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

Stem definitionDrug idCAS RN
non-steroid antiandrogens 4628 915087-33-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • enzalutamide
  • xtandi
  • MDV3100
  • MDV-3100
Enzalutamide is an androgen receptor inhibitor that acts on different steps in the androgen receptor signaling pathway. Enzalutamide has been shown to competitively inhibit androgen binding to androgen receptors and inhibit androgen receptor nuclear translocation and interaction with DNA. A major metabolite, N‑desmethyl enzalutamide, exhibited similar in vitro activity to enzalutamide. Enzalutamide decreased proliferation and induced cell death of prostate cancer cells in vitro, and decreased tumor volume in a mouse prostate cancer xenograft model.
  • Molecular weight: 464.44
  • Formula: C21H16F4N4O2S
  • CLOGP: 3.35
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 76.44
  • ALOGS: -5.53
  • ROTB: 4

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.16 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Aug. 31, 2012 FDA ASTELLAS
March 24, 2014 PMDA Astellas Pharma Inc

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 44.33 40.13 15 210 68109 50536790

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
Malignant neoplasm progression 5233.82 16.74 2312 35647 71547 29465021
Prostatic specific antigen increased 3056.93 16.74 976 36983 11588 29524980
Death 1883.20 16.74 2234 35725 339850 29196718
Fatigue 1075.56 16.74 1641 36318 315180 29221388
Underdose 898.22 16.74 392 37567 11477 29525091
Product size issue 697.99 16.74 159 37800 410 29536158
Hot flush 691.60 16.74 351 37608 14519 29522049
Decreased appetite 388.00 16.74 679 37280 144663 29391905
Dysphagia 368.03 16.74 401 37558 54525 29482043
Metastases to bone 342.52 16.74 192 37767 9706 29526862
Product use complaint 294.72 16.74 89 37870 855 29535713
Product storage error 289.76 16.74 149 37810 6321 29530247
Asthenia 287.43 16.74 759 37200 214491 29322077
Hormone-refractory prostate cancer 221.11 16.74 65 37894 564 29536004
Prostate cancer metastatic 204.14 16.74 108 37851 4858 29531710
Prostate cancer 202.22 16.74 204 37755 25323 29511245
Prescribed underdose 198.44 16.74 124 37835 7662 29528906
Bone pain 177.30 16.74 164 37795 18288 29518280
Back pain 161.36 16.74 385 37574 101899 29434669
Osteonecrosis of jaw 141.94 16.74 138 37821 16372 29520196
Toxicity to various agents 129.27 16.74 32 37927 173629 29362939
Product physical issue 123.05 16.74 58 37901 2030 29534538
Dizziness 107.08 16.74 504 37455 189180 29347388
Prostatic specific antigen abnormal 98.49 16.74 32 37927 398 29536170
Nausea 96.21 16.74 667 37292 288588 29247980
Drug ineffective 95.39 16.74 792 37167 362378 29174190
Intentional underdose 86.87 16.74 32 37927 591 29535977
Acute kidney injury 86.87 16.74 129 37830 265138 29271430
Completed suicide 86.60 16.74 8 37951 90238 29446330
Peripheral swelling 79.69 16.74 220 37739 63519 29473049
Muscular weakness 77.40 16.74 214 37745 61838 29474730
Spinal cord compression 76.35 16.74 51 37908 3531 29533037
Treatment noncompliance 74.61 16.74 121 37838 24106 29512462
Dysgeusia 73.60 16.74 116 37843 22558 29514010
Off label use 73.20 16.74 175 37784 300625 29235943
Pyrexia 71.84 16.74 165 37794 287457 29249111
Circumstance or information capable of leading to medication error 67.93 16.74 35 37924 1489 29535079
Fall 65.57 16.74 420 37539 176758 29359810
Hypotension 65.02 16.74 93 37866 194261 29342307
Foreign body in respiratory tract 64.00 16.74 18 37941 131 29536437
Cancer pain 63.90 16.74 39 37920 2308 29534260
Pneumonia 63.24 16.74 206 37753 319966 29216602
Memory impairment 52.80 16.74 133 37826 36337 29500231
Foreign body 50.76 16.74 25 37934 965 29535603
Product availability issue 48.12 16.74 25 37934 1082 29535486
Investigation 47.85 16.74 23 37936 841 29535727
Malaise 44.79 16.74 354 37605 159248 29377320
Bone lesion 42.57 16.74 32 37927 2672 29533896
Febrile neutropenia 42.34 16.74 49 37910 112191 29424377
Rhabdomyolysis 41.80 16.74 13 37946 60795 29475773
Infusion related reaction 41.78 16.74 4 37955 43882 29492686
Oxygen saturation decreased 40.49 16.74 5 37954 44932 29491636
Metastases to lymph nodes 39.13 16.74 36 37923 3981 29532587
Product packaging quantity issue 38.28 16.74 19 37940 746 29535822
Drug hypersensitivity 38.27 16.74 20 37939 68386 29468182
Blood creatinine increased 38.02 16.74 32 37927 85070 29451498
Tachycardia 37.89 16.74 23 37936 72387 29464181
Restless legs syndrome 36.59 16.74 45 37914 6939 29529629
Neutropenia 36.58 16.74 71 37888 131640 29404928
Breast tenderness 36.38 16.74 18 37941 702 29535866
Insomnia 36.25 16.74 216 37743 88545 29448023
Urinary tract infection 36.17 16.74 186 37773 72168 29464400
Constipation 35.23 16.74 259 37700 113901 29422667
Metastasis 33.93 16.74 31 37928 3398 29533170
Intentional dose omission 33.75 16.74 25 37934 2041 29534527
Arthralgia 33.46 16.74 299 37660 139318 29397250
Asthma 32.45 16.74 3 37956 33846 29502722
Choking 32.11 16.74 34 37925 4457 29532111
Hydronephrosis 31.61 16.74 47 37912 8683 29527885
Plasma cell myeloma 31.39 16.74 5 37954 37110 29499458
Adverse event 31.30 16.74 64 37895 15227 29521341
Psoriasis 30.51 16.74 3 37956 32224 29504344
Blood urine present 30.40 16.74 49 37910 9706 29526862
Weight decreased 29.67 16.74 310 37649 150595 29385973
Prostate cancer recurrent 29.61 16.74 17 37942 898 29535670
Metastases to bladder 29.36 16.74 8 37951 51 29536517
Urinary tract obstruction 29.15 16.74 28 37931 3269 29533299
Bradycardia 28.91 16.74 25 37934 65604 29470964
Condition aggravated 28.85 16.74 94 37865 146201 29390367
Haematuria 28.29 16.74 122 37837 44017 29492551
Metastases to spine 28.29 16.74 23 37936 2153 29534415
C-reactive protein increased 27.78 16.74 11 37948 44252 29492316
Aggression 27.47 16.74 6 37953 35535 29501033
Blood creatine phosphokinase increased 27.38 16.74 9 37950 40635 29495933
Respiratory failure 27.27 16.74 52 37907 97079 29439489
Hypoglycaemia 27.24 16.74 14 37945 48332 29488236
Marasmus 26.88 16.74 13 37946 482 29536086
White blood cell count decreased 26.73 16.74 41 37918 83321 29453247
Cough 26.70 16.74 79 37880 126648 29409920
Cardiac arrest 26.58 16.74 43 37916 85548 29451020
Cardio-respiratory arrest 26.56 16.74 16 37943 50585 29485983
Coma 26.11 16.74 9 37950 39441 29497127
Rheumatoid arthritis 25.73 16.74 5 37954 32147 29504421
Abdominal discomfort 25.23 16.74 125 37834 47778 29488790
Renal failure 24.93 16.74 74 37885 118525 29418043
Wheezing 24.91 16.74 6 37953 33234 29503334
Agitation 24.53 16.74 18 37941 51286 29485282
Sinusitis 24.22 16.74 7 37952 34343 29502225
Ageusia 23.99 16.74 42 37917 8896 29527672
Hospice care 23.92 16.74 31 37928 5037 29531531
Foreign body in throat 23.88 16.74 7 37952 60 29536508
Feeling abnormal 23.83 16.74 135 37824 54310 29482258
Hypoxia 23.48 16.74 16 37943 47363 29489205
Vision blurred 23.45 16.74 108 37851 40068 29496500
Blood urea increased 23.30 16.74 4 37955 28108 29508460
Drug reaction with eosinophilia and systemic symptoms 23.16 16.74 4 37955 27988 29508580
Poor quality product administered 22.94 16.74 18 37941 1601 29534967
Pancytopenia 22.93 16.74 45 37914 83123 29453445
Suicidal ideation 22.84 16.74 8 37951 34708 29501860
Metastases to liver 22.37 16.74 48 37911 11808 29524760
Suicide attempt 22.20 16.74 8 37951 34102 29502466
Respiratory distress 21.81 16.74 7 37952 32099 29504469
Septic shock 21.80 16.74 29 37930 62531 29474037
Cerebrovascular accident 21.19 16.74 170 37789 76741 29459827
Product use issue 21.00 16.74 21 37938 51423 29485145
Balance disorder 20.94 16.74 97 37862 36073 29500495
Melaena 20.83 16.74 7 37952 31169 29505399
Product odour abnormal 20.58 16.74 12 37947 653 29535915
Bronchitis 20.29 16.74 11 37948 36857 29499711
Therapeutic product effect incomplete 19.84 16.74 13 37946 39292 29497276
Metabolic acidosis 19.64 16.74 12 37947 37650 29498918
International normalised ratio increased 19.42 16.74 17 37942 44355 29492213
Multiple organ dysfunction syndrome 19.32 16.74 32 37927 63084 29473484
Renal impairment 19.14 16.74 48 37911 81285 29455283
Cognitive disorder 19.12 16.74 70 37889 23429 29513139
Stomatitis 19.11 16.74 12 37947 37101 29499467
Inappropriate schedule of product administration 18.63 16.74 109 37850 44363 29492205
Deep vein thrombosis 18.61 16.74 28 37931 57371 29479197
Bone cancer metastatic 18.21 16.74 7 37952 146 29536422
White blood cell count increased 18.15 16.74 13 37946 37503 29499065
Mucosal inflammation 18.02 16.74 9 37950 31586 29504982
Weight increased 17.46 16.74 46 37913 76621 29459947
Urethral intrinsic sphincter deficiency 17.37 16.74 4 37955 11 29536557
Staphylococcal infection 17.18 16.74 8 37951 29232 29507336
Chronic kidney disease 17.12 16.74 13 37946 36403 29500165
Blood glucose increased 17.05 16.74 31 37928 58953 29477615
Product expiration date issue 16.98 16.74 3 37956 0 29536568
Prostatic specific antigen decreased 16.97 16.74 6 37953 98 29536470

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
Malignant neoplasm progression 3185.53 17.29 1340 26393 111531 64359468
Prostatic specific antigen increased 2975.27 17.29 701 27032 8059 64462940
Death 1434.40 17.29 1363 26370 481342 63989657
Fatigue 698.90 17.29 1188 26545 747542 63723457
Underdose 575.22 17.29 261 27472 25568 64445431
Product size issue 471.71 17.29 96 27637 510 64470489
Hot flush 411.41 17.29 253 27480 45982 64425017
Decreased appetite 374.10 17.29 528 27205 280761 64190238
Prostate cancer 309.54 17.29 157 27576 19638 64451361
Asthenia 282.00 17.29 588 27145 427456 64043543
Metastases to bone 242.90 17.29 135 27598 20300 64450699
Prescribed underdose 192.46 17.29 111 27622 17904 64453095
Dysphagia 175.86 17.29 223 27510 106589 64364410
Prostate cancer metastatic 169.83 17.29 61 27672 3243 64467756
Product use complaint 150.95 17.29 47 27686 1599 64469400
Osteonecrosis of jaw 138.83 17.29 124 27609 39701 64431298
Hormone-refractory prostate cancer 127.20 17.29 30 27703 342 64470657
Bone pain 118.30 17.29 123 27610 47449 64423550
Back pain 111.83 17.29 296 27437 249875 64221124
Prostatic specific antigen abnormal 103.67 17.29 23 27710 195 64470804
Toxicity to various agents 93.48 17.29 21 27712 363492 64107507
Product storage error 89.09 17.29 61 27672 13257 64457742
Dizziness 82.93 17.29 385 27348 429778 64041221
Cancer pain 82.16 17.29 39 27694 4218 64466781
Intentional underdose 76.61 17.29 30 27703 2028 64468971
Muscular weakness 70.88 17.29 164 27569 127174 64343825
Completed suicide 68.71 17.29 8 27725 224406 64246593
Dysgeusia 61.69 17.29 88 27645 46959 64424040
Drug hypersensitivity 58.60 17.29 15 27718 237800 64233199
Infusion related reaction 58.32 17.29 3 27730 164464 64306535
Spinal cord compression 55.25 17.29 33 27700 5670 64465329
Rheumatoid arthritis 55.24 17.29 4 27729 164290 64306709
Haematuria 50.34 17.29 92 27641 60379 64410620
Foreign body in respiratory tract 44.90 17.29 13 27720 343 64470656
Product physical issue 44.31 17.29 24 27709 3425 64467574
Sinusitis 42.72 17.29 6 27727 145922 64325077
Bone lesion 40.33 17.29 26 27707 5111 64465888
Memory impairment 38.79 17.29 102 27631 85580 64385419
Constipation 36.74 17.29 195 27538 229142 64241857
Product availability issue 36.64 17.29 18 27715 2098 64468901
Fall 36.14 17.29 304 27429 416522 64054477
Treatment noncompliance 34.73 17.29 65 27668 43417 64427582
Weight decreased 34.19 17.29 225 27508 285514 64185485
Nausea 33.53 17.29 498 27235 785302 63685697
Blood urine present 32.86 17.29 40 27693 18300 64452699
Hydronephrosis 32.39 17.29 35 27698 14090 64456909
Oxygen saturation decreased 32.34 17.29 4 27729 107172 64363827
Metastases to lymph nodes 32.07 17.29 28 27705 8689 64462310
Prostate cancer recurrent 31.80 17.29 12 27721 733 64470266
Asthma 30.13 17.29 3 27730 95222 64375777
Marasmus 30.02 17.29 12 27721 856 64470143
Lower respiratory tract infection 29.89 17.29 3 27730 94611 64376388
Stomatitis 28.79 17.29 6 27727 109599 64361400
Restless legs syndrome 28.53 17.29 36 27697 17080 64453919
Insomnia 27.53 17.29 162 27571 197674 64273325
Metastases to spine 27.52 17.29 18 27715 3625 64467374
Hypotension 27.33 17.29 79 27654 380895 64090104
Metastasis 26.58 17.29 21 27712 5674 64465325
Ageusia 26.18 17.29 31 27702 13782 64457217
Urinary tract obstruction 25.92 17.29 18 27715 3999 64467000
Product use issue 25.42 17.29 17 27716 151698 64319301
Therapeutic product effect decreased 25.27 17.29 9 27724 115342 64355657
Drug ineffective 25.11 17.29 503 27230 839744 63631255
Tachycardia 24.74 17.29 17 27716 149562 64321437
Condition aggravated 24.73 17.29 80 27653 372346 64098653
Peripheral swelling 24.57 17.29 164 27569 208989 64262010
Blood testosterone increased 24.21 17.29 10 27723 776 64470223
Circumstance or information capable of leading to medication error 24.01 17.29 16 27717 3324 64467675
Malaise 23.95 17.29 268 27465 395979 64075020
Pyrexia 23.74 17.29 142 27591 558502 63912497
Acute kidney injury 23.69 17.29 106 27627 449134 64021865
Weight increased 23.07 17.29 35 27698 213313 64257686
Bradycardia 23.02 17.29 11 27722 118208 64352791
Nocturia 22.73 17.29 26 27707 11139 64459860
Intentional dose omission 22.51 17.29 19 27714 5633 64465366
Arthropathy 22.44 17.29 12 27721 120955 64350044
Drug level decreased 22.10 17.29 26 27707 11477 64459522
Vision blurred 22.05 17.29 87 27646 90229 64380770
Bronchitis 21.36 17.29 10 27723 108733 64362266
Cerebrovascular accident 21.33 17.29 116 27617 137467 64333532
Urethral intrinsic sphincter deficiency 20.78 17.29 4 27729 15 64470984
Prostatic specific antigen decreased 20.74 17.29 5 27728 63 64470936
Coma 20.67 17.29 6 27727 87609 64383390
Choking 20.55 17.29 24 27709 10514 64460485
Injection site erythema 20.50 17.29 3 27730 70797 64400202
Hypersomnia 20.34 17.29 33 27700 19684 64451315
Breast tenderness 20.22 17.29 12 27721 2037 64468962
Adrenocortical insufficiency acute 20.18 17.29 13 27720 2552 64468447
Wheezing 19.98 17.29 5 27728 80574 64390425
Cough 19.98 17.29 65 27668 302083 64168916
Hepatic enzyme increased 19.89 17.29 16 27717 129927 64341072
Anaemia 19.73 17.29 249 27484 378431 64092568
Metastases to bladder 18.71 17.29 6 27727 225 64470774
Infection 18.42 17.29 32 27701 184848 64286151
International normalised ratio abnormal 18.30 17.29 16 27717 4972 64466027
Balance disorder 18.24 17.29 78 27655 83848 64387151
Therapeutic product effect incomplete 18.14 17.29 11 27722 103471 64367528
Metastases to liver 18.14 17.29 35 27698 23906 64447093
Foreign body 18.12 17.29 12 27721 2467 64468532
Injection site pain 17.97 17.29 13 27720 111395 64359604
Hypersensitivity 17.81 17.29 36 27697 196416 64274583
Subdural haematoma 17.68 17.29 38 27695 28016 64442983
Hospice care 17.67 17.29 19 27714 7606 64463393
Gynaecomastia 17.60 17.29 17 27716 5999 64465000
Migraine 17.37 17.29 3 27730 62674 64408325

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L02BB04 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
FDA MoA N0000185506 Cytochrome P450 3A4 Inducers
FDA MoA N0000185507 Cytochrome P450 2C9 Inducers
FDA MoA N0000185607 Cytochrome P450 2C19 Inducers
CHEBI has role CHEBI:35497 antiandrogen
CHEBI has role CHEBI:35610 antineoplastic agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Metastasis from malignant tumor of prostate indication 314994000
Malignant tumor of prostate indication 399068003 DOID:10283




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.88 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
40MG XTANDI ASTELLAS N203415 Aug. 31, 2012 RX CAPSULE ORAL 9126941 May 15, 2026 THE TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (CRPC).
40MG XTANDI ASTELLAS N203415 Aug. 31, 2012 RX CAPSULE ORAL 9126941 May 15, 2026 THE TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER
40MG XTANDI ASTELLAS N203415 Aug. 31, 2012 RX CAPSULE ORAL 9126941 May 15, 2026 TREATMENT OF PATIENTS WITH CASTRATION-RESISTANT PROSTATE CANCER (CRPC)
40MG XTANDI ASTELLAS N213674 Aug. 4, 2020 RX TABLET ORAL 9126941 May 15, 2026 THE TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER
40MG XTANDI ASTELLAS N213674 Aug. 4, 2020 RX TABLET ORAL 9126941 May 15, 2026 TREATMENT OF PATIENTS WITH CASTRATION-RESISTANT PROSTATE CANCER (CRPC)
80MG XTANDI ASTELLAS N213674 Aug. 4, 2020 RX TABLET ORAL 9126941 May 15, 2026 THE TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER
80MG XTANDI ASTELLAS N213674 Aug. 4, 2020 RX TABLET ORAL 9126941 May 15, 2026 TREATMENT OF PATIENTS WITH CASTRATION-RESISTANT PROSTATE CANCER (CRPC)
40MG XTANDI ASTELLAS N203415 Aug. 31, 2012 RX CAPSULE ORAL 8183274 Aug. 24, 2026 THE TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (CRPC).
40MG XTANDI ASTELLAS N203415 Aug. 31, 2012 RX CAPSULE ORAL 8183274 Aug. 24, 2026 THE TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-RESISTANT PROSTATE CANCER WHO HAVE PREVIOUSLY RECEIVED DOCETAXEL
40MG XTANDI ASTELLAS N203415 Aug. 31, 2012 RX CAPSULE ORAL 8183274 Aug. 24, 2026 THE TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER
40MG XTANDI ASTELLAS N203415 Aug. 31, 2012 RX CAPSULE ORAL 8183274 Aug. 24, 2026 TREATMENT OF PATIENTS WITH CASTRATION-RESISTANT PROSTATE CANCER (CRPC)
40MG XTANDI ASTELLAS N213674 Aug. 4, 2020 RX TABLET ORAL 8183274 Aug. 24, 2026 THE TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER
40MG XTANDI ASTELLAS N213674 Aug. 4, 2020 RX TABLET ORAL 8183274 Aug. 24, 2026 TREATMENT OF PATIENTS WITH CASTRATION-RESISTANT PROSTATE CANCER (CRPC)
80MG XTANDI ASTELLAS N213674 Aug. 4, 2020 RX TABLET ORAL 8183274 Aug. 24, 2026 THE TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER
80MG XTANDI ASTELLAS N213674 Aug. 4, 2020 RX TABLET ORAL 8183274 Aug. 24, 2026 TREATMENT OF PATIENTS WITH CASTRATION-RESISTANT PROSTATE CANCER (CRPC)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
40MG XTANDI ASTELLAS N203415 Aug. 31, 2012 RX CAPSULE ORAL Dec. 16, 2022 TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC)
40MG XTANDI ASTELLAS N213674 Aug. 4, 2020 RX TABLET ORAL Dec. 16, 2022 TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC)
80MG XTANDI ASTELLAS N213674 Aug. 4, 2020 RX TABLET ORAL Dec. 16, 2022 TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Androgen receptor Nuclear hormone receptor ANTAGONIST EC50 7.31 CHEMBL CHEMBL
Prostate-specific antigen Surface antigen IC50 6.89 CHEMBL
Androgen receptor Transcription factor IC50 6.53 CHEMBL

External reference:

IDSource
93T0T9GKNU UNII
D10218 KEGG_DRUG
4031716 VUID
N0000185726 NUI
4031716 VANDF
C3496793 UMLSCUI
CHEBI:68534 CHEBI
CHEMBL1082407 ChEMBL_ID
15951529 PUBCHEM_CID
DB08899 DRUGBANK_ID
9621 INN_ID
C540278 MESH_SUPPLEMENTAL_RECORD_UI
6812 IUPHAR_LIGAND_ID
1307298 RXNORM
192757 MMSL
28802 MMSL
d07900 MMSL
014630 NDDF
703125003 SNOMEDCT_US
703684000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Xtandi HUMAN PRESCRIPTION DRUG LABEL 1 0469-0125 CAPSULE 40 mg ORAL NDA 27 sections
Xtandi HUMAN PRESCRIPTION DRUG LABEL 1 0469-0125 CAPSULE 40 mg ORAL NDA 27 sections
Xtandi HUMAN PRESCRIPTION DRUG LABEL 1 0469-0625 TABLET 40 mg ORAL NDA 27 sections
Xtandi HUMAN PRESCRIPTION DRUG LABEL 1 0469-0625 TABLET 40 mg ORAL NDA 27 sections
Xtandi HUMAN PRESCRIPTION DRUG LABEL 1 0469-0725 TABLET 80 mg ORAL NDA 27 sections
Xtandi HUMAN PRESCRIPTION DRUG LABEL 1 0469-0725 TABLET 80 mg ORAL NDA 27 sections
Xtandi HUMAN PRESCRIPTION DRUG LABEL 1 0469-1125 CAPSULE 40 mg ORAL NDA 27 sections
Xtandi HUMAN PRESCRIPTION DRUG LABEL 1 0469-1725 TABLET 40 mg ORAL NDA 27 sections