terconazole Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
systemic antifungal agents, miconazole derivatives 2599 67915-31-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • terconazole
  • terazol
  • termayazole
  • triaconazole
  • R-42470
  • Molecular weight: 532.47
  • Formula: C26H31Cl2N5O3
  • CLOGP: 4.81
  • LIPINSKI: 1
  • HAC: 8
  • HDO: 0
  • TPSA: 64.88
  • ALOGS: -4.66
  • ROTB: 8

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
80 mg V

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 31, 1987 FDA JANSSEN PHARMS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC G01AG02 GENITO URINARY SYSTEM AND SEX HORMONES
GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS
ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS
Triazole derivatives
FDA EPC N0000175487 Azole Antifungal
FDA Chemical/Ingredient N0000008217 Azoles
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000935 Antifungal Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Candidal vulvovaginitis indication 72605008 DOID:2272

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.72 Basic
pKa2 3.04 Basic
pKa3 1.55 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
D(1A) dopamine receptor GPCR Ki 4.89 DRUG MATRIX
Alpha-2A adrenergic receptor GPCR Ki 6.43 DRUG MATRIX
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.67 DRUG MATRIX
Sodium-dependent serotonin transporter Transporter Ki 5.22 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter Ki 4.60 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 5.63 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 5.44 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 5.90 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 5.80 DRUG MATRIX
Muscarinic acetylcholine receptor M1 GPCR Ki 5.86 DRUG MATRIX
Muscarinic acetylcholine receptor M2 GPCR Ki 5.34 DRUG MATRIX
Muscarinic acetylcholine receptor M3 GPCR Ki 5.51 DRUG MATRIX
Muscarinic acetylcholine receptor M4 GPCR Ki 5.72 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 5.50 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 7.21 DRUG MATRIX
Sodium-dependent dopamine transporter Transporter Ki 5.36 DRUG MATRIX
Alpha-1D adrenergic receptor GPCR Ki 5.27 DRUG MATRIX
Acetylcholinesterase Enzyme IC50 4.67 DRUG MATRIX
Tyrosine-protein kinase Fyn Kinase IC50 4.96 DRUG MATRIX
Sodium/nucleoside cotransporter 1 Transporter Ki 5.37 DRUG MATRIX
Lanosterol 14-alpha demethylase Enzyme IC50 5.52 CHEMBL
Lanosterol 14-alpha demethylase Enzyme INHIBITOR WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 4 GPCR Ki 5.61 DRUG MATRIX
Arachidonate 15-lipoxygenase Enzyme IC50 5.61 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 5.10 DRUG MATRIX
5-hydroxytryptamine receptor 1B GPCR Ki 4.39 DRUG MATRIX
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 6.71 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR IC50 4.88 CHEMBL

External reference:

IDSource
4019521 VUID
N0000147638 NUI
C0076115 UMLSCUI
D00888 KEGG_DRUG
0KJ2VE664U UNII
4815 INN_ID
25860005 SNOMEDCT_US
4019521 VANDF
002931 NDDF
5549 MMSL
37806 RXNORM
46326 MMSL
387140007 SNOMEDCT_US
CHEMBL1306 ChEMBL_ID
DB00251 DRUGBANK_ID
CHEBI:9451 CHEBI
441383 PUBCHEM_CID
C037815 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 0168-0346 CREAM 4 mg VAGINAL ANDA 13 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 0713-0552 SUPPOSITORY 80 mg VAGINAL ANDA 13 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 21695-844 CREAM 4 mg VAGINAL ANDA 12 sections
TERCONAZOLE HUMAN PRESCRIPTION DRUG LABEL 1 21695-933 CREAM 8 mg VAGINAL NDA 12 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 45802-717 SUPPOSITORY 80 mg VAGINAL ANDA 13 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 50090-0917 CREAM 4 mg VAGINAL ANDA 13 sections
TERCONAZOLE HUMAN PRESCRIPTION DRUG LABEL 1 50090-1901 CREAM 8 mg VAGINAL NDA AUTHORIZED GENERIC 13 sections
TERCONAZOLE HUMAN PRESCRIPTION DRUG LABEL 1 50090-2341 CREAM 4 mg VAGINAL NDA AUTHORIZED GENERIC 13 sections
Terazol 3 HUMAN PRESCRIPTION DRUG LABEL 1 50458-531 SUPPOSITORY 80 mg VAGINAL NDA 13 sections
Terazol 7 HUMAN PRESCRIPTION DRUG LABEL 1 50458-535 CREAM 4 mg VAGINAL NDA 13 sections
Terazol 3 HUMAN PRESCRIPTION DRUG LABEL 1 50458-536 CREAM 8 mg VAGINAL NDA 13 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 51672-1302 CREAM 8 mg VAGINAL ANDA 13 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 51672-1304 CREAM 4 mg VAGINAL ANDA 13 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 51672-1330 SUPPOSITORY 80 mg VAGINAL ANDA 13 sections
TERCONAZOLE HUMAN PRESCRIPTION DRUG LABEL 1 52959-811 CREAM 4 mg VAGINAL NDA 12 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 53002-7240 CREAM 8 mg VAGINAL ANDA 13 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 53002-8130 CREAM 4 mg VAGINAL ANDA 13 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 54868-5183 CREAM 8 mg VAGINAL ANDA 13 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 54868-6160 CREAM 4 mg VAGINAL ANDA 13 sections
TERCONAZOLE HUMAN PRESCRIPTION DRUG LABEL 1 55045-3259 CREAM 8 mg VAGINAL NDA 12 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 68071-1626 CREAM 8 mg VAGINAL ANDA 13 sections
Terconazole HUMAN PRESCRIPTION DRUG LABEL 1 70518-1185 CREAM 8 mg VAGINAL ANDA 13 sections