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lasofoxifene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antiestrogens or estrogen receptor modulators, clomifene and tamoxifen derivatives | 4308 | 180916-16-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a SERM whose biological actions are largely mediated through binding to estrogen receptors, this binding results in the activation of some estrogenic pathways and a blockade of others, Lasofoxifene produces tissue and cell-specific effects in estrogen-responsive tissues
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 60 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.831 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 6.266 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 6.012 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 30.130 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.730 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 4.990 | % | High | 1 |
| herg | hERG pIC50 | 5.450 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 4.365 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 8.395 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.980 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,INSR,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK | 52 | |||
| kinase-selectivity-class | CDK4,GRK2,PDK4 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 4.074 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 57.943 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.800 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 9.311 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 2.710 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 64.269 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 2.170 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 1.230 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 31.623 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 24, 2009 | EMA | Dr. Friedrich Eberth Arzneimittel GmbH |
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 | G03XC03 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM OTHER SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM Selective estrogen receptor modulators |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:50646 | bone density conservation agent |
| CHEBI has role | CHEBI:50792 | estrogen receptor antagonist |
| CHEBI has role | CHEBI:63951 | estrogen receptor agonist |
| CHEBI has role | CHEBI:77307 | cardioprotective agent |
Related Drugs by ATC class:
G03XC Selective estrogen receptor modulators 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Postmenopausal osteoporosis | indication | 102447009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.5 | acidic |
| pKa2 | 8.9 | Basic |
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 | AGONIST | IC50 | 8.89 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Estrogen receptor beta | Nuclear hormone receptor | AGONIST | IC50 | 8.74 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Estrogen receptor | Transcription factor | IC50 | 7.95 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D04672 | KEGG_DRUG |
| 190791-29-8 | SECONDARY_CAS_RN |
| C0963839 | UMLSCUI |
| CHEBI:135938 | CHEBI |
| C3D | PDB_CHEM_ID |
| CHEMBL328190 | ChEMBL_ID |
| CHEMBL6067998 | ChEMBL_ID |
| DB06202 | DRUGBANK_ID |
| C111332 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7542 | IUPHAR_LIGAND_ID |
| 7875 | INN_ID |
| 337G83N988 | UNII |
| 216416 | PUBCHEM_CID |
| 337G83N988 | INXIGHT DRUGS |
Pharmaceutical products:
None