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

Stem definition	Drug id	CAS RN
antiandrogens	4176	154229-18-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: abiraterone acetate zytiga CB-7630 CB7630	Abiraterone acetate is converted in vivo to abiraterone, an androgen biosynthesis inhibitor, that inhibits 17 alpha-hydroxylase/C17,20-lyase (CYP17). This enzyme is expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis. CYP17 catalyzes two sequential reactions: 1) the conversion of pregnenolone and progesterone to their 17alpha-hydroxy derivatives by 17alpha-hydroxylase activity and 2) the subsequent formation of dehydroepiandrosterone (DHEA) and androstenedione, respectively, by C17,20 lyase activity. DHEA and androstenedione are androgens and are precursors of testosterone. Inhibition of CYP17 by abiraterone can also result in increased mineralocorticoid production by the adrenals. Androgen sensitive prostatic carcinoma responds to treatment that decreases androgen levels. Androgen deprivation therapies, such as treatment with GnRH agonists or orchiectomy, decrease androgen production in the testes but do not affect androgen production by the adrenals or in the tumor. Abiraterone acetate decreased serum testosterone and other androgens in patients in the placebo-controlled clinical trial. It is not necessary to monitor the effect of abiraterone acetate on serum testosterone levels. Molecular weight: 391.56 Formula: C26H33NO2 CLOGP: 6.11 LIPINSKI: 1 HAC: 3 HDO: 0 TPSA: 39.19 ALOGS: -5.59 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

abiraterone acetate
zytiga
CB-7630
CB7630

Abiraterone acetate is converted in vivo to abiraterone, an androgen biosynthesis inhibitor, that inhibits 17 alpha-hydroxylase/C17,20-lyase (CYP17). This enzyme is expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis. CYP17 catalyzes two sequential reactions: 1) the conversion of pregnenolone and progesterone to their 17alpha-hydroxy derivatives by 17alpha-hydroxylase activity and 2) the subsequent formation of dehydroepiandrosterone (DHEA) and androstenedione, respectively, by C17,20 lyase activity. DHEA and androstenedione are androgens and are precursors of testosterone. Inhibition of CYP17 by abiraterone can also result in increased mineralocorticoid production by the adrenals. Androgen sensitive prostatic carcinoma responds to treatment that decreases androgen levels. Androgen deprivation therapies, such as treatment with GnRH agonists or orchiectomy, decrease androgen production in the testes but do not affect androgen production by the adrenals or in the tumor. Abiraterone acetate decreased serum testosterone and other androgens in patients in the placebo-controlled clinical trial. It is not necessary to monitor the effect of abiraterone acetate on serum testosterone levels.

Molecular weight: 391.56
Formula: C26H33NO2
CLOGP: 6.11
LIPINSKI: 1
HAC: 3
HDO: 0
TPSA: 39.19
ALOGS: -5.59
ROTB: 3

Status: OFP

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

Drug dosage:

Dose	Unit	Route
1	g	O

ADMET properties:

Property	Value	Reference
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
Sept. 5, 2011	EMA	Janssen-Cilag International N.V.
April 28, 2011	FDA	JANSSEN BIOTECH

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
Prostatic specific antigen increased	61.99	43.38	5	94	0	63488923

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
Death	2401.29	16.69	2588	37791	395461	34521091
Prostatic specific antigen increased	2269.08	16.69	790	39589	13890	34902662
Disease progression	762.78	16.69	771	39608	107306	34809246
Therapy cessation	720.45	16.69	364	40015	16609	34899943
Hot flush	647.82	16.69	346	40033	17720	34898832
Hypokalaemia	499.51	16.69	463	39916	57751	34858801
Hospitalisation	489.05	16.69	453	39926	56449	34860103
Metastases to bone	428.23	16.69	229	40150	11741	34904811
Prostate cancer metastatic	402.94	16.69	175	40204	5628	34910924
Osteonecrosis of jaw	288.79	16.69	206	40173	17683	34898869
Fatigue	250.17	16.69	964	39415	369689	34546863
Urinary tract infection	221.59	16.69	369	40010	83712	34832840
Malignant neoplasm progression	185.03	16.69	350	40029	87696	34828856
Therapy interrupted	172.58	16.69	136	40243	13561	34902991
Prostate cancer	169.87	16.69	219	40160	39430	34877122
Product size issue	162.93	16.69	52	40327	682	34915870
Hospice care	152.96	16.69	97	40282	6843	34909709
Product use complaint	146.46	16.69	57	40322	1375	34915177
Hormone-refractory prostate cancer	146.23	16.69	48	40331	692	34915860
Hypertension	121.64	16.69	390	39989	136053	34780499
Adverse event	120.49	16.69	128	40251	18749	34897803
Toxicity to various agents	116.51	16.69	43	40336	200319	34716233
Blood potassium decreased	113.50	16.69	121	40258	17794	34898758
Prescribed underdose	104.63	16.69	85	40294	8848	34907704
Bone pain	99.29	16.69	121	40258	20565	34895987
Dysphagia	94.55	16.69	217	40162	62164	34854388
Completed suicide	92.93	16.69	5	40374	98163	34818389
Prostatic specific antigen abnormal	85.73	16.69	32	40347	686	34915866
Oedema peripheral	84.52	16.69	317	40062	119495	34797057
Spinal cord compression	78.83	16.69	52	40327	3923	34912629
Incorrect dose administered	72.82	16.69	151	40228	40364	34876188
Decreased appetite	70.29	16.69	378	40001	166014	34750538
Haematuria	68.08	16.69	167	40212	49899	34866653
Hepatic function abnormal	66.83	16.69	154	40225	44209	34872343
Product dose omission issue	64.09	16.69	291	40088	119420	34797132
Acquired apparent mineralocorticoid excess	63.50	16.69	14	40365	34	34916518
Pyrexia	63.28	16.69	187	40192	332826	34583726
Blood alkaline phosphatase increased	62.97	16.69	122	40257	31053	34885499
Asthenia	61.76	16.69	489	39890	244762	34671790
Metastases to spine	56.64	16.69	36	40343	2548	34914004
Urinary tract obstruction	54.53	16.69	40	40339	3580	34912972
Fall	53.50	16.69	409	39970	202476	34714076
Metastases to lymph nodes	53.29	16.69	44	40335	4684	34911868
Fluid retention	50.41	16.69	102	40277	26785	34889767
Therapy change	48.62	16.69	35	40344	3042	34913510
Apparent mineralocorticoid excess	47.72	16.69	11	40368	35	34916517
Drug hypersensitivity	47.20	16.69	17	40362	80512	34836040
Chemotherapy	47.03	16.69	20	40359	609	34915943
Metastases to liver	45.68	16.69	67	40312	13596	34902956
Wrong technique in product usage process	44.68	16.69	116	40263	35870	34880682
Diabetes mellitus	44.41	16.69	137	40242	46736	34869816
Muscular weakness	44.16	16.69	184	40195	72713	34843839
Infusion related reaction	43.80	16.69	5	40374	53052	34863500
Overdose	42.92	16.69	26	40353	91033	34825519
Hyperaldosteronism	42.09	16.69	13	40366	152	34916400
Oedema	41.78	16.69	132	40247	45609	34870943
Back pain	41.17	16.69	261	40118	121528	34795024
Pruritus	40.86	16.69	63	40316	141918	34774634
Prostate cancer recurrent	40.81	16.69	21	40358	992	34915560
Metastases to lung	40.68	16.69	52	40327	9268	34907284
Febrile neutropenia	40.07	16.69	60	40319	136789	34779763
Intentional product use issue	39.81	16.69	10	40369	59806	34856746
Metastasis	39.43	16.69	35	40344	4109	34912443
Hydronephrosis	39.42	16.69	54	40325	10292	34906260
Acute coronary syndrome	39.04	16.69	62	40317	13483	34903069
Hypotension	38.80	16.69	129	40250	221520	34695032
Haemorrhage urinary tract	38.34	16.69	25	40354	1849	34914703
Cardiac failure	37.57	16.69	206	40173	91042	34825510
Liver function test abnormal	37.38	16.69	99	40280	30975	34885577
Wheezing	36.54	16.69	3	40376	41399	34875153
Intentional product misuse	35.94	16.69	5	40374	45606	34870946
Condition aggravated	35.63	16.69	109	40270	192087	34724465
Hepatotoxicity	35.04	16.69	77	40302	21408	34895144
Neuroendocrine carcinoma of prostate	34.58	16.69	7	40372	9	34916543
Metabolic acidosis	33.92	16.69	5	40374	43675	34872877
Psoriasis	33.74	16.69	3	40376	38809	34877743
Blood urine present	33.19	16.69	51	40328	10783	34905769
Asthma	32.86	16.69	5	40374	42651	34873901
Plasma cell myeloma	32.21	16.69	5	40374	42032	34874520
Urinary retention	31.57	16.69	103	40276	36185	34880367
Aggression	31.35	16.69	4	40375	38960	34877592
Agitation	30.56	16.69	14	40365	57385	34859167
Hypoxia	30.02	16.69	13	40366	55082	34861470
Coma	29.70	16.69	8	40371	45670	34870882
Anxiety	29.67	16.69	43	40336	99385	34817167
Peripheral swelling	29.64	16.69	170	40209	76371	34840181
Injection site pain	29.08	16.69	5	40374	39000	34877552
Hepatic enzyme increased	28.82	16.69	105	40274	38975	34877577
Cystitis	28.56	16.69	45	40334	9720	34906832
Bone lesion	28.14	16.69	25	40354	2938	34913614
Cardiac disorder	27.80	16.69	111	40268	43015	34873537
Pelvic pain	27.78	16.69	23	40356	2457	34914095
Acute biphenotypic leukaemia	27.59	16.69	8	40371	74	34916478
BRCA2 gene mutation	27.37	16.69	7	40372	38	34916514
Anaemia	27.26	16.69	399	39980	232936	34683616
Haemorrhage subcutaneous	26.97	16.69	22	40357	2302	34914250
Neutropenia	26.89	16.69	92	40287	156686	34759866
Radiotherapy	26.50	16.69	12	40367	426	34916126
Suicidal ideation	26.39	16.69	7	40372	40381	34876171
Liver disorder	26.34	16.69	91	40288	32906	34883646
Prostatic specific antigen decreased	26.10	16.69	9	40370	152	34916400
Polyneuropathy in malignant disease	25.93	16.69	10	40369	235	34916317
Rhabdomyolysis	24.84	16.69	149	40230	68014	34848538
Lactic acidosis	24.76	16.69	5	40374	34767	34881785
Acquired haemophilia	24.48	16.69	15	40364	995	34915557
Adverse drug reaction	24.37	16.69	82	40297	29260	34887292
Hypersensitivity	24.10	16.69	21	40358	61014	34855538
Multiple organ dysfunction syndrome	23.95	16.69	32	40347	76534	34840018
Blood testosterone increased	23.67	16.69	16	40363	1257	34915295
Bone cancer metastatic	23.48	16.69	9	40370	208	34916344
Oxygen saturation decreased	23.15	16.69	17	40362	53801	34862751
BRCA1 gene mutation	23.10	16.69	6	40373	35	34916517
Free prostate-specific antigen increased	23.06	16.69	4	40375	0	34916552
Staphylococcal infection	22.74	16.69	5	40374	32755	34883797
Erythema	22.22	16.69	43	40336	88737	34827815
Bradycardia	22.12	16.69	33	40346	75385	34841167
Depressed level of consciousness	21.96	16.69	11	40368	42830	34873722
Alanine aminotransferase increased	21.83	16.69	164	40215	80651	34835901
Retroperitoneal lymphadenopathy	21.51	16.69	13	40366	841	34915711
Blood creatinine increased	21.26	16.69	49	40330	94927	34821625
Drug reaction with eosinophilia and systemic symptoms	21.05	16.69	6	40373	33006	34883546
Urosepsis	21.01	16.69	46	40333	12753	34903799
Dementia	20.99	16.69	48	40331	13700	34902852
Cough	20.73	16.69	96	40283	150044	34766508
Sinusitis	20.68	16.69	11	40368	41391	34875161
Cardio-respiratory arrest	20.66	16.69	20	40359	55253	34861299
Fracture	20.64	16.69	32	40347	6817	34909735
Rash	20.47	16.69	162	40217	222590	34693962
Tachycardia	20.41	16.69	42	40337	84730	34831822
Metastases to soft tissue	20.39	16.69	10	40369	426	34916126
Angioedema	20.07	16.69	9	40370	37365	34879187
Pathological fracture	19.96	16.69	25	40354	4366	34912186
Peri-implantitis	19.64	16.69	7	40372	131	34916421
Constipation	19.57	16.69	243	40136	136739	34779813
Gastrointestinal tube insertion	19.36	16.69	14	40365	1225	34915327
Adrenal insufficiency	19.22	16.69	47	40332	14000	34902552
Surgery	18.99	16.69	47	40332	14110	34902442
Transaminases increased	18.88	16.69	71	40308	26752	34889800
Pyelonephritis acute	18.82	16.69	17	40362	2042	34914510
C-reactive protein increased	18.61	16.69	21	40358	54077	34862475
Lymphoedema	18.53	16.69	23	40356	3980	34912572
Groin pain	18.38	16.69	27	40352	5486	34911066
Nasopharyngitis	18.29	16.69	33	40346	69935	34846617
Mucosal inflammation	18.23	16.69	11	40368	38611	34877941
Pollakiuria	18.16	16.69	57	40322	19617	34896935
Productive cough	17.52	16.69	11	40368	37802	34878750
Hip fracture	17.50	16.69	41	40338	11884	34904668
Hyperglycaemia	17.50	16.69	91	40288	39389	34877163
Cardiac arrest	17.46	16.69	55	40324	96104	34820448
Coronary artery disease	17.45	16.69	18	40361	48287	34868265
Somnolence	17.20	16.69	68	40311	111048	34805504
Liver function test increased	17.10	16.69	46	40333	14519	34902033
Respiratory distress	17.05	16.69	10	40369	35655	34880897
White blood cell count decreased	17.04	16.69	55	40324	95390	34821162
Neuropathy peripheral	17.03	16.69	45	40334	83218	34833334
Cancer pain	16.83	16.69	18	40361	2654	34913898

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
Prostatic specific antigen increased	2188.83	17.06	545	27654	9841	79706348
Death	1526.55	17.06	1389	26810	565125	79151064
Disease progression	639.14	17.06	525	27674	183837	79532352
Hot flush	406.77	17.06	249	27950	54628	79661561
Hypokalaemia	348.37	17.06	335	27864	143705	79572484
Metastases to bone	324.89	17.06	163	28036	24264	79691925
Prostate cancer metastatic	323.00	17.06	99	28100	3908	79712281
Therapy cessation	316.08	17.06	185	28014	37377	79678812
Prostate cancer	285.58	17.06	166	28033	33102	79683087
Osteonecrosis of jaw	284.61	17.06	182	28017	43044	79673145
Hospitalisation	199.46	17.06	204	27995	94032	79622157
Fatigue	152.64	17.06	690	27509	929037	78787152
Malignant neoplasm progression	123.66	17.06	193	28006	135797	79580392
Hospice care	123.01	17.06	64	28135	10260	79705929
Urinary tract infection	122.92	17.06	288	27911	274224	79441965
Product size issue	119.69	17.06	32	28167	766	79715423
Haematuria	117.41	17.06	133	28066	68703	79647486
Hormone-refractory prostate cancer	106.10	17.06	26	28173	434	79715755
Blood potassium decreased	88.16	17.06	95	28104	46417	79669772
Oedema peripheral	88.12	17.06	241	27958	252047	79464142
Therapy interrupted	81.48	17.06	76	28123	31265	79684924
Decreased appetite	80.52	17.06	285	27914	342133	79374056
Product use complaint	76.83	17.06	30	28169	2453	79713736
Toxicity to various agents	76.20	17.06	27	28172	421513	79294676
Rhabdomyolysis	71.86	17.06	130	28069	103001	79613188
Prescribed underdose	71.82	17.06	69	28130	29445	79686744
Incorrect dose administered	71.33	17.06	110	28089	76520	79639669
Completed suicide	67.75	17.06	5	28194	245762	79470427
Asthenia	67.10	17.06	357	27842	511332	79204857
Apparent mineralocorticoid excess	66.03	17.06	12	28187	39	79716150
Infusion related reaction	65.47	17.06	4	28195	230233	79485956
Prostate cancer recurrent	65.02	17.06	20	28179	798	79715391
Drug hypersensitivity	63.55	17.06	14	28185	298902	79417287
Metastases to spine	60.84	17.06	30	28169	4294	79711895
Cardiac failure	58.12	17.06	152	28047	154690	79561499
Prostatic specific antigen abnormal	57.55	17.06	16	28183	445	79715744
Urinary retention	56.54	17.06	84	28115	56546	79659643
Acute coronary syndrome	50.65	17.06	49	28150	21084	79695105
Hypersensitivity	50.52	17.06	15	28184	262224	79453965
Bone pain	50.45	17.06	79	28120	55663	79660526
Hepatic function abnormal	49.45	17.06	91	28108	73016	79643173
Acquired apparent mineralocorticoid excess	48.47	17.06	9	28190	34	79716155
Arthropathy	47.69	17.06	4	28195	177107	79539082
Hypertension	47.51	17.06	237	27962	330755	79385434
Haemorrhage urinary tract	46.73	17.06	21	28178	2440	79713749
Hydronephrosis	44.74	17.06	42	28157	17412	79698777
Urinary tract obstruction	44.12	17.06	25	28174	4740	79711449
Therapy change	43.39	17.06	29	28170	7370	79708819
Neuroendocrine carcinoma of prostate	43.30	17.06	7	28192	8	79716181
Blood alkaline phosphatase increased	42.74	17.06	79	28120	63585	79652604
Atrial fibrillation	42.44	17.06	160	28039	197726	79518463
Muscular weakness	41.37	17.06	138	28061	160591	79555598
Sinusitis	39.86	17.06	10	28189	195491	79520698
Spinal cord compression	39.83	17.06	26	28173	6351	79709838
Hyperaldosteronism	39.78	17.06	12	28187	448	79715741
Metastases to lung	39.60	17.06	40	28159	18123	79698066
Metastases to lymph nodes	38.78	17.06	31	28168	10366	79705823
Dehydration	37.94	17.06	181	28018	248006	79468183
Fall	37.75	17.06	298	27901	487331	79228858
Myocardial infarction	37.12	17.06	146	28053	183983	79532206
Dysphagia	37.05	17.06	111	28088	122025	79594164
Back pain	36.25	17.06	207	27992	303973	79412216
Polyneuropathy in malignant disease	35.97	17.06	10	28189	278	79715911
Metastases to liver	35.71	17.06	47	28152	28267	79687922
Pruritus	35.38	17.06	53	28146	394595	79321594
Product dose omission issue	35.31	17.06	177	28022	247360	79468829
Asthma	33.89	17.06	4	28195	135091	79581098
Blood urine present	32.69	17.06	39	28160	21258	79694931
Intentional product use issue	32.55	17.06	7	28192	152105	79564084
Nasopharyngitis	31.63	17.06	26	28173	253855	79462334
Acute biphenotypic leukaemia	31.38	17.06	8	28191	158	79716031
Alopecia	30.98	17.06	22	28177	231333	79484856
Wheezing	30.42	17.06	3	28196	116661	79599528
Condition aggravated	29.91	17.06	85	28114	501039	79215150
Injection site pain	29.86	17.06	5	28194	129833	79586356
Constipation	29.48	17.06	186	28013	282864	79433325
Anaemia	29.12	17.06	262	27937	444753	79271436
Radiotherapy	28.65	17.06	10	28189	596	79715593
Diabetes mellitus	28.41	17.06	76	28123	78314	79637875
General physical health deterioration	28.13	17.06	180	28019	275058	79441131
Liver function test abnormal	28.06	17.06	67	28132	64408	79651781
Anxiety	27.92	17.06	28	28171	248484	79467705
Wound	27.79	17.06	4	28195	116175	79600014
Prostatic specific antigen decreased	26.32	17.06	6	28193	72	79716117
Musculoskeletal stiffness	25.67	17.06	15	28184	174993	79541196
Exposure during pregnancy	25.35	17.06	3	28196	101129	79615060
Peri-implantitis	24.67	17.06	7	28192	210	79715979
Chemotherapy	24.15	17.06	12	28187	1745	79714444
Pollakiuria	23.42	17.06	45	28154	37272	79678917
Blood testosterone increased	23.29	17.06	10	28189	1042	79715147
Acquired haemophilia	23.20	17.06	12	28187	1899	79714290
Drug intolerance	23.14	17.06	36	28163	264083	79452106
Pyrexia	23.13	17.06	143	28056	678566	79037623
Coma	22.87	17.06	4	28195	100645	79615544
Retroperitoneal lymphadenopathy	22.86	17.06	10	28189	1090	79715099
Urosepsis	21.84	17.06	36	28163	26459	79689730
Psoriasis	21.62	17.06	3	28196	89584	79626605
Rash	21.21	17.06	119	28080	578239	79137950
Intentional product misuse	21.15	17.06	4	28195	95161	79621028
Metastases to soft tissue	21.14	17.06	8	28191	601	79715588
Toxic cataract	20.63	17.06	4	28195	20	79716169
Prostate cancer stage IV	20.57	17.06	12	28187	2402	79713787
Cancer pain	20.34	17.06	16	28183	5229	79710960
Alanine aminotransferase increased	20.24	17.06	112	28087	162458	79553731
Blood glucose increased	19.88	17.06	87	28112	114888	79601301
Cough	19.87	17.06	65	28134	366724	79349465
Depressed level of consciousness	19.58	17.06	5	28194	96647	79619542
Haemorrhage subcutaneous	19.36	17.06	15	28184	4794	79711395
Overdose	19.29	17.06	22	28177	184184	79532005
Rib fracture	19.15	17.06	35	28164	27912	79688277
Pathological fracture	19.04	17.06	21	28178	10516	79705673
Fluid retention	18.89	17.06	61	28138	69748	79646441
Migraine	18.77	17.06	4	28195	87489	79628700
Gastroduodenal ulcer	18.74	17.06	7	28192	507	79715682
Bone lesion	18.64	17.06	16	28183	5903	79710286
Interstitial lung disease	18.56	17.06	84	28115	112516	79603673
Groin pain	18.52	17.06	23	28176	13057	79703132
Pyelonephritis acute	18.40	17.06	16	28183	6007	79710182
Arthritis	18.08	17.06	9	28190	114871	79601318
Dysuria	18.06	17.06	49	28150	50902	79665287
Injection site erythema	18.00	17.06	3	28196	78194	79637995
Platelet count decreased	17.87	17.06	124	28075	194540	79521649
Oxygen saturation decreased	17.63	17.06	12	28187	129035	79587154
Ischaemic stroke	17.28	17.06	37	28162	33094	79683095

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L02BX03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Other hormone antagonists and related agents
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D065607	Cytochrome P-450 Enzyme Inhibitors
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D006727	Hormone Antagonists
MeSH PA	D065606	Metabolic Side Effects of Drugs and Substances
MeSH PA	D065088	Steroid Synthesis Inhibitors
FDA MoA	N0000182137	Cytochrome P450 2D6 Inhibitors
FDA MoA	N0000182632	Cytochrome P450 17A1 Inhibitors
FDA EPC	N0000182633	Cytochrome P450 17A1 Inhibitor
FDA MoA	N0000187062	Cytochrome P450 2C8 Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:68640	17-alpha-hydroxylase/C17,20-lyase inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Malignant tumor of prostate	indication	399068003	DOID:10283
Metastatic castration-resistant prostate cancer	indication	427492003
Hyperbilirubinemia	contraindication	14783006	DOID:2741
Hypertensive disorder	contraindication	38341003	DOID:10763
Hypokalemia	contraindication	43339004
Body fluid retention	contraindication	43498006
Chronic heart failure	contraindication	48447003
Liver function tests abnormal	contraindication	166603001
Disease of liver	contraindication	235856003	DOID:409
Pregnancy, function	contraindication	289908002
Breastfeeding (mother)	contraindication	413712001

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.68	Basic

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
125MG	YONSA	SUN PHARM	N210308	May 22, 2018	RX	TABLET	ORAL	10292990	May 20, 2034	USE IN COMBINATION WITH METHYLPREDNISOLONE FOR THE TREATMENT OF PATIENTS WITH PROSTATE CANCER

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Steroid 17-alpha-hydroxylase/17,20 lyase	Enzyme	P05093	CP17A_HUMAN	INHIBITOR	IC50	8.54	CHEMBL	IUPHAR
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	5.57	CHEMBL
Androgen receptor	Nuclear hormone receptor	P10275	ANDR_HUMAN		EC50	4.77	CHEMBL
Cytochrome P450 11B1, mitochondrial	Enzyme	P15538	C11B1_HUMAN		IC50	5.79	CHEMBL
Cytochrome P450 11B2, mitochondrial	Enzyme	P19099	C11B2_HUMAN		IC50	5.76	CHEMBL
Cytochrome P450 17A1	Enzyme		CP17A_RAT		IC50	7.90	CHEMBL

External reference:

ID	Source
4030721	VUID
N0000182731	NUI
D09701	KEGG_DRUG
4030720	VANDF
4030721	VANDF
C2607886	UMLSCUI
CHEBI:68639	CHEBI
CHEBI:68642	CHEBI
AER	PDB_CHEM_ID
CHEMBL271227	ChEMBL_ID
CHEMBL254328	ChEMBL_ID
D000069501	MESH_DESCRIPTOR_UI
C089740	MESH_SUPPLEMENTAL_RECORD_UI
9288	IUPHAR_LIGAND_ID
EM5OCB9YJ6	UNII
9821849	PUBCHEM_CID
DB05812	DRUGBANK_ID
1100071	RXNORM
181225	MMSL
27860	MMSL
299803	MMSL
d07766	MMSL
013720	NDDF
013721	NDDF
699678007	SNOMEDCT_US
699679004	SNOMEDCT_US
767857007	SNOMEDCT_US
C0754011	UMLSCUI
7375	INN_ID
154229-19-3	SECONDARY_CAS_RN
132971	PUBCHEM_CID
6745	IUPHAR_LIGAND_ID
G819A456D0	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-1125	TABLET, FILM COATED	250 mg	ORAL	ANDA	27 sections
Abiraterone	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9597	TABLET	250 mg	ORAL	ANDA	26 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6920	TABLET	250 mg	ORAL	ANDA	29 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6920	TABLET	250 mg	ORAL	ANDA	29 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6921	TABLET, FILM COATED	500 mg	ORAL	ANDA	29 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6921	TABLET, FILM COATED	500 mg	ORAL	ANDA	29 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6924	TABLET, FILM COATED	250 mg	ORAL	ANDA	29 sections
Abiraterone acetate	HUMAN PRESCRIPTION DRUG LABEL	1	0591-4365	TABLET, FILM COATED	500 mg	ORAL	ANDA	28 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6948	TABLET	250 mg	ORAL	ANDA	28 sections
YONSA	HUMAN PRESCRIPTION DRUG LABEL	1	11014-0566	TABLET	125 mg	ORAL	Export only	1 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	16714-963	TABLET	250 mg	ORAL	ANDA	27 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	42291-024	TABLET	250 mg	ORAL	ANDA	27 sections
ABIRATERONE ACETATE	HUMAN PRESCRIPTION DRUG LABEL	1	42291-073	TABLET	500 mg	ORAL	ANDA	27 sections
ABIRATERONE ACETATE	HUMAN PRESCRIPTION DRUG LABEL	1	42291-073	TABLET	500 mg	ORAL	ANDA	27 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	42292-057	TABLET	250 mg	ORAL	ANDA	29 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	43598-358	TABLET	250 mg	ORAL	ANDA	27 sections
YONSA	HUMAN PRESCRIPTION DRUG LABEL	1	47335-401	TABLET	125 mg	ORAL	NDA	28 sections
YONSA	HUMAN PRESCRIPTION DRUG LABEL	1	47335-401	TABLET	125 mg	ORAL	NDA	28 sections
YONSA	HUMAN PRESCRIPTION DRUG LABEL	1	47335-401	TABLET	125 mg	ORAL	NDA	28 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	51407-181	TABLET	250 mg	ORAL	ANDA	29 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	51407-181	TABLET	250 mg	ORAL	ANDA	29 sections
AKEEGA	HUMAN PRESCRIPTION DRUG LABEL	2	57894-050	TABLET, FILM COATED	500 mg	ORAL	NDA	32 sections
AKEEGA	HUMAN PRESCRIPTION DRUG LABEL	2	57894-100	TABLET, FILM COATED	500 mg	ORAL	NDA	32 sections
Zytiga	HUMAN PRESCRIPTION DRUG LABEL	1	57894-150	TABLET	250 mg	ORAL	NDA	32 sections
Abiraterone acetate	HUMAN PRESCRIPTION DRUG LABEL	1	57894-155	TABLET	250 mg	ORAL	NDA AUTHORIZED GENERIC	31 sections
Zytiga	HUMAN PRESCRIPTION DRUG LABEL	1	57894-195	TABLET, FILM COATED	500 mg	ORAL	NDA	32 sections
Abiraterone acetate	HUMAN PRESCRIPTION DRUG LABEL	1	57894-199	TABLET, FILM COATED	500 mg	ORAL	NDA	31 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1165	TABLET	250 mg	ORAL	ANDA	26 sections
ABIRATERONE ACETATE	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1754	TABLET	500 mg	ORAL	ANDA	26 sections
Abiraterone Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	60505-4327	TABLET	250 mg	ORAL	ANDA	28 sections