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

Stem definitionDrug idCAS RN
non-steroid antiandrogens 367 90357-06-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ICI 176334
  • ICI-176334
  • bicalutamide
  • casodex
Bicalutamide is a non-steroidal androgen receptor inhibitor. It competitively inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue. Prostatic carcinoma is known to be androgen sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen.
  • Molecular weight: 430.37
  • Formula: C18H14F4N2O4S
  • CLOGP: 2.71
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 107.26
  • ALOGS: -4.67
  • ROTB: 6
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.01 mg/mL Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.94 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 100 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.903 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.661 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 73.961 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 2.042 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 7.370 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 29.330 % High 1
herg hERG pIC50 4.972 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.954 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 5.984 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 6.630 % High 1
kinase-safety-class ACVR2B,CDK5,EIF2AK3,GRK2,PDK1,PDK2,PDK4,PIK3CG 8
kinase-selectivity-class AXL,GRK2,PDK4 3
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 2.483 High 1
mh-clint Mouse hepatocyte intrinsic clearance 5.970 High 1
mppb Mouse plasma protein binding (% unbound) 8.080 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 11.324 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 1
pppb Pig plasma protein binding (% unbound) 13.090 % High 1
rh-clint Rat hepatocyte intrinsic clearance 3.459 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 39.010 % High 1
rppb Rat plasma protein binding (% unbound) 6.960 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 10.965 uM High 1

Approvals:

DateAgencyCompanyOrphan
Oct. 4, 1995 FDA ASTRAZENECA

FDA Adverse Event Reporting System (Female)

None

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 1274.97 13.40 468 28911 16457 42575499
Metastases to bone 481.91 13.40 225 29154 14584 42577372
Prostate cancer 403.77 13.40 295 29084 44348 42547608
Osteonecrosis of jaw 383.17 13.40 209 29170 18840 42573116
Prostate cancer metastatic 378.62 13.40 150 29229 6479 42585477
Hot flush 323.56 13.40 198 29181 22153 42569803
Malignant neoplasm progression 296.51 13.40 369 29010 108031 42483925
Interstitial lung disease 250.36 13.40 289 29090 78173 42513783
Hormone-refractory prostate cancer 169.03 13.40 51 29328 953 42591003
Haematuria 115.33 13.40 169 29210 57630 42534326
Prostate cancer recurrent 112.11 13.40 38 29341 1045 42590911
Metastases to lymph nodes 107.37 13.40 61 29318 5937 42586019
Osteonecrosis 104.46 13.40 87 29292 15778 42576178
Central nervous system mass 100.59 13.40 33 29346 818 42591138
Wall motion score index abnormal 100.44 13.40 33 29346 822 42591134
Airway remodelling 98.78 13.40 33 29346 867 42591089
Blood testosterone increased 98.40 13.40 38 29341 1529 42590427
Atopy 96.19 13.40 33 29346 942 42591014
Prostatic specific antigen abnormal 90.09 13.40 31 29348 893 42591063
Cardiac septal defect 88.93 13.40 31 29348 929 42591027
Eosinophilic myocarditis 85.17 13.40 33 29346 1340 42590616
Gynaecomastia 80.84 13.40 68 29311 12499 42579457
Torsade de pointes 80.29 13.40 58 29321 8536 42583420
Microangiopathy 78.68 13.40 33 29346 1649 42590307
Bone lesion 75.13 13.40 40 29339 3426 42588530
Metastases to lung 73.86 13.40 62 29317 11362 42580594
Bone pain 69.70 13.40 84 29295 23708 42568248
Breast cancer male 68.35 13.40 21 29358 418 42591538
Disease progression 67.44 13.40 235 29144 143421 42448535
Bone disorder 62.62 13.40 45 29334 6568 42585388
Hyperthyroidism 59.94 13.40 61 29318 14280 42577676
Hypocalcaemia 59.81 13.40 88 29291 30085 42561871
Drug abuse 59.76 13.40 3 29376 104768 42487188
Chronic sinusitis 59.37 13.40 34 29345 3358 42588598
Blood testosterone abnormal 59.03 13.40 20 29359 549 42591407
Tooth extraction 58.19 13.40 40 29339 5440 42586516
Toxicity to various agents 57.93 13.40 44 29335 229092 42362864
Metastasis 56.33 13.40 37 29342 4668 42587288
Eosinophilic pneumonia 55.15 13.40 37 29342 4837 42587119
Eosinophil count decreased 55.09 13.40 33 29346 3543 42588413
Blood immunoglobulin E increased 54.68 13.40 33 29346 3592 42588364
Hepatic function abnormal 53.34 13.40 113 29266 51454 42540502
Nasal polyps 52.84 13.40 33 29346 3818 42588138
Hydronephrosis 50.56 13.40 51 29328 11814 42580142
Off label use 49.30 13.40 250 29129 638085 41953871
Metastases to spine 48.98 13.40 29 29350 3048 42588908
Urinary retention 48.97 13.40 97 29282 42117 42549839
Neuroendocrine carcinoma of prostate 46.74 13.40 10 29369 40 42591916
Adrenal insufficiency 46.18 13.40 61 29318 18863 42573093
Polyneuropathy in malignant disease 46.14 13.40 15 29364 361 42591595
Exposed bone in jaw 45.10 13.40 22 29357 1567 42590389
Anti-androgen withdrawal syndrome 43.77 13.40 8 29371 10 42591946
Troponin increased 42.79 13.40 59 29320 19003 42572953
Asthenia 41.57 13.40 333 29046 280460 42311496
Metastases to liver 40.41 13.40 53 29326 16273 42575683
Completed suicide 39.55 13.40 9 29370 96456 42495500
Anaemia 38.59 13.40 327 29052 279951 42312005
Cardiac failure 37.91 13.40 160 29219 106696 42485260
Ventricular hypokinesia 37.71 13.40 34 29345 6850 42585106
COVID-19 35.16 13.40 18 29361 115930 42476026
Breast tenderness 34.35 13.40 15 29364 828 42591128
Pain in jaw 34.23 13.40 46 29333 14456 42577500
Eosinophil count increased 33.16 13.40 39 29340 10724 42581232
Cancer pain 33.15 13.40 24 29355 3543 42588413
Muscular weakness 32.75 13.40 129 29250 83369 42508587
Pituitary haemorrhage 32.36 13.40 10 29369 203 42591753
Nodule 31.50 13.40 41 29338 12493 42579463
Injection site induration 31.36 13.40 23 29356 3464 42588492
Electrocardiogram QT prolonged 30.31 13.40 87 29292 47858 42544098
Breast swelling 29.74 13.40 10 29369 268 42591688
Spinal cord compression 29.54 13.40 24 29355 4200 42587756
Eosinophilic granulomatosis with polyangiitis 29.48 13.40 33 29346 8605 42583351
Osteomyelitis 28.93 13.40 48 29331 18175 42573781
Urinary tract obstruction 28.40 13.40 23 29356 4008 42587948
Breast pain 27.93 13.40 16 29363 1581 42590375
Sequestrectomy 27.78 13.40 9 29370 214 42591742
Allodynia 27.66 13.40 14 29365 1080 42590876
Fatigue 27.57 13.40 437 28942 435204 42156752
Respiratory symptom 27.40 13.40 36 29343 11070 42580886
Lacrimation increased 27.30 13.40 37 29342 11721 42580235
Metastases to breast 27.03 13.40 5 29374 7 42591949
Bone sequestrum 26.88 13.40 11 29368 516 42591440
Decreased appetite 26.88 13.40 226 29153 192911 42399045
Intercepted product preparation error 26.55 13.40 29 29350 7360 42584596
Blood alkaline phosphatase increased 26.31 13.40 66 29313 33531 42558425
Retroperitoneal lymphadenopathy 25.46 13.40 13 29366 1021 42590935
Osteitis 24.39 13.40 15 29364 1689 42590267
Osteosclerosis 23.48 13.40 14 29365 1490 42590466
Abscess jaw 23.31 13.40 11 29368 728 42591228
Radiation injury 23.25 13.40 10 29369 532 42591424
Dysuria 23.22 13.40 60 29319 31036 42560920
Cerebral infarction 23.13 13.40 60 29319 31109 42560847
Syringe issue 23.10 13.40 29 29350 8527 42583429
Sepsis 23.09 13.40 66 29313 199268 42392688
Cystitis radiation 23.04 13.40 7 29372 134 42591822
Product dose omission issue 22.74 13.40 45 29334 154320 42437636
Injection site abscess 22.62 13.40 12 29367 1020 42590936
Gingivitis 22.51 13.40 20 29359 3953 42588003
Infusion related reaction 22.41 13.40 7 29372 60799 42531157
Testicular atrophy 21.77 13.40 10 29369 622 42591334
Bone debridement 21.67 13.40 7 29372 165 42591791
Drug hypersensitivity 21.56 13.40 22 29357 99367 42492589
Metastases to soft tissue 21.45 13.40 9 29370 450 42591506
Quality of life decreased 20.90 13.40 22 29357 5354 42586602
Cytokine release syndrome 20.73 13.40 3 29376 44524 42547432
Product monitoring error 20.67 13.40 20 29359 4403 42587553
Cholangitis sclerosing 20.47 13.40 14 29365 1888 42590068
Therapeutic product effect incomplete 20.06 13.40 12 29367 70927 42521029
Metastases to eye 19.99 13.40 6 29373 110 42591846
Neuroendocrine carcinoma 19.98 13.40 9 29370 535 42591421
Cough 19.88 13.40 60 29319 178043 42413913
Hyperadrenalism 19.63 13.40 5 29374 48 42591908
Radical prostatectomy 19.27 13.40 5 29374 52 42591904
Jaw disorder 19.02 13.40 14 29365 2119 42589837
Phyllodes tumour 18.90 13.40 4 29375 15 42591941
Bone trimming 18.84 13.40 3 29376 0 42591956
Androgens increased 18.84 13.40 3 29376 0 42591956
Renal disorder 18.71 13.40 53 29326 28927 42563029
Back pain 18.70 13.40 164 29215 141612 42450344
Breast discomfort 18.70 13.40 4 29375 16 42591940
Anaesthesia 18.62 13.40 5 29374 60 42591896
Conjunctival ulcer 18.54 13.40 5 29374 61 42591895
Loss of libido 18.49 13.40 16 29363 3054 42588902
Overdose 17.93 13.40 28 29351 105236 42486720
Purulent discharge 17.79 13.40 16 29363 3213 42588743
Mucosal inflammation 17.63 13.40 6 29373 49368 42542588
Radiation proctitis 17.46 13.40 6 29373 172 42591784
Rheumatoid arthritis 17.31 13.40 4 29375 42436 42549520
Bone fistula 17.08 13.40 4 29375 26 42591930
Haemorrhage urinary tract 17.06 13.40 13 29366 2073 42589883
Obesity 16.93 13.40 36 29343 16423 42575533
Ureteric rupture 16.76 13.40 3 29376 3 42591953
Gingival swelling 16.74 13.40 11 29368 1389 42590567
Prostatic specific antigen decreased 16.72 13.40 6 29373 196 42591760
Rash 16.72 13.40 117 29262 276837 42315119
Disseminated intravascular coagulation 16.65 13.40 46 29333 24748 42567208
Intentional product use issue 16.62 13.40 15 29364 71818 42520138
Pollakiuria 16.37 13.40 43 29336 22462 42569494
Toothache 16.31 13.40 23 29356 7560 42584396
Death 16.22 13.40 432 28947 470753 42121203
Bone swelling 16.21 13.40 7 29372 376 42591580
Breakthrough pain 16.09 13.40 8 29371 594 42591362
Oral surgery 15.94 13.40 8 29371 606 42591350
Wheezing 15.87 13.40 9 29370 54772 42537184
Abdominal wall haematoma 15.83 13.40 13 29366 2309 42589647
Metastases to pleura 15.73 13.40 8 29371 623 42591333
Psoriasis 15.56 13.40 7 29372 48597 42543359
Urinary tract infection 15.31 13.40 119 29260 99165 42492791
Cardiogenic shock 15.27 13.40 3 29376 35637 42556319
Hydroureter 15.17 13.40 7 29372 440 42591516
Product physical consistency issue 15.04 13.40 9 29370 964 42590992
Debridement 15.03 13.40 9 29370 965 42590991
Device leakage 14.88 13.40 26 29353 10259 42581697
Diarrhoea 14.87 13.40 226 29153 460623 42131333
Eye colour change 14.73 13.40 6 29373 278 42591678
Menopausal symptoms 14.69 13.40 3 29376 9 42591947
Nasopharyngitis 14.63 13.40 22 29357 83974 42507982
Urogenital haemorrhage 14.59 13.40 8 29371 726 42591230
Pathological fracture 14.38 13.40 18 29361 5275 42586681
Dermatitis allergic 14.35 13.40 23 29356 8460 42583496
Neuroendocrine carcinoma metastatic 14.24 13.40 5 29374 153 42591803
Hyperaesthesia 14.23 13.40 19 29360 5933 42586023
Metastases to penis 14.23 13.40 3 29376 11 42591945
Suicide attempt 14.20 13.40 7 29372 46093 42545863
Orchidectomy 14.07 13.40 4 29375 60 42591896
Metastatic salivary gland cancer 14.02 13.40 3 29376 12 42591944
Product use in unapproved indication 13.69 13.40 73 29306 184383 42407573
Spinal compression fracture 13.65 13.40 21 29358 7462 42584494
Prescribed underdose 13.61 13.40 25 29354 10257 42581699
Tachycardia 13.60 13.40 31 29348 101056 42490900
Hypersensitivity 13.55 13.40 18 29361 72352 42519604
Gingival abscess 13.42 13.40 5 29374 182 42591774

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
Prostatic specific antigen increased 1525.05 14.88 386 24125 12125 110552663
Prostate cancer 602.74 14.88 248 24263 37393 110527395
Metastases to bone 423.05 14.88 183 24328 31189 110533599
Prostate cancer metastatic 379.97 14.88 106 24405 4837 110559951
Osteonecrosis of jaw 348.82 14.88 183 24328 47834 110516954
Malignant neoplasm progression 324.05 14.88 285 24226 174282 110390506
Interstitial lung disease 290.09 14.88 243 24268 139091 110425697
Hot flush 232.95 14.88 158 24353 65878 110498910
Hormone-refractory prostate cancer 209.45 14.88 47 24464 863 110563925
Haematuria 191.99 14.88 154 24357 82851 110481937
Central nervous system mass 133.13 14.88 32 24479 802 110563986
Wall motion score index abnormal 132.87 14.88 32 24479 809 110563979
Airway remodelling 129.26 14.88 32 24479 910 110563878
Disease progression 125.38 14.88 207 24304 243827 110320961
Prostate cancer recurrent 123.60 14.88 31 24480 931 110563857
Atopy 122.81 14.88 32 24479 1122 110563666
Blood testosterone increased 121.29 14.88 33 24478 1369 110563419
Gynaecomastia 120.17 14.88 53 24458 9437 110555351
Cardiac septal defect 118.05 14.88 30 24481 951 110563837
Torsade de pointes 106.69 14.88 65 24446 22535 110542253
Eosinophilic myocarditis 104.09 14.88 32 24479 2053 110562735
Urinary retention 94.98 14.88 96 24415 69587 110495201
Microangiopathy 92.94 14.88 32 24479 2940 110561848
Metastases to lymph nodes 91.52 14.88 51 24460 14981 110549807
Metastases to lung 88.05 14.88 58 24453 23005 110541783
Hyperthyroidism 84.52 14.88 62 24449 29199 110535589
Hypocalcaemia 83.55 14.88 87 24424 65279 110499509
Anaemia 82.96 14.88 288 24223 546798 110017990
Prostatic specific antigen abnormal 82.87 14.88 21 24490 658 110564130
Hepatic function abnormal 78.69 14.88 98 24413 89197 110475591
Troponin increased 76.92 14.88 59 24452 29707 110535081
Death 75.88 14.88 331 24180 698538 109866250
Eosinophilic pneumonia 74.57 14.88 35 24476 7192 110557596
Eosinophil count decreased 71.04 14.88 32 24479 5986 110558802
Adrenal insufficiency 64.44 14.88 62 24449 42328 110522460
Blood immunoglobulin E increased 64.40 14.88 32 24479 7450 110557338
Osteonecrosis 64.27 14.88 56 24455 33685 110531103
Infusion related reaction 62.74 14.88 6 24505 381156 110183632
Cardiac failure 62.22 14.88 132 24379 187494 110377294
Metastasis 61.38 14.88 32 24479 8235 110556553
Polyneuropathy in malignant disease 58.70 14.88 15 24496 486 110564302
Hydronephrosis 55.68 14.88 42 24469 20623 110544165
Ventricular hypokinesia 54.84 14.88 33 24478 11181 110553607
Rheumatoid arthritis 54.20 14.88 3 24508 299610 110265178
Eosinophilic granulomatosis with polyangiitis 53.70 14.88 32 24479 10654 110554134
Breast cancer male 53.62 14.88 13 24498 338 110564450
Anti-androgen withdrawal syndrome 52.83 14.88 8 24503 10 110564778
Arthropathy 51.63 14.88 3 24508 287519 110277269
Respiratory symptom 50.85 14.88 35 24476 14910 110549878
Intercepted product preparation error 49.49 14.88 26 24485 6794 110557994
Blood testosterone abnormal 49.03 14.88 12 24499 325 110564463
Hormone-dependent prostate cancer 48.96 14.88 11 24500 203 110564585
Bone pain 48.81 14.88 66 24445 65067 110499721
Alopecia 48.00 14.88 11 24500 364742 110200046
Sinusitis 47.95 14.88 5 24506 296683 110268105
Asthenia 47.80 14.88 288 24223 688711 109876077
Nasal polyps 47.49 14.88 32 24479 13168 110551620
Joint swelling 46.46 14.88 20 24491 442825 110121963
Eosinophil count increased 46.38 14.88 38 24473 21020 110543768
Hypersensitivity 46.10 14.88 16 24495 403982 110160806
Neuroendocrine carcinoma of prostate 46.06 14.88 8 24503 34 110564754
Drug hypersensitivity 45.32 14.88 22 24489 454068 110110720
Electrocardiogram QT prolonged 44.93 14.88 84 24427 108876 110455912
Syringe issue 43.94 14.88 27 24484 9498 110555290
Bone lesion 43.02 14.88 24 24487 7063 110557725
Nasopharyngitis 42.67 14.88 17 24494 394344 110170444
Metastases to liver 41.49 14.88 45 24466 35341 110529447
Oesophageal ulcer haemorrhage 40.79 14.88 13 24498 939 110563849
Drug intolerance 40.10 14.88 20 24491 406492 110158296
Metastases to nervous system 40.00 14.88 10 24501 296 110564492
Pituitary haemorrhage 39.38 14.88 10 24501 316 110564472
Cancer pain 38.58 14.88 22 24489 6750 110558038
Erectile dysfunction 37.78 14.88 32 24479 18524 110546264
Therapeutic product effect decreased 37.29 14.88 5 24506 244311 110320477
Lower respiratory tract infection 37.04 14.88 5 24506 243101 110321687
Headache 36.74 14.88 89 24422 882288 109682500
Pemphigus 36.31 14.88 3 24508 214567 110350221
Metastases to spine 34.92 14.88 19 24492 5324 110559464
Exposed bone in jaw 34.88 14.88 17 24494 3794 110560994
Allodynia 34.23 14.88 14 24497 2069 110562719
Nodule 33.97 14.88 39 24472 32592 110532196
Drug interaction 33.94 14.88 208 24303 499975 110064813
Wheezing 32.97 14.88 8 24503 255222 110309566
Acute myocardial infarction 32.57 14.88 63 24448 83714 110481074
Dysuria 32.09 14.88 52 24459 60179 110504609
Loss of libido 31.79 14.88 15 24496 3118 110561670
Chronic sinusitis 31.35 14.88 33 24478 25051 110539737
Systemic lupus erythematosus 30.91 14.88 9 24502 254329 110310459
Lacrimation increased 30.56 14.88 36 24475 30914 110533874
Completed suicide 30.53 14.88 8 24503 242373 110322415
Contraindicated product administered 29.77 14.88 9 24502 248258 110316530
Blood alkaline phosphatase increased 29.63 14.88 55 24456 70880 110493908
Abdominal pain upper 29.05 14.88 21 24490 349090 110215698
Off label use 28.69 14.88 205 24306 1499980 109064808
Product monitoring error 28.25 14.88 20 24491 8907 110555881
Renal disorder 28.12 14.88 44 24467 49435 110515353
Testicular atrophy 27.80 14.88 8 24503 408 110564380
Prostatic specific antigen decreased 27.63 14.88 6 24505 94 110564694
Urinary tract obstruction 27.31 14.88 16 24495 5161 110559627
Blood chromogranin A increased 27.30 14.88 9 24502 724 110564064
Wound 27.22 14.88 9 24502 234428 110330360
Hepatic enzyme increased 27.10 14.88 19 24492 320873 110243915
Cholangitis sclerosing 26.98 14.88 14 24497 3568 110561220
Neuroendocrine carcinoma 26.20 14.88 9 24502 821 110563967
Disseminated intravascular coagulation 25.27 14.88 38 24473 41248 110523540
Decreased appetite 25.13 14.88 186 24325 475660 110089128
Bone disorder 24.93 14.88 27 24484 21165 110543623
Rash 24.73 14.88 96 24415 820868 109743920
Radiation injury 24.32 14.88 9 24502 1019 110563769
COVID-19 24.23 14.88 12 24499 245048 110319740
Gastrointestinal disorder 23.70 14.88 12 24499 241940 110322848
Toxicity to various agents 23.69 14.88 44 24467 480511 110084277
Metastases to soft tissue 23.49 14.88 8 24503 711 110564077
Pollakiuria 23.33 14.88 38 24473 44157 110520631
Bone debridement 23.30 14.88 7 24504 415 110564373
Platelet count decreased 23.27 14.88 107 24404 230336 110334452
Acute coronary syndrome 23.01 14.88 27 24484 23085 110541703
Conjunctival ulcer 22.87 14.88 5 24506 81 110564707
Radiation proctitis 22.84 14.88 6 24505 217 110564571
Syncope 22.68 14.88 97 24414 202439 110362349
Cerebral infarction 22.67 14.88 41 24470 51797 110512991
Androgens increased 22.24 14.88 3 24508 0 110564788
Therapeutic product effect incomplete 22.07 14.88 11 24500 223794 110340994
Discomfort 22.02 14.88 10 24501 214697 110350091
Cystitis radiation 21.98 14.88 6 24505 252 110564536
Blood lactate dehydrogenase increased 21.90 14.88 37 24474 44297 110520491
Intentional product use issue 21.84 14.88 14 24497 247892 110316896
Lymphopenia 21.83 14.88 35 24476 40135 110524653
Device leakage 21.65 14.88 22 24489 16026 110548762
Tooth extraction 21.65 14.88 20 24491 12971 110551817
Metastases to central nervous system 21.64 14.88 26 24485 22791 110541997
Blood cholesterol increased 21.61 14.88 7 24504 184778 110380010
Anxiety 21.42 14.88 27 24484 345051 110219737
Abdominal discomfort 21.29 14.88 34 24477 393824 110170964
Urogenital haemorrhage 21.20 14.88 8 24503 956 110563832
Soft tissue mass 20.83 14.88 9 24502 1524 110563264
Product use issue 20.83 14.88 23 24488 311672 110253116
Orchidectomy 20.77 14.88 4 24507 33 110564755
Haemorrhage urinary tract 20.76 14.88 11 24500 2925 110561863
Breast swelling 20.44 14.88 9 24502 1595 110563193
Metastases to eye 20.38 14.88 6 24505 332 110564456
Quality of life decreased 20.17 14.88 20 24491 14149 110550639
Polyuria 19.82 14.88 22 24489 17716 110547072
Blister 19.81 14.88 13 24498 227363 110337425
Metastases to breast 19.76 14.88 6 24505 369 110564419
Spinal cord compression 19.57 14.88 15 24496 7537 110557251
Bone sequestrum 19.29 14.88 8 24503 1225 110563563
Hyperadrenalism 19.26 14.88 4 24507 50 110564738
Breast tenderness 18.97 14.88 10 24501 2630 110562158
Loss of consciousness 18.97 14.88 90 24421 196216 110368572
Mobility decreased 18.83 14.88 15 24496 237407 110327381
Cardiac failure chronic 18.75 14.88 19 24492 13792 110550996
Libido decreased 18.10 14.88 13 24498 5922 110558866
Product physical consistency issue 18.09 14.88 8 24503 1432 110563356
Hydroureter 18.05 14.88 7 24504 901 110563887
Stomatitis 17.99 14.88 20 24491 270222 110294566
Product name confusion 17.94 14.88 5 24506 227 110564561
Breast pain 17.85 14.88 16 24495 9984 110554804
Metastases to penis 17.85 14.88 3 24508 10 110564778
Hyperaesthesia 17.74 14.88 19 24492 14708 110550080
Night sweats 17.69 14.88 4 24507 133979 110430809
Circulatory collapse 17.53 14.88 33 24478 42960 110521828
Subdural haematoma 17.45 14.88 30 24481 36424 110528364
Metastatic salivary gland cancer 17.42 14.88 3 24508 12 110564776
Breakthrough pain 17.40 14.88 8 24503 1568 110563220
Diabetes mellitus 17.38 14.88 55 24456 99326 110465462
Osteomyelitis 17.36 14.88 30 24481 36570 110528218
Ventricular fibrillation 17.21 14.88 32 24479 41281 110523507
Cerebral atrophy 17.14 14.88 15 24496 9070 110555718
Obstructive airways disorder 17.08 14.88 34 24477 46115 110518673
Fatigue 16.97 14.88 370 24141 1215588 109349200
Phyllodes tumour 16.97 14.88 4 24507 92 110564696
Osteitis 16.87 14.88 11 24500 4285 110560503
Urticaria 16.79 14.88 28 24483 318829 110245959
Bone cancer 16.75 14.88 9 24502 2461 110562327
Cough 16.57 14.88 50 24461 461591 110103197
Arrhythmia 16.53 14.88 43 24468 69532 110495256
Dehydration 16.32 14.88 112 24399 279399 110285389
Penile oedema 16.32 14.88 5 24506 317 110564471
Radical prostatectomy 16.27 14.88 3 24508 19 110564769
Hyperuricosuria 16.27 14.88 3 24508 19 110564769
Abdominal wall haematoma 16.27 14.88 12 24499 5693 110559095
Weight increased 16.12 14.88 44 24467 419600 110145188
Injection site induration 16.08 14.88 16 24495 11367 110553421
Treatment failure 15.88 14.88 23 24488 277211 110287577
Acquired gene mutation 15.83 14.88 9 24502 2745 110562043
Renal impairment 15.80 14.88 83 24428 188362 110376426
Hypogonadism 15.61 14.88 8 24503 1986 110562802
Infection 15.45 14.88 36 24475 362164 110202624
Hyperphosphaturia 15.44 14.88 4 24507 137 110564651
Bone trimming 15.34 14.88 3 24508 27 110564761
Renal failure 15.19 14.88 94 24417 226480 110338308
Psoriasis 15.18 14.88 6 24505 139987 110424801
Bronchitis 15.06 14.88 8 24503 157024 110407764
Pruritus 15.03 14.88 72 24439 581488 109983300
Retroperitoneal lymphadenopathy 14.95 14.88 7 24504 1429 110563359
Metastases to pelvis 14.94 14.88 6 24505 846 110563942

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L02AE51 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONES AND RELATED AGENTS
Gonadotropin releasing hormone analogues
ATC L02BB03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONE ANTAGONISTS AND RELATED AGENTS
Anti-androgens
FDA MoA N0000000243 Androgen Receptor Antagonists
FDA EPC N0000175560 Androgen Receptor Inhibitor
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35497 androgen antagonist
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35703 xenobiotic
CHEBI has role CHEBI:78298 environmental contaminant
MeSH PA D000726 Androgen Antagonists
MeSH PA D000970 Antineoplastic Agents
MeSH PA D006727 Hormone Antagonists

Related Drugs by ATC class:

L02AE Gonadotropin releasing hormone analogues 5 drugs
buserelingoserelinhistrelinleuprorelintriptorelin
L02BB Anti-androgens 5 drugs
apalutamidedarolutamideenzalutamideflutamidenilutamide

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

DiseaseRelationSNOMED_IDDOID
Metastatic Prostate Carcinoma indication
Advanced Prostatic Carcinoma off-label use
Interstitial pneumonia contraindication 64667001
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Liver function tests abnormal contraindication 166603001
Disease of liver contraindication 235856003 DOID:409
Drug-induced hepatitis contraindication 235876009
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.19 acidic
pKa2 11.84 acidic

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
Androgen receptor Nuclear hormone receptor ANTAGONIST Ki 7.72 CHEMBL CHEMBL
Cytochrome P450 2C19 Enzyme IC50 6 CHEMBL
Poly [ADP-ribose] polymerase 1 Enzyme IC50 9.24 CHEMBL
Tankyrase-1 Enzyme Kd 7.85 CHEMBL
Poly [ADP-ribose] polymerase 3 Enzyme Kd 7.62 CHEMBL
Poly [ADP-ribose] polymerase 4 Enzyme Kd 9.15 CHEMBL
Poly [ADP-ribose] polymerase 10 Enzyme Kd 5.24 CHEMBL
Mono [ADP-ribose] polymerase PARP16 Enzyme Kd 6 CHEMBL
Poly [ADP-ribose] polymerase 2 Enzyme IC50 9.70 CHEMBL
Poly [ADP-ribose] polymerase 8 Enzyme Kd 5.96 CHEMBL
Androgen receptor Transcription factor Ki 7.85 CHEMBL
Androgen receptor Transcription factor IC50 6.17 CHEMBL
Progesterone receptor Transcription factor IC50 5.25 CHEMBL
Progesterone receptor Transcription factor Ki 5.14 CHEMBL

External reference:

IDSource
4020950 VUID
N0000148428 NUI
D00961 KEGG_DRUG
151495 RXNORM
C0285590 UMLSCUI
CHEBI:3090 CHEBI
CHEMBL3137320 ChEMBL_ID
CHEMBL409 ChEMBL_ID
DB01128 DRUGBANK_ID
C053541 MESH_SUPPLEMENTAL_RECORD_UI
2375 PUBCHEM_CID
2863 IUPHAR_LIGAND_ID
7021 INN_ID
A0Z3NAU9DP UNII
165839 MMSL
4282 MMSL
4824 MMSL
d03850 MMSL
108766001 SNOMEDCT_US
386908000 SNOMEDCT_US
4020950 VANDF
005064 NDDF
A0Z3NAU9DP INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Bicalutamide HUMAN PRESCRIPTION DRUG LABEL 1 16729-023 TABLET 50 mg ORAL ANDA 26 sections
bicalutamide Human Prescription Drug Label 1 47335-485 TABLET, FILM COATED 50 mg ORAL ANDA 26 sections
Bicalutamide HUMAN PRESCRIPTION DRUG LABEL 1 51407-010 TABLET 50 mg ORAL NDA 27 sections
CASODEX HUMAN PRESCRIPTION DRUG LABEL 1 54868-4503 TABLET 50 mg ORAL NDA 25 sections
Bicalutamide HUMAN PRESCRIPTION DRUG LABEL 1 54868-6133 TABLET, FILM COATED 50 mg ORAL ANDA 28 sections
Bicalutamide HUMAN PRESCRIPTION DRUG LABEL 1 60429-177 TABLET, FILM COATED 50 mg ORAL ANDA 26 sections
Bicalutamide HUMAN PRESCRIPTION DRUG LABEL 1 60505-2642 TABLET 50 mg ORAL ANDA 26 sections
CASODEX HUMAN PRESCRIPTION DRUG LABEL 1 62559-680 TABLET 50 mg ORAL NDA 27 sections
Bicalutamide HUMAN PRESCRIPTION DRUG LABEL 1 62559-890 TABLET 50 mg ORAL NDA 27 sections
Bicalutamide HUMAN PRESCRIPTION DRUG LABEL 1 63629-8308 TABLET 50 mg ORAL ANDA 25 sections
Bicalutamide HUMAN PRESCRIPTION DRUG LABEL 1 71205-577 TABLET 50 mg ORAL ANDA 26 sections
Bicalutamide HUMAN PRESCRIPTION DRUG LABEL 1 72578-215 TABLET 50 mg ORAL ANDA 27 sections
bicalutamide HUMAN PRESCRIPTION DRUG LABEL 1 82804-082 TABLET, FILM COATED 50 mg ORAL ANDA 26 sections
Bicalutamide HUMAN PRESCRIPTION DRUG LABEL 1 84508-001 TABLET 50 mg ORAL ANDA 27 sections