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

Stem definitionDrug idCAS RN
pituitary hormone-release stimulating peptides 1559 53714-56-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • leuprorelin
  • leuprolide acetate
  • eligard
  • leupline
  • leuprolide
  • leuprorelin acetate
  • leuprorelin mesilate
A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE that regulates the synthesis and release of pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE.
  • Molecular weight: 1209.42
  • Formula: C59H84N16O12
  • CLOGP: -3.18
  • LIPINSKI: 3
  • HAC: 28
  • HDO: 16
  • TPSA: 429.04
  • ALOGS: -4.55
  • ROTB: 32

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
60 mcg implant
1 mg P
0.13 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 250 mg/mL 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) 0.01 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 0.38 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.54 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.90 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
May 24, 2022 EMA ACCORD HEALTHCARE S.L.U.
April 9, 1985 FDA

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
Intercepted product preparation error 757.83 17.04 127 13132 384 56278424
Hot flush 712.45 17.04 302 12957 46424 56232384
Syringe issue 635.28 17.04 141 13118 2315 56276493
Endometriosis 588.23 17.04 150 13109 4552 56274256
Occupational exposure to product 413.83 17.04 96 13163 1934 56276874
Pelvic pain 391.90 17.04 135 13124 11732 56267076
Device leakage 368.59 17.04 111 13148 6264 56272544
Ovarian hyperstimulation syndrome 338.74 17.04 92 13167 3572 56275236
Vaginal haemorrhage 272.39 17.04 129 13130 25544 56253264
Off label use 213.10 17.04 428 12831 555752 55723056
Heavy menstrual bleeding 204.87 17.04 92 13167 16117 56262691
Uterine leiomyoma 182.26 17.04 70 13189 8272 56270536
Abscess sterile 173.21 17.04 26 13233 26 56278782
Injury associated with device 166.93 17.04 52 13207 3281 56275527
Injection site abscess 157.36 17.04 39 13220 1047 56277761
Hysterectomy 142.14 17.04 59 13200 8532 56270276
Mood swings 118.42 17.04 64 13195 16683 56262125
Wrong technique in product usage process 108.79 17.04 98 13161 58070 56220738
Intermenstrual bleeding 102.06 17.04 44 13215 6983 56271825
Oestradiol increased 82.81 17.04 15 13244 79 56278729
Menstrual disorder 76.96 17.04 32 13227 4643 56274165
Injection site abscess sterile 76.11 17.04 11 13248 6 56278802
Ovarian cyst 76.04 17.04 46 13213 14820 56263988
Dysmenorrhoea 71.67 17.04 28 13231 3458 56275350
Uterine haemorrhage 71.25 17.04 28 13231 3512 56275296
Rheumatoid arthritis 70.93 17.04 5 13254 382599 55896209
Epiphysiolysis 68.49 17.04 11 13248 23 56278785
Haemorrhage 66.52 17.04 74 13185 56323 56222485
Injection site pain 65.87 17.04 107 13152 117011 56161797
Surgery 57.30 17.04 53 13206 32433 56246375
Depression 52.76 17.04 125 13134 179992 56098816
Anger 51.80 17.04 33 13226 11639 56267169
Amenorrhoea 51.69 17.04 30 13229 8956 56269852
Night sweats 50.18 17.04 55 13204 41158 56237650
Abdominal pain 49.08 17.04 153 13106 258652 56020156
Endometrial stromal sarcoma 48.00 17.04 8 13251 23 56278785
Breast cancer metastatic 47.86 17.04 35 13224 15434 56263374
Focal nodular hyperplasia 47.75 17.04 13 13246 508 56278300
Suicidal ideation 47.27 17.04 63 13196 57679 56221129
Vulvovaginal dryness 44.41 17.04 18 13241 2447 56276361
Fall 43.51 17.04 15 13244 357495 55921313
Joint swelling 41.16 17.04 9 13250 289791 55989017
Product dispensing error 40.63 17.04 26 13233 9238 56269570
Migraine 40.46 17.04 73 13186 86724 56192084
Aplastic anaemia 39.01 17.04 25 13234 8903 56269905
Blood luteinising hormone increased 37.96 17.04 8 13251 101 56278707
Infusion related reaction 37.90 17.04 3 13256 208928 56069880
Adnexa uteri pain 36.85 17.04 10 13249 386 56278422
Hepatic cytolysis 36.77 17.04 26 13233 10880 56267928
Pneumonia 36.14 17.04 26 13233 407072 55871736
Ovarian cyst ruptured 34.89 17.04 12 13247 1033 56277775
Injection site mass 34.76 17.04 30 13229 16763 56262045
Neoplasm progression 34.32 17.04 40 13219 31976 56246832
Neuroendocrine breast tumour 33.38 17.04 6 13253 30 56278778
Blood follicle stimulating hormone abnormal 33.31 17.04 5 13254 5 56278803
Adnexal torsion 32.45 17.04 9 13250 377 56278431
Maternal exposure before pregnancy 32.05 17.04 20 13239 6803 56272005
Metastases to liver 31.98 17.04 32 13227 21554 56257254
Toxicity to various agents 31.82 17.04 7 13252 224557 56054251
Headache 31.46 17.04 232 13027 558812 55719996
Product leakage 31.26 17.04 10 13249 687 56278121
Menstruation irregular 30.68 17.04 19 13240 6377 56272431
Depressed mood 30.25 17.04 40 13219 36319 56242489
Insomnia 29.70 17.04 106 13153 191754 56087054
Dyspareunia 29.08 17.04 13 13246 2247 56276561
Product physical consistency issue 28.94 17.04 9 13250 564 56278244
Abdominal discomfort 28.34 17.04 15 13244 277259 56001549
Dental fistula 28.24 17.04 9 13250 611 56278197
Breast enlargement 27.46 17.04 11 13248 1450 56277358
Precocious puberty 27.30 17.04 7 13252 216 56278592
Leiomyosarcoma recurrent 26.64 17.04 4 13255 4 56278804
Blood luteinising hormone decreased 26.51 17.04 5 13254 34 56278774
Prosopagnosia 26.38 17.04 5 13254 35 56278773
Adhesion 25.83 17.04 10 13249 1205 56277603
Uterine adhesions 25.27 17.04 5 13254 45 56278763
Vision blurred 24.71 17.04 58 13201 82885 56195923
Drug intolerance 24.69 17.04 16 13243 264802 56014006
Genital haemorrhage 24.63 17.04 17 13242 6845 56271963
Calcium deficiency 23.88 17.04 9 13250 1008 56277800
Injection site induration 23.33 17.04 18 13241 8597 56270211
Myomectomy 22.98 17.04 4 13255 16 56278792
Sinusitis 22.80 17.04 9 13250 197572 56081236
Wound 22.56 17.04 3 13256 138801 56140007
Laparoscopy 22.45 17.04 5 13254 83 56278725
Hypotension 22.19 17.04 16 13243 250492 56028316
Blood oestrogen increased 22.18 17.04 5 13254 88 56278720
Bone pain 21.85 17.04 41 13218 50144 56228664
Injection site erythema 21.82 17.04 53 13206 77395 56201413
Urinary tract infection 21.78 17.04 15 13244 240498 56038310
Infection 21.70 17.04 10 13249 200196 56078612
Idiopathic intracranial hypertension 21.57 17.04 11 13248 2543 56276265
Oophorectomy 21.38 17.04 7 13252 518 56278290
Nasopharyngitis 21.07 17.04 13 13246 220946 56057862
Intercepted product administration error 20.67 17.04 5 13254 121 56278687
Expired product administered 20.39 17.04 14 13245 5588 56273220
Amnesia 20.36 17.04 38 13221 46284 56232524
Wrong product administered 20.23 17.04 14 13245 5658 56273150
Drug hypersensitivity 20.23 17.04 21 13238 275184 56003624
Confusional state 20.19 17.04 12 13247 208143 56070665
Blood follicle stimulating hormone increased 19.54 17.04 5 13254 153 56278655
Ovarian disorder 19.48 17.04 7 13252 686 56278122
Autoimmune dermatitis 19.41 17.04 4 13255 45 56278763
Completed suicide 19.29 17.04 4 13255 133829 56144979
Libido decreased 19.27 17.04 10 13249 2398 56276410
Product administration error 18.93 17.04 24 13235 20905 56257903
Arthropathy 18.79 17.04 12 13247 200263 56078545
Haematocolpos 18.66 17.04 4 13255 55 56278753
Mood altered 18.33 17.04 19 13240 13336 56265472
Malignant neoplasm progression 18.26 17.04 48 13211 73539 56205269
Diarrhoea 18.23 17.04 83 13176 638424 55640384
Oestrogen receptor assay positive 18.02 17.04 6 13253 468 56278340
Inner ear disorder 17.98 17.04 6 13253 471 56278337
Blood oestrogen abnormal 17.91 17.04 3 13256 9 56278799
Placenta accreta 17.90 17.04 5 13254 215 56278593
Abdominal distension 17.62 17.04 49 13210 77577 56201231
Pelvic venous thrombosis 17.57 17.04 8 13251 1443 56277365
Uterine pain 17.33 17.04 5 13254 242 56278566
Blood oestrogen decreased 17.29 17.04 5 13254 244 56278564
Menopausal symptoms 17.27 17.04 9 13250 2176 56276632
Ovarian adhesion 17.24 17.04 3 13256 12 56278796
Device issue 17.22 17.04 23 13236 21083 56257725
Metastases to bone 17.06 17.04 22 13237 19486 56259322

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
Intercepted product preparation error 15063.90 14.24 2838 50476 326 31643704
Syringe issue 13638.51 14.24 2802 50512 2054 31641976
Device leakage 9684.30 14.24 2156 51158 3257 31640773
Wrong technique in product usage process 4867.46 14.24 1896 51418 31447 31612583
Prostatic specific antigen increased 2365.62 14.24 880 52434 12658 31631372
Hot flush 2282.33 14.24 900 52414 15296 31628734
Product physical consistency issue 1761.04 14.24 349 52965 145 31643885
Prostate cancer 1360.06 14.24 824 52490 36777 31607253
Prostate cancer metastatic 884.40 14.24 345 52969 5659 31638371
Intercepted medication error 832.82 14.24 188 53126 305 31643725
Death 797.26 14.24 1817 51497 358752 31285278
Blood testosterone abnormal 739.62 14.24 161 53153 197 31643833
Blood testosterone increased 672.28 14.24 184 53130 870 31643160
Intercepted product administration error 522.59 14.24 104 53210 46 31643984
Needle issue 476.51 14.24 214 53100 5059 31638971
Metastases to bone 446.89 14.24 259 53055 10589 31633441
Product leakage 396.57 14.24 102 53212 359 31643671
Prostatic specific antigen abnormal 390.39 14.24 102 53212 388 31643642
Osteonecrosis of jaw 335.48 14.24 257 53057 16814 31627216
Hormone-refractory prostate cancer 289.23 14.24 108 53206 1559 31642471
Product preparation error 282.88 14.24 109 53205 1723 31642307
Product administration error 259.65 14.24 211 53103 15036 31628994
Malignant neoplasm progression 235.21 14.24 452 52862 78546 31565484
Injection site pain 232.62 14.24 289 53025 34345 31609685
Terminal state 220.99 14.24 113 53201 3585 31640445
Toxicity to various agents 206.37 14.24 30 53284 181457 31462573
Injection site mass 167.66 14.24 111 53203 5753 31638277
Marasmus 161.13 14.24 52 53262 470 31643560
Prostate cancer recurrent 158.93 14.24 60 53254 894 31643136
Fatigue 151.09 14.24 1021 52293 334185 31309845
Incorrect route of product administration 148.92 14.24 137 53177 11536 31632494
Intercepted product storage error 135.13 14.24 37 53277 175 31643855
Circumstance or information capable of leading to medication error 125.78 14.24 59 53255 1544 31642486
Injection site induration 119.15 14.24 67 53247 2580 31641450
Completed suicide 106.54 14.24 14 53300 91500 31552530
Acute kidney injury 104.44 14.24 195 53119 279519 31364511
Injection site haemorrhage 97.61 14.24 97 53217 8988 31635042
Metastases to lymph nodes 96.63 14.24 70 53244 4198 31639832
Palliative care 93.10 14.24 34 53280 459 31643571
Injection site granuloma 92.61 14.24 18 53296 5 31644025
Drug interaction 86.34 14.24 136 53178 208407 31435623
Underdose 84.24 14.24 105 53209 12502 31631528
Diarrhoea 83.87 14.24 308 53006 352101 31291929
Pyrexia 81.51 14.24 252 53062 303588 31340442
Hydronephrosis 79.23 14.24 88 53226 9273 31634757
Injection site abscess 79.01 14.24 34 53280 722 31643308
Hypotension 76.84 14.24 142 53172 204476 31439554
Overdose 74.04 14.24 25 53289 84639 31559391
Bulbospinal muscular atrophy congenital 72.61 14.24 15 53299 11 31644019
Extra dose administered 70.75 14.24 53 53261 3347 31640683
Injection site necrosis 70.47 14.24 26 53288 362 31643668
Device connection issue 69.59 14.24 25 53289 321 31643709
Expired product administered 68.83 14.24 50 53264 3011 31641019
Pelvic mass 68.55 14.24 22 53292 195 31643835
Victim of child abuse 66.76 14.24 32 53282 880 31643150
Cough 65.72 14.24 78 53236 134736 31509294
Drug hypersensitivity 62.50 14.24 22 53292 72577 31571453
Injection site nodule 61.91 14.24 36 53278 1478 31642552
Bone pain 61.51 14.24 114 53200 19237 31624793
Neutropenia 61.45 14.24 88 53226 140276 31503754
Occupational exposure to product 60.83 14.24 23 53291 344 31643686
Product reconstitution quality issue 60.04 14.24 17 53297 93 31643937
Fall 57.89 14.24 521 52793 185568 31458462
Psoriasis 57.20 14.24 6 53308 46713 31597317
Injection site ulcer 57.05 14.24 20 53294 238 31643792
Vomiting 54.96 14.24 193 53121 223780 31420250
Intentional dose omission 54.60 14.24 42 53272 2760 31641270
Drug administered in wrong device 54.56 14.24 13 53301 30 31644000
Rheumatoid arthritis 54.00 14.24 8 53306 47801 31596229
Intercepted product prescribing error 53.91 14.24 16 53298 106 31643924
Foetal exposure during pregnancy 53.42 14.24 4 53310 40872 31603158
Cystitis radiation 52.83 14.24 15 53299 83 31643947
Interstitial lung disease 52.07 14.24 223 53091 61180 31582850
Blood creatinine increased 52.02 14.24 44 53270 89034 31554996
Pneumonia 49.88 14.24 345 52969 334967 31309063
Dyspnoea 49.83 14.24 356 52958 343123 31300907
Asthma 48.43 14.24 7 53307 42604 31601426
Suicide attempt 47.68 14.24 4 53310 37244 31606786
Urinary tract toxicity 47.49 14.24 10 53304 9 31644021
Drug abuse 46.92 14.24 47 53267 87711 31556319
Product colour issue 46.46 14.24 20 53294 425 31643605
Infection 45.99 14.24 42 53272 81889 31562141
Radiation proctitis 45.19 14.24 13 53301 76 31643954
Metastasis 45.17 14.24 42 53272 3582 31640448
Blood urea abnormal 44.41 14.24 23 53291 749 31643281
Intercepted product selection error 44.37 14.24 10 53304 16 31644014
White blood cell count decreased 44.26 14.24 49 53265 87349 31556681
Gynaecomastia 44.04 14.24 65 53249 9089 31634941
Metastases to lung 43.72 14.24 62 53252 8360 31635670
Rash 43.36 14.24 183 53131 201303 31442727
Off label use 43.34 14.24 375 52939 346899 31297131
Injection site erythema 43.23 14.24 83 53231 14379 31629651
Condition aggravated 43.15 14.24 137 53177 163872 31480158
Metastatic salivary gland cancer 43.12 14.24 8 53306 0 31644030
Cardiac arrest 42.87 14.24 52 53262 89010 31555020
Agitation 42.37 14.24 19 53295 54150 31589880
Reproductive toxicity 42.28 14.24 9 53305 9 31644021
Product preparation issue 42.13 14.24 17 53297 305 31643725
Renal impairment 42.01 14.24 50 53264 86299 31557731
Angioedema 41.98 14.24 4 53310 33614 31610416
Abdominal pain 41.94 14.24 117 53197 145835 31498195
Febrile neutropenia 41.84 14.24 89 53225 121760 31522270
Seizure 41.26 14.24 65 53249 99703 31544327
Plasma cell myeloma 40.93 14.24 22 53292 56509 31587521
Somnolence 39.99 14.24 66 53248 99379 31544651
Bone lesion 39.84 14.24 35 53279 2772 31641258
Nocturia 39.37 14.24 62 53252 9173 31634857
Nausea 39.08 14.24 331 52983 307616 31336414
Stress urinary incontinence 38.80 14.24 12 53302 93 31643937
Male sexual dysfunction 38.30 14.24 15 53299 248 31643782
Colon cancer stage III 38.00 14.24 14 53300 194 31643836
Sepsis 37.83 14.24 130 53184 151799 31492231
Cancer pain 36.79 14.24 32 53282 2501 31641529
Tachycardia 36.14 14.24 45 53269 76162 31567868
Prostatic specific antigen decreased 36.10 14.24 12 53302 120 31643910
Incorrect dose administered 36.00 14.24 137 53177 35615 31608415
Infusion related reaction 35.83 14.24 18 53296 48037 31595993
Metabolic acidosis 35.79 14.24 11 53303 39566 31604464
Blood electrolytes abnormal 35.45 14.24 21 53293 893 31643137
Injection site swelling 35.33 14.24 62 53252 10025 31634005
Back pain 35.31 14.24 309 53005 109104 31534926
International normalised ratio increased 35.15 14.24 16 53298 45207 31598823
Injection site inflammation 34.77 14.24 19 53295 691 31643339
Coma 34.50 14.24 13 53301 41137 31602893
Malignant transformation 34.49 14.24 20 53294 817 31643213
Pancreatitis 34.09 14.24 9 53305 35762 31608268
C-reactive protein increased 33.69 14.24 20 53294 48630 31595400
Sinusitis 33.55 14.24 10 53304 36686 31607344
Abscess sterile 33.13 14.24 8 53306 20 31644010
Epidural lipomatosis 33.01 14.24 19 53295 765 31643265
Platelet count decreased 32.85 14.24 87 53227 110348 31533682
Urticaria 32.85 14.24 29 53285 57488 31586542
Renal failure 32.43 14.24 103 53211 123227 31520803
Anti-androgen withdrawal syndrome 32.41 14.24 7 53307 8 31644022
Injection site abscess sterile 32.34 14.24 6 53308 0 31644030
Gastrointestinal haemorrhage 32.06 14.24 56 53258 82493 31561537
Pituitary haemorrhage 31.77 14.24 12 53302 179 31643851
Hip fracture 31.55 14.24 62 53252 10924 31633106
Metastases to spine 31.51 14.24 28 53286 2252 31641778
Septic shock 31.44 14.24 39 53275 66119 31577911
Product prescribing error 31.28 14.24 88 53226 19554 31624476
Product dosage form issue 30.91 14.24 8 53306 29 31644001
Asthenia 30.48 14.24 539 52775 224216 31419814
Mucosal inflammation 30.37 14.24 10 53304 34417 31609613
Pruritus 29.87 14.24 109 53205 125058 31518972
Product storage error 29.52 14.24 47 53267 7019 31637011
Blood creatine phosphokinase increased 29.42 14.24 17 53297 41957 31602073
Pollakiuria 29.29 14.24 81 53233 17821 31626209
Bone cancer 29.19 14.24 22 53292 1402 31642628
Haematuria 28.91 14.24 154 53160 46160 31597870
Thrombocytopenia 28.64 14.24 133 53181 142614 31501416
Metastases to soft tissue 28.50 14.24 12 53302 241 31643789
Bone cancer metastatic 28.25 14.24 11 53303 179 31643851
Dementia 27.65 14.24 63 53251 12297 31631733
Foreign body reaction 27.63 14.24 8 53306 48 31643982
Urinary retention 27.43 14.24 121 53193 33604 31610426
Haemoptysis 27.27 14.24 10 53304 32179 31611851
Cardiogenic shock 27.11 14.24 3 53311 22405 31621625
Product packaging quantity issue 27.10 14.24 17 53297 802 31643228
Bradycardia 26.95 14.24 47 53267 69280 31574750
Blood pressure increased 26.62 14.24 59 53255 79574 31564456
Pancytopenia 26.56 14.24 68 53246 87248 31556782
Fracture 26.55 14.24 42 53272 6238 31637792
Chest pain 26.51 14.24 104 53210 116853 31527177
Product quality issue 26.46 14.24 73 53241 16038 31627992
Hypersensitivity 26.33 14.24 33 53281 55710 31588320
Tremor 26.06 14.24 56 53258 76364 31567666
Drug reaction with eosinophilia and systemic symptoms 25.99 14.24 9 53305 30009 31614021
Chest discomfort 25.73 14.24 27 53287 49342 31594688
Intercepted product dispensing error 25.65 14.24 8 53306 64 31643966
Oxygen saturation decreased 25.45 14.24 27 53287 49088 31594942
Induration 25.36 14.24 17 53297 899 31643131
Urinary tract obstruction 24.95 14.24 30 53284 3441 31640589
Injection site discomfort 24.93 14.24 20 53294 1397 31642633
Product dispensing error 24.79 14.24 39 53275 5765 31638265
Femur fracture 24.71 14.24 45 53269 7488 31636542
Hyperkalaemia 24.67 14.24 44 53270 64307 31579723
Intentional product use issue 24.60 14.24 28 53286 49319 31594711
Macroenzyme creatine kinase 24.57 14.24 6 53308 16 31644014
Respiratory distress 24.37 14.24 13 53301 33540 31610490
White blood cell count increased 24.34 14.24 18 53296 38982 31605048
Spinal compression fracture 24.03 14.24 41 53273 6481 31637549
Child abuse 23.98 14.24 12 53302 363 31643667
Respiratory failure 23.77 14.24 89 53225 101360 31542670
Drug level increased 23.68 14.24 3 53311 20183 31623847
Bladder neck obstruction 23.60 14.24 9 53305 138 31643892
Leukopenia 23.58 14.24 38 53276 57790 31586240
Nasopharyngitis 23.57 14.24 44 53270 63201 31580829
Neutrophil count decreased 23.48 14.24 26 53288 46368 31597662
Radical prostatectomy 23.25 14.24 7 53307 49 31643981
Agranulocytosis 22.99 14.24 4 53310 21243 31622787
Loss of libido 22.87 14.24 24 53290 2371 31641659
Inappropriate schedule of product administration 22.77 14.24 155 53159 50668 31593362
Respiratory arrest 22.51 14.24 8 53306 26249 31617781
Testicular atrophy 22.42 14.24 13 53301 531 31643499
Liver function test abnormal 22.31 14.24 11 53303 29681 31614349
Product physical issue 22.25 14.24 23 53291 2232 31641798
Hypoglycaemia 22.20 14.24 32 53282 50914 31593116
Hepatic enzyme increased 21.86 14.24 17 53297 35891 31608139
Multiple organ dysfunction syndrome 21.61 14.24 52 53262 68151 31575879
Antiandrogen therapy 21.56 14.24 4 53310 0 31644030
Breast tenderness 21.36 14.24 14 53300 713 31643317
Anxiety 21.23 14.24 80 53234 90953 31553077
Disease progression 21.15 14.24 239 53075 90225 31553805
Aggression 21.05 14.24 19 53295 37272 31606758
Headache 20.78 14.24 203 53111 183449 31460581
Lower respiratory tract infection 20.42 14.24 11 53303 28226 31615804
Injection site infection 20.18 14.24 15 53299 936 31643094
Pancreatitis acute 19.98 14.24 9 53305 25591 31618439
Radiotherapy 19.96 14.24 11 53303 407 31643623
Rib fracture 19.60 14.24 58 53256 13258 31630772
Juvenile idiopathic arthritis 19.54 14.24 19 53295 1714 31642316
Bone density decreased 19.52 14.24 19 53295 1716 31642314
Mental status changes 19.51 14.24 19 53295 35949 31608081
Meningioma 19.42 14.24 17 53297 1340 31642690
Colitis ulcerative 18.96 14.24 4 53310 18525 31625505
Coagulopathy 18.94 14.24 4 53310 18511 31625519
Dysuria 18.88 14.24 86 53228 24208 31619822
Injection site discharge 18.87 14.24 7 53307 99 31643931
Product size issue 18.54 14.24 12 53302 598 31643432
Eosinophilia 18.42 14.24 8 53306 23245 31620785
Product administered at inappropriate site 18.41 14.24 19 53295 1841 31642189
Premature baby 18.28 14.24 4 53310 18062 31625968
Lymphocyte count decreased 18.20 14.24 6 53308 20643 31623387
Bronchitis 18.20 14.24 23 53291 38694 31605336
Neuroendocrine carcinoma of prostate 17.90 14.24 4 53310 6 31644024
Hypoxia 17.88 14.24 36 53278 50277 31593753
Eye haematoma 17.88 14.24 6 53308 62 31643968
Abdominal pain upper 17.84 14.24 52 53262 63950 31580080
Encephalopathy 17.79 14.24 17 53297 32457 31611573
Blood pressure fluctuation 17.73 14.24 8 53306 22728 31621302
Small cell carcinoma 17.54 14.24 7 53307 122 31643908
Metastases to breast 17.52 14.24 4 53310 7 31644023
Blood glucose increased 17.49 14.24 49 53265 61034 31582996
Injection site reaction 17.39 14.24 51 53263 11600 31632430
Metastases to liver 17.38 14.24 54 53260 12673 31631357
Haematochezia 17.06 14.24 26 53288 40438 31603592
Therapy non-responder 17.05 14.24 19 53295 33792 31610238
Transitional cell carcinoma 16.81 14.24 19 53295 2040 31641990
Lipid metabolism disorder 16.78 14.24 9 53305 315 31643715
Product use in unapproved indication 16.73 14.24 98 53216 99073 31544957
Muscular weakness 16.71 14.24 176 53138 65272 31578758
Traumatic fracture 16.68 14.24 9 53305 319 31643711
Ascites 16.67 14.24 27 53287 40986 31603044
Respiratory depression 16.62 14.24 58 53256 14452 31629578
Pituitary apoplexy 16.37 14.24 5 53309 37 31643993
Diabetes mellitus 16.30 14.24 125 53189 42431 31601599
Urethral intrinsic sphincter deficiency 16.29 14.24 4 53310 11 31644019
Injection site extravasation 16.26 14.24 21 53293 2589 31641441
Product availability issue 16.25 14.24 16 53298 1465 31642565
Anaplastic meningioma 16.17 14.24 3 53311 0 31644030
Blood testosterone normal 16.17 14.24 3 53311 0 31644030
Prostatic specific antigen 16.17 14.24 3 53311 0 31644030
Metastases to penis 16.17 14.24 3 53311 0 31644030
Shock 16.11 14.24 9 53305 22636 31621394
Pelvic pain 16.06 14.24 19 53295 2142 31641888
Erythema 16.06 14.24 75 53239 80330 31563700
Lactic acidosis 16.05 14.24 18 53296 31919 31612111
Metastases to spinal cord 16.03 14.24 4 53310 12 31644018
Stomatitis 16.00 14.24 26 53288 39412 31604618
Haemorrhage 15.87 14.24 35 53279 47299 31596731
Urine flow decreased 15.83 14.24 14 53300 1119 31642911
Ectopic ACTH syndrome 15.79 14.24 4 53310 13 31644017
Vipoma 15.79 14.24 4 53310 13 31644017
Psychotic disorder 15.66 14.24 9 53305 22284 31621746
Neurotoxicity 15.62 14.24 4 53310 16222 31627808
Anaphylactic reaction 15.58 14.24 16 53298 29537 31614493
Therapeutic response decreased 15.57 14.24 13 53301 26496 31617534
Eye colour change 15.46 14.24 8 53306 260 31643770
Heart rate decreased 15.25 14.24 15 53299 28251 31615779
Skin exfoliation 14.92 14.24 11 53303 23863 31620167
Hypervolaemia 14.91 14.24 6 53308 18245 31625785
Erectile dysfunction 14.88 14.24 68 53246 19167 31624863
Second primary malignancy 14.81 14.24 35 53279 6997 31637033
Diabetic ketoacidosis 14.75 14.24 5 53309 16900 31627130
Blood testosterone decreased 14.62 14.24 26 53288 4247 31639783
Staphylococcal infection 14.60 14.24 18 53296 30614 31613416
Wrong device used 14.59 14.24 4 53310 19 31644011
Bone marrow tumour cell infiltration 14.59 14.24 4 53310 19 31644011
Product use issue 14.48 14.24 48 53266 56711 31587319
Joint swelling 14.47 14.24 44 53270 53387 31590643
Enzyme induction 14.46 14.24 5 53309 57 31643973
Culture positive 14.42 14.24 11 53303 714 31643316
Tumour lysis syndrome 14.41 14.24 4 53310 15381 31628649
Urethral obstruction 14.38 14.24 5 53309 58 31643972
Wheezing 14.34 14.24 24 53290 35962 31608068
Pleural effusion 14.31 14.24 71 53243 74849 31569181

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
Intercepted product preparation error 12103.15 13.03 2008 46867 634 70878935
Syringe issue 10652.02 13.03 2001 46874 3327 70876242
Device leakage 7119.40 13.03 1574 47301 7734 70871835
Wrong technique in product usage process 3174.07 13.03 1331 47544 67367 70812202
Prostatic specific antigen increased 2296.60 13.03 638 48237 8828 70870741
Hot flush 1495.21 13.03 714 48161 48870 70830699
Product physical consistency issue 1317.71 13.03 250 48625 439 70879130
Prostate cancer 1170.87 13.03 523 48352 30640 70848929
Intercepted medication error 639.52 13.03 143 48732 734 70878835
Prostate cancer metastatic 576.69 13.03 180 48695 3789 70875780
Blood testosterone abnormal 561.58 13.03 101 48774 107 70879462
Blood testosterone increased 519.99 13.03 120 48755 726 70878843
Death 441.33 13.03 1037 47838 509024 70370545
Intercepted product administration error 394.68 13.03 76 48799 150 70879419
Metastases to bone 323.19 13.03 198 48677 22178 70857391
Prostatic specific antigen abnormal 305.37 13.03 63 48812 202 70879367
Needle issue 303.67 13.03 149 48726 10766 70868803
Osteonecrosis of jaw 300.03 13.03 239 48636 40763 70838806
Endometriosis 256.27 13.03 93 48782 3143 70876426
Product leakage 251.99 13.03 66 48809 715 70878854
Malignant neoplasm progression 234.58 13.03 350 48525 121389 70758180
Hormone-refractory prostate cancer 221.96 13.03 63 48812 941 70878628
Prostate cancer recurrent 195.57 13.03 54 48821 725 70878844
Pelvic pain 168.70 13.03 103 48772 11457 70868112
Toxicity to various agents 166.58 13.03 31 48844 382141 70497428
Rheumatoid arthritis 161.44 13.03 10 48865 291795 70587774
Injection site abscess 154.68 13.03 52 48823 1394 70878175
Occupational exposure to product 142.97 13.03 42 48833 713 70878856
Injection site pain 137.54 13.03 271 48604 117348 70762221
Ovarian hyperstimulation syndrome 133.19 13.03 58 48817 3182 70876387
Product preparation error 129.83 13.03 63 48812 4439 70875130
Product administration error 124.22 13.03 126 48749 29397 70850172
Abscess sterile 117.62 13.03 23 48852 51 70879518
Intercepted product storage error 106.00 13.03 26 48849 211 70879358
Completed suicide 104.23 13.03 16 48859 227119 70652450
Injection site mass 101.34 13.03 91 48784 18252 70861317
Victim of child abuse 93.53 13.03 32 48843 906 70878663
Vaginal haemorrhage 93.26 13.03 91 48784 20261 70859308
Hydronephrosis 92.98 13.03 80 48795 15162 70864407
Drug hypersensitivity 91.94 13.03 33 48842 262426 70617143
Injection site granuloma 90.54 13.03 18 48857 45 70879524
Infusion related reaction 77.90 13.03 20 48855 197514 70682055
Bulbospinal muscular atrophy congenital 77.75 13.03 14 48861 15 70879554
Incorrect route of product administration 76.73 13.03 93 48782 26399 70853170
Joint swelling 74.29 13.03 41 48834 253170 70626399
Sinusitis 73.02 13.03 14 48861 169181 70710388
Injection site haemorrhage 72.94 13.03 89 48786 25438 70854131
Injection site induration 70.36 13.03 55 48820 9113 70870456
Fatigue 69.45 13.03 869 48006 823450 70056119
Marasmus 67.30 13.03 25 48850 903 70878666
Cough 66.21 13.03 76 48799 325301 70554268
Terminal state 64.18 13.03 40 48835 4612 70874957
Nasopharyngitis 63.70 13.03 37 48838 222169 70657400
Circumstance or information capable of leading to medication error 62.89 13.03 36 48839 3554 70876015
Injection site abscess sterile 62.52 13.03 11 48864 9 70879560
Cystitis radiation 61.45 13.03 15 48860 119 70879450
Extra dose administered 60.98 13.03 46 48829 7231 70872338
Infection 60.56 13.03 35 48840 210750 70668819
Male sexual dysfunction 59.74 13.03 16 48859 190 70879379
Gynaecomastia 59.11 13.03 44 48831 6779 70872790
Uterine leiomyoma 59.06 13.03 41 48834 5666 70873903
Pelvic mass 58.94 13.03 24 48851 1112 70878457
Interstitial lung disease 58.69 13.03 182 48693 104503 70775066
Heavy menstrual bleeding 56.85 13.03 56 48819 12609 70866960
Overdose 55.04 13.03 24 48851 169721 70709848
Hysterectomy 55.01 13.03 39 48836 5573 70873996
Haematuria 54.21 13.03 129 48746 63444 70816125
Lower respiratory tract infection 53.37 13.03 7 48868 111906 70767663
Diarrhoea 52.97 13.03 320 48555 783021 70096548
Drug administered in wrong device 52.46 13.03 11 48864 39 70879530
Underdose 51.59 13.03 81 48794 29302 70850267
Metastases to lymph nodes 51.36 13.03 46 48829 9192 70870377
Product reconstitution quality issue 51.26 13.03 14 48861 180 70879389
Drug intolerance 51.21 13.03 48 48827 225639 70653930
Arthropathy 50.61 13.03 20 48855 150037 70729532
Metastatic salivary gland cancer 50.25 13.03 8 48867 0 70879569
Oestradiol increased 49.87 13.03 12 48863 89 70879480
Blood urea abnormal 49.77 13.03 22 48853 1251 70878318
Hepatic enzyme increased 49.64 13.03 23 48852 156967 70722602
Maternal exposure during pregnancy 48.80 13.03 10 48865 115335 70764234
Hypersensitivity 48.57 13.03 52 48823 229760 70649809
Mood swings 47.83 13.03 61 48814 18225 70861344
Rash 47.55 13.03 186 48689 510376 70369193
Wound 47.50 13.03 6 48869 98726 70780843
Condition aggravated 46.37 13.03 146 48729 427489 70452080
Epidural lipomatosis 45.52 13.03 19 48856 938 70878631
Malignant transformation 44.98 13.03 20 48855 1153 70878416
Metastases to liver 44.96 13.03 71 48804 25807 70853762
Systemic lupus erythematosus 44.88 13.03 8 48867 101894 70777675
Metastases to lung 44.72 13.03 56 48819 16428 70863141
Radiation proctitis 44.55 13.03 11 48864 92 70879477
Asthma 44.33 13.03 14 48861 120779 70758790
Epiphysiolysis 44.13 13.03 11 48864 96 70879473
Swelling 44.07 13.03 39 48836 188500 70691069
Hypotension 43.18 13.03 139 48736 404242 70475327
Product prescribing error 42.19 13.03 87 48788 38865 70840704
Therapeutic product effect decreased 42.14 13.03 23 48852 142995 70736574
Disease progression 41.88 13.03 216 48659 156456 70723113
Intentional dose omission 41.46 13.03 36 48839 6905 70872664
Pericarditis 41.11 13.03 5 48870 84700 70794869
Pituitary haemorrhage 40.83 13.03 13 48862 292 70879277
Bone pain 39.99 13.03 100 48775 50722 70828847
Expired product administered 39.80 13.03 34 48841 6379 70873190
Device connection issue 39.71 13.03 17 48858 894 70878675
Intercepted product selection error 39.64 13.03 7 48868 6 70879563
Injection site nodule 39.13 13.03 26 48849 3344 70876225
Anti-androgen withdrawal syndrome 38.64 13.03 7 48868 8 70879561
Bone lesion 38.30 13.03 31 48844 5399 70874170
Urinary tract obstruction 37.88 13.03 28 48847 4269 70875300
Urinary retention 37.87 13.03 100 48775 52420 70827149
Blood testosterone decreased 37.35 13.03 22 48853 2291 70877278
Somnolence 37.05 13.03 57 48818 215549 70664020
Psoriasis 36.85 13.03 11 48864 98422 70781147
Blood luteinising hormone increased 36.74 13.03 11 48864 200 70879369
Blood electrolytes abnormal 36.71 13.03 20 48855 1794 70877775
Dyspnoea 36.59 13.03 347 48528 769713 70109856
Product dosage form issue 36.11 13.03 8 48867 39 70879530
Drug interaction 36.09 13.03 138 48737 381303 70498266
Intentional product use issue 35.86 13.03 19 48856 120123 70759446
Nocturia 35.59 13.03 43 48832 12161 70867408
Metastasis 35.09 13.03 31 48844 6083 70873486
Endometrial stromal sarcoma 35.07 13.03 7 48868 18 70879551
Coma 34.87 13.03 10 48865 91834 70787735
Child abuse 34.38 13.03 12 48863 361 70879208
Injection site ulcer 34.01 13.03 14 48861 667 70878902
Product quality issue 33.97 13.03 69 48806 30492 70849077
Abdominal discomfort 33.86 13.03 60 48815 214598 70664971
Product colour issue 32.98 13.03 14 48861 721 70878848
Vomiting 32.71 13.03 257 48618 592854 70286715
Diabetes mellitus 32.34 13.03 116 48759 71708 70807861
Prostatic specific antigen decreased 32.28 13.03 8 48867 68 70879501
Dysmenorrhoea 32.19 13.03 21 48854 2619 70876950
Injury associated with device 32.02 13.03 22 48853 2990 70876579
Bronchitis 31.53 13.03 21 48854 117222 70762347
Intermenstrual bleeding 30.89 13.03 27 48848 5223 70874346
Menstrual disorder 30.79 13.03 23 48852 3563 70876006
Focal nodular hyperplasia 30.51 13.03 13 48862 676 70878893
Erectile dysfunction 30.47 13.03 42 48833 13520 70866049
Metastases to spine 29.45 13.03 23 48852 3806 70875763
Bladder neck obstruction 29.42 13.03 8 48867 101 70879468
Asthenia 29.23 13.03 460 48415 457206 70422363
Lipid metabolism disorder 28.61 13.03 10 48865 302 70879267
Loss of libido 28.36 13.03 19 48856 2478 70877091
Pyrexia 28.15 13.03 275 48600 606677 70272892
Back pain 28.08 13.03 298 48577 270854 70608715
Intercepted product dispensing error 27.22 13.03 8 48867 136 70879433
Neuroendocrine breast tumour 26.96 13.03 6 48869 30 70879539
Dysuria 26.94 13.03 81 48794 45713 70833856
Nausea 26.73 13.03 420 48455 851668 70027901
Psoriatic arthropathy 26.61 13.03 6 48869 64765 70814804
Meningioma 26.37 13.03 22 48853 3996 70875573
Respiratory depression 26.35 13.03 55 48820 24776 70854793
Incorrect dose administered 26.09 13.03 103 48772 66616 70812953
Pruritus 26.05 13.03 136 48739 345424 70534145
Palliative care 26.05 13.03 12 48863 752 70878817
Acute kidney injury 25.98 13.03 206 48669 474418 70405151
Intercepted product prescribing error 25.50 13.03 9 48866 280 70879289
Pollakiuria 25.44 13.03 65 48810 33396 70846173
Tachycardia 25.28 13.03 44 48831 158502 70721067
Neuroendocrine carcinoma of prostate 25.12 13.03 4 48871 0 70879569
Pituitary apoplexy 25.07 13.03 8 48867 181 70879388
Stomatitis 25.05 13.03 31 48844 128480 70751089
Metabolic acidosis 24.91 13.03 10 48865 74336 70805233
Cancer pain 24.61 13.03 23 48852 4851 70874718
Adnexa uteri pain 24.60 13.03 9 48866 311 70879258
Macroenzyme creatine kinase 24.48 13.03 5 48870 15 70879554
Angioedema 23.94 13.03 8 48867 66602 70812967
International normalised ratio increased 23.75 13.03 13 48862 80713 70798856
Dental fistula 23.70 13.03 10 48865 507 70879062
Foreign body reaction 23.04 13.03 7 48868 134 70879435
Oxygen saturation decreased 22.78 13.03 28 48847 116401 70763168
Metastases to soft tissue 22.54 13.03 9 48866 396 70879173
Leiomyosarcoma recurrent 22.35 13.03 4 48871 4 70879565
Product dispensing error 22.33 13.03 34 48841 11974 70867595
Injection site necrosis 22.14 13.03 13 48862 1346 70878223
Transitional cell carcinoma 22.11 13.03 16 48859 2361 70877208
Discomfort 22.09 13.03 24 48851 105412 70774157
Gastrointestinal disorder 22.09 13.03 24 48851 105403 70774166
Loss of personal independence in daily activities 21.78 13.03 16 48859 84894 70794675
Pancreatitis 21.71 13.03 8 48867 62660 70816909
Suicide attempt 21.70 13.03 14 48861 79496 70800073
Blood pressure fluctuation 21.36 13.03 7 48868 59005 70820564
Prosopagnosia 21.16 13.03 5 48870 34 70879535
Adnexal torsion 21 13.03 8 48867 310 70879259
Blister 20.93 13.03 23 48852 100503 70779066
Night sweats 20.91 13.03 72 48803 43612 70835957
Therapeutic product effect incomplete 20.29 13.03 32 48843 119850 70759719
Renal impairment 20.28 13.03 43 48832 143894 70735675
Injection site infection 20.07 13.03 14 48861 1950 70877619
Testicular atrophy 20.04 13.03 8 48867 352 70879217
Metastases to spinal cord 19.92 13.03 5 48870 45 70879524
Urine flow decreased 19.62 13.03 11 48864 1043 70878526
Spinal compression fracture 19.57 13.03 37 48838 15516 70864053
Eye haematoma 19.45 13.03 6 48869 121 70879448
Radical prostatectomy 19.35 13.03 4 48871 13 70879556
Prostatic mass 19.35 13.03 4 48871 13 70879556
Breast enlargement 19.34 13.03 12 48863 1372 70878197
Drug dependence 19.18 13.03 63 48812 37258 70842311
Tremor 19.12 13.03 50 48825 155574 70723995
Drug reaction with eosinophilia and systemic symptoms 19.12 13.03 8 48867 58005 70821564
Drug abuse 19.11 13.03 46 48829 147210 70732359
Blood creatinine increased 19.09 13.03 44 48831 142957 70736612
Pneumonia 18.94 13.03 293 48582 595939 70283630
Ill-defined disorder 18.94 13.03 7 48868 54734 70824835
Libido decreased 18.90 13.03 20 48855 4896 70874673
Urethral intrinsic sphincter deficiency 18.90 13.03 4 48871 15 70879554
Anaplastic meningioma 18.84 13.03 3 48872 0 70879569
Blood testosterone normal 18.84 13.03 3 48872 0 70879569
Product packaging quantity issue 18.80 13.03 11 48864 1131 70878438
Vulvovaginal dryness 18.75 13.03 13 48862 1793 70877776
Vipoma 18.70 13.03 4 48871 16 70879553
Lactic acidosis 18.37 13.03 11 48864 65013 70814556
Uterine haemorrhage 18.25 13.03 15 48860 2669 70876900
Prostatic obstruction 18.18 13.03 5 48870 66 70879503
Hypoglycaemia 18.14 13.03 23 48852 94341 70785228
Product size issue 18.04 13.03 9 48866 673 70878896
Therapy non-responder 17.85 13.03 16 48859 76899 70802670
Hospice care 17.82 13.03 25 48850 8180 70871389
Musculoskeletal stiffness 17.75 13.03 48 48827 147712 70731857
Product preparation issue 17.63 13.03 10 48865 970 70878599
Product storage error 17.57 13.03 34 48841 14507 70865062
Pulmonary embolism 17.40 13.03 174 48701 155693 70723876
Ovarian cyst 17.35 13.03 30 48845 11742 70867827
Precocious puberty 17.34 13.03 7 48868 317 70879252
Rib fracture 16.99 13.03 47 48828 25309 70854260
Oropharyngeal pain 16.98 13.03 25 48850 96285 70783284
Injection site inflammation 16.93 13.03 16 48859 3422 70876147
Respiratory arrest 16.89 13.03 8 48867 53925 70825644
Laparoscopy 16.83 13.03 4 48871 28 70879541
Chest discomfort 16.82 13.03 38 48837 124343 70755226
Irritable bowel syndrome 16.77 13.03 7 48868 50843 70828726
Cardiac ventricular scarring 16.77 13.03 3 48872 3 70879566
Arthritis 16.72 13.03 26 48849 97954 70781615
Urticaria 16.70 13.03 57 48818 162992 70716577
Blood pressure increased 16.66 13.03 70 48805 188447 70691122
Inappropriate schedule of product administration 16.64 13.03 129 48746 107426 70772143
Induration 16.62 13.03 12 48863 1764 70877805
Lymphadenopathy 16.47 13.03 72 48803 48719 70830850
Abdominal pain upper 16.43 13.03 73 48802 193529 70686040
Bone cancer metastatic 16.41 13.03 6 48869 207 70879362
Liver function test abnormal 16.37 13.03 11 48864 61135 70818434
Blood follicle stimulating hormone abnormal 16.30 13.03 3 48872 4 70879565
Injection site discomfort 16.21 13.03 18 48857 4651 70874918
Juvenile idiopathic arthritis 16.21 13.03 20 48855 5780 70873789
Prostate cancer stage IV 16.21 13.03 13 48862 2235 70877334
Agranulocytosis 16.02 13.03 4 48871 40294 70839275
Neuroendocrine carcinoma 16.02 13.03 8 48867 600 70878969
Product physical issue 15.89 13.03 16 48859 3698 70875871
Use of accessory respiratory muscles 15.74 13.03 7 48868 404 70879165
Agitation 15.73 13.03 25 48850 93350 70786219
Hypervolaemia 15.68 13.03 4 48871 39702 70839867
Cardiogenic shock 15.66 13.03 3 48872 36304 70843265
Cardiac arrest 15.62 13.03 57 48818 159777 70719792
Septic shock 15.42 13.03 34 48841 112224 70767345
Acute coronary syndrome 15.26 13.03 39 48836 20040 70859529
Stress urinary incontinence 14.93 13.03 11 48864 1669 70877900
Pathological fracture 14.89 13.03 25 48850 9558 70870011
Haematocolpos 14.82 13.03 4 48871 49 70879520
Bone marrow tumour cell infiltration 14.82 13.03 4 48871 49 70879520
Erythema 14.76 13.03 79 48796 199484 70680085
Oophorectomy 14.75 13.03 6 48869 277 70879292
Urethral stenosis 14.60 13.03 9 48866 1018 70878551
Inguinal hernia 14.50 13.03 19 48856 5826 70873743
Respiratory distress 14.41 13.03 10 48865 54640 70824929
Oncologic complication 14.34 13.03 6 48869 298 70879271
Blood cholesterol increased 14.33 13.03 14 48861 64590 70814979
Exposure during pregnancy 14.29 13.03 24 48851 87693 70791876
Autoimmune dermatitis 14.27 13.03 4 48871 57 70879512
Polyneuropathy in malignant disease 14.18 13.03 5 48870 155 70879414
Calcium deficiency 14.18 13.03 8 48867 768 70878801
Culture positive 14.10 13.03 9 48866 1081 70878488
Radiation injury 14.05 13.03 8 48867 782 70878787
Breast cancer male 14.04 13.03 6 48869 314 70879255
Myomectomy 14.02 13.03 3 48872 12 70879557
Alopecia 13.90 13.03 80 48795 198410 70681159
Hip fracture 13.89 13.03 47 48828 28216 70851353
Bone cancer 13.89 13.03 11 48864 1857 70877712
Inner ear disorder 13.78 13.03 7 48868 544 70879025
Drug withdrawal syndrome 13.50 13.03 3 48872 32712 70846857
Clavicle fracture 13.47 13.03 15 48860 3889 70875680
Carcinoid tumour 13.37 13.03 7 48868 579 70878990
Wheezing 13.37 13.03 28 48847 94142 70785427
Hysteroscopy 13.32 13.03 3 48872 16 70879553
Extradural neoplasm 13.32 13.03 3 48872 16 70879553
Injection site swelling 13.30 13.03 62 48813 43095 70836474
Ovarian cyst ruptured 13.30 13.03 8 48867 866 70878703
Traumatic fracture 13.26 13.03 8 48867 870 70878699
Bradycardia 13.15 13.03 43 48832 124572 70754997
Neovascular age-related macular degeneration 13.07 13.03 6 48869 373 70879196

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L02AE02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONES AND RELATED AGENTS
Gonadotropin releasing hormone analogues
ATC L02AE51 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONES AND RELATED AGENTS
Gonadotropin releasing hormone analogues
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:50751 anti-estrogenic drug
CHEBI has role CHEBI:63533 gonadotropin releasing hormone agonists
FDA MoA N0000175654 Gonadotropin Releasing Hormone Receptor Agonists
FDA EPC N0000175655 Gonadotropin Releasing Hormone Receptor Agonist
MeSH PA D000970 Antineoplastic Agents
MeSH PA D018931 Antineoplastic Agents, Hormonal
MeSH PA D005300 Fertility Agents, Female
MeSH PA D012102 Reproductive Control Agents

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

DiseaseRelationSNOMED_IDDOID
Endometriosis indication 129103003
Precocious puberty indication 400179000
Anemia due to Bleeding Uterine Leiomyoma indication
Advanced Prostatic Carcinoma indication
Malignant tumor of ovary off-label use 363443007 DOID:2394
Urinary tract obstruction contraindication 7163005 DOID:5200
Hypercholesterolemia contraindication 13644009
Myocardial infarction contraindication 22298006 DOID:5844
Hypertensive disorder contraindication 38341003 DOID:10763
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Cerebrovascular accident contraindication 230690007
Orchiectomy contraindication 236334001
Pregnancy, function contraindication 289908002
Osteopenia contraindication 312894000
Cardiovascular event risk contraindication 395112001
Breastfeeding (mother) contraindication 413712001
Obesity contraindication 414916001 DOID:9970
Smokes tobacco daily contraindication 449868002
Vertebral Metastases 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 9.65 acidic
pKa2 11.9 acidic
pKa3 12.73 acidic
pKa4 13.09 acidic
pKa5 13.39 acidic
pKa6 13.69 acidic
pKa7 10.75 Basic
pKa8 6.69 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
22.5MG ELIGARD KIT TOLMAR THERAP N021379 July 24, 2002 RX POWDER SUBCUTANEOUS 8470359 Oct. 15, 2023 METHOD OF TREATING CANCER
30MG ELIGARD KIT TOLMAR THERAP N021488 Feb. 13, 2003 RX POWDER SUBCUTANEOUS 8470359 Oct. 15, 2023 METHOD OF TREATING CANCER
45MG ELIGARD KIT TOLMAR THERAP N021731 Dec. 14, 2004 RX POWDER SUBCUTANEOUS 8470359 Oct. 15, 2023 METHOD OF TREATING CANCER
45MG FENSOLVI KIT TOLMAR N213150 May 1, 2020 RX POWDER SUBCUTANEOUS 8470359 Oct. 15, 2023 METHOD OF TREATING PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WITH CENTRAL PRECOCIOUS PUBERTY
45MG/VIAL LUPRON DEPOT ABBVIE ENDOCRINE INC N020517 June 17, 2011 RX INJECTABLE INJECTION 8921326 Feb. 5, 2031 PALLIATIVE TREATMENT OF PROSTATE CANCER

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
45MG FENSOLVI KIT TOLMAR N213150 May 1, 2020 RX POWDER SUBCUTANEOUS May 1, 2023 TREATMENT OF PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WITH CENTRAL PRECOCIOUS PUBERTY (CPP)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Gonadotropin-releasing hormone receptor GPCR AGONIST IC50 9.52 WOMBAT-PK CHEMBL
Gonadotropin-releasing hormone receptor GPCR IC50 9.30 CHEMBL

External reference:

IDSource
4019800 VUID
N0000147889 NUI
D00989 KEGG_DRUG
74381-53-6 SECONDARY_CAS_RN
4018977 VANDF
4019800 VANDF
C0085272 UMLSCUI
CHEBI:6427 CHEBI
CHEMBL1201199 ChEMBL_ID
CHEMBL1200775 ChEMBL_ID
DB00007 DRUGBANK_ID
C493311 MESH_SUPPLEMENTAL_RECORD_UI
1175 IUPHAR_LIGAND_ID
657181 PUBCHEM_CID
203217 RXNORM
11929 MMSL
43716 MMSL
4966 MMSL
8763 MMSL
d01353 MMSL
002675 NDDF
004751 NDDF
008314 NDDF
008315 NDDF
350364005 SNOMEDCT_US
397198002 SNOMEDCT_US
70562007 SNOMEDCT_US
D016729 MESH_DESCRIPTOR_UI
CHEMBL4802223 ChEMBL_ID
5025 INN_ID
37JNS02E7V UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Leuprolide Acetate HUMAN PRESCRIPTION DRUG LABEL 1 0185-7400 INJECTION, SOLUTION 1 mg SUBCUTANEOUS ANDA 25 sections