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

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 2079.25 18.64 444 16159 4240 50584281
Transplant rejection 1987.91 18.64 489 16114 9120 50579401
Ovarian cyst 1441.24 18.64 410 16193 13586 50574935
Acne 1296.72 18.64 408 16195 19187 50569334
Alopecia 416.58 18.64 454 16149 244593 50343928
Sleep disorder due to general medical condition, insomnia type 306.22 18.64 166 16437 31281 50557240
Product use in unapproved indication 252.78 18.64 246 16357 115573 50472948
Liver function test abnormal 231.64 18.64 157 16446 44182 50544339
Epstein-Barr virus infection 213.70 18.64 82 16521 6915 50581606
Post transplant lymphoproliferative disorder 183.09 18.64 64 16539 4140 50584381
Kidney transplant rejection 182.52 18.64 63 16540 3924 50584597
Thrombotic microangiopathy 182.26 18.64 78 16525 8713 50579808
Off label use 137.90 18.64 403 16200 474023 50114498
Immunosuppressant drug level increased 119.32 18.64 43 16560 3039 50585482
Kidney fibrosis 117.02 18.64 36 16567 1553 50586968
Pneumonia 115.09 18.64 327 16276 378074 50210447
Product use issue 102.31 18.64 179 16424 149296 50439225
Smooth muscle cell neoplasm 99.38 18.64 27 16576 744 50587777
Condition aggravated 95.37 18.64 262 16341 296796 50291725
Chronic allograft nephropathy 88.94 18.64 24 16579 644 50587877
Epstein-Barr virus associated lymphoproliferative disorder 86.35 18.64 29 16574 1660 50586861
Cytomegalovirus infection 82.90 18.64 59 16544 17903 50570618
Graft versus host disease 81.44 18.64 40 16563 6126 50582395
Human herpesvirus 6 infection 81.19 18.64 31 16572 2575 50585946
Liver transplant rejection 77.03 18.64 25 16578 1285 50587236
Polyomavirus-associated nephropathy 76.79 18.64 26 16577 1526 50586995
Graft versus host disease in gastrointestinal tract 75.72 18.64 30 16573 2751 50585770
Acute graft versus host disease 71.87 18.64 32 16571 3926 50584595
Alveolar proteinosis 69.60 18.64 17 16586 303 50588218
Arthralgia 65.72 18.64 31 16572 438671 50149850
Loss of personal independence in daily activities 62.96 18.64 95 16508 69955 50518566
BK virus infection 61.14 18.64 26 16577 2855 50585666
Cryptosporidiosis infection 61.01 18.64 15 16588 275 50588246
Graft versus host disease in skin 60.73 18.64 25 16578 2531 50585990
Rheumatoid arthritis 59.32 18.64 173 16430 202377 50386144
Heart transplant rejection 58.98 18.64 16 16587 438 50588083
Renal graft infection 58.55 18.64 13 16590 149 50588372
JC virus infection 58.02 18.64 22 16581 1793 50586728
MELAS syndrome 56.58 18.64 12 16591 109 50588412
Fatigue 56.54 18.64 91 16512 707510 49881011
Incorrect route of product administration 54.96 18.64 47 16556 18619 50569902
Rash 54.05 18.64 39 16564 437432 50151089
Adenovirus infection 52.40 18.64 24 16579 3144 50585377
Hypertriglyceridaemia 50.64 18.64 28 16575 5463 50583058
Skin squamous cell carcinoma metastatic 48.86 18.64 8 16595 12 50588509
Renal impairment 47.05 18.64 87 16516 75574 50512947
Blood creatinine increased 46.64 18.64 87 16516 76073 50512448
Pseudomonas infection 45.88 18.64 32 16571 9398 50579123
Morphoea 45.78 18.64 12 16591 287 50588234
Joint swelling 45.78 18.64 12 16591 245274 50343247
Posterior reversible encephalopathy syndrome 44.79 18.64 38 16565 14890 50573631
Fall 43.81 18.64 28 16575 334904 50253617
Pneumocystis jirovecii pneumonia 43.32 18.64 37 16566 14626 50573895
Nephropathy toxic 43.22 18.64 29 16574 8000 50580521
Drug level below therapeutic 42.74 18.64 22 16581 3718 50584803
Lymphocele 42.08 18.64 14 16589 778 50587743
Hypersensitivity 41.16 18.64 10 16593 215151 50373370
Complications of transplanted kidney 40.84 18.64 18 16585 2155 50586366
Polyomavirus viraemia 40.51 18.64 12 16591 454 50588067
Avian influenza 39.44 18.64 8 16595 57 50588464
Globulins decreased 39.39 18.64 10 16593 210 50588311
Hypogammaglobulinaemia 39.14 18.64 24 16579 5675 50582846
Chronic graft versus host disease 39.06 18.64 19 16584 2848 50585673
Dizziness 38.81 18.64 34 16569 346335 50242186
Pancreas transplant rejection 38.68 18.64 9 16594 129 50588392
Pneumonitis 38.57 18.64 48 16555 29462 50559059
Drug interaction 38.36 18.64 148 16455 199473 50389048
Drug level increased 38.32 18.64 39 16564 19229 50569292
Neurofibrosarcoma 37.58 18.64 9 16594 147 50588374
Cytomegalovirus infection reactivation 37.55 18.64 18 16585 2613 50585908
Proteinuria 37.47 18.64 36 16567 16561 50571960
Immunosuppressant drug level decreased 36.86 18.64 13 16590 862 50587659
Multiple organ dysfunction syndrome 36.60 18.64 62 16541 50275 50538246
Dysplasia 35.86 18.64 12 16591 679 50587842
Lymphopenia 35.49 18.64 34 16569 15587 50572934
Focal segmental glomerulosclerosis 34.89 18.64 14 16589 1327 50587194
Somnolence 34.32 18.64 5 16598 154980 50433541
Adjusted calcium decreased 33.68 18.64 8 16595 126 50588395
Bacillary angiomatosis 32.40 18.64 7 16596 70 50588451
Pain in extremity 31.50 18.64 26 16577 272839 50315682
Septic shock 30.94 18.64 62 16541 57113 50531408
Respiratory failure 30.68 18.64 82 16521 91099 50497422
Feeling abnormal 30.36 18.64 3 16600 125489 50463032
Jejunal perforation 30.10 18.64 7 16596 100 50588421
Bronchiolitis obliterans syndrome 29.85 18.64 7 16596 104 50588417
Dyspnoea 29.83 18.64 87 16516 547521 50041000
Alopecia scarring 29.60 18.64 7 16596 108 50588413
Babesiosis 29.42 18.64 8 16595 221 50588300
Endocarditis Q fever 29.30 18.64 5 16598 11 50588510
Hepatitis E 29.13 18.64 12 16591 1217 50587304
Overdose 28.95 18.64 85 16518 99642 50488879
Drug hypersensitivity 28.87 18.64 24 16579 250986 50337535
Sinusitis 28.80 18.64 10 16593 170548 50417973
Trichostasis spinulosa 28.71 18.64 5 16598 13 50588508
Mouth ulceration 28.03 18.64 40 16563 27984 50560537
Constipation 27.92 18.64 13 16590 185695 50402826
Product dose omission issue 27.43 18.64 13 16590 183825 50404696
Jarisch-Herxheimer reaction 27.42 18.64 8 16595 287 50588234
Hypoalbuminaemia 27.35 18.64 24 16579 9836 50578685
Skin graft rejection 27.28 18.64 5 16598 19 50588502
Graft thrombosis 27.09 18.64 7 16596 158 50588363
Abdominal discomfort 26.81 18.64 22 16581 231619 50356902
Acute graft versus host disease in skin 26.77 18.64 15 16588 3003 50585518
Therapeutic product effect decreased 26.64 18.64 6 16597 136044 50452477
Back pain 26.60 18.64 20 16583 220010 50368511
Haemodialysis 26.56 18.64 22 16581 8340 50580181
Escherichia bacteraemia 26.32 18.64 15 16588 3101 50585420
Swelling 25.94 18.64 17 16586 200855 50387666
Squamous cell carcinoma 25.92 18.64 21 16582 7718 50580803
Fibrosarcoma 25.85 18.64 4 16599 3 50588518
Muscle spasms 25.69 18.64 5 16598 125548 50462973
Drug level fluctuating 25.28 18.64 8 16595 379 50588142
Pruritus 24.92 18.64 34 16569 283534 50304987
Renal tubular necrosis 24.75 18.64 23 16580 10145 50578376
Disseminated mycobacterium avium complex infection 24.73 18.64 5 16598 35 50588486
Haemolytic uraemic syndrome 24.66 18.64 13 16590 2306 50586215
Rhinovirus infection 24.57 18.64 15 16588 3519 50585002
Chronic graft versus host disease in skin 24.45 18.64 9 16594 675 50587846
Transplant failure 24.15 18.64 11 16592 1422 50587099
Enterovirus infection 23.94 18.64 9 16594 716 50587805
Viraemia 23.80 18.64 10 16593 1065 50587456
Insomnia 23.68 18.64 14 16589 174851 50413670
Weight increased 23.58 18.64 19 16584 201872 50386649
Lung transplant rejection 23.42 18.64 9 16594 760 50587761
Nausea 23.41 18.64 136 16467 705262 49883259
Gait disturbance 23.33 18.64 10 16593 149995 50438526
Hepatic fibrosis 23.31 18.64 14 16589 3188 50585333
Trichodysplasia spinulosa 23.23 18.64 8 16595 494 50588027
Renal failure 22.90 18.64 82 16521 106551 50481970
Pulmonary alveolar haemorrhage 22.77 18.64 15 16588 4012 50584509
Interstitial lung disease 22.27 18.64 52 16551 53124 50535397
Bacterial translocation 22.16 18.64 6 16597 163 50588358
Cat scratch disease 22.06 18.64 6 16597 166 50588355
Pterygium 21.95 18.64 6 16597 169 50588352
Aspergillus infection 21.77 18.64 18 16585 6803 50581718
Bacterial colitis 21.73 18.64 5 16598 68 50588453
Anxiety 21.64 18.64 16 16587 177590 50410931
Chest pain 21.47 18.64 16 16587 176866 50411655
Q fever 21.28 18.64 5 16598 75 50588446
Klebsiella infection 20.94 18.64 18 16585 7176 50581345
Acute hepatitis C 20.92 18.64 5 16598 81 50588440
Salivary gland mass 20.64 18.64 5 16598 86 50588435
Pulmonary artery atresia 20.61 18.64 4 16599 22 50588499
Diabetes mellitus 20.59 18.64 48 16555 48985 50539536
Kussmaul respiration 20.23 18.64 6 16597 228 50588293
Thymus enlargement 20.17 18.64 5 16598 95 50588426
Blastomycosis 19.86 18.64 6 16597 243 50588278
Urinary tract infection pseudomonal 19.67 18.64 8 16595 785 50587736
Craniocerebral injury 19.59 18.64 11 16592 2210 50586311
Pleural effusion 19.54 18.64 65 16538 81389 50507132
Renal transplant 19.43 18.64 9 16594 1210 50587311
Syncope 19.27 18.64 5 16598 102997 50485524
Lower respiratory tract infection 19.04 18.64 4 16599 95197 50493324
Magnetic resonance imaging head abnormal 19.01 18.64 10 16593 1767 50586754
Hypoaesthesia 18.97 18.64 9 16594 127248 50461273
Human polyomavirus infection 18.88 18.64 6 16597 288 50588233

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 416.00 14.69 169 17500 9043 29547815
Product use in unapproved indication 353.33 14.69 340 17329 86535 29470323
Kidney transplant rejection 304.20 14.69 125 17544 6880 29549978
Off label use 297.15 14.69 591 17078 300209 29256649
Post transplant lymphoproliferative disorder 141.52 14.69 68 17601 5425 29551433
Liver transplant rejection 131.14 14.69 48 17621 1926 29554932
Adenovirus infection 129.78 14.69 60 17609 4387 29552471
Thrombotic microangiopathy 128.02 14.69 74 17595 8607 29548251
Cytomegalovirus infection 125.73 14.69 107 17562 23108 29533750
Immunosuppressant drug level increased 116.75 14.69 57 17612 4708 29552150
Acute graft versus host disease 108.75 14.69 58 17611 5766 29551092
Transplant failure 107.30 14.69 46 17623 2810 29554048
Product use issue 101.83 14.69 139 17530 51305 29505553
BK virus infection 96.78 14.69 50 17619 4657 29552201
Epstein-Barr virus infection 96.38 14.69 56 17613 6573 29550285
Nephropathy toxic 89.63 14.69 64 17605 10692 29546166
Squamous cell carcinoma 85.42 14.69 61 17608 10190 29546668
Chronic graft versus host disease 80.54 14.69 42 17627 3987 29552871
Squamous cell carcinoma of skin 78.02 14.69 56 17613 9430 29547428
Lymphocele 76.09 14.69 29 17640 1303 29555555
Blood creatinine increased 73.46 14.69 159 17510 84943 29471915
Cytomegalovirus viraemia 70.34 14.69 45 17624 6275 29550583
Complications of transplanted kidney 69.96 14.69 38 17631 3916 29552942
Chronic allograft nephropathy 69.84 14.69 26 17643 1094 29555764
Proteinuria 64.20 14.69 62 17607 15742 29541116
Cytomegalovirus infection reactivation 64.20 14.69 34 17635 3330 29553528
Nocardiosis 59.55 14.69 32 17637 3228 29553630
Epidermodysplasia verruciformis 59.02 14.69 14 17655 114 29556744
Graft versus host disease in skin 55.72 14.69 31 17638 3348 29553510
Transplant dysfunction 55.14 14.69 27 17642 2243 29554615
Renal impairment 54.86 14.69 138 17531 81195 29475663
Meningitis viral 54.85 14.69 20 17649 793 29556065
Skin squamous cell carcinoma recurrent 54.71 14.69 11 17658 36 29556822
Propionibacterium infection 53.77 14.69 15 17654 244 29556614
Brain abscess 51.14 14.69 27 17642 2628 29554230
Kidney fibrosis 48.68 14.69 24 17645 2023 29554835
Heart transplant rejection 48.10 14.69 20 17649 1131 29555727
Multiple organ dysfunction syndrome 47.79 14.69 112 17557 63004 29493854
Acute graft versus host disease in skin 46.50 14.69 31 17638 4633 29552225
Graft versus host disease in gastrointestinal tract 45.97 14.69 27 17642 3231 29553627
Graft versus host disease in liver 45.82 14.69 19 17650 1067 29555791
Bronchopulmonary aspergillosis 45.62 14.69 46 17623 12298 29544560
Dizziness 45.00 14.69 29 17640 189655 29367203
Interstitial lung disease 44.33 14.69 103 17566 57615 29499243
Herpes zoster meningoencephalitis 44.18 14.69 13 17656 258 29556600
Pneumonia cytomegaloviral 42.58 14.69 24 17645 2658 29554200
Impaired healing 42.03 14.69 46 17623 13512 29543346
Diaphragmatic hernia 40.19 14.69 12 17657 251 29556607
Fatigue 39.87 14.69 81 17588 316740 29240118
Cow pox 38.94 14.69 8 17661 30 29556828
Pericardial effusion 38.46 14.69 55 17614 21153 29535705
Central nervous system lymphoma 38.43 14.69 15 17654 719 29556139
Constipation 37.23 14.69 11 17658 114149 29442709
Mouth ulceration 37.19 14.69 38 17631 10317 29546541
Skin squamous cell carcinoma metastatic 36.92 14.69 8 17661 41 29556817
Pleocytosis 36.85 14.69 13 17656 468 29556390
Renal tubular atrophy 36.59 14.69 16 17653 1025 29555833
Human herpesvirus 8 infection 36.35 14.69 15 17654 832 29556026
Transitional cell carcinoma 35.35 14.69 19 17650 1916 29554942
Retinal scar 35.06 14.69 11 17658 273 29556585
Haemolytic uraemic syndrome 34.77 14.69 19 17650 1981 29554877
Hepatic cancer recurrent 34.40 14.69 11 17658 291 29556567
Hyperlipidaemia 34.40 14.69 40 17629 12550 29544308
Drug interaction 34.16 14.69 218 17451 197167 29359691
Cytomegalovirus chorioretinitis 33.43 14.69 22 17647 3216 29553642
Hypotension 32.59 14.69 41 17628 194313 29362545
Protothecosis 32.44 14.69 7 17662 35 29556823
Graft versus host disease 32.19 14.69 34 17635 9594 29547264
Nephrogenic diabetes insipidus 32.08 14.69 15 17654 1124 29555734
Tularaemia 31.32 14.69 8 17661 91 29556767
Scedosporium infection 30.66 14.69 13 17656 772 29556086
Drug level decreased 30.18 14.69 27 17642 6220 29550638
Diarrhoea haemorrhagic 29.59 14.69 26 17643 5848 29551010
Pharyngitis 29.50 14.69 28 17641 6955 29549903
Gastroenteritis norovirus 29.18 14.69 15 17654 1381 29555477
Metastases to lung 28.53 14.69 29 17640 7826 29549032
Anxiety 28.23 14.69 8 17661 85357 29471501
Right ventricular diastolic collapse 28.22 14.69 7 17662 70 29556788
Focal segmental glomerulosclerosis 28.22 14.69 16 17653 1791 29555067
Diffuse large B-cell lymphoma 28.11 14.69 26 17643 6250 29550608
Smooth muscle cell neoplasm 27.92 14.69 8 17661 144 29556714
Polyomavirus-associated nephropathy 27.80 14.69 20 17649 3376 29553482
Bradycardia 26.11 14.69 4 17665 65625 29491233
Drug effective for unapproved indication 25.78 14.69 14 17655 1441 29555417
Venoocclusive disease 25.61 14.69 17 17652 2522 29554336
Chronic graft versus host disease in liver 25.20 14.69 9 17660 336 29556522
Basal cell carcinoma 25.17 14.69 40 17629 16870 29539988
Ileal ulcer 24.90 14.69 10 17659 517 29556341
Enteritis 24.53 14.69 25 17644 6766 29550092
Ophthalmic herpes zoster 24.52 14.69 11 17658 749 29556109
Renal tubular necrosis 24.32 14.69 36 17633 14279 29542579
Malacoplakia 24.17 14.69 7 17662 131 29556727
Venoocclusive liver disease 24.15 14.69 25 17644 6892 29549966
Chronic graft versus host disease in skin 23.68 14.69 11 17658 812 29556046
Complications of transplanted heart 23.63 14.69 8 17661 254 29556604
Mycobacterium chelonae infection 23.52 14.69 10 17659 598 29556260
Neuroendocrine carcinoma of the skin 23.33 14.69 10 17659 610 29556248
Varicella 22.97 14.69 13 17656 1450 29555408
Philadelphia positive chronic myeloid leukaemia 22.09 14.69 6 17663 88 29556770
Lung transplant rejection 21.84 14.69 10 17659 714 29556144
Arthralgia 21.81 14.69 31 17638 139586 29417272
Aspergillus infection 21.51 14.69 29 17640 10552 29546306
Scleroderma 21.31 14.69 12 17657 1326 29555532
Syncope 21.31 14.69 11 17658 81360 29475498
Hepatitis B 21.26 14.69 21 17648 5476 29551382
Nausea 21.14 14.69 95 17574 289160 29267698
Escherichia infection 21.05 14.69 23 17646 6741 29550117
Hydronephrosis 21.00 14.69 26 17643 8704 29548154
Nail discolouration 20.84 14.69 10 17659 794 29556064
Drug level increased 20.82 14.69 39 17630 18748 29538110
Fall 20.79 14.69 47 17622 177131 29379727
Wound dehiscence 20.74 14.69 16 17653 3001 29553857
Escherichia urinary tract infection 20.64 14.69 16 17653 3023 29553835
Drug resistance 20.57 14.69 42 17627 21498 29535360
Obliterative bronchiolitis 20.51 14.69 11 17658 1105 29555753
Ureteric stenosis 20.51 14.69 11 17658 1105 29555753
Insomnia 20.43 14.69 14 17655 88747 29468111
Varicella zoster virus infection 20.27 14.69 12 17657 1456 29555402
Pruritus 20.24 14.69 24 17645 116825 29440033
Depression 20.18 14.69 13 17656 85134 29471724
Toxoplasmosis 20.04 14.69 11 17658 1156 29555702
Back pain 19.96 14.69 19 17650 102265 29454593
Splenic neoplasm malignancy unspecified 19.91 14.69 4 17665 13 29556845
Muscle spasms 19.91 14.69 7 17662 65075 29491783
Pseudomonas infection 19.46 14.69 28 17641 10824 29546034
Pneumonitis 19.30 14.69 48 17621 27996 29528862
Normocytic anaemia 19.28 14.69 13 17656 1979 29554879
Spirochaetal infection 19.27 14.69 4 17665 16 29556842
Abdominal wall abscess 19.18 14.69 8 17661 456 29556402
Cytomegalovirus colitis 18.98 14.69 14 17655 2455 29554403
Histology abnormal 18.95 14.69 7 17662 288 29556570
Livedo reticularis 18.72 14.69 13 17656 2075 29554783
Kaposi sarcoma inflammatory cytokine syndrome 18.71 14.69 4 17665 19 29556839
Lip haemorrhage 18.51 14.69 9 17660 736 29556122
Perinephric collection 18.51 14.69 6 17663 166 29556692
Skin erosion 18.42 14.69 12 17657 1724 29555134
Acne 18.33 14.69 25 17644 9195 29547663
Alternaria infection 18.25 14.69 7 17662 320 29556538
Bacterial sepsis 18.25 14.69 18 17651 4685 29552173
Viraemia 18.11 14.69 10 17659 1064 29555794
Joint swelling 17.66 14.69 4 17665 49626 29507232
Inferior vena cava stenosis 17.39 14.69 4 17665 28 29556830
Acute graft versus host disease in intestine 17.39 14.69 13 17656 2328 29554530
Posterior reversible encephalopathy syndrome 17.34 14.69 24 17645 8952 29547906
Cryptococcosis 17.14 14.69 12 17657 1940 29554918
SARS-CoV-2 RNA 17.04 14.69 4 17665 31 29556827
Somnolence 16.59 14.69 19 17650 93936 29462922
Overdose 16.56 14.69 14 17655 79805 29477053
Hyperhidrosis 16.49 14.69 9 17660 64531 29492327
Herpes virus infection 16.49 14.69 13 17656 2518 29554340
Drug ineffective for unapproved indication 16.37 14.69 30 17639 14184 29542674
Osmotic demyelination syndrome 16.29 14.69 8 17661 668 29556190
Anuria 16.21 14.69 24 17645 9517 29547341
Epstein-Barr viraemia 16.20 14.69 9 17660 969 29555889
Human polyomavirus infection 16.13 14.69 8 17661 683 29556175
Candida infection 16.12 14.69 31 17638 15194 29541664
Lactobacillus infection 16.02 14.69 5 17664 122 29556736
Peritoneal hernia 15.98 14.69 3 17666 6 29556852
Pulmonary toxicity 15.87 14.69 17 17652 4873 29551985
Haemorrhagic pneumonia 15.68 14.69 5 17664 131 29556727
Cachexia 15.41 14.69 19 17650 6330 29550528
Pyrexia 15.36 14.69 249 17420 287373 29269485
Pneumocystis jirovecii infection 15.34 14.69 10 17659 1438 29555420
Necrotising retinitis 15.33 14.69 8 17661 760 29556098
Microvillous inclusion disease 15.31 14.69 4 17665 50 29556808
Pulmonary cavitation 15.18 14.69 8 17661 775 29556083
Ovarian cyst 15.12 14.69 3 17666 9 29556849
Inappropriate schedule of product administration 15.01 14.69 4 17665 44468 29512390
Myocarditis toxoplasmal 14.83 14.69 4 17665 57 29556801
Pneumonia adenoviral 14.82 14.69 5 17664 157 29556701
Immunosuppressant drug level decreased 14.78 14.69 9 17660 1149 29555709
Atypical haemolytic uraemic syndrome 14.70 14.69 5 17664 161 29556697

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 2066.95 14.98 617 29594 16784 64451737
Transplant dysfunction 1880.43 14.98 468 29743 6240 64462281
Ovarian cyst 1352.27 14.98 401 29810 10617 64457904
Acne 1141.69 14.98 423 29788 22658 64445863
Product use in unapproved indication 611.01 14.98 567 29644 176051 64292470
Alopecia 440.43 14.98 461 29750 165229 64303292
Off label use 424.99 14.98 920 29291 631886 63836635
Kidney transplant rejection 340.54 14.98 138 30073 9373 64459148
Post transplant lymphoproliferative disorder 289.41 14.98 123 30088 9421 64459100
Sleep disorder due to general medical condition, insomnia type 283.86 14.98 168 30043 26102 64442419
Thrombotic microangiopathy 275.22 14.98 141 30070 16514 64452007
Epstein-Barr virus infection 251.63 14.98 121 30090 12367 64456154
Acute graft versus host disease 226.46 14.98 102 30109 8982 64459539
Product use issue 226.09 14.98 315 29896 151400 64317121
Adenovirus infection 211.70 14.98 91 30120 7164 64461357
Immunosuppressant drug level increased 182.50 14.98 82 30129 7177 64461344
Cytomegalovirus infection 177.81 14.98 144 30067 37055 64431466
BK virus infection 168.30 14.98 78 30133 7334 64461187
Liver function test abnormal 160.43 14.98 167 30044 59234 64409287
Chronic allograft nephropathy 138.17 14.98 44 30167 1477 64467044
Nephropathy toxic 129.11 14.98 88 30123 17426 64451095
Chronic graft versus host disease 126.98 14.98 61 30150 6215 64462306
Cytomegalovirus infection reactivation 125.81 14.98 59 30152 5697 64462824
Liver transplant rejection 119.42 14.98 47 30164 2952 64465569
Graft versus host disease in skin 117.46 14.98 55 30156 5292 64463229
Graft versus host disease in gastrointestinal tract 114.92 14.98 55 30156 5557 64462964
Graft versus host disease 108.03 14.98 72 30139 13741 64454780
Transplant failure 105.48 14.98 46 30165 3748 64464773
Squamous cell carcinoma 102.97 14.98 70 30141 13799 64454722
Blood creatinine increased 91.90 14.98 199 30012 135583 64332938
Renal impairment 88.11 14.98 195 30016 134822 64333699
Human herpesvirus 6 infection 87.43 14.98 43 30168 4611 64463910
Arthralgia 85.08 14.98 51 30160 442209 64026312
Smooth muscle cell neoplasm 82.59 14.98 26 30185 840 64467681
Complications of transplanted kidney 81.12 14.98 43 30168 5392 64463129
Acute graft versus host disease in skin 79.70 14.98 46 30165 6809 64461712
Polyomavirus-associated nephropathy 79.61 14.98 41 30170 4847 64463674
Multiple organ dysfunction syndrome 78.39 14.98 157 30054 101256 64367265
Proteinuria 76.70 14.98 79 30132 27644 64440877
Fatigue 76.58 14.98 147 30064 748583 63719938
Dizziness 74.14 14.98 56 30155 430107 64038414
Lymphocele 73.45 14.98 28 30183 1613 64466908
Epstein-Barr virus associated lymphoproliferative disorder 71.35 14.98 33 30178 3086 64465435
Fall 69.63 14.98 56 30155 416770 64051751
Pneumonia 67.90 14.98 471 29740 559105 63909416
Squamous cell carcinoma of skin 67.60 14.98 51 30160 11825 64456696
Epidermodysplasia verruciformis 67.08 14.98 16 30195 175 64468346
Skin squamous cell carcinoma metastatic 67.03 14.98 13 30198 46 64468475
Drug interaction 66.56 14.98 340 29871 361743 64106778
Joint swelling 65.64 14.98 11 30200 215371 64253150
Heart transplant rejection 65.03 14.98 24 30187 1263 64467258
Mouth ulceration 63.21 14.98 77 30134 32367 64436154
Condition aggravated 62.47 14.98 341 29870 372085 64096436
Bronchopulmonary aspergillosis 59.44 14.98 58 30153 19027 64449494
Interstitial lung disease 58.00 14.98 136 30075 97596 64370925
Rash 56.08 14.98 80 30131 458469 64010052
Constipation 55.64 14.98 19 30192 229318 64239203
Propionibacterium infection 54.52 14.98 15 30196 299 64468222
Human herpesvirus 8 infection 54.18 14.98 20 30191 1053 64467468
Cytomegalovirus viraemia 54.01 14.98 43 30168 10785 64457736
Nausea 53.63 14.98 189 30022 785611 63682910
Kidney fibrosis 53.37 14.98 27 30184 3074 64465447
Nocardiosis 52.80 14.98 31 30180 4736 64463785
Chronic graft versus host disease in skin 52.59 14.98 21 30190 1370 64467151
Pseudomonas infection 51.35 14.98 52 30159 17831 64450690
Posterior reversible encephalopathy syndrome 50.56 14.98 58 30153 22888 64445633
Alveolar proteinosis 49.49 14.98 16 30195 564 64467957
Haemolytic uraemic syndrome 49.47 14.98 28 30183 3993 64464528
MELAS syndrome 49.14 14.98 12 30199 146 64468375
Focal segmental glomerulosclerosis 48.83 14.98 25 30186 2919 64465602
Infusion related reaction 48.79 14.98 9 30202 164458 64304063
Pruritus 48.44 14.98 45 30166 312355 64156166
Hypersensitivity 48.12 14.98 16 30195 196436 64272085
Drug level increased 47.83 14.98 69 30142 34127 64434394
Back pain 47.81 14.98 29 30182 250142 64218379
Pericardial effusion 47.48 14.98 74 30137 39180 64429341
Rheumatoid arthritis 46.72 14.98 176 30035 164118 64304403
Pain in extremity 46.58 14.98 44 30167 303041 64165480
Syncope 45.96 14.98 9 30202 157626 64310895
Transitional cell carcinoma 45.92 14.98 22 30189 2227 64466294
JC virus infection 45.75 14.98 25 30186 3330 64465191
Skin squamous cell carcinoma recurrent 45.34 14.98 9 30202 37 64468484
Meningitis viral 44.85 14.98 20 30191 1718 64466803
Somnolence 44.24 14.98 20 30191 203625 64264896
Hypotension 44.08 14.98 69 30142 380905 64087616
Cryptosporidiosis infection 43.84 14.98 15 30196 632 64467889
Brain abscess 43.20 14.98 26 30185 4155 64464366
Aspergillus infection 42.31 14.98 45 30166 16334 64452187
Pancreas transplant rejection 41.28 14.98 12 30199 294 64468227
Loss of personal independence in daily activities 41.00 14.98 99 30112 72355 64396166
Cow pox 40.88 14.98 8 30203 30 64468491
Anxiety 40.84 14.98 22 30189 202627 64265894
Renal tubular atrophy 40.76 14.98 18 30193 1511 64467010
Graft versus host disease in liver 40.62 14.98 18 30193 1523 64466998
Diaphragmatic hernia 40.03 14.98 12 30199 328 64468193
Drug level decreased 39.69 14.98 37 30174 11466 64457055
Dyspnoea 39.48 14.98 188 30023 718486 63750035
Venoocclusive disease 39.17 14.98 24 30187 3961 64464560
Renal tubular necrosis 39.10 14.98 50 30161 22060 64446461
Herpes zoster meningoencephalitis 39.09 14.98 14 30197 676 64467845
Pneumocystis jirovecii pneumonia 39 14.98 56 30155 27578 64440943
Pneumonitis 37.73 14.98 77 30134 50288 64418233
Hyperlipidaemia 37.59 14.98 50 30161 22926 64445595
Pneumonia cytomegaloviral 37.29 14.98 24 30187 4315 64464206
Varicella zoster virus infection 37.16 14.98 23 30188 3865 64464656
Varicella 37.05 14.98 20 30191 2601 64465920
Hypertriglyceridaemia 36.67 14.98 35 30176 11170 64457351
Urticaria 36.07 14.98 12 30199 147305 64321216
Haemodialysis 35.67 14.98 42 30169 17035 64451486
Drug effective for unapproved indication 35.60 14.98 22 30189 3686 64464835
Incorrect route of product administration 35.53 14.98 49 30162 23249 64445272
Muscle spasms 35.39 14.98 11 30200 141012 64327509
Septic shock 35.12 14.98 119 30092 105318 64363203
Arthropathy 35.06 14.98 7 30204 120960 64347561
Therapeutic product effect decreased 34.88 14.98 6 30205 115345 64353176
Immunosuppressant drug level decreased 34.78 14.98 17 30194 1798 64466723
Protothecosis 34.31 14.98 7 30204 34 64468487
Avian influenza 34.28 14.98 8 30203 79 64468442
Retinal scar 34.10 14.98 11 30200 385 64468136
Drug level below therapeutic 34.03 14.98 28 30183 7356 64461165
Central nervous system lymphoma 33.75 14.98 17 30194 1918 64466603
Diffuse large B-cell lymphoma 33.22 14.98 32 30179 10329 64458192
Tularaemia 33.17 14.98 8 30203 92 64468429
Feeling abnormal 32.50 14.98 11 30200 133591 64334930
Insomnia 32.44 14.98 27 30184 197809 64270712
Respiratory failure 32.10 14.98 155 30056 161028 64307493
Bradycardia 31.93 14.98 8 30203 118211 64350310
Neurofibrosarcoma 31.62 14.98 9 30202 204 64468317
Drug hypersensitivity 31.55 14.98 39 30172 237776 64230745
Acute graft versus host disease in intestine 31.11 14.98 20 30191 3589 64464932
Viraemia 30.65 14.98 17 30194 2332 64466189
Globulins decreased 30.62 14.98 10 30201 364 64468157
Gastroenteritis norovirus 30.61 14.98 18 30193 2757 64465764
Venoocclusive liver disease 30.37 14.98 30 30181 9985 64458536
Lung transplant rejection 30.18 14.98 14 30197 1318 64467203
Chronic graft versus host disease in liver 30.15 14.98 11 30200 560 64467961
Cytomegalovirus chorioretinitis 29.98 14.98 22 30189 4890 64463631
Morphoea 29.82 14.98 10 30201 396 64468125
Rhinovirus infection 29.75 14.98 24 30187 6132 64462389
Pleocytosis 29.40 14.98 13 30198 1094 64467427
Adjusted calcium decreased 29.24 14.98 8 30203 156 64468365
Hyperhidrosis 29.17 14.98 11 30200 124909 64343612
Sinusitis 29.16 14.98 16 30195 145912 64322609
Right ventricular diastolic collapse 28.99 14.98 7 30204 81 64468440
Nephrogenic diabetes insipidus 28.36 14.98 15 30196 1872 64466649
Drug resistance 27.88 14.98 55 30156 35047 64433474
Scedosporium infection 27.85 14.98 13 30198 1241 64467280
Bacillary angiomatosis 27.79 14.98 8 30203 189 64468332
Alopecia scarring 27.76 14.98 7 30204 98 64468423
Drug ineffective for unapproved indication 27.46 14.98 51 30160 31082 64437439
Neuroendocrine carcinoma of the skin 27.30 14.98 12 30199 996 64467525
Malaise 27.11 14.98 95 30116 396152 64072369
Trichostasis spinulosa 26.94 14.98 5 30206 13 64468508
Musculoskeletal stiffness 26.90 14.98 12 30199 123194 64345327
Maternal exposure during pregnancy 26.86 14.98 6 30205 95878 64372643
PIK3CA related overgrowth spectrum 26.67 14.98 4 30207 0 64468521
Asthma 26.59 14.98 6 30205 95219 64373302
Epstein-Barr viraemia 26.20 14.98 14 30197 1783 64466738
Mucormycosis 26.08 14.98 24 30187 7317 64461204
Hypogammaglobulinaemia 26.07 14.98 28 30183 10271 64458250
Loss of consciousness 25.90 14.98 19 30192 148346 64320175
Plasmablastic lymphoma 25.84 14.98 9 30202 400 64468121
Bacterial sepsis 25.76 14.98 24 30187 7433 64461088
Renal graft infection 25.75 14.98 9 30202 404 64468117
Diabetes mellitus 25.73 14.98 79 30132 66395 64402126
Polyomavirus viraemia 25.67 14.98 12 30199 1150 64467371
Depression 25.43 14.98 29 30182 183262 64285259
Pleural effusion 25.40 14.98 122 30089 126437 64342084
Weight increased 25.25 14.98 38 30173 213310 64255211
Drug level fluctuating 24.95 14.98 10 30201 659 64467862
Cytomegalovirus colitis 24.90 14.98 18 30193 3910 64464611
COVID-19 24.83 14.98 77 30134 65063 64403458
Babesiosis 24.83 14.98 8 30203 279 64468242
Mobility decreased 24.81 14.98 5 30206 85835 64382686
Escherichia infection 24.80 14.98 33 30178 15135 64453386
Wheezing 24.78 14.98 4 30207 80575 64387946
Dyspepsia 24.67 14.98 4 30207 80308 64388213
Glomerulosclerosis 24.57 14.98 11 30200 954 64467567
Stem cell transplant 24.49 14.98 17 30194 3464 64465057
Skin graft rejection 24.22 14.98 5 30206 26 64468495
Gait disturbance 24.14 14.98 27 30184 172128 64296393
Human polyomavirus infection 23.99 14.98 11 30200 1008 64467513
Biopsy kidney abnormal 23.98 14.98 7 30204 174 64468347
Perinephric collection 23.90 14.98 8 30203 315 64468206
Escherichia bacteraemia 23.88 14.98 20 30191 5383 64463138
Scleroderma 23.74 14.98 19 30192 4799 64463722
Ophthalmic herpes zoster 23.66 14.98 14 30197 2170 64466351
Obliterative bronchiolitis 23.55 14.98 15 30196 2650 64465871
Contusion 23.50 14.98 12 30199 113953 64354568
Confusional state 23.43 14.98 55 30156 261089 64207432
Klebsiella infection 23.43 14.98 30 30181 13251 64455270
Bacterial colitis 23.16 14.98 6 30205 94 64468427
Musculoskeletal pain 22.95 14.98 5 30206 81289 64387232
Dysplasia 22.69 14.98 11 30200 1143 64467378
Enteritis 22.45 14.98 28 30183 12049 64456472
Pneumatosis intestinalis 22.38 14.98 19 30192 5210 64463311
Toxoplasmosis 22.20 14.98 14 30197 2430 64466091
Malacoplakia 21.81 14.98 7 30204 241 64468280
Renal transplant failure 21.75 14.98 12 30199 1628 64466893
Chest pain 21.73 14.98 49 30162 235931 64232590
Ureteric stenosis 21.72 14.98 11 30200 1255 64467266
Adenovirus reactivation 21.64 14.98 7 30204 247 64468274
Philadelphia positive chronic myeloid leukaemia 21.29 14.98 6 30205 131 64468390
Hyponatraemia 21.09 14.98 23 30188 148316 64320205
Trichodysplasia spinulosa 20.94 14.98 9 30202 707 64467814
Pulmonary cavitation 20.94 14.98 11 30200 1354 64467167
Product dose omission issue 20.88 14.98 37 30174 194710 64273811
Blister 20.88 14.98 6 30205 80961 64387560
Diarrhoea haemorrhagic 20.82 14.98 26 30185 11201 64457320
Blastomycosis 20.58 14.98 8 30203 486 64468035
Swelling 20.48 14.98 27 30184 160191 64308330
Salivary gland mass 20.39 14.98 5 30206 62 64468459
Glossodynia 20.38 14.98 3 30208 64693 64403828
Pneumocystis jirovecii infection 20.14 14.98 13 30198 2348 64466173
Inappropriate schedule of product administration 20.12 14.98 9 30202 92277 64376244
Jejunal perforation 20.08 14.98 7 30204 312 64468209
Spirochaetal infection 20.04 14.98 4 30207 17 64468504
Staphylococcal mediastinitis 20 14.98 3 30208 0 64468521
Osteoarthritis 19.80 14.98 3 30208 63333 64405188
Kaposi sarcoma inflammatory cytokine syndrome 19.68 14.98 4 30207 19 64468502
Haemophagocytic lymphohistiocytosis 19.64 14.98 32 30179 17577 64450944
Asthenia 19.53 14.98 119 30092 427925 64040596
Hepatitis B 19.51 14.98 21 30190 7724 64460797
Pulmonary toxicity 19.47 14.98 22 30189 8539 64459982
Heart rate increased 19.45 14.98 11 30200 98664 64369857
Vomiting 19.44 14.98 165 30046 550952 63917569
Headache 19.36 14.98 157 30054 529310 63939211
Hypoaesthesia 19.30 14.98 22 30189 139086 64329435
Drug intolerance 19.02 14.98 37 30174 187955 64280566
Pyrexia 19.01 14.98 367 29844 558277 63910244
Paraesthesia 18.97 14.98 21 30190 134501 64334020
Pneumonia haemophilus 18.60 14.98 9 30202 931 64467590
Cystitis viral 18.60 14.98 8 30203 630 64467891
Actinic keratosis 18.57 14.98 17 30194 5148 64463373
Blood pressure increased 18.30 14.98 33 30178 172519 64296002
Product administered to patient of inappropriate age 18.23 14.98 16 30195 4585 64463936
Lung infiltration 18.14 14.98 34 30177 20855 64447666
Graft thrombosis 18.14 14.98 7 30204 417 64468104
Fibrosarcoma 18.12 14.98 4 30207 30 64468491
Abdominal pain upper 18.10 14.98 34 30177 174996 64293525
Disseminated mycobacterium avium complex infection 18.07 14.98 5 30206 102 64468419
Jarisch-Herxheimer reaction 18.03 14.98 8 30203 679 64467842
Blood triglycerides increased 18.02 14.98 32 30179 18834 64449687
Graft loss 18.01 14.98 9 30202 998 64467523
SARS-CoV-2 RNA 18.01 14.98 4 30207 31 64468490
Ileal ulcer 18.00 14.98 9 30202 999 64467522
Cardio-respiratory arrest 17.96 14.98 12 30199 98381 64370140
Bladder transitional cell carcinoma 17.86 14.98 12 30199 2318 64466203
Chest discomfort 17.64 14.98 17 30194 116089 64352432
Hydronephrosis 17.59 14.98 27 30184 14098 64454423
Papilloma viral infection 17.49 14.98 10 30201 1454 64467067
Cat scratch disease 17.42 14.98 6 30205 258 64468263
Wound 17.41 14.98 7 30204 76470 64392051
Metastases to lung 17.38 14.98 28 30183 15236 64453285
Thymus enlargement 17.38 14.98 5 30206 118 64468403
Herpes simplex 17.34 14.98 23 30188 10513 64458008
Acute kidney injury 17.32 14.98 301 29910 448939 64019582
Psoriasis 17.26 14.98 6 30205 71697 64396824
Graft ischaemia 17.19 14.98 4 30207 39 64468482
Cardiac murmur functional 17.19 14.98 4 30207 39 64468482
Balance disorder 17.06 14.98 9 30202 83917 64384604
Arthritis 17.02 14.98 9 30202 83805 64384716
Chronic obstructive pulmonary disease 17.01 14.98 6 30205 71042 64397479
Livedo reticularis 16.99 14.98 14 30197 3683 64464838
Lymphoedema 16.89 14.98 22 30189 9883 64458638
Renal vessel disorder 16.69 14.98 6 30205 293 64468228
Splenic neoplasm malignancy unspecified 16.67 14.98 4 30207 45 64468476
Lymphopenia 16.64 14.98 37 30174 25620 64442901
Pterygium 16.53 14.98 6 30205 301 64468220
Respiratory distress 16.49 14.98 58 30153 52273 64416248
Bronchitis 16.43 14.98 16 30195 108727 64359794
Viral oesophagitis 16.39 14.98 3 30208 7 64468514
Exposure during pregnancy 16.28 14.98 8 30203 77667 64390854
Endocarditis 16.25 14.98 21 30190 9357 64459164
Normocytic anaemia 16.23 14.98 13 30198 3286 64465235
Inferior vena cava stenosis 16.07 14.98 4 30207 53 64468468
Alternaria infection 15.92 14.98 7 30204 581 64467940
Clostridium difficile infection 15.92 14.98 45 30166 36118 64432403
Therapeutic product effect incomplete 15.90 14.98 15 30196 103467 64365054
Abdominal discomfort 15.87 14.98 39 30172 182283 64286238
Acquired mitochondrial DNA mutation 15.85 14.98 3 30208 9 64468512
Coma 15.57 14.98 11 30200 87604 64380917
Myocarditis toxoplasmal 15.48 14.98 4 30207 62 64468459
Cerebral toxoplasmosis 15.45 14.98 10 30201 1816 64466705
Lower respiratory tract infection 15.39 14.98 13 30198 94601 64373920
HIV infection 15.31 14.98 8 30203 974 64467547
Microvillous inclusion disease 15.31 14.98 4 30207 65 64468456
Suicidal ideation 15.29 14.98 6 30205 66536 64401985
Optic neuropathy 15.11 14.98 12 30199 2999 64465522
Hepatitis E 15.09 14.98 11 30200 2420 64466101
Orbital apex syndrome 15.08 14.98 4 30207 69 64468452
Lactobacillus infection 15.08 14.98 5 30206 191 64468330
Peripheral swelling 15.06 14.98 49 30162 209104 64259417
Kussmaul respiration 15.03 14.98 6 30205 391 64468130

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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 (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
1MG/ML RAPAMUNE PF PRISM CV N021083 Sept. 15, 1999 RX SOLUTION ORAL May 28, 2022 TREATMENT OF LYMPHANGIOLEIOMYOMATOSIS (LAM)
0.5MG RAPAMUNE PF PRISM CV N021110 Jan. 25, 2010 RX TABLET ORAL May 28, 2022 TREATMENT OF LYMPHANGIOLEIOMYOMATOSIS (LAM)
1MG RAPAMUNE PF PRISM CV N021110 Aug. 25, 2000 RX TABLET ORAL May 28, 2022 TREATMENT OF LYMPHANGIOLEIOMYOMATOSIS (LAM)
2MG RAPAMUNE PF PRISM CV N021110 Aug. 22, 2002 RX TABLET ORAL May 28, 2022 TREATMENT OF LYMPHANGIOLEIOMYOMATOSIS (LAM)
5MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** RAPAMUNE PF PRISM CV N021110 Feb. 23, 2004 DISCN TABLET ORAL May 28, 2022 TREATMENT OF LYMPHANGIOLEIOMYOMATOSIS (LAM)
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

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
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 0008-1040 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 0008-1042 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 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 29 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 16714-188 TABLET, FILM COATED 1 mg ORAL ANDA 29 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 16714-189 TABLET, FILM COATED 2 mg ORAL ANDA 29 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 55111-654 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 59762-1002 TABLET, SUGAR COATED 1 mg ORAL NDA AUTHORIZED GENERIC 31 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 59762-1003 TABLET, SUGAR COATED 2 mg ORAL NDA AUTHORIZED GENERIC 31 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 59762-1205 SOLUTION 1 mg ORAL NDA AUTHORIZED GENERIC 34 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 60505-6197 SOLUTION 1 mg ORAL ANDA 31 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 65841-771 TABLET, FILM COATED 0.50 mg ORAL ANDA 1 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 66689-347 SOLUTION 1 mg ORAL ANDA 29 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 66689-347 SOLUTION 1 mg ORAL ANDA 29 sections
Sirolimus Human Prescription Drug Label 1 67877-746 TABLET 0.50 mg ORAL ANDA 29 sections
Sirolimus Human Prescription Drug Label 1 67877-747 TABLET 1 mg ORAL ANDA 29 sections
Sirolimus Human Prescription Drug Label 1 67877-748 TABLET 2 mg ORAL ANDA 29 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 68084-915 TABLET 1 mg ORAL ANDA 30 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 68382-520 TABLET, FILM COATED 0.50 mg ORAL ANDA 27 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 68462-682 TABLET, FILM COATED 0.50 mg ORAL ANDA 29 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 68462-683 TABLET, FILM COATED 1 mg ORAL ANDA 29 sections
sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 68462-684 TABLET, FILM COATED 2 mg ORAL ANDA 29 sections
Sirolimus HUMAN PRESCRIPTION DRUG LABEL 1 69238-1594 SOLUTION 1 mg ORAL ANDA 30 sections
HYFTOR HUMAN PRESCRIPTION DRUG LABEL 1 73683-101 GEL 2 mg TOPICAL NDA 27 sections