All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

estriol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
estrogens	3187	50-27-1

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: estriol destriol estratriol ovestrion

A hydroxylated metabolite of ESTRADIOL or ESTRONE that has a hydroxyl group at C3, 16-alpha, and 17-beta position. Estriol is a major urinary estrogen. During PREGNANCY, a large amount of estriol is produced by the PLACENTA. Isomers with inversion of the hydroxyl group or groups are called epiestriol. Molecular weight: 288.39 Formula: C18H24O3 CLOGP: 3.20 LIPINSKI: 0 HAC: 3 HDO: 3 TPSA: 60.69 ALOGS: -3.38 ROTB: 0

Drug dosage:

Dose	Unit	Route
2	mg	O
2	mg	P
0.20	mg	V

ADMET properties:

Property	Value	Reference
S (Water solubility)	0.03 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	2.618		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	0.951		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	44.157	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	17.947	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	8.720	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	22.870	%	High	1
herg	hERG pIC50	4.614	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	17.783	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	5.559	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	7.500	%	High	1
kinase-safety-class	ACVR2B,BRAF,BTK,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PRKDC,TEK,TGFBR1,ZAP70	21
kinase-selectivity-class	EIF2AK3,GRK2,MAP2K6	3
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	3.631		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	112.202		High	1
mppb	Mouse plasma protein binding (% unbound)	9.560		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	8.279		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	14.040	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	129.122	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	56.810	%	High	1
rppb	Rat plasma protein binding (% unbound)	10.110	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	157.036	uM	High	1

Approvals:

Date	Agency	Company	Orphan
None	FDA

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
Cardiospasm	327.85	21.93	77	10561	3369	90614440
Palmoplantar keratoderma	326.50	21.93	77	10561	3430	90614379
Sleep terror	308.04	21.93	77	10561	4387	90613422
Pruritus genital	306.44	21.93	77	10561	4481	90613328
Atrial tachycardia	285.57	21.93	77	10561	5913	90611896
Carotid artery occlusion	281.22	21.93	77	10561	6265	90611544
Tension headache	277.33	21.93	79	10559	7430	90610379
Anosmia	260.42	21.93	80	10558	9768	90608041
Immunisation	250.70	21.93	57	10581	2156	90615653
Facial pain	233.53	21.93	79	10559	13103	90604706
Muscle twitching	224.21	21.93	90	10548	24112	90593697
Subarachnoid haemorrhage	217.19	21.93	81	10557	17823	90599986
Pain of skin	214.43	21.93	78	10560	16004	90601805
Lip swelling	211.26	21.93	99	10539	38511	90579298
Vasculitis	195.13	21.93	80	10558	22613	90595196
Ventricular tachycardia	188.56	21.93	80	10558	24628	90593181
Tinnitus	177.36	21.93	91	10547	43011	90574798
Blindness	173.27	21.93	77	10561	26491	90591318
Eye pruritus	169.87	21.93	78	10560	28949	90588860
Diplopia	167.54	21.93	77	10561	28637	90589172
Cognitive disorder	151.79	21.93	97	10541	69310	90548499
Disturbance in attention	147.64	21.93	83	10555	47026	90570783
Angioedema	145.18	21.93	92	10546	64784	90553025
Transient ischaemic attack	143.30	21.93	79	10559	43097	90574712
Hallucination	121.90	21.93	83	10555	65876	90551933
Rash papular	120.02	21.93	55	10583	20300	90597509
Dry skin	102.57	21.93	84	10554	87989	90529820
Persistent genital arousal disorder	101.09	21.93	22	10616	678	90617131
Hyperhidrosis	99.59	21.93	100	10538	136205	90481604
Blood glucose increased	96.83	21.93	84	10554	95162	90522647
Feeling abnormal	96.15	21.93	108	10530	167127	90450682
Palpitations	95.68	21.93	98	10540	136630	90481179
Intentional product misuse	91.03	21.93	79	10559	89525	90528284
Amnesia	89.33	21.93	85	10553	108420	90509389
Visual impairment	89.23	21.93	93	10545	132272	90485537
Heart rate increased	86.47	21.93	85	10553	112817	90504992
Myocardial infarction	85.31	21.93	82	10556	105890	90511919
Tachycardia	74.29	21.93	92	10546	157581	90460228
Memory impairment	72.70	21.93	102	10536	197142	90420667
Migraine	70.97	21.93	99	10539	190293	90427516
Muscular weakness	67.60	21.93	101	10537	206565	90411244
COVID-19	60.25	21.93	86	10552	168757	90449052
Dehydration	55.14	21.93	89	10549	194358	90423451
Back pain	48.85	21.93	112	10526	317063	90300746
Mucosal erosion	48.80	21.93	15	10623	1830	90615979
Insomnia	43.04	21.93	110	10528	333364	90284445
Genital erosion	42.21	21.93	10	10628	453	90617356
Thirst decreased	39.58	21.93	9	10629	340	90617469
Nausea	37.44	21.93	240	10398	1110076	89507733
Anxiety	34.71	21.93	97	10541	309675	90308134
Pneumonia	32.85	21.93	17	10621	638042	89979767
Dizziness	31.02	21.93	144	10494	589140	90028669
Infusion related reaction	30.42	21.93	6	10632	416774	90201035
Malaise	29.24	21.93	141	10497	585845	90031964
Drug ineffective	29.10	21.93	76	10562	1384222	89233587
Chest pain	28.18	21.93	92	10546	319553	90298256
Arthropathy	27.30	21.93	5	10633	366237	90251572
Glossodynia	27.23	21.93	3	10635	321776	90296033
Abdominal pain upper	26.89	21.93	93	10545	332581	90285228
Swelling	26.74	21.93	8	10630	419050	90198759
Conjunctivitis	25.99	21.93	23	10615	26683	90591126
Drug hypersensitivity	25.92	21.93	11	10627	463598	90154211
Death	25.26	21.93	11	10627	456540	90161269
Wound	25.20	21.93	3	10635	302977	90314832
Lip blister	24.22	21.93	10	10628	2868	90614941
Pericarditis	24.02	21.93	78	10560	270073	90347736
Thyrotoxic periodic paralysis	23.42	21.93	4	10634	32	90617777
Mouth ulceration	23.23	21.93	26	10612	39948	90577861
Hepatic enzyme increased	22.80	21.93	7	10631	360729	90257080
Discomfort	22.12	21.93	3	10635	274332	90343477

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
Cardiospasm	369.34	322.59	76	4820	1831	42614608
Palmoplantar keratoderma	345.31	322.59	74	4822	2180	42614259
Pruritus genital	333.68	322.59	74	4822	2565	42613874
Sleep terror	326.08	322.59	74	4822	2852	42613587

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
Cardiospasm	654.55	28.70	147	14010	4820	110570322
Palmoplantar keratoderma	631.94	28.70	145	14012	5242	110569900
Pruritus genital	604.36	28.70	145	14012	6377	110568765
Sleep terror	602.43	28.70	145	14012	6465	110568677
Atrial tachycardia	564.83	28.70	147	14010	9031	110566111
Tension headache	558.00	28.70	147	14010	9471	110565671
Carotid artery occlusion	554.01	28.70	146	14011	9419	110565723
Anosmia	524.70	28.70	148	14009	12324	110562818
Facial pain	490.11	28.70	147	14010	15192	110559950
Immunisation	467.63	28.70	103	14054	3080	110572062
Pain of skin	443.38	28.70	145	14012	19884	110555258
Subarachnoid haemorrhage	405.82	28.70	150	14007	29552	110545590
Muscle twitching	404.67	28.70	150	14007	29785	110545357
Lip swelling	376.36	28.70	165	13992	50502	110524640
Vasculitis	371.30	28.70	148	14009	35725	110539417
Eye pruritus	370.04	28.70	144	14013	32631	110542511
Blindness	362.45	28.70	146	14011	36213	110538929
Diplopia	339.15	28.70	145	14012	41749	110533393
Tinnitus	326.91	28.70	158	13999	60382	110514760
Ventricular tachycardia	323.93	28.70	148	14009	49861	110525281
Disturbance in attention	299.53	28.70	150	14007	61845	110513297
Transient ischaemic attack	289.23	28.70	148	14009	63834	110511308
Cognitive disorder	266.80	28.70	156	14001	87355	110487787
Rash papular	265.13	28.70	108	14049	27531	110547611
Angioedema	259.90	28.70	160	13997	98340	110476802
Amnesia	232.70	28.70	153	14004	105255	110469887
Hallucination	230.68	28.70	150	14007	101282	110473860
Dry skin	227.35	28.70	152	14005	107501	110467641
Visual impairment	216.94	28.70	161	13996	134267	110440875
Feeling abnormal	199.01	28.70	173	13984	180538	110394604
Palpitations	197.00	28.70	163	13994	159049	110416093
Blood glucose increased	192.36	28.70	149	14008	132347	110442795
Heart rate increased	187.89	28.70	152	14005	143682	110431460
Hyperhidrosis	185.75	28.70	169	13988	187129	110388013
Intentional product misuse	183.29	28.70	145	14012	132759	110442383
Migraine	172.37	28.70	156	14001	171496	110403646
Memory impairment	157.81	28.70	158	13999	196786	110378356
Muscular weakness	149.11	28.70	171	13986	248297	110326845
Myocardial infarction	146.40	28.70	150	14007	191933	110383209
Tachycardia	135.99	28.70	156	14001	226489	110348653
Pericarditis	125.05	28.70	147	14010	218967	110356175
COVID-19	118.16	28.70	151	14006	244909	110330233
Dehydration	111.48	28.70	157	14000	279354	110295788
Persistent genital arousal disorder	105.51	28.70	23	14134	653	110574489
Insomnia	104.97	28.70	175	13982	360415	110214727
Back pain	102.62	28.70	176	13981	370820	110204322
Anxiety	89.28	28.70	159	13998	344919	110230223
Chest pain	84.31	28.70	163	13994	376212	110198930
Alopecia	84.20	28.70	160	13997	364593	110210549
Peripheral swelling	79.76	28.70	166	13991	403868	110171274
Abdominal pain upper	79.16	28.70	152	14005	348959	110226183
Drug ineffective	77.44	28.70	50	14107	1520490	109054652
Abdominal discomfort	75.61	28.70	160	13997	393698	110181444
Pneumonia	67.38	28.70	15	14142	876699	109698443
Intentional product use issue	63.75	28.70	114	14043	247792	110327350
Death	60.03	28.70	9	14148	698860	109876282
Malaise	57.83	28.70	203	13954	671616	109903526
Dizziness	53.37	28.70	203	13954	697990	109877152
Adverse drug reaction	47.59	28.70	63	14094	105496	110469646
Headache	44.86	28.70	227	13930	882150	109692992
Pruritus	42.67	28.70	167	13990	581393	109993749
Mucosal erosion	41.25	28.70	15	14142	2809	110572333
Nausea	39.77	28.70	282	13875	1235408	109339734
Thirst decreased	38.25	28.70	9	14148	362	110574780
Vomiting	37.32	28.70	221	13936	910454	109664688
Drug hypersensitivity	36.41	28.70	7	14150	454083	110121059
Acute kidney injury	36.34	28.70	18	14139	635412	109939730
Condition aggravated	36.11	28.70	25	14132	734811	109840331
Genital erosion	35.78	28.70	10	14147	801	110574341
Anaemia	33.61	28.70	14	14143	547072	110028070
Infusion related reaction	32.47	28.70	5	14152	381157	110193985

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	G03CA04	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ESTROGENS Natural and semisynthetic estrogens, plain
ATC	G03CC06	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ESTROGENS Estrogens, combinations with other drugs
CHEBI has role	CHEBI:35705	immunosuppressive agent
CHEBI has role	CHEBI:50114	estrogen
CHEBI has role	CHEBI:75771	mouse metabolite
CHEBI has role	CHEBI:76967	human xenobiotic metabolite
CHEBI has role	CHEBI:77746	human metabolite

Related Drugs by ATC class:

G03CA Natural and semisynthetic estrogens, plain 7 drugs

chlorotrianiseneconjugated estrogensestetrolestradiolestroneethinylestradiolpromestriene

G03CC Estrogens, combinations with other drugs 6 drugs

bazedoxifeneconjugated estrogensdienestroldiethylstilbestrolestronemethallenestril

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

None

🐶 Veterinary Drug Use

Species	Use	Relation
Dogs	Control of estrogen-responsive urinary incontinence	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
Incurin	Intervet Inc.	1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.13	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Estrogen receptor	Nuclear hormone receptor	P03372	ESR1_HUMAN	AGONIST	Ki	8.67		IUPHAR	IUPHAR
Glucocorticoid receptor	Nuclear hormone receptor	P04150	GCR_HUMAN		Ki	4.75		DRUG MATRIX
Estrogen receptor beta	Nuclear hormone receptor	Q92731	ESR2_HUMAN	AGONIST	Ki	8.40		IUPHAR
Corticosteroid-binding globulin	Secreted	P08185	CBG_HUMAN		Ki	5		CHEMBL
Sex hormone-binding globulin	Secreted	P04278	SHBG_HUMAN		Kd	6.63		CHEMBL
Alpha-synuclein	Transporter	P37840	SYUA_HUMAN		IC50	4.70		CHEMBL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.26		DRUG MATRIX
Olfactory receptor 51E2	GPCR	Q9H255	O51E2_HUMAN		EC50	4.28		CHEMBL
Arachidonate 15-lipoxygenase	Enzyme		LOX15_RABIT		IC50	5.06		DRUG MATRIX
Lanosterol 14-alpha demethylase	Enzyme		CP51_MYCTU		Kd	4		CHEMBL

External reference:

ID	Source
N0000167513	NUI
D00185	KEGG_DRUG
C0014927	UMLSCUI
CHEBI:27974	CHEBI
ESL	PDB_CHEM_ID
CHEMBL193482	ChEMBL_ID
DB04573	DRUGBANK_ID
D004964	MESH_DESCRIPTOR_UI
5756	PUBCHEM_CID
2821	IUPHAR_LIGAND_ID
FB33469R8E	UNII
4094	RXNORM
132550	MMSL
18220	MMSL
NOCODE	MMSL
d05027	MMSL
001285	NDDF
354050008	SNOMEDCT_US
708043004	SNOMEDCT_US
73723004	SNOMEDCT_US
FB33469R8E	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
BiEST 2.5 Estrogen Cream	HUMAN OTC DRUG LABEL	2	82018-0007	CREAM	2 mg	TRANSDERMAL	unapproved drug other	10 sections
BiEST 2.5 Estrogen Cream (Lavender scented)	HUMAN OTC DRUG LABEL	2	82018-0008	CREAM	2 mg	TRANSDERMAL	unapproved drug other	10 sections
BiEST 5.0 Estrogen Cream	HUMAN OTC DRUG LABEL	2	82018-0009	CREAM	4 mg	TRANSDERMAL	unapproved drug other	10 sections
Estriol 5.0 Cream	HUMAN OTC DRUG LABEL	1	82018-0010	CREAM	5 mg	TRANSDERMAL	unapproved drug other	10 sections
Natural Revita Vaginal Moisturizer	HUMAN OTC DRUG LABEL	1	82018-0025	CREAM	0.08 mg	TRANSDERMAL	unapproved drug other	10 sections
Balance Plus Cream	HUMAN OTC DRUG LABEL	4	82018-0028	CREAM	240 mg	TRANSDERMAL	unapproved drug other	10 sections
BiEST 5.0 Estrogen Cream - 3.6oz	HUMAN OTC DRUG LABEL	2	82018-0029	CREAM	4 mg	TRANSDERMAL	unapproved drug other	10 sections
3.6oz BiEST 2.5 Estrogen Cream	HUMAN OTC DRUG LABEL	2	82018-0030	CREAM	2 mg	TRANSDERMAL	unapproved drug other	10 sections
Estriol cream	HUMAN OTC DRUG LABEL	2	84735-014	CREAM	2 g	TOPICAL	OTC Monograph Drug	9 sections
Estriol cream	HUMAN OTC DRUG LABEL	2	84735-014	CREAM	2 g	TOPICAL	OTC Monograph Drug	9 sections
Estriol Cream	HUMAN OTC DRUG LABEL	1	84763-013	CREAM	0.00 g	TOPICAL	OTC Monograph Drug	11 sections
BUNUSS Estriol Face	HUMAN OTC DRUG LABEL	1	84867-024	CREAM	3 g	TOPICAL	OTC Monograph Drug	8 sections
Arthcal Estriol Face Cream for Women	HUMAN OTC DRUG LABEL	3	85212-0016	CREAM	0.20 g	EXTRACORPOREAL	OTC Monograph Drug	10 sections
Arthcal ESTROGEN	HUMAN OTC DRUG LABEL	1	85212-0038	CREAM	0.20 g	CUTANEOUS	ANDA	10 sections
Flocean INTIMATE COMFORT	HUMAN OTC DRUG LABEL	1	85248-055	CREAM	0.10 g	TOPICAL	unapproved drug other	13 sections
Beilloso Women Estriol	HUMAN OTC DRUG LABEL	1	85248-137	CREAM	0.10 g	TOPICAL	unapproved drug other	13 sections
JOVYNEX WOMEN ESTRIOL	HUMAN OTC DRUG LABEL	1	85248-154	CREAM	0.10 g	TOPICAL	unapproved drug other	13 sections
JARDIENT	HUMAN OTC DRUG LABEL	1	85646-003	CREAM	0.36 g	TOPICAL	OTC Monograph Drug	12 sections
JARDIENT Estriol Cream	HUMAN OTC DRUG LABEL	1	85646-006	CREAM	0.36 g	TOPICAL	OTC Monograph Drug	12 sections
Vigority Estriol Cream	HUMAN OTC DRUG LABEL	1	85739-003	CREAM	3 mg	TOPICAL	OTC Monograph Drug	13 sections
MYEVER	HUMAN OTC DRUG LABEL	1	87066-5915	CREAM	0.20 g	TOPICAL	OTC Monograph Drug	14 sections
DVO Estriol cream	HUMAN OTC DRUG LABEL	1	87204-503	CREAM	0.20 g	TOPICAL	OTC Monograph Drug	10 sections
Estriol 5000 mcg 5 g	HUMAN OTC DRUG LABEL	1	87250-105	CREAM	5 g	TRANSDERMAL	unapproved drug other	11 sections
ESTRIOL	HUMAN OTC DRUG LABEL	1	87255-006	CREAM	0.20 g	TOPICAL	OTC Monograph Drug	12 sections
Estriol Cream	HUMAN OTC DRUG LABEL	1	87278-010	CREAM	0.00 g	VAGINAL	OTC Monograph Drug	11 sections
Estriol Cream	HUMAN OTC DRUG LABEL	1	87704-001	CREAM	0.00 g	TOPICAL	OTC Monograph Drug	10 sections
LEMOTO BIOIDENTICAL ESTROGEN VAGINAL Cream	HUMAN OTC DRUG LABEL	1	87786-010	CREAM	0.10 g	TOPICAL	unapproved drug other	13 sections
MOROVAN	HUMAN OTC DRUG LABEL	1	87800-2524	CREAM	0.20 g	TOPICAL	OTC Monograph Drug	14 sections