Scroll

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

Stem definition	Drug id	CAS RN
	2561	10540-29-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: tamoxifen tamoxifen citrate tamoxifene tamoxifene citrate	One of the SELECTIVE ESTROGEN RECEPTOR MODULATORS with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the ENDOMETRIUM. Molecular weight: 371.52 Formula: C26H29NO CLOGP: 6.82 LIPINSKI: 1 HAC: 2 HDO: 0 TPSA: 12.47 ALOGS: -5.56 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tamoxifen
tamoxifen citrate
tamoxifene
tamoxifene citrate

One of the SELECTIVE ESTROGEN RECEPTOR MODULATORS with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the ENDOMETRIUM.

Molecular weight: 371.52
Formula: C26H29NO
CLOGP: 6.82
LIPINSKI: 1
HAC: 2
HDO: 0
TPSA: 12.47
ALOGS: -5.56
ROTB: 8

Status: OFP

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

Drug dosage:

Dose	Unit	Route
20	mg	O

ADMET properties:

Show entries

Search:

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.18 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.50 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI

Showing 1 to 4 of 4 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
Dec. 30, 1977	FDA

FDA Adverse Event Reporting System (Female)

Show entries

Search:

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
Metastases to bone	1811.70	11.70	627	39240	20392	63428763
Malignant neoplasm progression	1639.79	11.70	867	39000	81254	63367901
Metastases to liver	1061.57	11.70	438	39429	23201	63425954
Metastases to lung	595.02	11.70	243	39624	12507	63436648
Metastases to lymph nodes	509.33	11.70	192	39675	7966	63441189
Breast cancer recurrent	490.55	11.70	159	39708	4182	63444973
Breast cancer metastatic	434.13	11.70	191	39676	11827	63437328
Disease progression	417.48	11.70	447	39420	122311	63326844
Neoplasm progression	397.99	11.70	261	39606	36167	63412988
Osteonecrosis of jaw	241.57	11.70	190	39677	34933	63414222

Showing 1 to 10 of 386 entries

Previous1 2 3 4 5…39Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

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
Metastases to bone	89.16	26.03	28	1251	11942	34943710
Carbohydrate antigen 15-3 increased	63.54	26.03	9	1270	69	34955583
Metastases to lung	53.86	26.03	18	1261	9302	34946350
Metastases to central nervous system	36.35	26.03	13	1266	8192	34947460
Breast cancer metastatic	32.83	26.03	5	1274	66	34955586
Metastases to the mediastinum	32.03	26.03	6	1273	285	34955367
Malignant neoplasm progression	31.72	26.03	26	1253	88020	34867632
PIK3CA-activated mutation	31.02	26.03	5	1274	97	34955555
Hepatic lesion	28.91	26.03	9	1270	3703	34951949
Encapsulating peritoneal sclerosis	27.81	26.03	6	1273	583	34955069

Showing 1 to 10 of 10 entries

Previous1Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

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
Metastases to bone	1327.15	12.46	459	31004	23968	79688957
Malignant neoplasm progression	827.74	12.46	567	30896	135423	79577502
Metastases to liver	602.21	12.46	270	31193	28044	79684881
Metastases to lung	524.13	12.46	215	31248	17948	79694977
Breast cancer metastatic	380.72	12.46	139	31324	8463	79704462
Breast cancer recurrent	377.13	12.46	107	31356	2870	79710055
Metastases to lymph nodes	376.38	12.46	145	31318	10252	79702673
Neoplasm progression	257.16	12.46	191	31272	51491	79661434
Breast cancer	243.88	12.46	157	31306	33624	79679301
Disease progression	233.76	12.46	324	31139	184038	79528887

Showing 1 to 10 of 288 entries

Previous1 2 3 4 5…29Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	L02BA01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Anti-estrogens
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:37700	protein kinase C inhibitors
CHEBI has role	CHEBI:48422	angiogenesis antagonist
CHEBI has role	CHEBI:50646	antiosteoporotic
CHEBI has role	CHEBI:50792	estrogen receptor antagonists
CHEBI has role	CHEBI:50837	oestrogen antagonist
CHEBI has role	CHEBI:62872	quinoline oxidase inhibitors
FDA EPC	N0000175826	Estrogen Agonist/Antagonist
FDA MoA	N0000000168	Selective Estrogen Receptor Modulators

Showing 1 to 10 of 17 entries

Previous1 2Next

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

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Infiltrating duct carcinoma of breast	indication	408643008	DOID:3008
Carcinoma of female breast	indication	447782002
Prevention of Breast Carcinoma	indication
Pain of breast	off-label use	53430007
Endometrial carcinoma	off-label use	254878006	DOID:2871
Malignant tumor of ovary	off-label use	363443007	DOID:2394
Hypercalcemia	contraindication	66931009	DOID:12678
Leukopenia	contraindication	84828003	DOID:615
Bilateral cataracts	contraindication	95722004
Deep venous thrombosis	contraindication	128053003

Showing 1 to 10 of 17 entries

Previous1 2Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.61	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Estrogen receptor	Nuclear hormone receptor	P03372	ESR1_HUMAN	MODULATOR	Ki	7.51	CHEMBL	CHEMBL
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN		Ki	5.00	DRUG MATRIX
Prostaglandin G/H synthase 2	Enzyme	P35354	PGH2_HUMAN		IC50	4.46	WOMBAT-PK
Prostaglandin G/H synthase 1	Enzyme	P23219	PGH1_HUMAN		IC50	5.36	DRUG MATRIX
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN		Ki	5.15	DRUG MATRIX
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	5.37	DRUG MATRIX
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	5.34	DRUG MATRIX
Adenosine receptor A2a	GPCR	P29274	AA2AR_HUMAN		Ki	5.40	DRUG MATRIX
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.14	DRUG MATRIX
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	7.50	WOMBAT-PK

Showing 1 to 10 of 67 entries

Previous1 2 3 4 5 6 7Next

External reference:

Show entries

Search:

ID	Source
002670	NDDF
004826	NDDF
094ZI81Y45	UNII
1016	IUPHAR_LIGAND_ID
10324	RXNORM
2281	MMSL
2733526	PUBCHEM_CID
3299	INN_ID
373345002	SNOMEDCT_US
4018462	VANDF

Showing 1 to 10 of 27 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
SOLTAMOX	HUMAN PRESCRIPTION DRUG LABEL	1	51862-682	LIQUID	20 mg	ORAL	NDA	33 sections
Tamoxifen Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0144	TABLET	10 mg	ORAL	ANDA	26 sections
Tamoxifen Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0144	TABLET	10 mg	ORAL	ANDA	26 sections
Tamoxifen Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0144	TABLET	10 mg	ORAL	ANDA	26 sections
Tamoxifen Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0274	TABLET	20 mg	ORAL	ANDA	26 sections
Tamoxifen Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0274	TABLET	20 mg	ORAL	ANDA	26 sections
Tamoxifen Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0274	TABLET	20 mg	ORAL	ANDA	26 sections
Tamoxifen Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2472	TABLET	10 mg	ORAL	ANDA	25 sections
Tamoxifen Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2472	TABLET	10 mg	ORAL	ANDA	25 sections
Tamoxifen Citrate	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2473	TABLET	20 mg	ORAL	ANDA	25 sections

Showing 1 to 10 of 30 entries

Previous1 2 3Next