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

Stem definition	Drug id	CAS RN
non-steroid antiandrogens	4628	915087-33-1

Description:

Molecule	Description
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: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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: ONP

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

Drug dosage:

Dose	Unit	Route
0.16	g	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Aug. 31, 2012	FDA	ASTELLAS
March 24, 2014	PMDA	Astellas Pharma Inc

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	12.88	acidic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Androgen receptor	Nuclear hormone receptor	P10275	ANDR_HUMAN	ANTAGONIST	EC50	7.31	CHEMBL	CHEMBL
Glucocorticoid receptor	Nuclear hormone receptor	P04150	GCR_HUMAN		Ki	4.85	CHEMBL
Prostate-specific antigen	Surface antigen	P07288	KLK3_HUMAN		IC50	6.89	CHEMBL
Androgen receptor	Transcription factor		ANDR_RAT		IC50	6.53	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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