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

Stem definition	Drug id	CAS RN
estrogen antagonists, including estrogen receptor down-regulators	1255	129453-61-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ZD9238 fulvestrant faslodex ICI 182,780	An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer. Molecular weight: 606.78 Formula: C32H47F5O3S CLOGP: 7.54 LIPINSKI: 2 HAC: 3 HDO: 2 TPSA: 57.53 ALOGS: -4.96 ROTB: 15 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ZD9238
fulvestrant
faslodex
ICI 182,780

An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.

Molecular weight: 606.78
Formula: C32H47F5O3S
CLOGP: 7.54
LIPINSKI: 2
HAC: 3
HDO: 2
TPSA: 57.53
ALOGS: -4.96
ROTB: 15

Status: OFP

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

Drug dosage:

Dose	Unit	Route
8.30	mg	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.00 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	4.15 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	11.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	16 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
March 10, 2004	EMA
April 25, 2002	FDA	ASTRAZENECA

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	4083.97	15.02	1860	60472	80261	63346429
Metastases to bone	2757.91	15.02	961	61371	20058	63406632
Neoplasm progression	2566.44	15.02	1057	61275	35371	63391319
Metastases to liver	2242.95	15.02	851	61481	22788	63403902
Neutropenia	1377.90	15.02	1233	61099	173772	63252918
White blood cell count decreased	872.56	15.02	865	61467	138239	63288451
Tumour marker increased	762.01	15.02	255	62077	4660	63422030
Metastases to lung	694.94	15.02	309	62023	12441	63414249
Osteonecrosis of jaw	550.56	15.02	373	61959	34750	63391940
Disease progression	522.97	15.02	623	61709	122135	63304555
Breast cancer metastatic	513.42	15.02	246	62086	11772	63414918
Neutrophil count decreased	445.26	15.02	399	61933	56007	63370683
Metastases to lymph nodes	407.26	15.02	186	62146	7972	63418718
Carbohydrate antigen 15-3 increased	396.14	15.02	116	62216	1332	63425358
PIK3CA-activated mutation	362.32	15.02	101	62231	958	63425732
Drug ineffective	346.54	15.02	312	62020	1044453	62382237
Fatigue	318.82	15.02	1709	60623	886319	62540371
Metastasis	305.90	15.02	133	62199	5064	63421626
Metastases to pleura	284.95	15.02	92	62240	1493	63425197
Leukopenia	264.62	15.02	352	61980	76938	63349752
Death	255.32	15.02	877	61455	373504	63053186
Bone pain	248.41	15.02	287	62045	54354	63372336
Metastases to spine	234.08	15.02	96	62236	3153	63423537
Breast cancer recurrent	216.73	15.02	99	62233	4242	63422448
Metastases to skin	213.72	15.02	75	62257	1588	63425102
Breast cancer	211.35	15.02	249	62083	48134	63378556
Thrombocytopenia	209.58	15.02	460	61872	150697	63275993
Infusion related reaction	206.24	15.02	8	62324	245513	63181177
Joint swelling	201.05	15.02	39	62293	327627	63099063
Maternal exposure during pregnancy	200.59	15.02	3	62329	220059	63206631
Rheumatoid arthritis	198.25	15.02	13	62319	253806	63172884
Bone lesion	193.89	15.02	101	62231	5780	63420910
Pleural effusion	187.82	15.02	332	62000	92878	63333812
Hyperglycaemia	185.40	15.02	217	62115	41650	63385040
Metastases to central nervous system	183.66	15.02	130	62202	12975	63413715
Systemic lupus erythematosus	178.24	15.02	6	62326	208912	63217778
Hepatic lesion	176.85	15.02	89	62243	4736	63421954
Therapeutic product effect decreased	174.51	15.02	3	62329	193184	63233506
Pseudocirrhosis	168.86	15.02	51	62281	656	63426034
Ascites	168.64	15.02	204	62128	40524	63386166
Palmar-plantar erythrodysaesthesia syndrome	166.22	15.02	155	62177	22860	63403830
Arthropathy	154.85	15.02	23	62309	234769	63191921
Asthenia	144.38	15.02	750	61582	382854	63043836
Hot flush	143.73	15.02	212	62120	50947	63375743
Metastases to peritoneum	139.54	15.02	68	62264	3374	63423316
Decreased appetite	135.46	15.02	546	61786	250506	63176184
Anaemia	135.04	15.02	608	61724	292822	63133868
Full blood count abnormal	133.15	15.02	160	62172	31557	63395133
Red blood cell count decreased	128.22	15.02	178	62154	40467	63386223
Drug hypersensitivity	126.65	15.02	74	62258	310613	63116077
Glossodynia	121.49	15.02	16	62316	178860	63247830
Platelet count decreased	118.46	15.02	314	62018	115808	63310882
Osteonecrosis	115.05	15.02	131	62201	24399	63402291
Pericarditis	115.02	15.02	3	62329	131576	63295114
Treatment failure	107.56	15.02	31	62301	199012	63227678
Second primary malignancy	107.07	15.02	77	62255	7876	63418814
Carcinoembryonic antigen increased	103.31	15.02	45	62287	1720	63424970
Musculoskeletal stiffness	95.69	15.02	31	62301	184587	63242103
Intentional product use issue	95.65	15.02	8	62324	127884	63298806
Hepatic failure	94.76	15.02	144	62188	35512	63391178
Nausea	92.88	15.02	1260	61072	853211	62573479
Neuropathy peripheral	91.25	15.02	282	62050	113385	63313305
Off label use	91.09	15.02	348	61984	674114	62752576
Mucosal inflammation	89.14	15.02	163	62169	46765	63379925
Hypotension	87.74	15.02	83	62249	272521	63154169
Malignant pleural effusion	86.60	15.02	45	62287	2561	63424129
Infusion site coldness	85.00	15.02	23	62309	193	63426497
Swelling	82.74	15.02	89	62243	275289	63151401
Wound	81.85	15.02	29	62303	163234	63263456
Polyneuropathy	78.95	15.02	84	62248	14505	63412185
Bone marrow failure	78.83	15.02	119	62213	29171	63397519
Helicobacter infection	77.92	15.02	3	62329	92782	63333908
Metastases to chest wall	77.18	15.02	27	62305	566	63426124
Gamma-glutamyltransferase decreased	76.07	15.02	23	62309	297	63426393
Cancer pain	75.23	15.02	44	62288	3161	63423529
Condition aggravated	74.64	15.02	179	62153	402038	63024652
Full blood count decreased	73.29	15.02	108	62224	25916	63400774
Bone disorder	72.70	15.02	97	62235	21229	63405461
Discomfort	72.29	15.02	37	62295	167337	63259353
Tumour marker abnormal	71.76	15.02	23	62309	364	63426326
Diarrhoea	71.14	15.02	1039	61293	714327	62712363
Lymphangiosis carcinomatosa	69.14	15.02	32	62300	1413	63425277
Abdominal lymphadenopathy	67.58	15.02	26	62306	719	63425971
Haematotoxicity	67.40	15.02	63	62269	9313	63417377
Metastases to pelvis	67.32	15.02	23	62309	448	63426242
Spinal pain	66.46	15.02	73	62259	13066	63413624
Fall	66.32	15.02	183	62149	392151	63034539
Lymphoedema	66.26	15.02	69	62263	11623	63415067
Overdose	65.78	15.02	16	62316	115062	63311628
Bone sequestrum	65.45	15.02	31	62301	1443	63425247
Asthma	65.06	15.02	22	62310	127539	63299151
Injection site necrosis	65.04	15.02	30	62302	1314	63425376
Skin toxicity	64.28	15.02	46	62286	4668	63422022
Sinusitis	63.98	15.02	77	62255	226576	63200114
Myelosuppression	61.95	15.02	95	62237	23608	63403082
Metastases to spinal cord	61.07	15.02	16	62316	117	63426573
Pleural neoplasm	60.48	15.02	20	62312	351	63426339
Invasive ductal breast carcinoma	60.39	15.02	52	62280	6906	63419784
Fibromyalgia	60.20	15.02	5	62327	80415	63346275
Mobility decreased	59.90	15.02	22	62310	121137	63305553
Hypersensitivity	59.35	15.02	124	62208	292561	63134129
Stomatitis	58.88	15.02	281	62051	138444	63288246
Pneumonia	57.51	15.02	242	62090	456525	62970165
Intentional overdose	57.23	15.02	4	62328	74148	63352542
Oestradiol increased	55.96	15.02	14	62318	83	63426607
Osteolysis	55.96	15.02	35	62297	2839	63423851
Metastases to thorax	55.56	15.02	17	62315	229	63426461
Metastases to adrenals	53.06	15.02	22	62310	743	63425947
Metastases to the mediastinum	51.41	15.02	19	62313	469	63426221
Lymphadenopathy	50.89	15.02	115	62217	38343	63388347
Back pain	50.62	15.02	437	61895	263708	63162982
Toxicity to various agents	49.90	15.02	105	62227	247145	63179545
Drug intolerance	49.89	15.02	147	62185	308514	63118176
Cough	49.83	15.02	472	61860	292271	63134419
Metastatic neoplasm	49.77	15.02	38	62294	4257	63422433
Oral pain	49.39	15.02	95	62237	28299	63398391
Interstitial lung disease	49.10	15.02	153	62179	61755	63364935
Lower respiratory tract infection	49.07	15.02	35	62297	132272	63294418
Metastases to retroperitoneum	48.68	15.02	14	62318	150	63426540
Confusional state	48.03	15.02	100	62232	236280	63190410
Portal hypertension	46.94	15.02	35	62297	3784	63422906
Abdominal discomfort	46.83	15.02	160	62172	320725	63105965
Invasive lobular breast carcinoma	46.53	15.02	21	62311	874	63425816
Adverse event	45.94	15.02	6	62326	67553	63359137
Electrocardiogram PR shortened	45.11	15.02	15	62317	268	63426422
Tooth extraction	45.07	15.02	53	62279	10211	63416479
Adnexa uteri mass	44.95	15.02	18	62314	555	63426135
Taste disorder	44.83	15.02	61	62271	13601	63413089
Bradycardia	44.22	15.02	9	62323	73218	63353472
Pneumonitis	44.04	15.02	103	62229	35119	63391571
Drug interaction	44.01	15.02	100	62232	229031	63197659
Therapeutic product effect incomplete	43.91	15.02	35	62297	125021	63301669
Adverse drug reaction	43.80	15.02	12	62320	79702	63346988
Acute kidney injury	43.61	15.02	124	62208	263291	63163399
Isosthenuria	43.60	15.02	12	62320	108	63426582
Infusion site induration	43.20	15.02	22	62310	1200	63425490
Eastern Cooperative Oncology Group performance status worsened	42.66	15.02	22	62310	1232	63425458
Psoriasis	42.62	15.02	16	62316	86941	63339749
Nasopharyngitis	42.60	15.02	119	62213	254138	63172552
Hormone receptor positive breast cancer	42.36	15.02	17	62315	527	63426163
Blister	42.33	15.02	39	62293	129775	63296915
Epistaxis	42.19	15.02	162	62170	72563	63354127
General physical health deterioration	41.64	15.02	339	61993	201063	63225627
Recurrent cancer	40.72	15.02	25	62307	1962	63424728
Carbohydrate antigen 27.29 increased	40.61	15.02	10	62322	55	63426635
Suicide attempt	40.04	15.02	6	62326	60912	63365778
Metastases to eye	39.90	15.02	12	62320	152	63426538
Bone cancer metastatic	39.54	15.02	12	62320	157	63426533
Bladder hypertrophy	39.37	15.02	13	62319	227	63426463
Haemoglobin decreased	39.29	15.02	261	62071	145224	63281466
Metastases to meninges	39.22	15.02	27	62305	2575	63424115
Aspartate aminotransferase increased	38.38	15.02	183	62149	90094	63336596
Hepatic enzyme increased	38.28	15.02	89	62243	202239	63224451
Arthritis	37.59	15.02	35	62297	115886	63310804
Neoplasm	37.48	15.02	41	62291	7304	63419386
Blood bilirubin increased	37.38	15.02	100	62232	37040	63389650
Hypermetabolism	37.03	15.02	12	62320	197	63426493
Suicidal ideation	37.02	15.02	8	62324	62413	63364277
Cardio-respiratory arrest	36.98	15.02	7	62325	59952	63366738
Headache	36.91	15.02	421	61911	632820	62793870
Tumour flare	36.84	15.02	14	62318	374	63426316
Ejection fraction decreased	36.75	15.02	73	62259	22259	63404431
Hepatic function abnormal	36.37	15.02	99	62233	37043	63389647
Pyelitis	36.32	15.02	12	62320	210	63426480
Constipation	35.94	15.02	358	61974	224585	63202105
Bone marrow infiltration	35.41	15.02	16	62316	668	63426022
Ill-defined disorder	35.39	15.02	18	62314	81737	63344953
Hospitalisation	34.97	15.02	20	62312	85061	63341629
Post-traumatic neck syndrome	34.80	15.02	23	62309	2051	63424639
Jaw disorder	34.77	15.02	34	62298	5315	63421375
Superinfection	34.54	15.02	25	62307	2582	63424108
Metastases to bone marrow	34.47	15.02	14	62318	448	63426242
Tumour marker decreased	34.33	15.02	9	62323	66	63426624
Weight increased	34.11	15.02	136	62196	260656	63166034
Hypertransaminasaemia	33.91	15.02	37	62295	6572	63420118
Loss of consciousness	33.44	15.02	40	62292	118081	63308609
Drug resistance	33.08	15.02	71	62261	22862	63403828
Alopecia	32.85	15.02	489	61843	337047	63089643
Jaundice	32.78	15.02	82	62250	29169	63397521
Gastrointestinal disorder	32.53	15.02	49	62283	131190	63295500
Metastases to kidney	32.50	15.02	11	62321	208	63426482
Onychoclasis	32.21	15.02	35	62297	6187	63420503
Oxygen saturation decreased	32.10	15.02	24	62308	88561	63338129
Bone marrow disorder	31.64	15.02	23	62309	2391	63424299
Dry skin	31.59	15.02	125	62207	56762	63369928
BRAF gene mutation	31.35	15.02	8	62324	52	63426638
Nephroangiosclerosis	31.33	15.02	10	62322	156	63426534
Transaminases increased	31.11	15.02	84	62248	31283	63395407
Hepatic echinococciasis	30.84	15.02	8	62324	56	63426634
Hip arthroplasty	30.61	15.02	5	62327	47641	63379049
Prehypertension	30.25	15.02	7	62325	28	63426662
Creatinine renal clearance increased	30.10	15.02	14	62318	625	63426065
Metastases to soft tissue	30.06	15.02	10	62322	179	63426511
Acquired gene mutation	29.90	15.02	16	62316	967	63425723
Neoplasm recurrence	29.82	15.02	23	62309	2615	63424075
Hepatic cancer metastatic	29.60	15.02	12	62320	382	63426308
Vasodilatation	29.55	15.02	22	62310	2373	63424317
Blood bilirubin abnormal	29.54	15.02	16	62316	991	63425699
Tachycardia	29.39	15.02	44	62288	118112	63308578
Injury	29.00	15.02	18	62314	73229	63353461
Dysgeusia	28.70	15.02	106	62226	46604	63380086
Loss of personal independence in daily activities	28.56	15.02	32	62300	97258	63329432
Metastases to bladder	28.48	15.02	10	62322	212	63426478
Dyspnoea exertional	28.41	15.02	126	62206	60176	63366514
Blood creatinine increased	28.34	15.02	165	62167	87679	63339011
Cytopenia	28.23	15.02	45	62287	11556	63415134
Pulmonary mass	28.16	15.02	66	62266	22530	63404160
Decreased immune responsiveness	27.91	15.02	29	62303	4872	63421818
Seizure	27.86	15.02	55	62277	132579	63294111
Pain in jaw	27.82	15.02	100	62232	43396	63383294
Exposed bone in jaw	27.73	15.02	23	62309	2902	63423788
Cardiac arrest	27.65	15.02	30	62302	92515	63334175
Inappropriate schedule of product administration	27.56	15.02	37	62295	103928	63322762
Wheezing	27.45	15.02	32	62300	95563	63331127
Osteomyelitis	27.14	15.02	71	62261	25949	63400741
Blood pressure increased	27.01	15.02	76	62256	161986	63264704
Product use issue	26.96	15.02	118	62214	220402	63206288
Mouth swelling	26.91	15.02	28	62304	4712	63421978
Pathological fracture	26.82	15.02	38	62294	8796	63417894
Tremor	26.78	15.02	56	62276	132183	63294507
Oestrogen receptor assay positive	26.58	15.02	12	62320	500	63426190
Pustule	26.49	15.02	18	62314	1681	63425009
Pulmonary tumour thrombotic microangiopathy	26.39	15.02	7	62325	54	63426636
Osteosclerosis	25.81	15.02	25	62307	3863	63422827
Musculoskeletal chest pain	25.64	15.02	61	62271	21022	63405668
Malignant peritoneal neoplasm	25.61	15.02	13	62319	704	63425986
International normalised ratio increased	25.48	15.02	7	62325	46418	63380272
Hydronephrosis	25.45	15.02	41	62291	10621	63416069
Joint neoplasm	25.43	15.02	7	62325	63	63426627
Lacrimation increased	25.42	15.02	60	62272	20571	63406119
Cardiac failure congestive	25.42	15.02	32	62300	92401	63334289
Ovarian disorder	25.39	15.02	13	62319	717	63425973
Osteoarthritis	25.20	15.02	34	62298	95309	63331381
Metastases to nervous system	25.05	15.02	7	62325	67	63426623
Hepatic cyst	24.97	15.02	28	62304	5126	63421564
Type 2 diabetes mellitus	24.87	15.02	16	62316	63852	63362838
Hypoglycaemia	24.86	15.02	14	62318	60051	63366639
Retinal detachment	24.86	15.02	30	62302	5939	63420751
Soft tissue neoplasm	24.60	15.02	7	62325	72	63426618
Spinal cord compression	24.44	15.02	25	62307	4123	63422567
Granulocytopenia	24.43	15.02	29	62303	5643	63421047
Bone cancer	24.22	15.02	16	62316	1426	63425264
Carcinoid tumour pulmonary	24.17	15.02	11	62321	467	63426223
RET gene mutation	24.15	15.02	5	62327	10	63426680
Urticaria	23.93	15.02	83	62249	165719	63260971
Bone debridement	23.84	15.02	9	62323	236	63426454
Vulvovaginal dryness	23.81	15.02	21	62311	2880	63423810
White blood cell count abnormal	23.78	15.02	30	62302	6212	63420478
Injection site hypoaesthesia	23.76	15.02	11	62321	486	63426204
Bile duct stenosis	23.71	15.02	15	62317	1241	63425449
Peritoneal disorder	23.65	15.02	11	62321	491	63426199
Bronchitis	23.58	15.02	55	62277	124880	63301810
Intestinal metastasis	23.55	15.02	8	62324	153	63426537
Transaminases	23.54	15.02	7	62325	85	63426605
Mediastinal disorder	23.49	15.02	10	62322	361	63426329
Blood cholesterol increased	23.40	15.02	35	62297	93997	63332693
Pulmonary embolism	23.33	15.02	195	62137	116489	63310201
Vein disorder	23.33	15.02	27	62305	5114	63421576
Peripheral swelling	23.32	15.02	159	62173	265783	63160907
Agitation	23.23	15.02	15	62317	59742	63366948
Nail disorder	23.19	15.02	44	62288	12971	63413719
Body surface area increased	23.13	15.02	6	62326	42	63426648
Hyponatraemia	22.99	15.02	47	62285	111853	63314837
Metabolic acidosis	22.58	15.02	8	62324	45061	63381629
Plasma cell myeloma	22.55	15.02	4	62328	35901	63390789
Erysipelas	22.53	15.02	33	62299	7872	63418818
Oral disorder	22.45	15.02	35	62297	8819	63417871
Hyperchromic anaemia	22.43	15.02	6	62326	48	63426642
Somnolence	22.21	15.02	95	62237	178590	63248100
Gene mutation	22.14	15.02	16	62316	1649	63425041
COVID-19	22.08	15.02	188	62144	112915	63313775
Influenza	22.05	15.02	46	62286	108676	63318014
Blood pressure fluctuation	21.91	15.02	9	62323	46308	63380382
Fluid retention	21.84	15.02	16	62316	59670	63367020
Metastases to breast	21.84	15.02	9	62323	299	63426391
Oestradiol abnormal	21.80	15.02	6	62326	54	63426636
Feeling cold	21.74	15.02	62	62270	23826	63402864
Red blood cell sedimentation rate increased	21.70	15.02	8	62324	43974	63382716
Heart rate increased	21.63	15.02	37	62295	94201	63332489
Dyskinesia	21.38	15.02	3	62329	31999	63394691
Platelet count abnormal	21.15	15.02	21	62311	3343	63423347
Hepatotoxicity	21.06	15.02	82	62250	36959	63389731
Hallucination	20.98	15.02	14	62318	54803	63371887
Drug ineffective for unapproved indication	20.96	15.02	4	62328	34059	63392631
Pancreatitis	20.93	15.02	11	62321	49044	63377646
Gingivitis	20.93	15.02	33	62299	8396	63418294
Gamma-glutamyltransferase increased	20.72	15.02	77	62255	33954	63392736
Orthostatic hypotension	20.71	15.02	5	62327	36155	63390535
Elliptocytosis	20.64	15.02	6	62326	67	63426623
Septic shock	20.57	15.02	21	62311	66608	63360082
Medication error	20.49	15.02	13	62319	52271	63374419
Gastrointestinal haemorrhage	20.41	15.02	30	62302	81146	63345544
Skin sensitisation	20.33	15.02	12	62320	877	63425813
Weight decreased	20.28	15.02	383	61949	276415	63150275
Malignant ascites	20.12	15.02	12	62320	894	63425796
Cytogenetic analysis abnormal	19.94	15.02	12	62320	908	63425782
Sepsis	19.91	15.02	80	62252	153043	63273647
Mean cell haemoglobin decreased	19.90	15.02	25	62307	5154	63421536
Breast pain	19.88	15.02	33	62299	8765	63417925
Treatment noncompliance	19.80	15.02	6	62326	37319	63389371
Gingival swelling	19.71	15.02	23	62309	4395	63422295
Breast cancer stage IV	19.63	15.02	16	62316	1970	63424720
Gingival erythema	19.56	15.02	11	62321	733	63425957
Joint range of motion decreased	19.55	15.02	4	62328	32424	63394266
Prescribed underdose	19.33	15.02	3	62329	29686	63397004
Infection	19.11	15.02	139	62193	229034	63197656
Coma	19.07	15.02	21	62311	64343	63362347
Metastases to uterus	19.02	15.02	6	62326	90	63426600
BRCA2 gene mutation	18.89	15.02	6	62326	92	63426598
Aphthous ulcer	18.79	15.02	42	62290	13896	63412794
Generalised tonic-clonic seizure	18.74	15.02	3	62329	29013	63397677
Product quality issue	18.60	15.02	6	62326	35859	63390831
Uterine mass	18.53	15.02	8	62324	299	63426391
Metastases to ovary	18.42	15.02	9	62323	449	63426241
Nail avulsion	18.32	15.02	7	62325	190	63426500
Pleural disorder	18.20	15.02	10	62322	637	63426053
Hormone refractory breast cancer	18.18	15.02	4	62328	12	63426678
Transaminases abnormal	17.93	15.02	10	62322	656	63426034
Intentional product misuse	17.91	15.02	20	62312	60897	63365793
Product use in unapproved indication	17.78	15.02	103	62229	178977	63247713
Foot deformity	17.72	15.02	3	62329	27850	63398840
Overflow diarrhoea	17.60	15.02	6	62326	116	63426574
Depressed level of consciousness	17.58	15.02	21	62311	62057	63364633
Pain	17.58	15.02	574	61758	740054	62686636
Glomerular filtration rate decreased	17.56	15.02	40	62292	13401	63413289
Pneumonia aspiration	17.53	15.02	6	62326	34534	63392156
Herpes zoster	17.48	15.02	34	62298	82428	63344262
Syncope	17.45	15.02	58	62274	117327	63309363
Angioedema	17.37	15.02	13	62319	47952	63378738
Pancytopenia	17.30	15.02	158	62174	96775	63329915
Blood creatinine abnormal	17.25	15.02	18	62314	3038	63423652
Ear infection	17.16	15.02	8	62324	38205	63388485
Drug reaction with eosinophilia and systemic symptoms	16.96	15.02	6	62326	33830	63392860
Unresponsive to stimuli	16.94	15.02	6	62326	33810	63392880
Debridement	16.87	15.02	12	62320	1206	63425484
Hyperkalaemia	16.83	15.02	17	62315	54186	63372504
Lymphadenopathy mediastinal	16.68	15.02	17	62315	2791	63423899
Laryngitis viral	16.65	15.02	5	62327	63	63426627
No adverse event	16.63	15.02	10	62322	41395	63385295
Injection site mass	16.57	15.02	48	62284	18608	63408082
Therapy partial responder	16.54	15.02	34	62298	10624	63416066
Myocardial infarction	16.52	15.02	47	62285	99846	63326844
Metastases to muscle	16.47	15.02	6	62326	142	63426548
Cachexia	16.46	15.02	24	62308	5702	63420988
Gingival pain	16.32	15.02	29	62303	8133	63418557
Gastrointestinal submucosal tumour	16.09	15.02	4	62328	23	63426667
Adenocarcinoma	15.98	15.02	17	62315	2933	63423757
Platelet disorder	15.98	15.02	14	62318	1902	63424788
Encephalopathy	15.98	15.02	9	62323	38611	63388079
Radiation fibrosis - lung	15.95	15.02	4	62328	24	63426666
Body surface area decreased	15.95	15.02	4	62328	24	63426666
Blood creatine phosphokinase increased	15.94	15.02	5	62327	30425	63396265
Sequestrectomy	15.93	15.02	10	62322	816	63425874
Excessive granulation tissue	15.86	15.02	10	62322	823	63425867
Mucinous breast carcinoma	15.81	15.02	4	62328	25	63426665
Infusion site haemorrhage	15.62	15.02	22	62310	5064	63421626
Blood creatinine decreased	15.59	15.02	23	62309	5522	63421168
Glycosylated haemoglobin	15.43	15.02	5	62327	82	63426608
Breast injury	15.32	15.02	5	62327	84	63426606
Aspartate aminotransferase abnormal	15.28	15.02	11	62321	1127	63425563
Incorrect dose administered	15.23	15.02	22	62310	59946	63366744
Invasive breast carcinoma	15.22	15.02	9	62323	660	63426030
Product dose omission in error	15.16	15.02	27	62305	7585	63419105
Tumour pain	15.10	15.02	12	62320	1425	63425265
Mean cell volume increased	15.04	15.02	18	62314	3533	63423157

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
Xerosis	53.10	49.57	9	521	595	34955806

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
Neoplasm progression	2136.84	15.34	898	48428	50784	79644278
Metastases to bone	1780.38	15.34	641	48685	23786	79671276
Malignant neoplasm progression	1776.11	15.34	1082	48244	134908	79560154
Metastases to liver	1317.99	15.34	536	48790	27778	79667284
Neutropenia	935.56	15.34	1014	48312	286696	79408366
White blood cell count decreased	919.66	15.34	829	48497	187459	79507603
Tumour marker increased	582.79	15.34	180	49146	4092	79690970
Fatigue	498.70	15.34	1476	47850	928251	78766811
Metastases to lung	479.13	15.34	231	49095	17932	79677130
Osteonecrosis of jaw	445.56	15.34	297	49029	42929	79652133
Breast cancer metastatic	366.44	15.34	153	49173	8449	79686613
Neutrophil count decreased	341.00	15.34	352	48974	93607	79601455
Carbohydrate antigen 15-3 increased	306.04	15.34	82	49244	1097	79693965
Metastases to lymph nodes	279.51	15.34	134	49192	10263	79684799
Disease progression	259.79	15.34	433	48893	183929	79511133
Bone pain	237.55	15.34	228	49098	55514	79639548
Breast cancer recurrent	201.22	15.34	74	49252	2903	79692159
Drug ineffective	196.22	15.34	229	49097	1080684	78614378
PIK3CA-activated mutation	195.31	15.34	50	49276	553	79694509
Pseudocirrhosis	184.58	15.34	49	49277	631	79694431
Bone lesion	173.55	15.34	81	49245	5838	79689224
Metastases to pleura	172.63	15.34	56	49270	1498	79693564
Alopecia	171.78	15.34	416	48910	230939	79464123
Breast cancer	170.69	15.34	152	49174	33629	79661433
Hot flush	161.17	15.34	184	49142	54693	79640369
Metastases to skin	158.57	15.34	54	49272	1685	79693377
Asthenia	155.58	15.34	677	48649	511012	79184050
Nausea	148.13	15.34	1054	48272	956142	78738920
Full blood count abnormal	141.96	15.34	149	49177	40325	79654737
Metastases to spine	141.92	15.34	64	49262	4260	79690802
Metastasis	138.79	15.34	73	49253	6807	79688255
Death	129.12	15.34	690	48636	565824	79129238
Leukopenia	127.16	15.34	245	49081	116268	79578794
Metastases to central nervous system	125.62	15.34	94	49232	16281	79678781
Decreased appetite	122.78	15.34	477	48849	341941	79353121
Red blood cell count decreased	119.32	15.34	162	49164	57351	79637711
Infusion related reaction	111.56	15.34	8	49318	230229	79464833
Thrombocytopenia	107.94	15.34	385	48941	264874	79430188
Hepatic lesion	102.42	15.34	60	49266	6899	79688163
Hypotension	99.75	15.34	76	49250	440241	79254821
Stomatitis	97.37	15.34	253	49073	146504	79548558
Acute kidney injury	97.10	15.34	107	49219	519297	79175765
Full blood count decreased	96.30	15.34	100	49226	26719	79668343
Platelet count decreased	95.52	15.34	301	49025	194363	79500699
Hyperglycaemia	93.32	15.34	161	49165	70174	79624888
Infusion site coldness	93.24	15.34	23	49303	216	79694846
Joint swelling	90.04	15.34	33	49293	288613	79406449
Carcinoembryonic antigen increased	89.75	15.34	38	49288	2171	79692891
Rheumatoid arthritis	88.59	15.34	12	49314	208458	79486604
Therapeutic product effect decreased	87.90	15.34	3	49323	163860	79531202
Off label use	84.53	15.34	284	49042	906931	78788131
Pleural effusion	83.91	15.34	238	49088	145024	79550038
Gamma-glutamyltransferase decreased	82.42	15.34	23	49303	361	79694701
Palmar-plantar erythrodysaesthesia syndrome	82.25	15.34	102	49224	33032	79662030
Second primary malignancy	79.37	15.34	68	49258	14282	79680780
Osteonecrosis	79.25	15.34	97	49229	30998	79664064
Spinal pain	77.22	15.34	69	49257	15323	79679739
Toxicity to various agents	75.31	15.34	90	49236	421450	79273612
Diarrhoea	74.86	15.34	852	48474	879637	78815425
Oral pain	74.34	15.34	95	49231	31703	79663359
Anaemia	73.02	15.34	498	48828	444517	79250545
Neuropathy peripheral	72.52	15.34	222	49104	141083	79553979
Drug interaction	71.68	15.34	91	49235	415092	79279970
Metastases to peritoneum	70.48	15.34	40	49286	4332	79690730
Pneumonia	70.46	15.34	194	49132	660052	79035010
Intentional product use issue	68.98	15.34	7	49319	152105	79542957
Overdose	68.63	15.34	15	49311	184191	79510871
Cancer pain	66.26	15.34	41	49285	5204	79689858
Ascites	64.87	15.34	144	49182	75418	79619644
Lymphangiosis carcinomatosa	64.77	15.34	30	49296	2124	79692938
Skin toxicity	64.38	15.34	48	49278	8266	79686796
Systemic lupus erythematosus	62.34	15.34	3	49323	121146	79573916
Injection site necrosis	61.96	15.34	26	49300	1452	79693610
Bone disorder	61.08	15.34	67	49259	19046	79676016
Tumour marker abnormal	60.33	15.34	17	49309	277	79694785
Adnexa uteri mass	59.69	15.34	18	49308	376	79694686
Bradycardia	59.53	15.34	7	49319	135550	79559512
Arthropathy	59.13	15.34	18	49308	177093	79517969
Drug hypersensitivity	58.66	15.34	59	49267	298857	79396205
Myelosuppression	58.43	15.34	96	49230	40200	79654862
Back pain	58.18	15.34	354	48972	303826	79391236
Cough	58.06	15.34	407	48919	366382	79328680
Lymphoedema	57.09	15.34	53	49273	12360	79682702
Infusion site induration	54.49	15.34	22	49304	1113	79693949
Metastases to pelvis	54.32	15.34	19	49307	643	79694419
Metastases to chest wall	53.94	15.34	18	49308	527	79694535
Bone marrow failure	53.92	15.34	106	49220	51001	79644061
Metastases to eye	52.80	15.34	15	49311	252	79694810
Pericarditis	52.31	15.34	3	49323	104233	79590829
Fall	51.41	15.34	144	49182	487485	79207577
Intentional overdose	50.40	15.34	4	49322	105956	79589106
Electrocardiogram PR shortened	50.35	15.34	15	49311	300	79694762
Mucosal inflammation	49.77	15.34	130	49196	75450	79619612
Sepsis	49.71	15.34	56	49270	269372	79425690
Isosthenuria	48.81	15.34	12	49314	111	79694951
Abdominal lymphadenopathy	47.80	15.34	21	49305	1313	79693749
Treatment failure	47.50	15.34	23	49303	170463	79524599
Tooth extraction	46.85	15.34	45	49281	10950	79684112
Cardiac arrest	46.77	15.34	24	49302	172072	79522990
Condition aggravated	46.41	15.34	157	49169	500967	79194095
Post-traumatic neck syndrome	44.47	15.34	23	49303	2071	79692991
Cardio-respiratory arrest	44.33	15.34	7	49319	108503	79586559
Hepatic failure	44.17	15.34	109	49217	61103	79633959
Lymphadenopathy	42.94	15.34	99	49227	53148	79641914
Metastases to retroperitoneum	42.61	15.34	14	49312	390	79694672
Confusional state	41.36	15.34	84	49242	317913	79377149
Asthma	41.16	15.34	16	49310	135079	79559983
Musculoskeletal stiffness	41.12	15.34	29	49297	174979	79520083
Carbohydrate antigen 27.29 increased	40.46	15.34	9	49317	51	79695011
Tumour marker decreased	40.31	15.34	9	49317	52	79695010
Pleural neoplasm	39.81	15.34	13	49313	355	79694707
Mobility decreased	39.73	15.34	13	49313	122162	79572900
Lacrimation increased	38.77	15.34	58	49268	22419	79672643
Metastases to breast	38.66	15.34	12	49314	277	79694785
Taste disorder	38.13	15.34	48	49278	15775	79679287
Constipation	37.89	15.34	302	49024	282748	79412314
Metastases to meninges	37.68	15.34	25	49301	3576	79691486
Hyperkalaemia	37.50	15.34	12	49314	114386	79580676
Pain in jaw	37.42	15.34	86	49240	46065	79648997
Dry skin	36.90	15.34	109	49217	67886	79627176
Loss of consciousness	36.68	15.34	30	49296	167913	79527149
Pyelitis	36.64	15.34	12	49314	331	79694731
Prehypertension	36.41	15.34	7	49319	16	79695046
Portal hypertension	35.92	15.34	32	49294	7076	79687986
International normalised ratio increased	35.68	15.34	5	49321	84716	79610346
Osteolysis	34.89	15.34	26	49300	4472	79690590
Hepatic echinococciasis	34.76	15.34	8	49318	54	79695008
Malignant pleural effusion	34.25	15.34	23	49303	3357	79691705
Metastases to thorax	33.71	15.34	10	49316	197	79694865
Metastases to the mediastinum	33.39	15.34	13	49313	597	79694465
Vasodilatation	33.02	15.34	22	49304	3169	79691893
Tachycardia	32.71	15.34	37	49289	177731	79517331
Haematotoxicity	32.60	15.34	44	49282	15475	79679587
Haemoglobin decreased	32.50	15.34	242	49084	221877	79473185
Suicide attempt	32.44	15.34	6	49320	82926	79612136
Ovarian disorder	32.42	15.34	12	49314	479	79694583
Bladder hypertrophy	32.42	15.34	13	49313	646	79694416
Ejection fraction decreased	32.07	15.34	68	49258	34509	79660553
Hormone receptor positive breast cancer	31.92	15.34	11	49315	356	79694706
Hypertransaminasaemia	31.68	15.34	38	49288	11886	79683176
Vein disorder	31.64	15.34	26	49300	5156	79689906
Hypermetabolism	31.60	15.34	11	49315	367	79694695
Creatinine renal clearance increased	31.51	15.34	14	49312	899	79694163
Gastrointestinal haemorrhage	31.50	15.34	27	49299	147692	79547370
Oxygen saturation decreased	30.82	15.34	21	49305	129026	79566036
Superinfection	30.78	15.34	25	49301	4877	79690185
Septic shock	30.66	15.34	19	49307	122782	79572280
Metastases to bladder	30.49	15.34	10	49316	277	79694785
Oestradiol increased	30.43	15.34	8	49318	99	79694963
Decreased immune responsiveness	30.39	15.34	26	49300	5449	79689613
Metastases to spinal cord	30.20	15.34	7	49319	49	79695013
Metabolic acidosis	30.16	15.34	7	49319	82522	79612540
Drug intolerance	30.06	15.34	75	49251	264044	79431018
Infusion site haemorrhage	29.97	15.34	22	49304	3698	79691364
Onychoclasis	29.97	15.34	26	49300	5552	79689510
Hypoglycaemia	29.38	15.34	13	49313	101581	79593481
Syncope	29.21	15.34	41	49285	179408	79515654
Joint neoplasm	28.64	15.34	7	49319	63	79694999
Hyponatraemia	28.59	15.34	41	49285	177807	79517255
Nephroangiosclerosis	28.57	15.34	10	49316	339	79694723
Dysgeusia	28.53	15.34	89	49237	57088	79637974
Breast pain	28.21	15.34	30	49296	8235	79686827
Mouth swelling	28.14	15.34	26	49300	6025	79689037
Invasive lobular breast carcinoma	28.12	15.34	12	49314	699	79694363
Myocardial infarction	28.10	15.34	44	49282	184085	79510977
Malignant peritoneal neoplasm	28.07	15.34	12	49314	702	79694360
Cardiac failure congestive	28.03	15.34	28	49298	142374	79552688
Seizure	27.99	15.34	46	49280	188788	79506274
Irritable bowel syndrome	27.86	15.34	3	49323	62238	79632824
Metastases to kidney	27.70	15.34	11	49315	533	79694529
Feeling cold	27.22	15.34	57	49269	28672	79666390
Agitation	26.94	15.34	14	49312	99701	79595361
Interstitial lung disease	26.75	15.34	139	49187	112461	79582601
Soft tissue neoplasm	26.74	15.34	7	49319	85	79694977
Fibromyalgia	26.62	15.34	4	49322	64336	79630726
Product dose omission in error	26.10	15.34	28	49298	7760	79687302
Pulmonary tumour thrombotic microangiopathy	26.03	15.34	7	49319	95	79694967
BRCA2 gene mutation	26.03	15.34	7	49319	95	79694967
Pustule	26.01	15.34	16	49310	2009	79693053
Atrial fibrillation	25.94	15.34	52	49274	197834	79497228
Neoplasm	25.79	15.34	30	49296	9086	79685976
Mean cell haemoglobin decreased	25.63	15.34	25	49301	6199	79688863
Exposed bone in jaw	25.55	15.34	20	49306	3700	79691362
Blood creatine phosphokinase increased	25.39	15.34	5	49321	66085	79628977
Pneumonitis	25.25	15.34	89	49237	60771	79634291
Suicidal ideation	25.03	15.34	8	49318	76332	79618730
Vulvovaginal dryness	24.64	15.34	16	49310	2208	79692854
Peritoneal disorder	24.50	15.34	11	49315	724	79694338
Osteosclerosis	24.40	15.34	20	49306	3951	79691111
Hospitalisation	24.34	15.34	14	49312	94222	79600840
Adverse event	24.33	15.34	4	49322	60210	79634852
Skin sensitisation	24.26	15.34	12	49314	983	79694079
Toothache	24.26	15.34	44	49282	19926	79675136
Recurrent cancer	24.16	15.34	17	49309	2676	79692386
Epistaxis	24.00	15.34	134	49192	111381	79583681
Nail avulsion	23.98	15.34	7	49319	130	79694932
Blood pressure fluctuation	23.94	15.34	6	49320	67139	79627923
Pneumonia aspiration	23.84	15.34	6	49320	66961	79628101
Psoriasis	23.58	15.34	13	49313	89574	79605488
Adverse drug reaction	23.54	15.34	6	49320	66386	79628676
Blood pressure increased	23.29	15.34	61	49265	211299	79483763
Hallucination	23.22	15.34	12	49314	85733	79609329
Metastases to soft tissue	23.17	15.34	10	49316	599	79694463
Angioedema	23.16	15.34	9	49317	76026	79619036
Osteomyelitis	23.15	15.34	58	49268	32807	79662255
Invasive ductal breast carcinoma	23.02	15.34	23	49303	5869	79689193
Metastases to uterus	22.99	15.34	6	49320	72	79694990
Transaminases	22.62	15.34	6	49320	77	79694985
Therapeutic product effect incomplete	22.42	15.34	33	49293	141612	79553450
Discomfort	22.19	15.34	27	49299	125590	79569472
Metastatic neoplasm	22.17	15.34	21	49305	5021	79690041
Tremor	22.03	15.34	45	49281	170038	79525024
Unresponsive to stimuli	21.90	15.34	4	49322	55784	79639278
Bone sequestrum	21.87	15.34	12	49314	1217	79693845
Oral disorder	21.78	15.34	29	49297	10066	79684996
Febrile neutropenia	21.59	15.34	72	49254	230927	79464135
Elliptocytosis	21.57	15.34	6	49320	93	79694969
Madarosis	21.30	15.34	16	49310	2786	79692276
Coronary artery disease	21.22	15.34	7	49319	65467	79629595
RET gene mutation	21.17	15.34	4	49322	8	79695054
Hypersensitivity	21.07	15.34	87	49239	262152	79432910
Metastases to ovary	20.94	15.34	8	49318	349	79694713
Pathological fracture	20.81	15.34	29	49297	10508	79684554
Coma	20.73	15.34	19	49307	100630	79594432
Glossodynia	20.70	15.34	20	49306	103317	79591745
Hepatic cyst	20.60	15.34	22	49304	6067	79688995
Plasma cell myeloma	20.52	15.34	4	49322	53255	79641807
Wound	20.49	15.34	25	49301	116154	79578908
Tooth disorder	20.30	15.34	48	49278	26185	79668877
Blood pressure systolic increased	20.29	15.34	8	49318	66978	79628084
Mental status changes	20.28	15.34	8	49318	66951	79628111
Aphthous ulcer	20.25	15.34	37	49289	16852	79678210
Depressed level of consciousness	20.20	15.34	18	49308	96634	79598428
Musculoskeletal chest pain	19.91	15.34	46	49280	24718	79670344
Transaminases abnormal	19.85	15.34	10	49316	852	79694210
Gingival pain	19.65	15.34	26	49300	8972	79686090
Nail disorder	19.61	15.34	30	49296	11822	79683240
Gingivitis	19.60	15.34	26	49300	8995	79686067
Hepatotoxicity	19.53	15.34	73	49253	51279	79643783
Pancreatitis	19.48	15.34	9	49317	68566	79626496
Drug ineffective for unapproved indication	19.42	15.34	4	49322	51234	79643828
Neoplasm recurrence	19.39	15.34	18	49308	4196	79690866
Inappropriate schedule of product administration	19.38	15.34	33	49293	133595	79561467
Respiratory failure	19.33	15.34	53	49273	180858	79514204
Injury	19.33	15.34	12	49314	77484	79617578
Swelling	19.27	15.34	69	49257	216642	79478420
Aspartate aminotransferase increased	19.11	15.34	149	49177	138492	79556570
Body surface area increased	19.07	15.34	6	49320	145	79694917
Bone debridement	19.06	15.34	8	49318	447	79694615
Dysarthria	19.01	15.34	9	49317	67613	79627449
Laryngitis viral	18.93	15.34	5	49321	63	79694999
Drug reaction with eosinophilia and systemic symptoms	18.93	15.34	8	49318	64236	79630826
Sinusitis	18.91	15.34	60	49266	195441	79499621
Excessive granulation tissue	18.91	15.34	10	49316	942	79694120
Encephalopathy	18.90	15.34	9	49317	67388	79627674
Cytopenia	18.80	15.34	40	49286	20343	79674719
Adenocarcinoma	18.66	15.34	17	49309	3869	79691193
Eastern Cooperative Oncology Group performance status worsened	18.44	15.34	13	49313	2052	79693010
Dorsal ramus syndrome	18.40	15.34	4	49322	20	79695042
Overflow diarrhoea	18.30	15.34	6	49320	166	79694896
Hydronephrosis	18.16	15.34	36	49290	17418	79677644
Medication error	18.01	15.34	10	49316	68632	79626430
Lower respiratory tract infection	17.76	15.34	33	49293	129187	79565875
Chronic obstructive pulmonary disease	17.74	15.34	16	49310	85403	79609659
Breast injury	17.71	15.34	5	49321	82	79694980
Loose tooth	17.70	15.34	15	49311	3102	79691960
Blood creatinine decreased	17.69	15.34	23	49303	7802	79687260
Retinal detachment	17.60	15.34	25	49301	9222	79685840
Heart rate decreased	17.38	15.34	11	49315	70305	79624757
Intentional product misuse	17.29	15.34	20	49306	95145	79599917
Melaena	17.28	15.34	8	49318	60882	79634180
Mucinous breast carcinoma	17.26	15.34	4	49322	28	79695034
Sequestrectomy	16.97	15.34	9	49317	853	79694209
Carcinoid tumour pulmonary	16.92	15.34	7	49319	377	79694685
Wheezing	16.74	15.34	29	49297	116635	79578427
Product use in unapproved indication	16.61	15.34	89	49237	250270	79444792
Congenital haematological disorder	16.47	15.34	4	49322	35	79695027
Parosmia	16.46	15.34	21	49305	6993	79688069
Bone cancer	16.44	15.34	12	49314	2000	79693062
Hepatic enzyme increased	16.33	15.34	58	49268	182552	79512510
Unevaluable event	16.25	15.34	7	49319	55578	79639484
Treatment noncompliance	16.23	15.34	6	49320	52262	79642800
Fractured sacrum	16.22	15.34	11	49315	1632	79693430
Ascariasis	15.87	15.34	3	49323	6	79695056
Debridement	15.62	15.34	11	49315	1734	79693328
Abdominal wall cyst	15.56	15.34	4	49322	45	79695017
Breast mass	15.50	15.34	20	49306	6734	79688328
White blood cell disorder	15.40	15.34	14	49312	3178	79691884

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L02BA03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Anti-estrogens
FDA MoA	N0000000145	Estrogen Receptor Antagonists
FDA MoA	N0000000168	Selective Estrogen Receptor Modulators
FDA EPC	N0000175582	Estrogen Receptor Antagonist
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D018931	Antineoplastic Agents, Hormonal
MeSH PA	D004965	Estrogen Antagonists
MeSH PA	D065171	Estrogen Receptor Antagonists
MeSH PA	D006727	Hormone Antagonists
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:50792	estrogen receptor antagonists
CHEBI has role	CHEBI:50837	oestrogen antagonist

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

Disease	Relation	SNOMED_ID	DOID
Metastatic Breast Cancer Progression Post-Antiestrogen Therapy	indication
Blood coagulation disorder	contraindication	64779008	DOID:1247
Disease of liver	contraindication	235856003	DOID:409
Pregnancy, function	contraindication	289908002
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
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	10.92	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
250MG/5ML (50MG/ML)	FULVESTRANT	FRESENIUS KABI USA	N210326	May 20, 2019	RX	SOLUTION	INTRAMUSCULAR	10188663	Feb. 14, 2034	TREATMENT OF HORMONE RECEPTOR POSITIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN
250MG/5ML (50MG/ML)	FULVESTRANT	FRESENIUS KABI USA	N210326	May 20, 2019	RX	SOLUTION	INTRAMUSCULAR	9833459	Feb. 14, 2034	TREATMENT OF HORMONE RECEPTOR POSITIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN
250MG/5ML (50MG/ML)	FULVESTRANT	FRESENIUS KABI USA	N210326	May 20, 2019	RX	SOLUTION	INTRAMUSCULAR	9271990	May 17, 2034	TREATMENT OF HORMONE RECEPTOR POSITIVE ADVANCED BREAST CANCER IN POSTMENOPAUSAL WOMEN

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Estrogen receptor	Nuclear hormone receptor	P03372	ESR1_HUMAN	ANTAGONIST	Ki	9.62	WOMBAT-PK	CHEMBL
Estrogen receptor beta	Nuclear hormone receptor	Q92731	ESR2_HUMAN	ANTAGONIST	Ki	8.74	WOMBAT-PK	CHEMBL
Progesterone receptor	Nuclear hormone receptor	P06401	PRGR_HUMAN		IC50	9.68	CHEMBL
G-protein coupled estrogen receptor 1	GPCR	Q99527	GPER1_HUMAN		EC50	7	WOMBAT-PK
Bile acid receptor	Nuclear hormone receptor	Q96RI1	NR1H4_HUMAN		IC50	6.10	CHEMBL
Steroid hormone receptor ERR1	Nuclear hormone receptor	P11474	ERR1_HUMAN		IC50	8.70	CHEMBL
Bifunctional epoxide hydrolase 2	Enzyme	P34913	HYES_HUMAN		Ki	7.59	CHEMBL
Nuclear receptor subfamily 1 group I member 2	Nuclear hormone receptor	O75469	NR1I2_HUMAN		EC50	5.71	CHEMBL
NAD-dependent protein deacylase sirtuin-5, mitochondrial	Enzyme	Q9NXA8	SIR5_HUMAN		IC50	5.58	CHEMBL
Estrogen receptor	Transcription factor		ESR1_RAT		IC50	8.23	CHEMBL
Beta-lactamase TEM	Enzyme		BLAT_ECOLX		IC50	4.25	CHEMBL

External reference:

ID	Source
4021350	VUID
N0000148770	NUI
D01161	KEGG_DRUG
4021350	VANDF
C0935916	UMLSCUI
CHEBI:31638	CHEBI
FVS	PDB_CHEM_ID
CHEMBL1358	ChEMBL_ID
D000077267	MESH_DESCRIPTOR_UI
DB00947	DRUGBANK_ID
1015	IUPHAR_LIGAND_ID
7712	INN_ID
22X328QOC4	UNII
104741	PUBCHEM_CID
203870	RXNORM
16618	MMSL
300687	MMSL
43430	MMSL
d04799	MMSL
009642	NDDF
385519002	SNOMEDCT_US
404845006	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9022	INJECTION	50 mg	INTRAMUSCULAR	ANDA	25 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9022	INJECTION	50 mg	INTRAMUSCULAR	ANDA	25 sections
FASLODEX	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0720	INJECTION	50 mg	INTRAMUSCULAR	NDA	25 sections
FASLODEX	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0720	INJECTION	50 mg	INTRAMUSCULAR	NDA	25 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0310-7720	INJECTION	50 mg	INTRAMUSCULAR	NDA authorized generic	25 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0310-7720	INJECTION	50 mg	INTRAMUSCULAR	NDA authorized generic	25 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0591-5019	INJECTION	250 mg	INTRAMUSCULAR	NDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0591-5019	INJECTION	250 mg	INTRAMUSCULAR	NDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0591-5019	INJECTION	250 mg	INTRAMUSCULAR	NDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0781-3079	INJECTION	50 mg	INTRAMUSCULAR	ANDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0781-3492	INJECTION	50 mg	INTRAMUSCULAR	ANDA	26 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	0781-9055	INJECTION	50 mg	INTRAMUSCULAR	ANDA	27 sections
FULVESTRANT	HUMAN PRESCRIPTION DRUG LABEL	1	16714-070	INJECTION, SOLUTION	50 mg	INTRAMUSCULAR	ANDA	18 sections
FULVESTRANT	HUMAN PRESCRIPTION DRUG LABEL	1	16714-070	INJECTION, SOLUTION	50 mg	INTRAMUSCULAR	ANDA	18 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	16714-118	INJECTION	50 mg	INTRAMUSCULAR	ANDA	26 sections
FULVESTRANT	HUMAN PRESCRIPTION DRUG LABEL	1	16729-436	INJECTION	250 mg	INTRAMUSCULAR	ANDA	25 sections
fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	25021-462	INJECTION, SOLUTION	50 mg	INTRAMUSCULAR	ANDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	43598-262	INJECTION, SOLUTION	50 mg	INTRAMUSCULAR	ANDA	27 sections
Fulvestrant	Human Prescription Drug Label	1	55150-394	INJECTION	50 mg	INTRAVENOUS	ANDA	27 sections
Fulvestrant	Human Prescription Drug Label	1	62332-650	INJECTION	50 mg	INTRAMUSCULAR	ANDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	63323-715	INJECTION, SOLUTION	50 mg	INTRAMUSCULAR	NDA	28 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	67457-311	INJECTION	50 mg	INTRAMUSCULAR	ANDA	28 sections
fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	68001-424	INJECTION, SOLUTION	50 mg	INTRAMUSCULAR	ANDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	68001-484	INJECTION, SOLUTION	250 mg	INTRAMUSCULAR	ANDA	27 sections
Fulvestrant68001-510	HUMAN PRESCRIPTION DRUG LABEL	1	68001-510	INJECTION	50 mg	INTRAMUSCULAR	ANDA	27 sections
FULVESTRANT	HUMAN PRESCRIPTION DRUG LABEL	1	68001-522	INJECTION	250 mg	INTRAMUSCULAR	ANDA	25 sections
FULVESTRANT	HUMAN PRESCRIPTION DRUG LABEL	1	68001-522	INJECTION	250 mg	INTRAMUSCULAR	ANDA	25 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	68462-317	INJECTION	50 mg	INTRAMUSCULAR	ANDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	68462-317	INJECTION	50 mg	INTRAMUSCULAR	ANDA	27 sections
Fulvestrant	HUMAN PRESCRIPTION DRUG LABEL	1	70121-1463	INJECTION, SOLUTION	250 mg	INTRAMUSCULAR	ANDA	27 sections