 10 34015 769 79709594
Skin graft rejection 24.23 14.69 5 34020 29 79710334
Escherichia bacteraemia 24.12 14.69 21 34004 6541 79703822
Renal graft infection 24.06 14.69 9 34016 541 79709822
Chest pain 24.01 14.69 53 33972 282251 79428112
Glomerulosclerosis 23.96 14.69 11 34014 1111 79709252
Babesiosis 23.71 14.69 8 34017 355 79710008
Perinephric collection 23.58 14.69 8 34017 361 79710002
Hydronephrosis 23.58 14.69 33 33992 17421 79692942
Lower respiratory tract infection 23.38 14.69 13 34012 129207 79581156
Bacterial colitis 23.37 14.69 6 34019 100 79710263
Pulmonary haemorrhage 23.21 14.69 30 33995 14687 79695676
Injection site erythema 23.15 14.69 3 34022 78194 79632169
Herpes simplex 22.68 14.69 27 33998 12160 79698203
Periorbital infection 22.63 14.69 6 34019 114 79710249
Dry mouth 22.49 14.69 5 34020 88014 79622349
Diabetes mellitus 22.38 14.69 79 33946 78311 79632052
Product dose omission issue 22.28 14.69 45 33980 247492 79462871
Osteoarthritis 22.23 14.69 5 34020 87304 79623059
Abdominal discomfort 22.21 14.69 46 33979 250681 79459682
Ophthalmic herpes zoster 22.20 14.69 14 34011 2670 79707693
Toxoplasmosis 22.13 14.69 14 34011 2683 79707680
Blood pressure increased 22.10 14.69 35 33990 211325 79499038
Hyponatraemia 22.07 14.69 26 33999 177822 79532541
Heart rate increased 22.05 14.69 12 34013 120712 79589651
Enteritis 21.87 14.69 29 33996 14554 79695809
Dysplasia 21.75 14.69 11 34014 1375 79708988
Ureteric stenosis 21.70 14.69 11 34014 1381 79708982
Vomiting 21.66 14.69 181 33844 665647 79044716
Cystitis viral 21.61 14.69 9 34016 719 79709644
Metastases to lung 21.14 14.69 32 33993 18131 79692232
Psoriasis 21.13 14.69 6 34019 89581 79620782
Renal transplant failure 21.11 14.69 12 34013 1895 79708468
Product administered to patient of inappropriate age 20.87 14.69 18 34007 5535 79704828
Haemophagocytic lymphohistiocytosis 20.65 14.69 35 33990 21802 79688561
Pneumonia haemophilus 20.46 14.69 10 34015 1162 79709201
Salivary gland mass 20.42 14.69 5 34020 68 79710295
Peripheral swelling 20.25 14.69 54 33971 269563 79440800
Spirochaetal infection 20.23 14.69 4 34021 18 79710345
Lymphopenia 20.18 14.69 42 33983 30515 79679848
Exposure during pregnancy 20.06 14.69 9 34016 101123 79609240
Asthenia 20.02 14.69 132 33893 511557 79198806
Pulmonary cavitation 19.91 14.69 11 34014 1645 79708718
Hepatitis B 19.86 14.69 21 34004 8311 79702052
Disease recurrence 19.69 14.69 52 33973 44057 79666306
Chronic obstructive pulmonary disease 19.64 14.69 6 34019 85413 79624950
Jejunal perforation 19.59 14.69 7 34018 369 79709994
Discomfort 19.52 14.69 15 34010 125602 79584761
Kaposi sarcoma inflammatory cytokine syndrome 19.41 14.69 4 34021 23 79710340
Disseminated varicella zoster virus infection 19.38 14.69 8 34017 625 79709738
Adenovirus reactivation 19.36 14.69 7 34018 382 79709981
Balance disorder 19.29 14.69 9 34016 98848 79611515
Pneumocystis jirovecii infection 18.84 14.69 13 34012 2881 79707482
Clostridium difficile infection 18.72 14.69 50 33975 42635 79667728
Skin mass 18.65 14.69 20 34005 8043 79702320
Lymphangioma 18.61 14.69 4 34021 29 79710334
Respiratory distress 18.59 14.69 61 33964 58278 79652085
Graft loss 18.51 14.69 9 34016 1034 79709329
Chest discomfort 18.43 14.69 19 34006 138025 79572338
SARS-CoV-2 RNA 18.38 14.69 4 34021 31 79710332
Graft thrombosis 18.37 14.69 7 34018 443 79709920
Pulmonary toxicity 18.32 14.69 25 34000 12889 79697474
Encephalitis eastern equine 18.20 14.69 3 34022 3 79710360
Lung infiltration 18.16 14.69 34 33991 22878 79687485
Fibrosarcoma 18.16 14.69 4 34021 33 79710330
Cardio-respiratory arrest 18.11 14.69 12 34013 108498 79601865
Hepatic angiosarcoma 18.05 14.69 4 34021 34 79710329
Cytomegalovirus oesophagitis 17.97 14.69 8 34017 752 79709611
Pneumonia pseudomonal 17.96 14.69 17 34008 5894 79704469
Microangiopathic haemolytic anaemia 17.96 14.69 10 34015 1517 79708846
Ileal ulcer 17.82 14.69 9 34016 1121 79709242
Memory impairment 17.80 14.69 13 34012 111721 79598642
Staphylococcal infection 17.73 14.69 60 33965 58235 79652128
Actinic keratosis 17.65 14.69 17 34008 6025 79704338
Lymphoedema 17.57 14.69 24 34001 12389 79697974
Cardiac murmur functional 17.56 14.69 4 34021 39 79710324
Intussusception 17.53 14.69 9 34016 1161 79709202
Bladder transitional cell carcinoma 17.48 14.69 12 34013 2638 79707725
Chronic kidney disease 17.47 14.69 65 33960 66089 79644274
Thymus enlargement 17.45 14.69 5 34020 128 79710235
Bronchitis 17.42 14.69 18 34007 130626 79579737
Aplasia pure red cell 17.41 14.69 19 34006 7791 79702572
Graft ischaemia 17.38 14.69 4 34021 41 79710322
Therapeutic product effect incomplete 17.26 14.69 21 34004 141624 79568739
Urine protein/creatinine ratio increased 17.08 14.69 9 34016 1225 79709138
Renal vessel disorder 16.91 14.69 6 34019 310 79710053
Livedo reticularis 16.86 14.69 14 34011 4089 79706274
Papilloma viral infection 16.78 14.69 10 34015 1724 79708639
Nasopharyngitis 16.78 14.69 54 33971 253827 79456536
Gastrooesophageal reflux disease 16.77 14.69 12 34013 104234 79606129
Viral oesophagitis 16.67 14.69 3 34022 7 79710356
Splenic neoplasm malignancy unspecified 16.51 14.69 4 34021 52 79710311
Adverse drug reaction 16.51 14.69 4 34021 66388 79643975
Pterygium 16.46 14.69 6 34019 335 79710028
Renal failure 16.45 14.69 144 33881 200824 79509539
Inferior vena cava stenosis 16.44 14.69 4 34021 53 79710310
Suicidal ideation 16.43 14.69 6 34019 76334 79634029
Post transplant distal limb syndrome 16.42 14.69 7 34018 593 79709770
Opportunistic infection 16.32 14.69 12 34013 2938 79707425
Palpitations 16.26 14.69 18 34007 126592 79583771
Red blood cell burr cells present 16.23 14.69 4 34021 56 79710307
Decreased appetite 16.23 14.69 83 33942 342335 79368028
Jarisch-Herxheimer reaction 16.21 14.69 8 34017 949 79709414
Hepatitis E 16.19 14.69 12 34013 2974 79707389
Acquired mitochondrial DNA mutation 16.13 14.69 3 34022 9 79710354
Complications of transplanted heart 15.99 14.69 6 34019 364 79709999
ABO incompatibility 15.89 14.69 3 34022 10 79710353
Endocarditis 15.78 14.69 21 34004 10576 79699787
Depressed level of consciousness 15.72 14.69 11 34014 96641 79613722
Myocarditis toxoplasmal 15.68 14.69 4 34021 65 79710298
Alternaria infection 15.55 14.69 7 34018 675 79709688
Parvovirus B19 infection 15.55 14.69 9 34016 1471 79708892
Cat scratch disease 15.52 14.69 6 34019 395 79709968
Pyrexia 15.24 14.69 388 33637 678321 79032042
Injury 15.21 14.69 7 34018 77489 79632874
Kussmaul respiration 15.15 14.69 6 34019 421 79709942
Orbital apex syndrome 15.14 14.69 4 34021 75 79710288
COVID-19 15.06 14.69 117 33908 157557 79552806
Cachexia 15.04 14.69 21 34004 11062 79699301
Disseminated mycobacterium avium complex infection 15.04 14.69 5 34020 212 79710151
Hallucination 14.98 14.69 9 34016 85736 79624627
HIV infection 14.98 14.69 8 34017 1119 79709244
Incorrect dose administered 14.92 14.69 7 34018 76623 79633740
Blood pressure systolic increased 14.87 14.69 5 34020 66981 79643382
Acute hepatitis C 14.86 14.69 5 34020 220 79710143
Kaposi's sarcoma 14.84 14.69 7 34018 752 79709611
Rabies 14.75 14.69 3 34022 16 79710347
Acinetobacter infection 14.70 14.69 11 34014 2766 79707597

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EG04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Mammalian target of rapamycin (mTOR) kinase inhibitors
ATC L04AA10 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
ATC S01XA23 SENSORY ORGANS
OPHTHALMOLOGICALS
OTHER OPHTHALMOLOGICALS
Other ophthalmologicals
FDA MoA N0000175076 Protein Kinase Inhibitors
FDA PE N0000175550 Decreased Immunologic Activity
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:35705 immunosuppressive agents
CHEBI has role CHEBI:36047 antibacterial drugs
CHEBI has role CHEBI:68481 mTOR inhibitors
CHEBI has role CHEBI:149553 anticoronaviral drug
CHEBI has role CHEBI:176497 geroprotectors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000175624 mTOR Inhibitors
FDA EPC N0000175625 mTOR Inhibitor Immunosuppressant
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000903 Antibiotics, Antineoplastic
MeSH PA D000935 Antifungal Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents

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

DiseaseRelationSNOMED_IDDOID
Gorham's disease indication 1515008
Tuberous sclerosis syndrome indication 7199000 DOID:13515
Lymphangiectasis indication 48087001
Pulmonary lymphangioleiomyomatosis indication 277844007 DOID:3319
Lymphangioma indication 400178008 DOID:1475
Lymphangiomatosis indication 403546006
Renal cell carcinoma indication 702391001 DOID:4450
Prevention of Kidney Transplant Rejection indication
Coronavirus infection off-label use 186747009
Prevention of Cardiac Transplant Rejection off-label use
Hypercholesterolemia contraindication 13644009
Hyperbilirubinemia contraindication 14783006 DOID:2741
Transplantation of liver contraindication 18027006
Progressive multifocal leukoencephalopathy contraindication 22255007 DOID:643
Cytomegalovirus infection contraindication 28944009
Proteinuria contraindication 29738008 DOID:576
Hypertensive disorder contraindication 38341003 DOID:10763
Infectious disease contraindication 40733004
Body fluid retention contraindication 43498006
Gastrointestinal perforation contraindication 51875005
Hyperlipidemia contraindication 55822004 DOID:1168
Acute infectious disease contraindication 63171007
Interstitial pneumonia contraindication 64667001
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Transplant of lung contraindication 88039007
Kidney disease contraindication 90708001 DOID:557
Secondary malignant neoplasm of cerebrum contraindication 94248000
Malignant lymphoma contraindication 118600007 DOID:0060058
Perioperative care contraindication 133897009
Cerebrovascular accident contraindication 230690007
Interstitial lung disease contraindication 233703007 DOID:3082
Lymphedema contraindication 234097001 DOID:4977
Disease of liver contraindication 235856003 DOID:409
Impaired wound healing contraindication 271618001
Peripheral edema contraindication 271809000
Pregnancy, function contraindication 289908002
Hypertriglyceridemia contraindication 302870006
Primary malignant neoplasm contraindication 372087000
Malignant neoplasm of skin contraindication 372130007 DOID:4159
Pericardial effusion contraindication 373945007 DOID:118
Surgical procedure contraindication 387713003
Ascites contraindication 389026000
Breastfeeding (mother) contraindication 413712001
Pneumocystosis jiroveci pneumonia contraindication 415125002 DOID:11339
Malignant neoplasm of brain contraindication 428061005 DOID:1319
Bronchial Anastomotic Dehiscence in Lung Transplant contraindication
Pleural Effusions contraindication
Sirolimus Toxicity contraindication
Hepatic Artery Thrombosis in Liver Transplant contraindication
BK Polyomavirus Reactivation Nephropathy contraindication




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.5 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG/VIAL FYARRO AADI N213312 Nov. 22, 2021 RX POWDER INTRAVENOUS 8911786 Feb. 14, 2029 TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED UNRESECTABLE OR METASTATIC MALIGNANT PERIVASCULAR EPITHELIOID CELL TUMOR (PECOMA)
100MG/VIAL FYARRO AADI N213312 Nov. 22, 2021 RX POWDER INTRAVENOUS 10973806 June 29, 2036 TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED UNRESECTABLE OR METASTATIC MALIGNANT PERIVASCULAR EPITHELIOID CELL TUMOR (PECOMA) WITH A DOSE BETWEEN ABOUT 56 MG/M2 AND ABOUT 100 MG/M2 ADMINISTERED ON DAYS 1 AND 8 OF A 21-DAY CYCLE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG/VIAL FYARRO AADI N213312 Nov. 22, 2021 RX POWDER INTRAVENOUS Nov. 22, 2024 NEW PRODUCT
0.2% HYFTOR NOBELPHARMA N213478 March 22, 2022 RX GEL TOPICAL March 22, 2025 NEW PRODUCT
100MG/VIAL FYARRO AADI N213312 Nov. 22, 2021 RX POWDER INTRAVENOUS Nov. 22, 2028 FOR THE TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED UNRESECTABLE OR METASTATIC MALIGNANT PERIVASCULAR EPITHELIOID CELL TUMOR (PECOMA)
0.2% HYFTOR NOBELPHARMA N213478 March 22, 2022 RX GEL TOPICAL March 22, 2029 TREATMENT OF FACIAL ANGIOFIBROMA ASSOCIATED WITH TUBEROUS SCLEROSIS IN ADULTS AND PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Peptidyl-prolyl cis-trans isomerase FKBP1A Enzyme INHIBITOR Kd 8.96 WOMBAT-PK CHEMBL
Cytochrome P450 3A4 Enzyme IC50 5.70 DRUG MATRIX
Multidrug resistance protein 1 Transporter IC50 6.20 WOMBAT-PK
ATP-binding cassette sub-family G member 2 Transporter IC50 5.72 CHEMBL
Cytochrome P450 2C9 Enzyme IC50 5.70 DRUG MATRIX
Serine/threonine-protein kinase mTOR Kinase IC50 10 CHEMBL
Peptidyl-prolyl cis-trans isomerase FKBP3 Enzyme Kd 9.70 WOMBAT-PK
Cytochrome P450 2C19 Enzyme IC50 5.40 DRUG MATRIX
Peptidyl-prolyl cis-trans isomerase FKBP1B Enzyme Kd 9.70 CHEMBL
Peptidyl-prolyl cis-trans isomerase FKBP5 Enzyme Ki 8.52 CHEMBL
Programmed cell death protein 4 Nuclear other EC50 7.30 CHEMBL
Eukaryotic translation initiation factor 4E Nuclear other Kd 9.30 CHEMBL
Sodium/nucleoside cotransporter 1 Transporter Ki 6.43 DRUG MATRIX
Peptidyl-prolyl cis-trans isomerase FKBP1A Enzyme IC50 9 CHEMBL
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 Enzyme IC50 4.11 CHEMBL
Serine/threonine-protein kinase mTOR Kinase IC50 10.30 CHEMBL

External reference:

IDSource
4021176 VUID
N0000148624 NUI
D00753 KEGG_DRUG
4021176 VANDF
C0072980 UMLSCUI
CHEBI:9168 CHEBI
CHEMBL413 ChEMBL_ID
D020123 MESH_DESCRIPTOR_UI
DB00877 DRUGBANK_ID
6031 IUPHAR_LIGAND_ID
7104 INN_ID
W36ZG6FT64 UNII
5284616 PUBCHEM_CID
258355 RXNORM
210889 MMSL
31418 MMSL
8303 MMSL
d04453 MMSL
007885 NDDF
116109004 SNOMEDCT_US
387014003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1030 SOLUTION 1 mg ORAL NDA 34 sections
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1030 SOLUTION 1 mg ORAL NDA 34 sections
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1030 SOLUTION 1 mg ORAL NDA 34 sections
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1040 TABLET, SUGAR COATED 0.50 mg ORAL NDA 34 sections
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1040 TABLET, SUGAR COATED 0.50 mg ORAL NDA 34 sections
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1040 TABLET, SUGAR COATED 0.50 mg ORAL NDA 34 sections
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1041 TABLET, SUGAR COATED 1 mg ORAL NDA 34 sections
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1041 TABLET, SUGAR COATED 1 mg ORAL NDA 34 sections
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1041 TABLET, SUGAR COATED 1 mg ORAL NDA 34 sections
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1042 TABLET, SUGAR COATED 2 mg ORAL NDA 34 sections
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1042 TABLET, SUGAR COATED 2 mg ORAL NDA 34 sections
Rapamune HUMAN PRESCRIPTION DRUG LABEL 1 0008-1042 TABLET, SUGAR COATED 2 mg ORAL NDA 34 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 0904-7147 TABLET, FILM COATED 1 mg ORAL ANDA 29 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 0904-7147 TABLET, FILM COATED 1 mg ORAL ANDA 29 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 0904-7248 TABLET 1 mg ORAL ANDA 29 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 13668-658 SOLUTION 1 mg ORAL ANDA 22 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 16714-187 TABLET, FILM COATED 0.50 mg ORAL ANDA 30 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 16714-187 TABLET, FILM COATED 0.50 mg ORAL ANDA 30 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 16714-188 TABLET, FILM COATED 1 mg ORAL ANDA 30 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 16714-188 TABLET, FILM COATED 1 mg ORAL ANDA 30 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 16714-189 TABLET, FILM COATED 2 mg ORAL ANDA 30 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 16714-189 TABLET, FILM COATED 2 mg ORAL ANDA 30 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 50268-718 TABLET 1 mg ORAL ANDA 29 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 55111-653 TABLET 1 mg ORAL ANDA 28 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 55111-653 TABLET 1 mg ORAL ANDA 28 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 55111-654 TABLET 2 mg ORAL ANDA 28 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 55111-654 TABLET 2 mg ORAL ANDA 28 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 59762-1001 TABLET, SUGAR COATED 0.50 mg ORAL NDA AUTHORIZED GENERIC 31 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 59762-1001 TABLET, SUGAR COATED 0.50 mg ORAL NDA AUTHORIZED GENERIC 31 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 59762-1002 TABLET, SUGAR COATED 1 mg ORAL NDA AUTHORIZED GENERIC 31 sections