fluticasone furoate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4554 397864-44-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fluticasone furoate
  • avamys
  • veramyst
Fluticasone furoate is a synthetic trifluorinated corticosteroid with anti‑inflammatory activity. Fluticasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor. The precise mechanism of corticosteroid action on asthma is not known. Inflammation is an important component in the pathogenesis of asthma. Corticosteroids have been shown to have a wide range of actions on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) involved in inflammation. These anti-inflammatory actions of corticosteroids contribute to their efficacy in asthma.
  • Molecular weight: 538.58
  • Formula: C27H29F3O6S
  • CLOGP: 4.26
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 1
  • TPSA: 93.81
  • ALOGS: -4.09
  • ROTB: 6

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
0.20 mg N
0.11 mg N
0.60 mg Inhal.aerosol
0.60 mg Inhal.powder
1.50 mg Inhal.solution

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 4.95 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 13.40 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 10.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
April 27, 2007 FDA GLAXOSMITHKLINE
April 22, 2009 PMDA GlaxoSmithKline K.K.

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
Macular degeneration 460.12 18.99 161 12134 14227 50578602
Asthma 455.32 18.99 278 12017 89059 50503770
Wheezing 359.79 18.99 210 12085 61837 50530992
Obstructive airways disorder 337.13 18.99 131 12164 15521 50577308
Full blood count abnormal 198.60 18.99 102 12193 23286 50569543
Nasal congestion 171.94 18.99 123 12172 50997 50541832
Dyspnoea 134.54 18.99 361 11934 547247 50045582
Therapeutic product effect incomplete 115.24 18.99 126 12169 91389 50501440
Bronchial haemorrhage 112.65 18.99 26 12269 494 50592335
Bronchial neoplasm 111.90 18.99 25 12270 408 50592421
Gastrooesophageal reflux disease 102.82 18.99 109 12186 76319 50516510
Nasal turbinate hypertrophy 101.04 18.99 25 12270 645 50592184
Cough 99.98 18.99 196 12099 241068 50351761
Sleep disorder due to a general medical condition 95.54 18.99 43 12252 7328 50585501
Chest discomfort 95.35 18.99 115 12180 92607 50500222
Endometrial ablation 94.76 18.99 25 12270 838 50591991
Productive cough 94.67 18.99 88 12207 52606 50540223
Bronchial disorder 92.35 18.99 26 12269 1116 50591713
Bronchiectasis 87.67 18.99 45 12250 10238 50582591
Nasal polyps 83.14 18.99 29 12266 2525 50590304
Blepharospasm 82.80 18.99 30 12265 2918 50589911
Hyper IgE syndrome 79.81 18.99 19 12276 415 50592414
Total lung capacity increased 79.54 18.99 21 12274 706 50592123
Rhonchi 78.21 18.99 27 12268 2280 50590549
Asthma-chronic obstructive pulmonary disease overlap syndrome 78.10 18.99 19 12276 456 50592373
Throat clearing 77.82 18.99 23 12272 1175 50591654
Respiratory tract inflammation 75.68 18.99 19 12276 521 50592308
Dust allergy 74.93 18.99 19 12276 543 50592286
Sputum discoloured 71.31 18.99 43 12252 13352 50579477
Blood immunoglobulin E increased 69.99 18.99 25 12270 2334 50590495
Malignant mediastinal neoplasm 69.95 18.99 18 12277 546 50592283
Dyspnoea exertional 65.21 18.99 71 12224 51162 50541667
Breath sounds abnormal 63.26 18.99 33 12262 7759 50585070
Restrictive pulmonary disease 61.50 18.99 20 12275 1404 50591425
Rhinitis 61.29 18.99 33 12262 8268 50584561
Taste disorder 61.21 18.99 33 12262 8291 50584538
Affective disorder 60.15 18.99 28 12267 5153 50587676
Blood test abnormal 59.38 18.99 36 12259 11283 50581546
Secretion discharge 58.85 18.99 34 12261 9757 50583072
Granuloma 55.61 18.99 26 12269 4832 50587997
Rhinorrhoea 53.00 18.99 64 12231 51519 50541310
Haemoptysis 48.40 18.99 44 12251 25529 50567300
Polycystic ovaries 47.16 18.99 19 12276 2465 50590364
Sleep apnoea syndrome 47.01 18.99 42 12253 23826 50569003
Chronic obstructive pulmonary disease 46.46 18.99 61 12234 53374 50539455
Sarcoidosis 45.80 18.99 23 12272 4994 50587835
Lung hyperinflation 45.45 18.99 15 12280 1103 50591726
Eczema 44.82 18.99 40 12255 22662 50570167
Nasal obstruction 42.52 18.99 14 12281 1022 50591807
Chronic sinusitis 41.41 18.99 23 12272 6122 50586707
Respiratory disorder 41.03 18.99 44 12251 31143 50561686
Rhinitis allergic 40.62 18.99 24 12271 7176 50585653
Lactose intolerance 39.81 18.99 17 12278 2553 50590276
Eye pruritus 39.43 18.99 29 12266 12505 50580324
Death 37.66 18.99 16 12279 325363 50267466
Toxicity to various agents 37.49 18.99 4 12291 212495 50380334
Sinusitis 34.23 18.99 105 12190 170453 50422376
Forced expiratory volume decreased 33.93 18.99 18 12277 4376 50588453
Dyslipidaemia 33.89 18.99 20 12275 5968 50586861
Herpes zoster 33.51 18.99 61 12234 70725 50522104
Ligament pain 33.29 18.99 8 12287 182 50592647
Rales 31.19 18.99 23 12272 9955 50582874
Weight decreased 31.12 18.99 121 12174 221124 50371705
Crystal arthropathy 31.08 18.99 8 12287 243 50592586
Migraine 30.84 18.99 61 12234 75219 50517610
Ear pruritus 30.40 18.99 14 12281 2512 50590317
Sneezing 30.23 18.99 26 12269 14018 50578811
Blood pressure diastolic abnormal 30.22 18.99 22 12273 9339 50583490
Epilepsy 29.38 18.99 31 12264 21536 50571293
Bronchitis 28.68 18.99 72 12223 104087 50488742
Alopecia 26.84 18.99 13 12282 245034 50347795
Asthmatic crisis 25.98 18.99 11 12284 1617 50591212
Ankle fracture 25.81 18.99 25 12270 15697 50577132
Swelling face 25.74 18.99 46 12249 52549 50540280
Blood pressure systolic increased 25.58 18.99 37 12258 35412 50557417
Sinus pain 25.56 18.99 12 12283 2249 50590580
Seasonal allergy 25.34 18.99 24 12271 14652 50578177
Angioedema 25.28 18.99 38 12257 37638 50555191
Blood pressure systolic abnormal 24.62 18.99 18 12277 7688 50585141
Pertussis 23.71 18.99 8 12287 630 50592199
Arthropathy 23.22 18.99 5 12290 157901 50434928
Blood pressure diastolic increased 22.91 18.99 17 12278 7426 50585403
Subclavian vein thrombosis 21.74 18.99 10 12285 1789 50591040
Sensitivity to weather change 21.43 18.99 15 12280 5986 50586843
Stress 21.32 18.99 43 12252 53750 50539079
Cardiac murmur 21.27 18.99 19 12276 10765 50582064
Sinus tachycardia 21.11 18.99 26 12269 21328 50571501
Stent placement 20.82 18.99 12 12283 3426 50589403
Lung neoplasm malignant 20.63 18.99 22 12273 15462 50577367
Eosinophilia 20.55 18.99 24 12271 18628 50574201
Paraesthesia 20.45 18.99 70 12225 120173 50472656
Eosinophil count increased 20.34 18.99 17 12278 8813 50584016
Radioallergosorbent test positive 20.30 18.99 4 12291 34 50592795
Dyspnoea at rest 20.16 18.99 12 12283 3635 50589194
Restless legs syndrome 20.15 18.99 22 12273 15875 50576954
Chondrocalcinosis pyrophosphate 19.81 18.99 8 12287 1044 50591785
Respiratory gas exchange disorder 19.69 18.99 6 12289 340 50592489
Oral pruritus 19.26 18.99 9 12286 1669 50591160

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
Asthma 259.88 20.73 130 5897 33719 29534781
Wheezing 184.88 20.73 103 5924 33137 29535363
Nasal polyps 81.39 20.73 25 6002 1744 29566756
Appendicolith 79.39 20.73 29 5998 3451 29565049
Therapeutic product effect incomplete 73.13 20.73 62 5965 39243 29529257
Sleep disorder due to a general medical condition 70.96 20.73 26 6001 3120 29565380
Obstructive airways disorder 69.03 20.73 37 5990 10979 29557521
Nasal congestion 67.20 20.73 44 5983 18835 29549665
Foetal malformation 66.81 20.73 13 6014 125 29568375
Trisomy 18 62.26 20.73 13 6014 183 29568317
Appendicitis 53.63 20.73 29 5998 8750 29559750
Cough 52.36 20.73 93 5934 126634 29441866
Full blood count abnormal 51.02 20.73 34 5993 14979 29553521
Rhinitis 50.74 20.73 23 6004 4755 29563745
Sputum discoloured 49.59 20.73 25 6002 6538 29561962
Seasonal allergy 46.22 20.73 22 6005 5080 29563420
Ocular discomfort 41.98 20.73 15 6012 1674 29566826
Middle insomnia 40.96 20.73 21 6006 5687 29562813
Stress 40.13 20.73 34 5993 21456 29547044
Dyspnoea 39.00 20.73 150 5877 326582 29241918
Eye pruritus 37.18 20.73 18 6009 4314 29564186
Chest discomfort 36.67 20.73 46 5981 45937 29522563
Anosmia 36.00 20.73 14 6013 1977 29566523
Nasal oedema 35.94 20.73 9 6018 293 29568207
Forced expiratory volume decreased 34.56 20.73 15 6012 2798 29565702
Loss of personal independence in daily activities 33.33 20.73 33 5994 25407 29543093
Cardiogenic shock 33.07 20.73 29 5998 19161 29549339
Productive cough 32.79 20.73 36 5991 31223 29537277
Pharyngeal paraesthesia 32.18 20.73 9 6018 451 29568049
SARS-CoV-2 sepsis 32.07 20.73 7 6020 123 29568377
Glaucoma 32.06 20.73 18 6009 5839 29562661
Central obesity 31.80 20.73 9 6018 471 29568029
Victim of child abuse 30.80 20.73 10 6017 835 29567665
Eczema 30.27 20.73 24 6003 13802 29554698
Nasal disorder 29.10 20.73 11 6016 1438 29567062
Dermatitis atopic 27.81 20.73 12 6015 2207 29566293
Dermatitis allergic 27.18 20.73 16 6011 5672 29562828
Polyp 26.70 20.73 13 6014 3152 29565348
Nasal septum deviation 25.67 20.73 9 6018 950 29567550
Gastroenteritis eosinophilic 25.22 20.73 6 6021 157 29568343
Eosinophilic pneumonia chronic 25.07 20.73 6 6021 161 29568339
Ocular hyperaemia 24.74 20.73 18 6009 9109 29559391
Lung diffusion disorder 23.23 20.73 5 6022 82 29568418
Cortisol decreased 23.02 20.73 8 6019 823 29567677
Faecal calprotectin 22.83 20.73 4 6023 20 29568480
Alpha 2 globulin decreased 22.83 20.73 4 6023 20 29568480
Otosalpingitis 22.83 20.73 4 6023 20 29568480
Sex hormone binding globulin decreased 22.67 20.73 4 6023 21 29568479
Free androgen index decreased 22.67 20.73 4 6023 21 29568479
Androgen insensitivity syndrome 22.51 20.73 4 6023 22 29568478
Viral acanthoma 22.51 20.73 4 6023 22 29568478
Testicular microlithiasis 22.22 20.73 4 6023 24 29568476
Conjunctivitis 22.19 20.73 16 6011 7982 29560518
Dehydroepiandrosterone decreased 22.08 20.73 4 6023 25 29568475
Urine calcium/creatinine ratio increased 22.08 20.73 4 6023 25 29568475
Blood test abnormal 21.92 20.73 14 6013 5735 29562765
Ventricular fibrillation 21.59 20.73 21 6006 15812 29552688
Rhinorrhoea 21.21 20.73 24 6003 21495 29547005
Creatinine urine decreased 20.79 20.73 4 6023 36 29568464

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
Asthma 580.85 16.97 339 16168 94886 64387339
Wheezing 486.20 16.97 285 16222 80294 64401931
Obstructive airways disorder 357.34 16.97 155 16352 23030 64459195
Full blood count abnormal 241.25 16.97 128 16379 29629 64452596
Nasal congestion 229.46 16.97 159 16348 59499 64422726
Therapeutic product effect incomplete 162.09 16.97 164 16343 103318 64378907
Nasal polyps 150.30 16.97 50 16457 3579 64478646
Dyspnoea 144.23 16.97 456 16051 718218 63764007
Cough 138.56 16.97 264 16243 301884 64180341
Sleep disorder due to a general medical condition 133.16 16.97 57 16450 8177 64474048
Chest discomfort 114.96 16.97 145 16362 115961 64366264
Productive cough 112.69 16.97 115 16392 73088 64409137
Bronchial neoplasm 110.03 16.97 25 16482 418 64481807
Nasal turbinate hypertrophy 108.70 16.97 26 16481 549 64481676
Sputum discoloured 106.96 16.97 63 16444 17793 64464432
Rhinitis 106.55 16.97 53 16454 10712 64471513
Gastrooesophageal reflux disease 100.58 16.97 115 16392 83028 64399197
Endometrial ablation 95.31 16.97 25 16482 776 64481449
Rhonchi 90.92 16.97 34 16473 3429 64478796
Bronchial haemorrhage 89.27 16.97 26 16481 1196 64481029
Bronchiectasis 87.62 16.97 51 16456 14089 64468136
Throat clearing 86.94 16.97 26 16481 1312 64480913
Blood test abnormal 81.04 16.97 47 16460 12896 64469329
Hyper IgE syndrome 76.34 16.97 19 16488 476 64481749
Bronchial disorder 75.23 16.97 26 16481 2089 64480136
Total lung capacity increased 74.27 16.97 20 16487 688 64481537
Eczema 71.61 16.97 60 16447 29660 64452565
Blepharospasm 70.29 16.97 28 16479 3347 64478878
Appendicolith 69.54 16.97 28 16479 3441 64478784
Rhinorrhoea 69.22 16.97 81 16426 59888 64422337
Eye pruritus 68.90 16.97 42 16465 12617 64469608
Respiratory tract inflammation 67.53 16.97 19 16488 771 64481454
Restrictive pulmonary disease 66.94 16.97 24 16483 2148 64480077
Malignant mediastinal neoplasm 65.14 16.97 17 16490 517 64481708
Affective disorder 63.94 16.97 32 16475 6548 64475677
Blood immunoglobulin E increased 63.43 16.97 27 16480 3817 64478408
Toxicity to various agents 63.23 16.97 9 16498 363504 64118721
Forced expiratory volume decreased 62.65 16.97 32 16475 6835 64475390
Dust allergy 62.14 16.97 19 16488 1034 64481191
Breath sounds abnormal 61.68 16.97 38 16469 11631 64470594
Stress 58.89 16.97 75 16432 60459 64421766
Seasonal allergy 54.01 16.97 35 16472 11691 64470534
Secretion discharge 53.36 16.97 35 16472 11929 64470296
Taste disorder 53.14 16.97 32 16475 9401 64472824
Asthma-chronic obstructive pulmonary disease overlap syndrome 52.63 16.97 17 16490 1108 64481117
Sleep apnoea syndrome 49.78 16.97 49 16458 29783 64452442
Granuloma 49.39 16.97 27 16480 6614 64475611
Polycystic ovaries 48.81 16.97 19 16488 2136 64480089
Rhinitis allergic 47.05 16.97 28 16479 8050 64474175
Sinusitis 46.33 16.97 110 16397 145818 64336407
Respiratory disorder 45.41 16.97 51 16456 36060 64446165
Dyspnoea exertional 44.72 16.97 73 16434 73657 64408568
Middle insomnia 44.06 16.97 32 16475 12845 64469380
Lung hyperinflation 42.95 16.97 16 16491 1596 64480629
Lactose intolerance 42.94 16.97 17 16490 1999 64480226
Death 39.79 16.97 39 16468 482666 63999559
Migraine 39.29 16.97 63 16444 62614 64419611
Bronchitis 38.96 16.97 86 16421 108657 64373568
Chronic obstructive pulmonary disease 38.64 16.97 67 16440 70981 64411244
Anosmia 38.60 16.97 20 16487 4397 64477828
Nasal obstruction 38.09 16.97 14 16493 1345 64480880
Blood pressure diastolic increased 37.43 16.97 27 16480 10725 64471500
Chronic sinusitis 37.15 16.97 22 16485 6270 64475955
Loss of personal independence in daily activities 36.40 16.97 66 16441 72388 64409837
Lower respiratory tract infection 36.38 16.97 77 16430 94537 64387688
Polyp 35.95 16.97 22 16485 6651 64475574
Appendicitis 33.94 16.97 28 16479 13541 64468684
Swelling face 33.75 16.97 57 16450 59109 64423116
Herpes zoster 33.45 16.97 67 16440 79120 64403105
Sarcoidosis 32.44 16.97 20 16487 6126 64476099
Ligament pain 32.35 16.97 8 16499 195 64482030
Eosinophilic pneumonia chronic 32.21 16.97 9 16498 356 64481869
Anaemia 31.87 16.97 30 16477 378650 64103575
Thrombocytopenia 31.69 16.97 9 16498 223792 64258433
Cardiac murmur 31.32 16.97 25 16482 11538 64470687
Blood pressure diastolic abnormal 30.66 16.97 25 16482 11892 64470333
Nasal oedema 30.54 16.97 11 16496 997 64481228
Haemoptysis 30.33 16.97 49 16458 48999 64433226
SARS-CoV-2 sepsis 30.32 16.97 7 16500 126 64482099
Sneezing 29.14 16.97 27 16480 15224 64467001
Ear pruritus 29.02 16.97 14 16493 2646 64479579
Victim of child abuse 28.26 16.97 10 16497 861 64481364
Weight decreased 28.23 16.97 146 16361 285593 64196632
Ankle fracture 28.02 16.97 26 16481 14684 64467541
Acute kidney injury 27.91 16.97 45 16462 449195 64033030
Asthmatic crisis 27.87 16.97 12 16495 1744 64480481
Ocular discomfort 26.30 16.97 15 16492 3984 64478241
Oropharyngeal pain 26.06 16.97 65 16442 88802 64393423
Blood pressure systolic increased 26.05 16.97 46 16461 49407 64432818
Atopy 25.55 16.97 7 16500 257 64481968
Neutropenia 25.27 16.97 15 16492 239609 64242616
Dehydration 25.16 16.97 12 16495 216751 64265474
Dyslipidaemia 25.07 16.97 20 16487 9222 64473003
Eosinophilia 24.86 16.97 39 16468 38037 64444188
Epilepsy 24.23 16.97 36 16471 33495 64448730
Cardiac arrest 24.14 16.97 5 16502 154059 64328166
Throat irritation 23.46 16.97 35 16472 32676 64449549
Crepitations 23.35 16.97 18 16489 7897 64474328
Haemoglobin decreased 22.33 16.97 11 16496 195052 64287173
Nasal disorder 22.21 16.97 12 16495 2872 64479353
Cortisol decreased 21.92 16.97 10 16497 1667 64480558
Blood pressure systolic abnormal 21.75 16.97 19 16488 9923 64472302
Rales 21.74 16.97 23 16484 15206 64467019
Gastroenteritis eosinophilic 21.70 16.97 6 16501 228 64481997
Platelet count decreased 21.52 16.97 8 16499 167703 64314522
Lung neoplasm malignant 21.52 16.97 27 16480 21421 64460804
Sensitivity to weather change 21.43 16.97 16 16491 6698 64475527
Eosinophil count increased 21.37 16.97 22 16485 14090 64468135
Pertussis 21.33 16.97 8 16499 813 64481412
Paraesthesia 21.10 16.97 79 16428 134443 64347782
Pharyngeal paraesthesia 20.64 16.97 10 16497 1907 64480318
Sinus pain 20.57 16.97 11 16496 2578 64479647
Lung diffusion disorder 20.45 16.97 5 16502 116 64482109
Autism spectrum disorder 20.27 16.97 8 16499 933 64481292
Radioallergosorbent test positive 20.19 16.97 4 16503 33 64482192
Central obesity 20.04 16.97 9 16498 1446 64480779
Influenza 19.66 16.97 66 16441 106465 64375760
Eosinophilic granulomatosis with polyangiitis 19.47 16.97 11 16496 2871 64479354
Gastrointestinal haemorrhage 19.32 16.97 5 16502 132307 64349918
Cardiac failure congestive 18.95 16.97 5 16502 130575 64351650
Eosinophilic bronchitis 18.91 16.97 6 16501 369 64481856
Ocular hyperaemia 18.91 16.97 26 16481 22538 64459687
Respiratory failure 18.58 16.97 9 16498 161174 64321051
Overdose 18.26 16.97 9 16498 159557 64322668
Ovarian cyst 18.19 16.97 18 16489 11000 64471225
Oral pruritus 18.19 16.97 9 16498 1796 64480429
Sinus disorder 18.11 16.97 22 16485 16886 64465339
Febrile neutropenia 18.08 16.97 13 16494 187644 64294581
Asthenia 17.44 16.97 54 16453 427990 64054235
Respiratory tract infection 17.43 16.97 33 16474 37374 64444851
Paraesthesia oral 17.28 16.97 19 16488 13112 64469113
Malignant neoplasm progression 17.00 16.97 4 16503 112867 64369358

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC D07AC17 DERMATOLOGICALS
CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
CORTICOSTEROIDS, PLAIN
Corticosteroids, potent (group III)
ATC R01AD08 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Corticosteroids
ATC R01AD12 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Corticosteroids
ATC R01AD58 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Corticosteroids
ATC R03AK06 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03AK10 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03AK11 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03AL08 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC R03BA05 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
Glucocorticoids
ATC R03BA09 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
Glucocorticoids
FDA MoA N0000175450 Corticosteroid Hormone Receptor Agonists
FDA EPC N0000175576 Corticosteroid
CHEBI has role CHEBI:49167 anti-asthmatic drugs
CHEBI has role CHEBI:50857 anti-allergic drugs
MeSH PA D018926 Anti-Allergic Agents
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D001993 Bronchodilator Agents
MeSH PA D003879 Dermatologic Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D019141 Respiratory System Agents
CHEBI has role CHEBI:50266 Prodrugs

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic obstructive lung disease indication 13645005 DOID:3083
Allergic rhinitis indication 61582004
Chronic bronchitis indication 63480004 DOID:6132
Pulmonary emphysema indication 87433001
Asthma indication 195967001 DOID:2841
Chronic Non-Allergic Rhinitis indication
Mycosis contraindication 3218000 DOID:1564
Ocular hypertension contraindication 4210003 DOID:9282
Epistaxis contraindication 12441001
Measles contraindication 14189004 DOID:8622
Disease caused by parasite contraindication 17322007
Glaucoma contraindication 23986001 DOID:1686
Viral disease contraindication 34014006 DOID:934
Hypercortisolism contraindication 47270006
Perforation of nasal septum contraindication 80142000
Bacterial infectious disease contraindication 87628006
Operation on nose contraindication 88733004
Bilateral cataracts contraindication 95722004
Pulmonary tuberculosis contraindication 154283005 DOID:2957
Ophthalmic herpes simplex contraindication 186542001
Varicella-zoster virus infection contraindication 309465005
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Exposure to varicella contraindication 444453009
Nasal Candidiasis contraindication
Nasal Trauma contraindication
Nasal Septal Ulcers contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.49 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.1MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 May 10, 2013 RX POWDER INHALATION RE44874 March 23, 2023 FOR THE LONG-TERM, ONCE-DAILY MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH COPD, INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA, ALSO TO REDUCE EXACERBATIONS OF COPD IN PATIENTS WITH A HISTORY OF EXACERBATIONS
0.1MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 May 10, 2013 RX POWDER INHALATION RE44874 March 23, 2023 INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.2MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 April 30, 2015 RX POWDER INHALATION RE44874 March 23, 2023 INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION RE44874 March 23, 2023 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION RE44874 March 23, 2023 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA; AND ASTHMA
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 9, 2020 RX POWDER INHALATION RE44874 March 23, 2023 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA; AND ASTHMA
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 8309572 April 27, 2025 METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA TOPICAL APPLICATION
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 9, 2020 RX POWDER INHALATION 8309572 April 27, 2025 METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA TOPICAL APPLICATION
0.1MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 May 10, 2013 RX POWDER INHALATION 7439393 May 21, 2025 INDICATED FOR LONG-TERM, ONCE-DAILY MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PTS WITH COPD, INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA, ALSO TO REDUCE EXACERBATIONS OF COPD IN PTS WITH A HISTORY OF EXACERBATIONS
0.1MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 May 10, 2013 RX POWDER INHALATION 7439393 May 21, 2025 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING BRONCHITIS AND/OR EMPHYSEMA
0.1MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 May 10, 2013 RX POWDER INHALATION 7439393 May 21, 2025 INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.1MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 May 10, 2013 RX POWDER INHALATION 7439393 May 21, 2025 INDICATED FOR THE ONCE-DAILY TREATMENT OF ASTHMA IN PATIENTS 18 YEARS AND OLDER
0.2MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 April 30, 2015 RX POWDER INHALATION 7439393 May 21, 2025 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING BRONCHITIS AND/OR EMPHYSEMA
0.2MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 April 30, 2015 RX POWDER INHALATION 7439393 May 21, 2025 INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.2MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 April 30, 2015 RX POWDER INHALATION 7439393 May 21, 2025 INDICATED FOR THE ONCE-DAILY TREATMENT OF ASTHMA IN PATIENTS 18 YEARS AND OLDER
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 7439393 May 21, 2025 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 7439393 May 21, 2025 MAINTENANCE TREATMENT OF ASTHMA IN PATIENTS 18 YRS AND OLDER, OR CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 9, 2020 RX POWDER INHALATION 7439393 May 21, 2025 MAINTENANCE TREATMENT OF ASTHMA IN PATIENTS 18 YRS AND OLDER, OR CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 8183257 July 27, 2025 METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA INHALATION
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 8183257 July 27, 2025 METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA TOPICAL APPLICATION
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 9, 2020 RX POWDER INHALATION 8183257 July 27, 2025 METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA TOPICAL APPLICATION
0.1MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 May 10, 2013 RX POWDER INHALATION 8511304 June 14, 2027 INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.1MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 May 10, 2013 RX POWDER INHALATION 8511304 June 14, 2027 LONG-TERM, ONCE DAILY MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PTS WITH COPD, INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA, ALSO TO REDUCE EXACERBATIONS OF COPD IN PATIENTS WITH A HISTORY OF EXACERBATIONS
0.2MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 April 30, 2015 RX POWDER INHALATION 8511304 June 14, 2027 INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 8511304 June 14, 2027 METHOD OF DISPENSING A COMBINATION MEDICAMENT PRODUCT FROM CLAIMED DELIVERY DEVICE, FOR EXAMPLE FOR THE TREATMENT OF ASTHMA OR COPD
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 9, 2020 RX POWDER INHALATION 8511304 June 14, 2027 METHOD OF DISPENSING A COMBINATION MEDICAMENT PRODUCT FROM CLAIMED DELIVERY DEVICE, FOR EXAMPLE FOR THE TREATMENT OF ASTHMA OR COPD
0.1MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 May 10, 2013 RX POWDER INHALATION 11116721 Feb. 26, 2029 INDICATED FOR LONG-TERM, ONCE-DAILY MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PTS WITH COPD, INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA, ALSO TO REDUCE EXACERBATIONS OF COPD IN PTS WITH A HISTORY OF EXACERBATIONS
0.1MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 May 10, 2013 RX POWDER INHALATION 11116721 Feb. 26, 2029 INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.2MG/INH;EQ 0.025MG BASE/INH BREO ELLIPTA GLAXO GRP LTD N204275 April 30, 2015 RX POWDER INHALATION 11116721 Feb. 26, 2029 INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 11090294 Nov. 29, 2030 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) COMPRISING THE ONCE PER DAY ADMINISTRATION OF TRELEGY ELLIPTA, 100 MCG FLUTICASONE FUROATE/62.5 MCG UMECLIDINIUM/25 MCG VILANTEROL

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION Sept. 9, 2023 MAINTENANCE TREATMENT OF ASTHMA IN PATIENTS AGED 18 YEARS AND OLDER
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 9, 2020 RX POWDER INHALATION Sept. 9, 2023 NEW STRENGTH

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Glucocorticoid receptor Nuclear hormone receptor AGONIST IC50 10.12 CHEMBL CHEMBL
Mineralocorticoid receptor Nuclear hormone receptor IC50 6.83 CHEMBL
Progesterone receptor Nuclear hormone receptor IC50 7.68 CHEMBL
Androgen receptor Transcription factor IC50 5.73 CHEMBL
Glucocorticoid receptor Transcription factor IC50 8.30 CHEMBL

External reference:

IDSource
D06315 KEGG_DRUG
4026165 VUID
N0000179800 NUI
4020529 VANDF
4026165 VANDF
CHEBI:74899 CHEBI
CHEBI:5134 CHEBI
GW6 PDB_CHEM_ID
CHEMBL1676 ChEMBL_ID
C523187 MESH_SUPPLEMENTAL_RECORD_UI
10892 IUPHAR_LIGAND_ID
6699 IUPHAR_LIGAND_ID
8521 INN_ID
90566-53-3 SECONDARY_CAS_RN
DB08906 DRUGBANK_ID
JS86977WNV UNII
9854489 PUBCHEM_CID
5311101 PUBCHEM_CID
DB13867 DRUGBANK_ID
41126 RXNORM
109674 MMSL
23848 MMSL
51966 MMSL
d01296 MMSL
004952 NDDF
012173 NDDF
108632003 SNOMEDCT_US
397192001 SNOMEDCT_US
426409006 SNOMEDCT_US
C1948374 UMLSCUI
C0082607 UMLSCUI
CHEMBL1201396 ChEMBL_ID
5636 INN_ID
D000068298 MESH_DESCRIPTOR_UI
CUT2W21N7U UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
FLONASE SENSIMISTALLERGY RELIEF HUMAN OTC DRUG LABEL 1 0135-0615 SPRAY, METERED 27.50 ug NASAL NDA 16 sections
FLONASE SENSIMISTALLERGY RELIEF HUMAN OTC DRUG LABEL 1 0135-0616 SPRAY, METERED 27.50 ug NASAL NDA 16 sections
Breo Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 0173-0859 POWDER 100 ug RESPIRATORY (INHALATION) NDA 26 sections
Breo Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 0173-0859 POWDER 100 ug RESPIRATORY (INHALATION) NDA 26 sections
Arnuity Ellipta HUMAN PRESCRIPTION DRUG LABEL 1 0173-0874 POWDER 100 ug RESPIRATORY (INHALATION) NDA 27 sections
Arnuity Ellipta HUMAN PRESCRIPTION DRUG LABEL 1 0173-0876 POWDER 200 ug RESPIRATORY (INHALATION) NDA 27 sections
Breo Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 0173-0882 POWDER 200 ug RESPIRATORY (INHALATION) NDA 26 sections
Breo Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 0173-0882 POWDER 200 ug RESPIRATORY (INHALATION) NDA 26 sections
Trelegy Ellipta HUMAN PRESCRIPTION DRUG LABEL 3 0173-0887 POWDER 100 ug RESPIRATORY (INHALATION) NDA 27 sections
Trelegy Ellipta HUMAN PRESCRIPTION DRUG LABEL 3 0173-0887 POWDER 100 ug RESPIRATORY (INHALATION) NDA 27 sections
Arnuity Ellipta HUMAN PRESCRIPTION DRUG LABEL 1 0173-0888 POWDER 50 ug RESPIRATORY (INHALATION) NDA 27 sections
Trelegy Ellipta HUMAN PRESCRIPTION DRUG LABEL 3 0173-0893 POWDER 200 ug RESPIRATORY (INHALATION) NDA 27 sections
Trelegy Ellipta HUMAN PRESCRIPTION DRUG LABEL 3 0173-0893 POWDER 200 ug RESPIRATORY (INHALATION) NDA 27 sections
FLONASE SENSIMISTALLERGY RELIEF HUMAN OTC DRUG LABEL 1 50090-5967 SPRAY, METERED 27.50 ug NASAL NDA 17 sections
Veramyst HUMAN PRESCRIPTION DRUG LABEL 1 54868-6168 SPRAY, METERED 27.50 ug NASAL NDA 27 sections
Fluticasone Furoate and Vilanterol HUMAN PRESCRIPTION DRUG LABEL 2 66993-135 POWDER 100 ug RESPIRATORY (INHALATION) NDA authorized generic 26 sections
Fluticasone Furoate and Vilanterol HUMAN PRESCRIPTION DRUG LABEL 2 66993-136 POWDER 200 ug RESPIRATORY (INHALATION) NDA authorized generic 26 sections
Breo Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 70518-2028 POWDER 100 ug RESPIRATORY (INHALATION) NDA 27 sections
Breo Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 70518-2028 POWDER 100 ug RESPIRATORY (INHALATION) NDA 27 sections