enzalutamide ๐Ÿถ 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, Nโ€‘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: ONP

  • 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 43.69 37.00 15 229 82106 63406672

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 5422.83 16.65 2441 39039 85605 34829846
Prostatic specific antigen increased 3437.55 16.65 1087 40393 13593 34901858
Death 1833.43 16.65 2287 39193 395762 34519689
Fatigue 1092.58 16.65 1725 39755 368928 34546523
Underdose 913.06 16.65 405 41075 13375 34902076
Hot flush 758.66 16.65 388 41092 17678 34897773
Product size issue 690.99 16.65 163 41317 571 34914880
Metastases to bone 442.04 16.65 236 41244 11734 34903717
Decreased appetite 403.20 16.65 713 40767 165679 34749772
Dysphagia 391.55 16.65 424 41056 61957 34853494
Product storage error 353.97 16.65 179 41301 7943 34907508
Product use complaint 317.49 16.65 102 41378 1330 34914121
Asthenia 316.58 16.65 813 40667 244438 34671013
Prostate cancer metastatic 264.92 16.65 132 41348 5671 34909780
Hormone-refractory prostate cancer 233.06 16.65 69 41411 671 34914780
Prescribed underdose 229.53 16.65 139 41341 8794 34906657
Bone pain 205.47 16.65 181 41299 20505 34894946
Osteonecrosis of jaw 205.18 16.65 170 41310 17719 34897732
Prostate cancer 205.14 16.65 244 41236 39405 34876046
Back pain 163.96 16.65 411 41069 121378 34794073
Prostatic specific antigen abnormal 150.43 16.65 49 41431 669 34914782
Toxicity to various agents 138.13 16.65 34 41446 200328 34715123
Product physical issue 134.60 16.65 64 41416 2477 34912974
Dizziness 108.37 16.65 529 40951 217992 34697459
Off label use 99.10 16.65 220 41260 419304 34496147
Intentional underdose 90.86 16.65 33 41447 635 34914816
Acute kidney injury 87.64 16.65 142 41338 304846 34610605
Completed suicide 87.20 16.65 8 41472 98160 34817291
Spinal cord compression 84.84 16.65 55 41425 3920 34911531
Cancer pain 82.92 16.65 47 41433 2625 34912826
Muscular weakness 80.70 16.65 229 41251 72668 34842783
Nausea 79.45 16.65 680 40800 339228 34576223
Pyrexia 77.39 16.65 176 41304 332837 34582614
Fall 74.02 16.65 452 41028 202433 34713018
Treatment noncompliance 72.31 16.65 124 41356 27976 34887475
Hypotension 71.61 16.65 95 41385 221554 34693897
Drug ineffective 71.13 16.65 840 40640 455911 34459540
Dysgeusia 70.92 16.65 119 41361 26378 34889073
Peripheral swelling 70.16 16.65 225 41255 76316 34839135
Metastases to lymph nodes 69.42 16.65 52 41428 4676 34910775
Circumstance or information capable of leading to medication error 65.41 16.65 35 41445 1744 34913707
Foreign body in respiratory tract 63.05 16.65 18 41462 152 34915299
Product availability issue 60.74 16.65 34 41446 1853 34913598
Pneumonia 58.63 16.65 227 41253 362400 34553051
Memory impairment 56.88 16.65 145 41335 43173 34872278
Febrile neutropenia 52.47 16.65 51 41429 136798 34778653
Bone lesion 51.27 16.65 36 41444 2927 34912524
Foreign body 50.69 16.65 25 41455 1049 34914402
Infusion related reaction 47.98 16.65 4 41476 53053 34862398
Investigation 47.96 16.65 23 41457 907 34914544
Oxygen saturation decreased 46.17 16.65 5 41475 53813 34861638
Malaise 45.46 16.65 376 41104 185449 34730002
Rhabdomyolysis 44.17 16.65 13 41467 68150 34847301
Malignant spinal cord compression 42.38 16.65 13 41467 144 34915307
Product packaging quantity issue 42.00 16.65 21 41459 908 34914543
Drug hypersensitivity 41.31 16.65 22 41458 80507 34834944
Insomnia 39.38 16.65 234 41246 103673 34811778
Asthma 39.17 16.65 3 41477 42653 34872798
Hydronephrosis 38.29 16.65 54 41426 10292 34905159
Urinary tract infection 38.29 16.65 199 41281 83882 34831569
Restless legs syndrome 37.64 16.65 48 41432 8306 34907145
Prostate cancer recurrent 37.44 16.65 20 41460 993 34914458
Condition aggravated 37.30 16.65 111 41369 192085 34723366
Haematuria 36.95 16.65 137 41343 49929 34865522
Choking 36.58 16.65 37 41443 4978 34910473
Breast tenderness 36.55 16.65 18 41462 753 34914698
Arthralgia 35.82 16.65 333 41147 169708 34745743
Adverse event 35.67 16.65 73 41407 18804 34896647
Neutropenia 35.37 16.65 84 41396 156694 34758757
Psoriasis 34.88 16.65 3 41477 38809 34876642
Blood urine present 33.54 16.65 52 41428 10782 34904669
Cough 33.43 16.65 81 41399 150059 34765392
Blood testosterone increased 33.18 16.65 20 41460 1253 34914198
Tachycardia 33.16 16.65 31 41449 84741 34830710
Blood creatinine increased 32.38 16.65 39 41441 94937 34820514
C-reactive protein increased 32.10 16.65 12 41468 54086 34861365
Marasmus 31.48 16.65 15 41465 583 34914868
Constipation 31.25 16.65 273 41207 136709 34778742
Plasma cell myeloma 31.20 16.65 6 41474 42031 34873420
Metastasis 31.00 16.65 31 41449 4113 34911338
Wheezing 30.53 16.65 6 41474 41396 34874055
Metastases to spine 30.53 16.65 25 41455 2559 34912892
Ageusia 29.87 16.65 48 41432 10260 34905191
Foreign body in throat 29.65 16.65 9 41471 96 34915355
Rheumatoid arthritis 29.37 16.65 5 41475 38233 34877218
Weight decreased 29.34 16.65 329 41151 175972 34739479
Metastases to bladder 28.97 16.65 8 41472 59 34915392
Respiratory failure 28.83 16.65 53 41427 108519 34806932
Urinary tract obstruction 28.79 16.65 28 41452 3592 34911859
Sinusitis 28.51 16.65 7 41473 41395 34874056
Metastases to liver 28.42 16.65 55 41425 13608 34901843
Poor quality product administered 28.05 16.65 21 41459 1886 34913565
Aggression 28.00 16.65 6 41474 38958 34876493
Hypoglycaemia 27.91 16.65 15 41465 54625 34860826
BRCA1 gene mutation 27.83 16.65 7 41473 34 34915417
Coma 27.32 16.65 10 41470 45668 34869783
Cardiac arrest 27.29 16.65 45 41435 96114 34819337
BRCA2 gene mutation 27.19 16.65 7 41473 38 34915413
Therapeutic product effect incomplete 27.12 16.65 13 41467 50528 34864923
Cardio-respiratory arrest 27.04 16.65 16 41464 55257 34860194
Blood creatine phosphokinase increased 26.53 16.65 10 41470 44847 34870604
COVID-19 26.26 16.65 32 41448 77518 34837933
Agitation 26.19 16.65 18 41462 57381 34858070
White blood cell count decreased 25.86 16.65 46 41434 95399 34820052
Intentional product use issue 25.68 16.65 20 41460 59796 34855655
Bradycardia 25.67 16.65 31 41449 75387 34840064
Suicidal ideation 25.62 16.65 8 41472 40380 34875071
Feeling abnormal 25.62 16.65 145 41335 63090 34852361
Renal failure 24.87 16.65 76 41404 130481 34784970
Vision blurred 24.63 16.65 114 41366 45849 34869602
Suicide attempt 24.37 16.65 8 41472 39108 34876343
Cerebrovascular accident 24.22 16.65 178 41302 84633 34830818
Hypoxia 24.19 16.65 18 41462 55077 34860374
Balance disorder 24.17 16.65 104 41376 40550 34874901
Product use in unapproved indication 24.13 16.65 66 41414 117433 34798018
Intentional dose omission 24.03 16.65 25 41455 3475 34911976
Multiple organ dysfunction syndrome 23.47 16.65 34 41446 76532 34838919
Peri-implantitis 23.28 16.65 8 41472 130 34915321
Pelvic pain 23.22 16.65 21 41459 2459 34912992
Mucosal inflammation 22.20 16.65 9 41471 38613 34876838
Abdominal pain 21.74 16.65 110 41370 163508 34751943
Blood urea increased 21.17 16.65 5 41475 30359 34885092
Septic shock 20.96 16.65 33 41447 71801 34843650
Abdominal discomfort 20.90 16.65 132 41348 59703 34855748
Weight increased 20.84 16.65 50 41430 92983 34822468
Melaena 20.73 16.65 8 41472 35372 34880079
Drug reaction with eosinophilia and systemic symptoms 20.13 16.65 7 41473 33005 34882446
Pancytopenia 19.87 16.65 53 41427 95104 34820347
Bone cancer metastatic 19.75 16.65 8 41472 209 34915242
Product odour abnormal 19.73 16.65 12 41468 764 34914687
Hospice care 19.68 16.65 32 41448 6908 34908543
Product use issue 19.45 16.65 28 41452 63188 34852263
Respiratory distress 19.40 16.65 9 41471 35656 34879795
Second primary malignancy 19.23 16.65 34 41446 7852 34907599
Cognitive disorder 19.10 16.65 76 41404 28617 34886834
Wrong technique in product usage process 19.09 16.65 89 41391 35897 34879554
International normalised ratio increased 18.86 16.65 17 41463 47310 34868141
Lower respiratory tract infection 18.80 16.65 7 41473 31630 34883821
Metastases to lung 18.75 16.65 37 41443 9283 34906168
Cystitis 18.73 16.65 38 41442 9727 34905724
Bronchitis 18.05 16.65 14 41466 41949 34873502
Urethral intrinsic sphincter deficiency 17.68 16.65 4 41476 11 34915440
Neuroendocrine carcinoma 17.40 16.65 9 41471 418 34915033
White blood cell count increased 17.36 16.65 14 41466 41137 34874314
Lymphocyte count decreased 17.28 16.65 3 41477 22619 34892832
Stomatitis 17.27 16.65 15 41465 42499 34872952
Product expiration date issue 17.21 16.65 3 41477 0 34915451
Deep vein thrombosis 17.18 16.65 32 41448 65216 34850235
Ascites 17.09 16.65 18 41462 46553 34868898
Metabolic acidosis 17.04 16.65 16 41464 43664 34871787
Drug level increased 16.72 16.65 3 41477 22093 34893358
Staphylococcal infection 16.72 16.65 9 41471 32751 34882700
Blood pressure decreased 16.66 16.65 22 41458 51493 34863958

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 3441.94 17.78 1446 29151 134544 79579247
Prostatic specific antigen increased 3429.47 17.78 795 29802 9591 79704200
Death 1450.30 17.78 1401 29196 565113 79148678
Fatigue 684.90 17.78 1248 29349 928479 78785312
Underdose 577.94 17.78 273 30324 32878 79680913
Product size issue 467.78 17.78 98 30499 700 79713091
Hot flush 461.50 17.78 278 30319 54599 79659192
Decreased appetite 374.66 17.78 552 30045 341866 79371925
Prostate cancer 336.35 17.78 190 30407 33078 79680713
Metastases to bone 318.02 17.78 165 30432 24262 79689529
Asthenia 292.25 17.78 620 29977 511069 79202722
Prostate cancer metastatic 245.73 17.78 82 30515 3925 79709866
Osteonecrosis of jaw 203.84 17.78 153 30444 43073 79670718
Dysphagia 192.97 17.78 236 30361 121900 79591891
Prescribed underdose 186.71 17.78 125 30472 29389 79684402
Product use complaint 177.22 17.78 57 30540 2426 79711365
Hormone-refractory prostate cancer 145.06 17.78 34 30563 426 79713365
Bone pain 140.90 17.78 138 30459 55604 79658187
Prostatic specific antigen abnormal 139.75 17.78 33 30564 428 79713363
Back pain 120.15 17.78 320 30277 303860 79409931
Product storage error 100.86 17.78 68 30529 16158 79697633
Cancer pain 99.99 17.78 46 30551 5199 79708592
Toxicity to various agents 96.17 17.78 22 30575 421518 79292273
Intentional underdose 79.53 17.78 31 30566 2323 79711468
Dizziness 76.63 17.78 401 30196 526040 79187751
Infusion related reaction 75.31 17.78 3 30594 230234 79483557
Muscular weakness 69.40 17.78 175 30422 160554 79553237
Completed suicide 66.68 17.78 8 30589 245759 79468032
Haematuria 65.05 17.78 104 30493 68732 79645059
Rheumatoid arthritis 64.10 17.78 4 30593 208466 79505325
Drug hypersensitivity 63.51 17.78 18 30579 298898 79414893
Spinal cord compression 60.58 17.78 35 30562 6342 79707449
Dysgeusia 60.48 17.78 91 30506 57086 79656705
Malignant spinal cord compression 56.77 17.78 13 30584 146 79713645
Bone lesion 54.94 17.78 32 30565 5887 79707904
Sinusitis 53.93 17.78 6 30591 195495 79518296
Product physical issue 53.66 17.78 28 30569 4157 79709634
Blood testosterone increased 50.77 17.78 18 30579 1034 79712757
Metastases to lymph nodes 49.42 17.78 37 30560 10360 79703431
Product availability issue 46.62 17.78 25 30572 3922 79709869
Foreign body in respiratory tract 44.71 17.78 13 30584 392 79713399
Fall 43.56 17.78 328 30269 487301 79226490
Asthma 40.33 17.78 3 30594 135092 79578699
Hydronephrosis 40.01 17.78 41 30556 17413 79696378
Prostate cancer recurrent 39.49 17.78 14 30583 804 79712987
Lower respiratory tract infection 38.20 17.78 3 30594 129217 79584574
Memory impairment 36.60 17.78 110 30487 111624 79602167
Therapeutic product effect decreased 36.43 17.78 9 30588 163854 79549937
Marasmus 36.37 17.78 14 30583 1014 79712777
Oxygen saturation decreased 35.48 17.78 4 30593 129043 79584748
Arthropathy 35.20 17.78 12 30585 177099 79536692
Blood urine present 34.95 17.78 42 30555 21255 79692536
Constipation 34.64 17.78 206 30391 282844 79430947
Treatment noncompliance 33.91 17.78 67 30530 52201 79661590
Metastases to spine 31.45 17.78 20 30577 4304 79709487
Ageusia 30.96 17.78 35 30562 16597 79697194
Stomatitis 30.84 17.78 9 30588 146748 79567043
Restless legs syndrome 30.34 17.78 38 30559 20054 79693737
Weight decreased 30.03 17.78 236 30361 354962 79358829
Condition aggravated 29.75 17.78 96 30501 501028 79212763
Weight increased 29.37 17.78 38 30559 277348 79436443
Wheezing 28.83 17.78 5 30592 116659 79597132
Peri-implantitis 28.61 17.78 8 30589 209 79713582
Hypotension 28.53 17.78 81 30516 440236 79273555
Anaemia 28.44 17.78 278 30319 444737 79269054
Second primary malignancy 28.09 17.78 31 30566 14319 79699472
Insomnia 27.81 17.78 175 30422 244995 79468796
Hepatic enzyme increased 27.65 17.78 18 30579 182592 79531199
Product use issue 27.51 17.78 24 30573 209798 79503993
Pyrexia 27.32 17.78 151 30446 678558 79035233
Therapeutic product effect incomplete 25.81 17.78 11 30586 141634 79572157
Infection 25.70 17.78 33 30564 241679 79472112
Off label use 25.60 17.78 224 30373 906991 78806800
Metastasis 25.20 17.78 21 30576 6859 79706932
Cerebrovascular accident 25.08 17.78 122 30475 155170 79558621
Nausea 25.05 17.78 510 30087 956686 78757105
Urinary tract obstruction 25.00 17.78 18 30579 4747 79709044
Hypersensitivity 24.72 17.78 39 30558 262200 79451591
Vision blurred 24.69 17.78 93 30504 105805 79607986
Metastases to liver 24.33 17.78 41 30556 28273 79685518
Nocturia 24.13 17.78 28 30569 13653 79700138
Cough 24.10 17.78 67 30530 366722 79347069
Seizure 24.09 17.78 139 30458 188695 79525096
Choking 23.44 17.78 26 30571 12075 79701716
Circumstance or information capable of leading to medication error 23.24 17.78 16 30581 3932 79709859
Alopecia 23.17 17.78 33 30564 231322 79482469
Blood cholesterol increased 22.02 17.78 3 30594 83717 79630074
C-reactive protein increased 21.98 17.78 11 30586 129016 79584775
Nasopharyngitis 21.86 17.78 40 30557 253841 79459950
Malaise 21.75 17.78 285 30312 489584 79224207
Coma 21.46 17.78 6 30591 100643 79613148
Gynaecomastia 21.25 17.78 20 30577 7661 79706130
Urethral intrinsic sphincter deficiency 21.24 17.78 4 30593 15 79713776
Migraine 21.08 17.78 4 30593 87489 79626302
Blister 20.64 17.78 10 30587 119466 79594325
Prostatic specific antigen decreased 20.62 17.78 5 30592 73 79713718
Hypersomnia 20.60 17.78 34 30563 23052 79690739
Breast tenderness 20.36 17.78 12 30585 2256 79711535
Joint swelling 20.26 17.78 51 30546 288595 79425196
Product packaging quantity issue 20.13 17.78 10 30587 1339 79712452
Subdural haematoma 20.03 17.78 40 30557 31394 79682397
Drug level decreased 19.80 17.78 26 30571 14376 79699415
Cardiac failure 19.76 17.78 114 30483 154728 79559063
Bronchitis 19.60 17.78 13 30584 130631 79583160
Acute kidney injury 19.56 17.78 118 30479 519286 79194505
Adrenocortical insufficiency acute 19.50 17.78 13 30584 3030 79710761
Treatment failure 19.47 17.78 22 30575 170464 79543327
Balance disorder 19.18 17.78 82 30515 98775 79615016
Blood testosterone abnormal 18.96 17.78 6 30591 242 79713549
Drug ineffective 18.88 17.78 545 30052 1080368 78633423
Foreign body in throat 18.66 17.78 7 30590 472 79713319
Follicular cystitis 18.52 17.78 3 30594 3 79713788
Tachycardia 18.15 17.78 25 30572 177743 79536048
Metastases to bladder 18.10 17.78 6 30591 281 79713510
Injection site pain 18.07 17.78 14 30583 129824 79583967
Intentional product use issue 18.07 17.78 19 30578 152093 79561698
Peripheral swelling 17.96 17.78 170 30427 269447 79444344
Injection site erythema 17.95 17.78 4 30593 78193 79635598
International normalised ratio abnormal 17.87 17.78 16 30581 5752 79708039

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

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




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 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)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Androgen receptor Nuclear hormone receptor ANTAGONIST EC50 7.31 CHEMBL CHEMBL
Glucocorticoid receptor Nuclear hormone receptor Ki 4.85 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 0469-0125 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 0469-0625 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 0469-0725 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 0469-1125 CAPSULE 40 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
Xtandi HUMAN PRESCRIPTION DRUG LABEL 1 0469-1725 TABLET 40 mg ORAL NDA 27 sections
Xtandi HUMAN PRESCRIPTION DRUG LABEL 1 0469-1725 TABLET 40 mg ORAL NDA 27 sections