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

Stem definition	Drug id	CAS RN
androgens/anabolic steroids	3356	58-18-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: methyltestosterone 17-Methyltestosteron androsan androsten	A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL). Molecular weight: 302.46 Formula: C20H30O2 CLOGP: 3.93 LIPINSKI: 0 HAC: 2 HDO: 1 TPSA: 37.30 ALOGS: -4.34 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

methyltestosterone
17-Methyltestosteron
androsan
androsten

A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL).

Molecular weight: 302.46
Formula: C20H30O2
CLOGP: 3.93
LIPINSKI: 0
HAC: 2
HDO: 1
TPSA: 37.30
ALOGS: -4.34
ROTB: 0

Status: OFP

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

Drug dosage:

Dose	Unit	Route
25	mg	O

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	50 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	0.03 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
Dec. 3, 1973	FDA	VALEANT PHARM INTL

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	G03BA02	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ANDROGENS 3-oxoandrosten (4) derivatives
ATC	G03EA01	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ANDROGENS AND FEMALE SEX HORMONES IN COMBINATION Androgens and estrogens
ATC	G03EK01	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ANDROGENS AND FEMALE SEX HORMONES IN COMBINATION Androgens and female sex hormones in combination with other drugs
FDA CS	M0001109	Androstanes
FDA MoA	N0000000146	Androgen Receptor Agonists
MeSH PA	D045930	Anabolic Agents
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D018931	Antineoplastic Agents, Hormonal
MeSH PA	D006728	Hormones
FDA EPC	N0000175824	Androgen
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:50113	androgene

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

Disease	Relation	SNOMED_ID	DOID
Deficiency of testosterone biosynthesis	indication	38825009
Inhibition of lactation procedure	indication	43141007
Male hypogonadism	indication	48723006
Menopausal flushing	indication	198436008
Delayed puberty	indication	400003000
Hormone receptor positive malignant neoplasm of breast	indication	417181009
Primary Hypogonadism due to Orchitis	indication
Primary Hypogonadism due to Bilateral Torsion	indication
LHRH Deficiency	indication
Bilateral Anorchia	indication
Undescended testicle	off-label use	204878001	DOID:11383
Noonan's syndrome	off-label use	205824006	DOID:3490
Klinefelter's syndrome, XXY	off-label use	405769009
Hyperlipoproteinemia	contraindication	3744001	DOID:1168
Hypocalcemia	contraindication	5291005
Hypercholesterolemia	contraindication	13644009
Myocardial infarction	contraindication	22298006	DOID:5844
Chloasma	contraindication	36209000
Migraine	contraindication	37796009	DOID:6364
Hypertensive disorder	contraindication	38341003	DOID:10763
Disorder of gallbladder	contraindication	39621005	DOID:0060262
Hypothyroidism	contraindication	40930008	DOID:1459
Body fluid retention	contraindication	43498006
Thrombosis of retinal vein	contraindication	46085004
Humoral hypercalcemia of malignancy	contraindication	47709007
Dementia	contraindication	52448006
Hepatic porphyria	contraindication	55056006	DOID:3133
Systemic lupus erythematosus	contraindication	55464009	DOID:9074
Thrombophlebitis	contraindication	64156001	DOID:3875
Intermenstrual bleeding - irregular	contraindication	64996003
Hypercalcemia	contraindication	66931009	DOID:12678
Diabetes mellitus	contraindication	73211009	DOID:9351
Heart failure	contraindication	84114007	DOID:6000
Epilepsy	contraindication	84757009	DOID:1826
Breast lump	contraindication	89164003
Kidney disease	contraindication	90708001	DOID:557
Uterine leiomyoma	contraindication	95315005	DOID:13223
Neoplasm of liver	contraindication	126851005	DOID:3571
Neoplasm of prostate	contraindication	126906006	DOID:10283
Deep venous thrombosis	contraindication	128053003
Endometriosis	contraindication	129103003
Mammography abnormal	contraindication	168750009
Asthma	contraindication	195967001	DOID:2841
Cerebrovascular accident	contraindication	230690007
Pulmonary thromboembolism	contraindication	233935004
Thrombophilia	contraindication	234467004	DOID:2452
Disease of liver	contraindication	235856003	DOID:409
Endometrial carcinoma	contraindication	254878006	DOID:2871
Benign prostatic hyperplasia	contraindication	266569009
Edema	contraindication	267038008
Chorea	contraindication	271700006
Pregnancy, function	contraindication	289908002
Hypertriglyceridemia	contraindication	302870006
Functional visual loss	contraindication	313165001
Malignant tumor of ovary	contraindication	363443007	DOID:2394
Thromboembolic disorder	contraindication	371039008
Cardiovascular event risk	contraindication	395112001
Breastfeeding (mother)	contraindication	413712001
Disorder of coronary artery	contraindication	414024009
Obesity	contraindication	414916001	DOID:9970
Estrogen receptor positive tumor	contraindication	416053008
Family history of malignant neoplasm of breast	contraindication	429740004
Hypertensive urgency	contraindication	443482000
Carcinoma of female breast	contraindication	447782002
Smokes tobacco daily	contraindication	449868002
Breast Carcinoma in Males	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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])	Bioact source	MoA source
Androgen receptor	Nuclear hormone receptor	P10275	ANDR_HUMAN	AGONIST	EC50	9.66	IUPHAR	CHEMBL
Glucocorticoid receptor	Nuclear hormone receptor	P04150	GCR_HUMAN		Ki	6.08	DRUG MATRIX
Sex hormone-binding globulin	Secreted	P04278	SHBG_HUMAN		Kd	8.43	CHEMBL
Androgen receptor	Transcription factor		ANDR_RAT		IC50	7.80	CHEMBL
Progesterone receptor	Transcription factor		Q690N0_BOVIN		Ki	7.48	DRUG MATRIX

External reference:

ID	Source
4017433	VUID
N0000145821	NUI
D00408	KEGG_DRUG
4017433	VANDF
C0025826	UMLSCUI
CHEBI:27436	CHEBI
CHEMBL1395	ChEMBL_ID
D008777	MESH_DESCRIPTOR_UI
DB06710	DRUGBANK_ID
6945	IUPHAR_LIGAND_ID
399	INN_ID
V9EFU16ZIF	UNII
6010	PUBCHEM_CID
6904	RXNORM
1048	MMSL
5096	MMSL
d00295	MMSL
001249	NDDF
126161000	SNOMEDCT_US
42348003	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
MethylTESTOSTERone	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1408	CAPSULE	10 mg	ORAL	ANDA	25 sections
METHITEST	HUMAN PRESCRIPTION DRUG LABEL	1	0115-7037	TABLET	10 mg	ORAL	ANDA	12 sections
COVARYX	HUMAN PRESCRIPTION DRUG LABEL	2	11528-010	TABLET, COATED	2.50 mg	ORAL	unapproved drug other	14 sections
COVARYXHS	HUMAN PRESCRIPTION DRUG LABEL	2	11528-020	TABLET, COATED	1.25 mg	ORAL	unapproved drug other	14 sections
Esterified Estrogen and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	13925-180	TABLET	1.25 mg	ORAL	unapproved drug other	22 sections
Esterified Estrogen and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	13925-181	TABLET	2.50 mg	ORAL	unapproved drug other	22 sections
EEMT	HUMAN PRESCRIPTION DRUG LABEL	2	15310-010	TABLET, COATED	2.50 mg	ORAL	unapproved drug other	13 sections
EEMTHS	HUMAN PRESCRIPTION DRUG LABEL	2	15310-020	TABLET, COATED	1.25 mg	ORAL	unapproved drug other	13 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	50220-001	TABLET, FILM COATED	1.25 mg	ORAL	Unapproved drug other	13 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	50220-002	TABLET, FILM COATED	2.50 mg	ORAL	Unapproved drug other	13 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	51293-639	TABLET	1.25 mg	ORAL	UNAPPROVED DRUG OTHER	14 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	51293-639	TABLET	1.25 mg	ORAL	UNAPPROVED DRUG OTHER	14 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	51293-640	TABLET	2.50 mg	ORAL	UNAPPROVED DRUG OTHER	14 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	51293-640	TABLET	2.50 mg	ORAL	UNAPPROVED DRUG OTHER	14 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	53746-077	TABLET	1.25 mg	ORAL	unapproved drug other	14 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	53746-077	TABLET	1.25 mg	ORAL	unapproved drug other	14 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	53746-078	TABLET	2.50 mg	ORAL	unapproved drug other	14 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	53746-078	TABLET	2.50 mg	ORAL	unapproved drug other	14 sections
ESTERIFIED ESTROGENS AND METHYLTESTOSTERONE	HUMAN PRESCRIPTION DRUG LABEL	2	58657-405	TABLET	2.50 mg	ORAL	unapproved drug other	18 sections
ESTERIFIED ESTROGENS AND METHYLTESTOSTERONE	HUMAN PRESCRIPTION DRUG LABEL	2	58657-405	TABLET	2.50 mg	ORAL	unapproved drug other	18 sections
ESTERIFIED ESTROGENS AND METHYLTESTOSTERONE	HUMAN PRESCRIPTION DRUG LABEL	2	58657-406	TABLET	1.25 mg	ORAL	unapproved drug other	18 sections
ESTERIFIED ESTROGENS AND METHYLTESTOSTERONE	HUMAN PRESCRIPTION DRUG LABEL	2	58657-406	TABLET	1.25 mg	ORAL	unapproved drug other	18 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	62559-149	TABLET	2.50 mg	ORAL	Unapproved drug other	27 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	62559-150	TABLET	1.25 mg	ORAL	Unapproved drug other	27 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	63629-1979	TABLET	2.50 mg	ORAL	Unapproved drug other	27 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	63629-1979	TABLET	2.50 mg	ORAL	Unapproved drug other	27 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	63629-1980	TABLET	1.25 mg	ORAL	Unapproved drug other	27 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	63629-1980	TABLET	1.25 mg	ORAL	Unapproved drug other	27 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	63629-9177	TABLET	2.50 mg	ORAL	UNAPPROVED DRUG OTHER	14 sections
Esterified Estrogens and Methyltestosterone	HUMAN PRESCRIPTION DRUG LABEL	2	63629-9177	TABLET	2.50 mg	ORAL	UNAPPROVED DRUG OTHER	14 sections