goserelin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
pituitary hormone-release stimulating peptides 1327 65807-02-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • goserelin
  • Decapeptide I
  • zoladex
  • goserelin acetate
A synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE. Goserelin is used in treatments of malignant NEOPLASMS of the prostate, uterine fibromas, and metastatic breast cancer.
  • Molecular weight: 1269.43
  • Formula: C59H84N18O14
  • CLOGP: -5.05
  • LIPINSKI: 3
  • HAC: 32
  • HDO: 18
  • TPSA: 493.39
  • ALOGS: -4.48
  • ROTB: 33

Drug dosage:

DoseUnitRoute
0.13 mg implant

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 20 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.04 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
Dec. 29, 1989 FDA ASTRAZENECA

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
Malignant neoplasm progression 1144.54 20.25 473 13333 106397 90508244
Metastases to bone 1072.54 20.25 314 13492 25191 90589450
Metastases to liver 874.12 20.25 276 13530 28531 90586110
Neutropenia 602.35 20.25 392 13414 224512 90390129
Metastases to lung 319.62 20.25 112 13694 15879 90598762
Neoplasm progression 249.56 20.25 126 13680 44360 90570281
Breast cancer metastatic 235.08 20.25 88 13718 15044 90599597
Metastases to lymph nodes 230.22 20.25 81 13725 11608 90603033
PIK3CA-activated mutation 181.04 20.25 41 13765 1163 90613478
Tumour marker increased 169.01 20.25 54 13752 5753 90608888
Disease progression 163.31 20.25 157 13649 156458 90458183
Breast cancer 153.73 20.25 98 13708 53663 90560978
Bone lesion 135.94 20.25 47 13759 6390 90608251
Metastases to central nervous system 135.74 20.25 62 13744 17480 90597161
Metastases to skin 133.73 20.25 36 13770 2104 90612537
Hot flush 132.87 20.25 93 13713 59395 90555246
Carbohydrate antigen 15-3 increased 131.26 20.25 35 13771 1972 90612669
Metastases to spine 130.65 20.25 40 13766 3703 90610938
Metastases to pleura 93.83 20.25 27 13779 2017 90612624
Jaundice 92.23 20.25 59 13747 32458 90582183
Abdominal lymphadenopathy 92.23 20.25 23 13783 992 90613649
Metastases to peritoneum 90.30 20.25 31 13775 4124 90610517
Aspartate aminotransferase increased 84.90 20.25 91 13715 102846 90511795
Bone disorder 83.60 20.25 49 13757 23071 90591570
Alanine aminotransferase increased 82.81 20.25 96 13710 118242 90496399
Hepatotoxicity 78.30 20.25 61 13745 45781 90568860
Breast cancer recurrent 78.20 20.25 30 13776 5473 90609168
Neuropathy peripheral 77.80 20.25 100 13706 136870 90477771
Hepatic lesion 77.31 20.25 30 13776 5643 90608998
Lymphadenopathy 76.21 20.25 60 13746 45715 90568926
Metastases to the mediastinum 75.57 20.25 18 13788 639 90614002
Oestradiol decreased 72.95 20.25 13 13793 102 90614539
Breast mass 71.85 20.25 33 13773 9414 90605227
Invasive breast carcinoma 69.18 20.25 18 13788 921 90613720
Metastases to nervous system 68.67 20.25 12 13794 83 90614558
Leukopenia 67.61 20.25 80 13726 100630 90514011
Invasive lobular breast carcinoma 67.55 20.25 18 13788 1011 90613630
Metastases to spinal cord 66.62 20.25 14 13792 277 90614364
White blood cell count decreased 59.75 20.25 98 13708 167011 90447630
Pleural effusion 59.28 20.25 79 13727 111912 90502729
Metastases to adrenals 58.98 20.25 16 13790 962 90613679
Osteonecrosis of jaw 58.18 20.25 48 13758 39055 90575586
Myelosuppression 58.16 20.25 55 13751 53536 90561105
Haematotoxicity 57.34 20.25 31 13775 12504 90602137
Neutrophil count decreased 56.79 20.25 62 13744 71470 90543171
Ascites 55.68 20.25 51 13755 47689 90566952
Invasive ductal breast carcinoma 55.38 20.25 26 13780 7792 90606849
Bone pain 55.00 20.25 57 13749 61926 90552715
Dermatitis 52.53 20.25 36 13770 22184 90592457
Metastases to pelvis 52.07 20.25 13 13793 563 90614078
Blood bilirubin increased 51.79 20.25 47 13759 43423 90571218
Palmar-plantar erythrodysaesthesia syndrome 51.59 20.25 39 13767 27984 90586657
Pneumonitis 51.15 20.25 47 13759 44123 90570518
Drug ineffective 49.23 20.25 85 13721 1384213 89230428
Osteolysis 49.18 20.25 19 13787 3531 90611110
Dilatation intrahepatic duct acquired 48.36 20.25 13 13793 755 90613886
Hormone receptor positive breast cancer 48.14 20.25 13 13793 768 90613873
Menopausal symptoms 48.14 20.25 18 13788 3060 90611581
Gamma-glutamyltransferase increased 47.12 20.25 42 13764 37910 90576731
Pleural neoplasm 45.40 20.25 11 13795 420 90614221
Carcinoid tumour pulmonary 43.35 20.25 11 13795 509 90614132
Spinal pain 43.19 20.25 28 13778 15739 90598902
CYP3A4 polymorphism 43.15 20.25 8 13798 80 90614561
Metastatic neoplasm 40.35 20.25 18 13788 4797 90609844
Metastasis 39.17 20.25 19 13787 6118 90608523
Selenium deficiency 39.05 20.25 7 13799 57 90614584
Ultrasound foetal abnormal 38.73 20.25 8 13798 145 90614496
Mood swings 38.52 20.25 29 13777 20673 90593968
Metastases to ovary 38.33 20.25 10 13796 517 90614124
Blood alkaline phosphatase increased 36.98 20.25 41 13765 48038 90566603
Mucinous breast carcinoma 36.89 20.25 6 13800 25 90614616
Bilirubin conjugated abnormal 36.82 20.25 7 13799 81 90614560
Pulmonary hypoplasia 36.55 20.25 9 13797 368 90614273
Osteonecrosis 36.52 20.25 31 13775 26210 90588431
Arthropathy 36.50 20.25 6 13800 366236 90248405
Adnexa uteri mass 36.31 20.25 10 13796 636 90614005
Osteitis condensans 35.83 20.25 6 13800 31 90614610
Mucosal inflammation 35.75 20.25 44 13762 57581 90557060
Joint swelling 35.73 20.25 16 13790 503284 90111357
Oophorectomy bilateral 34.54 20.25 7 13799 115 90614526
Febrile neutropenia 34.29 20.25 75 13731 158274 90456367
Lymphoedema 34.22 20.25 23 13783 13730 90600911
Drug hypersensitivity 34.09 20.25 14 13792 463595 90151046
Pathological fracture 33.67 20.25 20 13786 9640 90605001
Lymphadenopathy mediastinal 33.64 20.25 14 13792 3153 90611488
Body surface area increased 33.35 20.25 6 13800 50 90614591
Merycism 32.59 20.25 8 13798 323 90614318
Tumour flare 32.46 20.25 9 13797 587 90614054
Endometrial hyperplasia 32.21 20.25 10 13796 969 90613672
Hepatic cytolysis 32.15 20.25 31 13775 30885 90583756
Fibrous histiocytoma 32.11 20.25 9 13797 611 90614030
Oestradiol abnormal 32.09 20.25 6 13800 63 90614578
Therapeutic product effect decreased 31.40 20.25 3 13803 277568 90337073
Pleural disorder 30.83 20.25 9 13797 707 90613934
Oestradiol increased 29.52 20.25 6 13800 100 90614541
Fatigue 29.43 20.25 286 13520 1153737 89460904
Bone marrow infiltration 29.39 20.25 9 13797 833 90613808
Condition aggravated 28.79 20.25 29 13777 595516 90019125
Breast cancer female 28.02 20.25 21 13785 14865 90599776
Arachnoid cyst 27.97 20.25 7 13799 306 90614335
Libido decreased 27.75 20.25 12 13794 2970 90611671
Hydrothorax 27.58 20.25 9 13797 1024 90613617
Gastrointestinal bacterial infection 27.19 20.25 9 13797 1071 90613570
Hypersensitivity 27.10 20.25 18 13788 454659 90159982
Hepatic cyst 26.62 20.25 15 13791 6553 90608088
Osteosclerosis 26.45 20.25 13 13793 4307 90610334
Uterine mass 26.01 20.25 7 13799 408 90614233
Nasopharyngitis 25.81 20.25 15 13791 407089 90207552
Central nervous system lesion 25.49 20.25 18 13788 11628 90603013
Metastases to eye 25.47 20.25 6 13800 203 90614438
Amenorrhoea 25.39 20.25 18 13788 11704 90602937
Pelvic pain 25.27 20.25 20 13786 15337 90599304
Confusional state 24.81 20.25 14 13792 386191 90228450
Cholestasis 24.61 20.25 29 13777 36270 90578371
Skin fragility 24.52 20.25 8 13798 910 90613731
Swelling 24.42 20.25 17 13789 419041 90195600
Metastases to stomach 24.37 20.25 6 13800 245 90614396
Uterine leiomyoma 24.26 20.25 17 13789 10847 90603794
Pericarditis 23.65 20.25 6 13800 270145 90344496
Musculoskeletal chest pain 23.17 20.25 23 13783 23727 90590914
Mobility decreased 23.07 20.25 5 13801 250729 90363912
Lower respiratory tract infection 23.06 20.25 5 13801 250654 90363987
Disturbance in attention 23.04 20.25 32 13774 47077 90567564
Depressed mood 22.91 20.25 33 13773 50189 90564452
Cervical polyp 22.85 20.25 6 13800 318 90614323
Uterine polyp 22.84 20.25 10 13796 2550 90612091
Oligohydramnios 22.75 20.25 14 13792 7187 90607454
Sinusitis 22.67 20.25 12 13794 343076 90271565
Anaemia 22.65 20.25 110 13696 352692 90261949
Hyperbilirubinaemia 22.61 20.25 18 13788 13918 90600723
Vitamin B complex deficiency 22.16 20.25 7 13799 718 90613923
Hepatic cancer 22.12 20.25 12 13794 4869 90609772
Eosinophilic pneumonia 22.07 20.25 10 13796 2763 90611878
Hypotension 22.06 20.25 11 13795 325386 90289255
Blister 21.68 20.25 6 13800 254992 90359649
Paraparesis 21.52 20.25 10 13796 2928 90611713
Wheezing 21.40 20.25 5 13801 238075 90376566
Pruritus 21.25 20.25 31 13775 541494 90073147
Tooth extraction 21.13 20.25 16 13790 11497 90603144
Pneumonia 20.92 20.25 41 13765 638018 89976623
Therapy partial responder 20.87 20.25 21 13785 22022 90592619
Infection 20.69 20.25 15 13791 362079 90252562
HER2 positive breast cancer 20.64 20.25 6 13800 464 90614177
Breast pain 20.29 20.25 15 13791 10403 90604238

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
Prostatic specific antigen increased 366.26 15.90 150 12420 16775 42591990
Osteonecrosis of jaw 284.64 15.90 130 12440 18919 42589846
Metastases to bone 240.04 15.90 107 12463 14702 42594063
Malignant neoplasm progression 220.43 15.90 211 12359 108189 42500576
Prostate cancer metastatic 157.89 15.90 63 12507 6566 42602199
Prostate cancer 147.82 15.90 115 12455 44528 42564237
Central nervous system mass 133.19 15.90 34 12536 817 42607948
Wall motion score index abnormal 133.04 15.90 34 12536 821 42607944
Airway remodelling 131.31 15.90 34 12536 866 42607899
Hot flush 129.01 15.90 81 12489 22270 42586495
Atopy 128.61 15.90 34 12536 941 42607824
Cardiac septal defect 119.61 15.90 32 12538 928 42607837
Eosinophilic myocarditis 117.08 15.90 34 12536 1339 42607426
Microangiopathy 110.27 15.90 34 12536 1648 42607117
Interstitial lung disease 102.68 15.90 121 12449 78341 42530424
Osteonecrosis 100.44 15.90 61 12509 15804 42592961
Eosinophil count decreased 88.68 15.90 35 12535 3541 42605224
Blood immunoglobulin E increased 88.21 15.90 35 12535 3590 42605175
Eosinophilic pneumonia 87.93 15.90 38 12532 4836 42603929
Chronic sinusitis 86.93 15.90 34 12536 3358 42605407
Haematuria 85.49 15.90 95 12475 57704 42551061
Nasal polyps 82.75 15.90 34 12536 3817 42604948
Ventricular hypokinesia 63.89 15.90 34 12536 6850 42601915
Malignant spinal cord compression 61.37 15.90 13 12557 132 42608633
Lacrimation increased 58.90 15.90 39 12531 11719 42597046
Eosinophilic granulomatosis with polyangiitis 56.69 15.90 34 12536 8604 42600161
Osteomyelitis 51.85 15.90 43 12527 18180 42590585
Respiratory symptom 51.23 15.90 35 12535 11071 42597694
Eosinophil count increased 49.84 15.90 34 12536 10729 42598036
Bone pain 47.57 15.90 46 12524 23746 42585019
Nodule 47.41 15.90 35 12535 12499 42596266
Osteitis 46.93 15.90 18 12552 1686 42607079
Hypocalcaemia 45.27 15.90 50 12520 30123 42578642
Tooth extraction 45.11 15.90 25 12545 5455 42603310
Obesity 43.05 15.90 37 12533 16422 42592343
Lymphopenia 38.13 15.90 39 12531 21524 42587241
Blood testosterone increased 37.67 15.90 15 12555 1552 42607213
Death 37.47 15.90 252 12318 470933 42137832
Pain in jaw 36.71 15.90 32 12538 14470 42594295
Pituitary haemorrhage 35.75 15.90 9 12561 204 42608561
Bone disorder 35.72 15.90 23 12547 6590 42602175
Drug ineffective 35.57 15.90 84 12486 630113 41978652
Off label use 35.30 15.90 86 12484 638249 41970516
Exposed bone in jaw 34.03 15.90 14 12556 1575 42607190
Hepatic function abnormal 33.59 15.90 57 12513 51510 42557255
Pituitary tumour benign 32.75 15.90 12 12558 990 42607775
Metastases to liver 31.57 15.90 31 12539 16295 42592470
Metastases to spine 30.83 15.90 16 12554 3061 42605704
Renal disorder 30.32 15.90 40 12530 28940 42579825
Respiratory tract infection 30.15 15.90 38 12532 26284 42582481
Viral infection 29.89 15.90 35 12535 22448 42586317
Contracted bladder 28.02 15.90 5 12565 18 42608747
Bone sequestrum 27.69 15.90 9 12561 518 42608247
PO2 increased 27.26 15.90 9 12561 544 42608221
Toxicity to various agents 27.22 15.90 17 12553 229119 42379646
Cancer pain 25.92 15.90 15 12555 3552 42605213
Device expulsion 25.86 15.90 6 12564 95 42608670
Obstructive airways disorder 25.63 15.90 34 12536 24725 42584040
Gingival erythema 25.41 15.90 6 12564 103 42608662
Metastasis 24.52 15.90 16 12554 4689 42604076
Bone lesion 23.67 15.90 14 12556 3452 42605313
Haemoglobin decreased 23.44 15.90 89 12481 132382 42476383
Ubiquinone decreased 22.98 15.90 4 12566 12 42608753
Urinary retention 22.79 15.90 43 12527 42171 42566594
Bone debridement 22.69 15.90 6 12564 166 42608599
Purulent discharge 21.94 15.90 13 12557 3216 42605549
Gingivitis 21.91 15.90 14 12556 3959 42604806
Blood alkaline phosphatase increased 21.69 15.90 37 12533 33560 42575205
Eosinophilic cystitis 21.62 15.90 5 12565 78 42608687
Prostate cancer recurrent 21.37 15.90 9 12561 1074 42607691
Arterial injury 21.24 15.90 7 12563 421 42608344
Sequestrectomy 21.15 15.90 6 12564 217 42608548
Spinal cord compression 21.12 15.90 14 12556 4210 42604555
Metastases to lymph nodes 21.01 15.90 16 12554 5982 42602783
PCO2 decreased 19.92 15.90 10 12560 1784 42606981
Hypertension 19.41 15.90 99 12471 167105 42441660
Injection site haematoma 19.26 15.90 10 12560 1915 42606850
Breast cancer 18.92 15.90 6 12564 319 42608446
Memory impairment 18.75 15.90 44 12526 50178 42558587
Injection site haemorrhage 18.55 15.90 20 12550 11716 42597049
Terminal state 18.20 15.90 13 12557 4410 42604355
Haemorrhage 16.37 15.90 47 12523 60516 42548249
Gingival swelling 16.13 15.90 8 12562 1392 42607373
Productive cough 15.90 15.90 42 12528 51525 42557240

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
Metastases to bone 872.74 14.96 301 21785 31071 110536142
Malignant neoplasm progression 763.10 14.96 459 21627 174108 110393105
Metastases to liver 541.05 14.96 219 21867 35167 110532046
Neutropenia 403.20 14.96 432 21654 374188 110193025
Prostatic specific antigen increased 305.30 14.96 109 21977 12402 110554811
Osteonecrosis of jaw 258.83 14.96 145 21941 47872 110519341
Metastases to lymph nodes 205.69 14.96 86 22000 14946 110552267
Hot flush 194.86 14.96 136 21950 65900 110501313
Metastases to lung 185.28 14.96 91 21995 22972 110544241
Prostate cancer 153.67 14.96 95 21991 37546 110529667
Breast cancer metastatic 153.07 14.96 64 22022 11117 110556096
Neoplasm progression 151.92 14.96 116 21970 64479 110502734
Central nervous system mass 141.73 14.96 33 22053 801 110566412
Wall motion score index abnormal 141.45 14.96 33 22053 808 110566405
Prostate cancer metastatic 139.47 14.96 48 22038 4895 110562318
Airway remodelling 137.73 14.96 33 22053 909 110566304
PIK3CA-activated mutation 132.40 14.96 30 22056 643 110566570
Atopy 131.07 14.96 33 22053 1121 110566092
Cardiac septal defect 126.20 14.96 31 22055 950 110566263
Carbohydrate antigen 15-3 increased 125.31 14.96 34 22052 1553 110565660
Breast mass 112.79 14.96 47 22039 8094 110559119
Eosinophilic myocarditis 111.74 14.96 33 22053 2052 110565161
Eosinophilic pneumonia 111.27 14.96 45 22041 7182 110560031
Disease progression 105.62 14.96 181 21905 243853 110323360
Bone lesion 101.85 14.96 42 22044 7045 110560168
Microangiopathy 100.22 14.96 33 22053 2939 110564274
Osteonecrosis 96.02 14.96 68 22018 33673 110533540
Eosinophil count decreased 91.03 14.96 37 22049 5981 110561232
Bone pain 83.94 14.96 83 22003 65050 110502163
Breast cancer 79.32 14.96 64 22022 38478 110528735
Metastases to central nervous system 79.21 14.96 52 22034 22765 110544448
Metastases to spine 77.92 14.96 32 22054 5311 110561902
Interstitial lung disease 76.18 14.96 115 21971 139219 110427994
Oestradiol decreased 74.14 14.96 13 22073 67 110567146
Blood immunoglobulin E increased 73.76 14.96 34 22052 7448 110559765
Drug ineffective 69.35 14.96 124 21962 1520416 109046797
Myelosuppression 68.14 14.96 89 21997 94251 110472962
Haematuria 67.38 14.96 83 22003 82922 110484291
Metastases to the mediastinum 67.36 14.96 18 22068 775 110566438
Invasive breast carcinoma 67.32 14.96 18 22068 777 110566436
Malignant spinal cord compression 64.67 14.96 13 22073 153 110567060
Hepatic lesion 63.71 14.96 32 22054 8461 110558752
Infusion related reaction 63.54 14.96 3 22083 381159 110186054
Ventricular hypokinesia 63.48 14.96 35 22051 11179 110556034
Tumour marker increased 62.73 14.96 27 22059 5033 110562180
Eosinophilic granulomatosis with polyangiitis 59.53 14.96 33 22053 10653 110556560
Breast cancer recurrent 59.39 14.96 24 22062 3822 110563391
Respiratory symptom 59.16 14.96 37 22049 14908 110552305
Leukopenia 58.66 14.96 106 21980 148685 110418528
Alanine aminotransferase increased 56.66 14.96 118 21968 183655 110383558
Abdominal lymphadenopathy 56.46 14.96 19 22067 1809 110565404
Metastases to skin 55.95 14.96 20 22066 2279 110564934
Osteolysis 54.14 14.96 25 22061 5498 110561715
Nasal polyps 53.05 14.96 33 22053 13167 110554046
Menopausal symptoms 50.64 14.96 19 22067 2482 110564731
Lymphoedema 49.34 14.96 33 22053 14896 110552317
Lymphadenopathy 48.87 14.96 62 22024 63773 110503440
Hormone receptor positive breast cancer 48.55 14.96 13 22073 564 110566649
Blood alkaline phosphatase increased 48.25 14.96 65 22021 70870 110496343
Metastases to pelvis 47.92 14.96 14 22072 838 110566375
Bone disorder 47.48 14.96 37 22049 21155 110546058
White blood cell count decreased 46.43 14.96 125 21961 229265 110337948
Aspartate aminotransferase increased 46.17 14.96 100 21986 159836 110407377
Lymphopenia 45.93 14.96 48 22038 40122 110527091
Rheumatoid arthritis 45.09 14.96 4 22082 299609 110267604
Dilatation intrahepatic duct acquired 43.68 14.96 13 22073 830 110566383
Death 42.91 14.96 262 21824 698607 109868606
Metastasis 41.90 14.96 24 22062 8243 110558970
Mucinous breast carcinoma 41.58 14.96 7 22079 27 110567186
Eosinophil count increased 41.28 14.96 34 22052 21024 110546189
Lacrimation increased 40.90 14.96 40 22046 30910 110536303
Arthropathy 40.28 14.96 5 22081 287517 110279696
Ultrasound foetal abnormal 40.21 14.96 8 22078 89 110567124
Blood bilirubin increased 39.10 14.96 61 22025 75911 110491302
Drug hypersensitivity 39.08 14.96 21 22065 454069 110113144
Tooth extraction 38.85 14.96 27 22059 12964 110554249
Spinal pain 38.63 14.96 31 22055 18484 110548729
Hypersensitivity 37.30 14.96 17 22069 403981 110163232
Hepatic function abnormal 36.95 14.96 65 22021 89230 110477983
Adnexa uteri mass 36.49 14.96 10 22076 474 110566739
Pathological fracture 35.97 14.96 25 22061 12007 110555206
CYP3A4 polymorphism 35.86 14.96 7 22079 70 110567143
Metastases to pleura 35.78 14.96 14 22072 2049 110565164
Selenium deficiency 35.68 14.96 7 22079 72 110567141
Pituitary haemorrhage 35.43 14.96 9 22077 317 110566896
Jaundice 35.39 14.96 51 22035 59185 110508028
Invasive lobular breast carcinoma 35.26 14.96 11 22075 823 110566390
Osteitis 34.63 14.96 17 22069 4279 110562934
Oophorectomy bilateral 34.62 14.96 7 22079 85 110567128
Joint swelling 34.56 14.96 23 22063 442822 110124391
Chronic sinusitis 34.24 14.96 33 22053 25051 110542162
Osteitis condensans 34.21 14.96 6 22080 31 110567182
Nodule 33.79 14.96 37 22049 32594 110534619
Metastases to peritoneum 33.11 14.96 18 22068 5592 110561621
Nasopharyngitis 32.82 14.96 19 22067 394342 110172871
Osteomyelitis 31.97 14.96 38 22048 36562 110530651
Hypocalcaemia 31.59 14.96 51 22035 65315 110501898
Mobility decreased 31.21 14.96 5 22081 237417 110329796
Pleural effusion 31.20 14.96 92 21994 177617 110389596
Anaemia 30.98 14.96 201 21885 546885 110020328
Pericarditis 30.23 14.96 4 22082 219110 110348103
Merycism 29.88 14.96 8 22078 347 110566866
Neuropathy peripheral 29.76 14.96 91 21995 179186 110388027
Blood testosterone increased 29.66 14.96 11 22075 1391 110565822
Haematotoxicity 29.27 14.96 28 22058 21054 110546159
Bilirubin conjugated abnormal 29.21 14.96 7 22079 193 110567020
Metastases to meninges 29.01 14.96 16 22070 5112 110562101
Neutrophil count decreased 28.69 14.96 70 22016 120871 110446342
Hepatotoxicity 28.66 14.96 48 22038 63352 110503861
Endometrial hyperplasia 28.60 14.96 9 22077 693 110566520
Contracted bladder 28.17 14.96 5 22081 28 110567185
Sinusitis 28.14 14.96 12 22074 296676 110270537
Hepatic mass 28.04 14.96 13 22073 2885 110564328
Paraparesis 27.92 14.96 15 22071 4551 110562662
Completed suicide 27.91 14.96 7 22079 242374 110324839
Bone sequestrum 27.29 14.96 10 22076 1223 110565990
Gamma-glutamyltransferase increased 27.16 14.96 46 22040 61263 110505950
Urticaria 27.05 14.96 15 22071 318842 110248371
Fibrous histiocytoma 27.02 14.96 9 22077 830 110566383
Febrile neutropenia 27.00 14.96 130 21956 316637 110250576
Libido decreased 26.83 14.96 16 22070 5919 110561294
Wound 26.55 14.96 7 22079 234430 110332783
Fatigue 26.51 14.96 364 21722 1215594 109351619
International normalised ratio abnormal 25.82 14.96 16 22070 6341 110560872
Prostate cancer recurrent 25.82 14.96 9 22077 953 110566260
Dental fistula 25.81 14.96 8 22078 586 110566627
Electrocardiogram QT prolonged 25.77 14.96 63 22023 108897 110458316
Pneumonitis 25.77 14.96 51 22035 76480 110490733
Metastases to eye 25.56 14.96 7 22079 331 110566882
Body surface area increased 25.41 14.96 6 22080 155 110567058
Osteosclerosis 25.30 14.96 14 22072 4501 110562712
Pleural disorder 24.97 14.96 9 22077 1050 110566163
Cancer pain 24.89 14.96 16 22070 6756 110560457
Haemoglobin decreased 24.86 14.96 107 21979 248620 110318593
Skin fragility 24.19 14.96 9 22077 1149 110566064
Pleural neoplasm 24.16 14.96 7 22079 407 110566806
Decreased appetite 24.03 14.96 170 21916 475676 110091537
Bone debridement 24.02 14.96 7 22079 415 110566798
Carcinoid tumour pulmonary 23.99 14.96 7 22079 417 110566796
Toxicity to various agents 23.79 14.96 37 22049 480518 110086695
Viral infection 23.71 14.96 40 22046 53099 110514114
Arachnoid cyst 23.58 14.96 7 22079 443 110566770
Wheezing 23.14 14.96 11 22075 255219 110311994
Peripheral swelling 23.12 14.96 28 22058 404006 110163207
Off label use 22.89 14.96 191 21895 1499994 109067219
Hormone receptor positive HER2 negative breast cancer 22.88 14.96 6 22080 240 110566973
Lymphadenopathy mediastinal 22.77 14.96 14 22072 5470 110561743
Palmar-plantar erythrodysaesthesia syndrome 22.59 14.96 34 22052 40991 110526222
Cervical polyp 22.42 14.96 6 22080 260 110566953
Gastrointestinal bacterial infection 22.42 14.96 9 22077 1409 110565804
Obstructive airways disorder 22.28 14.96 36 22050 46113 110521100
Pituitary tumour benign 22.16 14.96 11 22075 2836 110564377
Mood swings 22.13 14.96 25 22061 22787 110544426
Pelvic pain 21.81 14.96 21 22065 15921 110551292
Hypotension 21.74 14.96 45 22041 523804 110043409
Ubiquinone decreased 21.64 14.96 4 22082 29 110567184
PO2 increased 21.59 14.96 9 22077 1550 110565663
Metastases to nervous system 21.58 14.96 6 22080 300 110566913
Platelet count decreased 21.40 14.96 97 21989 230346 110336867
Overdose 21.31 14.96 10 22076 233784 110333429
Hydrothorax 21.06 14.96 9 22077 1649 110565564
Empty sella syndrome 20.49 14.96 5 22081 149 110567064
Renal disorder 20.44 14.96 36 22050 49443 110517770
Eosinophilic cystitis 20.06 14.96 5 22081 163 110567050
Oestradiol abnormal 19.75 14.96 4 22082 49 110567164
Uterine polyp 19.51 14.96 9 22077 1974 110565239
Breast pain 19.30 14.96 16 22070 9984 110557229
Exposed bone in jaw 19.14 14.96 11 22075 3800 110563413
Folliculitis 18.99 14.96 5 22081 167648 110399565
Gingivitis 18.84 14.96 16 22070 10315 110556898
Lymphangioleiomyomatosis 18.39 14.96 5 22081 230 110566983
Periodontitis 18.39 14.96 12 22074 5196 110562017
Amenorrhoea 18.29 14.96 15 22071 9216 110557997
PCO2 decreased 18.26 14.96 10 22076 3151 110564062
Pulmonary embolism 18.24 14.96 88 21998 214386 110352827
Dermatitis 18.15 14.96 25 22061 27812 110539401
Vitamin B complex deficiency 18.08 14.96 7 22079 996 110566217
Breast swelling 18.06 14.96 8 22078 1596 110565617
BRCA1 gene mutation 18.01 14.96 4 22082 78 110567135
Metastases to spinal cord 17.99 14.96 5 22081 250 110566963
Application site haematoma 17.96 14.96 4 22082 79 110567134
Breast injury 17.96 14.96 4 22082 79 110567134
Hepatic cytolysis 17.71 14.96 36 22050 55017 110512196
Asthenia 17.36 14.96 212 21874 688787 109878426
Axillary lymphadenectomy 17.26 14.96 4 22082 95 110567118
Biliary colic 17.24 14.96 11 22075 4586 110562627
Glucocorticoid deficiency 16.96 14.96 7 22079 1175 110566038
Discomfort 16.94 14.96 11 22075 214696 110352517
Ocular icterus 16.75 14.96 12 22074 6041 110561172
Oestradiol increased 16.66 14.96 4 22082 111 110567102
Haemorrhage 16.63 14.96 53 22033 106639 110460574
Spinal cord compression 16.51 14.96 13 22073 7539 110559674
Respiratory tract infection 16.50 14.96 41 22045 71576 110495637
Uterine leiomyoma 16.14 14.96 13 22073 7787 110559426
Loss of personal independence in daily activities 16.02 14.96 5 22081 150015 110417198
Musculoskeletal chest pain 16.02 14.96 24 22062 28823 110538390
Infection 15.97 14.96 30 22056 362170 110205043
Suspected counterfeit product 15.87 14.96 6 22080 800 110566413
Metastases to ovary 15.76 14.96 5 22081 395 110566818
Bone trimming 15.65 14.96 3 22083 27 110567186
Type 2 diabetes mellitus 15.52 14.96 8 22078 177224 110389989
Intentional product use issue 15.46 14.96 16 22070 247890 110319323
Abdominal discomfort 15.36 14.96 35 22051 393823 110173390
Abdominal pain upper 15.32 14.96 29 22057 349082 110218131
Intermenstrual bleeding 15.30 14.96 12 22074 6922 110560291
Pseudocirrhosis 15.08 14.96 6 22080 917 110566296
Central nervous system lesion 15.01 14.96 17 22069 15536 110551677

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L02AE03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONES AND RELATED AGENTS
Gonadotropin releasing hormone analogues
CHEBI has role CHEBI:35610 antineoplastic agent
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

Related Drugs by ATC class:

L02AE Gonadotropin releasing hormone analogues 5 drugs
bicalutamidebuserelinhistrelinleuprorelintriptorelin

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

DiseaseRelationSNOMED_IDDOID
Endometriosis indication 129103003
Hormone receptor positive malignant neoplasm of breast indication 417181009
Advanced Prostatic Carcinoma indication
Endometrial Ablation Adjunct indication
Urinary tract obstruction contraindication 7163005 DOID:5200
Hypercholesterolemia contraindication 13644009
Hypertensive disorder contraindication 38341003 DOID:10763
Hypercalcemia contraindication 66931009 DOID:12678
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Pregnancy, function contraindication 289908002
Bilateral orchidectomy contraindication 386634006
Cardiovascular event risk contraindication 395112001
Breastfeeding (mother) contraindication 413712001
Obesity contraindication 414916001 DOID:9970
Smokes tobacco daily contraindication 449868002
Bone Metastases contraindication
Vertebral Metastases contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.85 acidic
pKa2 9.65 acidic
pKa3 11.9 acidic
pKa4 12.55 acidic
pKa5 13.03 acidic
pKa6 13.27 acidic
pKa7 13.43 acidic
pKa8 10.75 Basic
pKa9 6.69 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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

External reference:

IDSource
N0000007256 NUI
D00573 KEGG_DRUG
145781-92-6 SECONDARY_CAS_RN
4019508 VANDF
C0120107 UMLSCUI
CHEBI:5523 CHEBI
CHEMBL1201247 ChEMBL_ID
CHEMBL1200501 ChEMBL_ID
D017273 MESH_DESCRIPTOR_UI
DB00014 DRUGBANK_ID
3879 IUPHAR_LIGAND_ID
5943 INN_ID
0F65R8P09N UNII
5311128 PUBCHEM_CID
203146 RXNORM
1550 MMSL
4799 MMSL
d01354 MMSL
003532 NDDF
006407 NDDF
008308 NDDF
008309 NDDF
108771008 SNOMEDCT_US
108773006 SNOMEDCT_US
126138002 SNOMEDCT_US
0F65R8P09N INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ZOLADEX HUMAN PRESCRIPTION DRUG LABEL 1 50090-3466 IMPLANT 3.60 mg SUBCUTANEOUS NDA 26 sections
ZOLADEX HUMAN PRESCRIPTION DRUG LABEL 1 70720-950 IMPLANT 3.60 mg SUBCUTANEOUS NDA 27 sections
ZOLADEX HUMAN PRESCRIPTION DRUG LABEL 1 70720-951 IMPLANT 10.80 mg SUBCUTANEOUS NDA 27 sections