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fluoroestradiol F 18 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 5395 | 94153-53-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Fluoroestradiol F 18 binds ER and it is a radioactive diagnostic agent indicated for positron emission tomography (PET) imaging. The following binding affinity: Kd = 0.13 ± 0.02 nM, Bmax = 1901 ± 89 fmol/mg, and IC50 = 0.085 nM, was determined in an ER-positive human breast cancer cell line (MCF-7). Fluoroestradiol F 18 is indicated for characterization of estrogen receptor status of known or suspected metastatic lesions in patients with confirmed ER-positive breast cancer.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.472 | Moderate | 0.79 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.456 | Moderate | 0.79 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 59.704 | 10^-6 cm/s | Moderate | 0.79 |
| dh-clint | Dog hepatocyte intrinsic clearance | 28.774 | uL/min/10^6 cells | Moderate | 0.79 |
| dppb | Dog plasma protein binding (% unbound) | 2.330 | % | Moderate | 0.79 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 6.770 | % | Moderate | 0.79 |
| herg | hERG pIC50 | 4.670 | pIC50 | Moderate | 0.79 |
| hh-clint | Human hepatocyte intrinsic clearance | 50.350 | uL/min/10^6 cells | Moderate | 0.79 |
| hlm-clint | Human liver microsomal intrinsic clearance | 10.789 | uL/min/mg protein | Moderate | 0.79 |
| hppb | Human plasma protein binding (% unbound) | 2.260 | % | Moderate | 0.79 |
| kinase-safety-class | ACVR2B,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,PDK1,PDK2,PDK4,PIK3CA,PIK3CG,PRKDC,TGFBR1 | 15 | |||
| kinase-selectivity-class | EIF2AK3,GRK2 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.791 | Moderate | 0.79 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 146.893 | Moderate | 0.79 | |
| mppb | Mouse plasma protein binding (% unbound) | 3.140 | Moderate | 0.79 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 5.346 | Moderate | 0.79 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 6.060 | % | Moderate | 0.79 |
| rh-clint | Rat hepatocyte intrinsic clearance | 162.930 | uL/min/10^6 cells | Moderate | 0.79 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 26.190 | % | Moderate | 0.79 |
| rppb | Rat plasma protein binding (% unbound) | 3.850 | % | Moderate | 0.79 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 18.197 | uM | Moderate | 0.79 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 20, 2020 | FDA | ZIONEXA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| No adverse event | 31.27 | 26.49 | 5 | 3 | 73834 | 110515457 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | V09IX11 | VARIOUS DIAGNOSTIC RADIOPHARMACEUTICALS TUMOUR DETECTION Other diagnostic radiopharmaceuticals for tumour detection |
| FDA MoA | N0000175869 | Positron Emitting Activity |
| FDA EPC | N0000177914 | Radioactive Diagnostic Agent |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
V09IX Other diagnostic radiopharmaceuticals for tumour detection 10 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Positron emission tomography | indication | 82918005 |
🐶 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]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Estrogen receptor | Nuclear hormone receptor | BINDING AGENT | IC50 | 10.07 | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| D11829 | KEGG_DRUG |
| T32277KB09 | UNII |
| 92817-10-2 | SECONDARY_CAS_RN |
| C1831937 | UMLSCUI |
| CHEBI:757767 | CHEBI |
| CHEMBL4594261 | ChEMBL_ID |
| 10869981 | PUBCHEM_CID |
| DB15690 | DRUGBANK_ID |
| CHEMBL1627367 | ChEMBL_ID |
| 926372005 | SNOMEDCT_US |
| 926373000 | SNOMEDCT_US |
| 363734 | MMSL |
| 41114 | MMSL |
| d09952 | MMSL |
| 018375 | NDDF |
| 2372221 | RXNORM |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| CERIANNA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72874-001 | INJECTION | 100 mCi | INTRAVENOUS | NDA | 26 sections |
| CERIANNA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72874-001 | INJECTION | 100 mCi | INTRAVENOUS | NDA | 26 sections |