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bazedoxifene 🐶 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 | 4334 | 198481-32-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
an estrogen agonist/antagonist that acts as an agonist in some estrogen-sensitive tissues and an antagonist in others
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 20 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 15.40 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 6.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.02 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 30 hours | Lombardo F, Berellini G, Obach RS |
| BA (Bioavailability) | 6 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.143 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 18.535 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 2.415 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 62.951 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.640 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 3.500 | % | High | 1 |
| herg | hERG pIC50 | 5.423 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 15.885 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 35.156 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.550 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BRAF,BTK,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK2,CDK4,CDK5,CDK9,CHEK1,CLK4,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FLT3,GAK,GRK2,GSK3B,INSR,IRAK1,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAP4K5,MAPK10,MAPK7,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PRKCD,PRKCZ,PRKDC,SGK1,SIK2,SIK3,SRC,STK10,STK33,SYK,TEK,TGFBR1,TNIK,TTK,ULK1,ULK2,ZAP70 | 94 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CDK4,MAP2K6,SIK2,STK33,TEK | 8 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 19.907 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 28.054 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 91.833 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.570 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 44.055 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.550 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.068 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 65.615 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 2.330 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.760 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 6.966 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 3, 2013 | FDA | WYETH PHARMS PFIZER |
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 | G03CC07 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ESTROGENS Estrogens, combinations with other drugs |
| ATC | G03XC02 | 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 |
| FDA MoA | N0000000168 | Selective Estrogen Receptor Modulators |
| MeSH PA | D006727 | Hormone Antagonists |
| MeSH PA | D020845 | Selective Estrogen Receptor Modulators |
| MeSH PA | D020847 | Estrogen Receptor Modulators |
| MeSH PA | D050071 | Bone Density Conservation Agents |
| FDA EPC | N0000175826 | Estrogen Agonist/Antagonist |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:50646 | bone density conservation agent |
| CHEBI has role | CHEBI:35705 | immunosuppressive agent |
Related Drugs by ATC class:
G03CC Estrogens, combinations with other drugs 6 drugs
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 | |
| Menopausal flushing | indication | 198436008 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.36 | acidic |
| pKa2 | 11.25 | acidic |
| pKa3 | 8.67 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 20MG BASE;0.45MG | DUAVEE | WYETH PHARMS | N022247 | Oct. 3, 2013 | RX | TABLET | ORAL | 7683051 | March 10, 2027 | PREVENTION OF POSTMENOPAUSAL OSTEOPOROSIS |
| EQ 20MG BASE;0.45MG | DUAVEE | WYETH PHARMS | N022247 | Oct. 3, 2013 | RX | TABLET | ORAL | 7683051 | March 10, 2027 | TREATMENT OF MODERATE TO SEVERE VASOMOTOR SYMPTOMS ASSOCIATED WITH MENOPAUSE |
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 | MODULATOR | IC50 | 9.22 | CHEMBL | CHEMBL | |||
| Estrogen receptor beta | Nuclear hormone receptor | MODULATOR | IC50 | 8.42 | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D03062 | KEGG_DRUG |
| 198481-33-3 | SECONDARY_CAS_RN |
| 4033041 | VANDF |
| C2346970 | UMLSCUI |
| CHEBI:135947 | CHEBI |
| 29S | PDB_CHEM_ID |
| CHEMBL46740 | ChEMBL_ID |
| CHEMBL2106615 | ChEMBL_ID |
| DB06401 | DRUGBANK_ID |
| C447119 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7355 | IUPHAR_LIGAND_ID |
| 8168 | INN_ID |
| Q16TT9C5BK | UNII |
| 154257 | PUBCHEM_CID |
| 1441386 | RXNORM |
| 27928 | MMSL |
| d07783 | MMSL |
| 015232 | NDDF |
| 015233 | NDDF |
| 440186005 | SNOMEDCT_US |
| 702401005 | SNOMEDCT_US |
| 895426008 | SNOMEDCT_US |
| Q16TT9C5BK | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Duavee | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0008-1123 | TABLET, FILM COATED | 20 mg | ORAL | NDA | 34 sections |
| Duavee | HUMAN PRESCRIPTION DRUG LABEL | 2 | 63539-122 | TABLET, FILM COATED | 20 mg | ORAL | NDA | 33 sections |