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

Stem definitionDrug idCAS RN
androgens/anabolic steroids 4609 315-37-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • testosterone enanthate
  • testosterone heptylate
  • testosterone oenanthate
  • testosterone enantate
  • Molecular weight: 400.60
  • Formula: C26H40O3
  • CLOGP: 7
  • LIPINSKI: 1
  • HAC: 3
  • HDO: 0
  • TPSA: 43.37
  • ALOGS: -5.94
  • ROTB: 7
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 4 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.766 High 0.80
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.798 High 0.80
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 22.542 10^-6 cm/s High 0.80
dh-clint Dog hepatocyte intrinsic clearance 145.881 uL/min/10^6 cells High 0.80
dppb Dog plasma protein binding (% unbound) 0.270 % High 0.80
fcs-ppb Fetal calf serum protein binding (% unbound) 0.420 % High 0.80
herg hERG pIC50 4.973 pIC50 High 0.80
hh-clint Human hepatocyte intrinsic clearance 129.718 uL/min/10^6 cells High 0.80
hlm-clint Human liver microsomal intrinsic clearance 128.529 uL/min/mg protein High 0.80
hppb Human plasma protein binding (% unbound) 0.290 % High 0.80
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP2K6,MAP3K7,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,STK33,SYK,TEK,TGFBR1 29
kinase-selectivity-class EIF2AK3,GRK2 2
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.082 High 0.80
mh-clint Mouse hepatocyte intrinsic clearance 311.172 High 0.80
mppb Mouse plasma protein binding (% unbound) 0.440 High 0.80
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.143 High 0.80
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 1.110 % High 0.80
rh-clint Rat hepatocyte intrinsic clearance 291.743 uL/min/10^6 cells High 0.80
rh-fuinc Rat hepatocyte fraction unbound in incubation 3.370 % High 0.80
rppb Rat plasma protein binding (% unbound) 0.340 % High 0.80
solubility-dd Solubility at pH 7.4 in DMSO 1.208 uM High 0.80

Approvals:

DateAgencyCompanyOrphan
Dec. 24, 1953 FDA ENDO PHARMS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Device dislocation 150.99 32.66 38 1422 7793 42612082
Device malfunction 143.00 32.66 40 1420 12287 42607588
Product dose omission issue 117.57 32.66 70 1390 154295 42465580
Faecal calprotectin increased 44.91 32.66 12 1448 3082 42616793
Pharyngitis streptococcal 42.16 32.66 12 1448 3888 42615987
Drug ineffective 41.00 32.66 75 1385 630122 41989753
Product use in unapproved indication 38.67 32.66 39 1421 184417 42435458
Accidental exposure to product 34.88 32.66 16 1444 20377 42599498
Migraine 34.48 32.66 17 1443 25397 42594478
Hot flush 33.48 32.66 16 1444 22335 42597540
Focal segmental glomerulosclerosis 32.84 32.66 9 1451 2539 42617336

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Device malfunction 164.18 32.84 46 2062 25512 110561679
Device dislocation 154.38 32.84 46 2062 31658 110555533
Product dose omission issue 102.64 32.84 68 2040 321714 110265477
Ear congestion 55.05 32.84 13 2095 3652 110583539
Faecal calprotectin increased 42.64 32.84 12 2096 6707 110580484
Migraine 39.92 32.84 30 2078 171622 110415569
Thyroid disorder 39.12 32.84 14 2094 16955 110570236
Secondary hypogonadism 35.40 32.84 7 2101 856 110586335
Pharyngitis streptococcal 34.59 32.84 12 2096 13265 110573926
Focal segmental glomerulosclerosis 33.72 32.84 9 2099 4136 110583055
Bronchitis 33.32 32.84 26 2082 157006 110430185

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
FDA CS M0001109 Androstanes
FDA MoA N0000000146 Androgen Receptor Agonists
MeSH PA D000728 Androgens
MeSH PA D006728 Hormones
FDA EPC N0000175824 Androgen
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:50113 androgen
CHEBI has role CHEBI:74518 anti-obesity agent
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:35705 immunosuppressive agent
CHEBI has role CHEBI:50779 appetite enhancer
CHEBI has role CHEBI:50864 insulin-sensitizing drug
CHEBI has role CHEBI:75771 mouse metabolite
CHEBI has role CHEBI:77746 human metabolite
CHEBI has role CHEBI:83056 <em>Daphnia magna</em> metabolite
CHEBI has role CHEBI:176497 geroprotector
CHEBI has role CHEBI:231911 renoprotective agent

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

DiseaseRelationSNOMED_IDDOID
Deficiency of testosterone biosynthesis indication 38825009
Male hypogonadism indication 48723006
Menopausal flushing indication 198436008
Undescended testicle indication 204878001 DOID:11383
Delayed puberty indication 400003000
Klinefelter's syndrome, XXY indication 405769009
Hormone receptor positive malignant neoplasm of breast indication 417181009
LHRH Deficiency indication
Hyperlipoproteinemia contraindication 3744001 DOID:1168
Gynecomastia contraindication 4754008 DOID:12698
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
Chronic heart failure contraindication 48447003
Dementia contraindication 52448006
Hepatic porphyria contraindication 55056006 DOID:3133
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Heart disease contraindication 56265001 DOID:114
Thrombophlebitis contraindication 64156001 DOID:3875
Intermenstrual bleeding - irregular contraindication 64996003
Diabetes mellitus contraindication 73211009 DOID:9351
Sleep apnea contraindication 73430006 DOID:0050847
Epilepsy contraindication 84757009 DOID:1826
Breast lump contraindication 89164003
Kidney disease contraindication 90708001 DOID:557
Uterine leiomyoma contraindication 95315005 DOID:13223
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
Chronic lung disease contraindication 413839001
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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG/0.5ML (100MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 10821072 June 4, 2033 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
100MG/0.5ML (100MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 11844804 June 4, 2033 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
50MG/0.5ML (50MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 10821072 June 4, 2033 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
50MG/0.5ML (50MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 11844804 June 4, 2033 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
75MG/0.5ML (75MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 10821072 June 4, 2033 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
75MG/0.5ML (75MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 11844804 June 4, 2033 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
100MG/0.5ML (100MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 11160751 Oct. 7, 2034 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
50MG/0.5ML (50MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 11160751 Oct. 7, 2034 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
75MG/0.5ML (75MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 11160751 Oct. 7, 2034 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
100MG/0.5ML (100MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 10238662 Feb. 19, 2035 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
100MG/0.5ML (100MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 10912782 Feb. 19, 2035 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
50MG/0.5ML (50MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 10238662 Feb. 19, 2035 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
50MG/0.5ML (50MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 10912782 Feb. 19, 2035 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
75MG/0.5ML (75MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 10238662 Feb. 19, 2035 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
75MG/0.5ML (75MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 10912782 Feb. 19, 2035 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
100MG/0.5ML (100MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 9950125 Sept. 4, 2036 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
50MG/0.5ML (50MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 9950125 Sept. 4, 2036 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY
75MG/0.5ML (75MG/0.5ML) XYOSTED (AUTOINJECTOR) ANTARES PHARMA INC N209863 Sept. 28, 2018 RX SOLUTION SUBCUTANEOUS 9950125 Sept. 4, 2036 METHOD OF ADMINISTERING TESTOSTERONE ENANTHATE SUBCUTANEOUSLY

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Androgen receptor Nuclear hormone receptor AGONIST CHEMBL CHEMBL

External reference:

IDSource
D00958 KEGG_DRUG
4017482 VUID
N0000179264 NUI
4017482 VANDF
4017484 VANDF
TES PDB_CHEM_ID
CHEMBL1200335 ChEMBL_ID
C004648 MESH_SUPPLEMENTAL_RECORD_UI
DB13944 DRUGBANK_ID
DB00624 DRUGBANK_ID
10379 RXNORM
2966 MMSL
3019 MMSL
399960 MMSL
5552 MMSL
5554 MMSL
d00558 MMSL
001245 NDDF
001247 NDDF
109033004 SNOMEDCT_US
116071004 SNOMEDCT_US
43688007 SNOMEDCT_US
C0076189 UMLSCUI
C0039601 UMLSCUI
CHEBI:6980 CHEBI
9416 PUBCHEM_CID
6013 PUBCHEM_CID
1900 INN_ID
D013739 MESH_DESCRIPTOR_UI
7Z6522T8N9 UNII
CHEBI:17347 CHEBI
7Z6522T8N9 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TESTOSTERONE ENANTHATE HUMAN PRESCRIPTION DRUG LABEL 1 0143-9750 INJECTION, SOLUTION 200 mg INTRAMUSCULAR ANDA 28 sections
XYOSTED HUMAN PRESCRIPTION DRUG LABEL 1 54436-200 INJECTION 100 mg SUBCUTANEOUS NDA 34 sections
XYOSTED HUMAN PRESCRIPTION DRUG LABEL 1 54436-250 INJECTION 50 mg SUBCUTANEOUS NDA 34 sections
XYOSTED HUMAN PRESCRIPTION DRUG LABEL 1 54436-275 INJECTION 75 mg SUBCUTANEOUS NDA 34 sections
TESTOSTERONE ENANTHATE Human Prescription Drug Label 1 55150-336 INJECTION, SOLUTION 200 mg INTRAMUSCULAR ANDA 26 sections