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

Stem definitionDrug idCAS RN
5403 1762-34-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • abametapir
  • xeglyze
  • Ha44
Abametapir is a metalloproteinase inhibitor. Metalloproteinases have a role in physiological processes critical to egg development and survival of lice.
  • Molecular weight: 184.24
  • Formula: C12H12N2
  • CLOGP: 2.56
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 25.78
  • ALOGS: -2.27
  • ROTB: 1

  • Status: OFM

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.595 Moderate 0.70
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.767 Moderate 0.70
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 97.275 10^-6 cm/s Moderate 0.70
dh-clint Dog hepatocyte intrinsic clearance 304.789 uL/min/10^6 cells Moderate 0.70
dppb Dog plasma protein binding (% unbound) 19.560 % Moderate 0.70
fcs-ppb Fetal calf serum protein binding (% unbound) 31.420 % Moderate 0.70
herg hERG pIC50 4.446 pIC50 Moderate 0.70
hh-clint Human hepatocyte intrinsic clearance 201.837 uL/min/10^6 cells Moderate 0.70
hlm-clint Human liver microsomal intrinsic clearance 680.769 uL/min/mg protein Moderate 0.70
hppb Human plasma protein binding (% unbound) 10.750 % Moderate 0.70
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,ITK,MAP3K21,MAPK7,MARK4,PDK4,PRKDC,SIK2,SIK3,STK33,TEK 24
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.310 Moderate 0.70
mh-clint Mouse hepatocyte intrinsic clearance 887.156 Moderate 0.70
mppb Mouse plasma protein binding (% unbound) 13.090 Moderate 0.70
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.075 Moderate 0.70
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 26.010 % Moderate 0.70
rh-clint Rat hepatocyte intrinsic clearance 236.048 uL/min/10^6 cells Moderate 0.70
rh-fuinc Rat hepatocyte fraction unbound in incubation 93.170 % Moderate 0.70
rppb Rat plasma protein binding (% unbound) 13.380 % Moderate 0.70
solubility-dd Solubility at pH 7.4 in DMSO 193.197 uM Moderate 0.70

Approvals:

DateAgencyCompanyOrphan
July 24, 2020 FDA DR REDDYS LABS SA

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:

SourceCodeDescription
ATC P03AX07 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ECTOPARASITICIDES, INCL. SCABICIDES, INSECTICIDES AND REPELLENTS
ECTOPARASITICIDES, INCL. SCABICIDES
Other ectoparasiticides, incl. scabicides
CHEBI has role CHEBI:35442 antiparasitic agent

Related Drugs by ATC class:

P03AX Other ectoparasiticides, incl. scabicides 4 drugs

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

DiseaseRelationSNOMED_IDDOID
Pediculosis capitis indication 81000006 DOID:5501




🐶 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
0.74% XEGLYZE LNHC N206966 July 24, 2020 DISCN LOTION TOPICAL 7812163 Oct. 28, 2026 TOPICAL TREATMENT OF HEAD LICE INFESTATION IN PATIENTS 6 MONTHS OF AGE AND OLDER
0.74% XEGLYZE LNHC N206966 July 24, 2020 DISCN LOTION TOPICAL 10292389 Dec. 17, 2034 TOPICAL TREATMENT OF HEAD LICE INFESTATION IN PATIENTS 6 MONTHS OF AGE AND OLDER

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
C-C chemokine receptor type 5 GPCR EC50 5.64 CHEMBL
Histone deacetylase 6 Enzyme IC50 5.99 CHEMBL
C-C chemokine receptor type 1 GPCR EC50 4.80 CHEMBL
C-C chemokine receptor type 8 GPCR EC50 5.12 CHEMBL

External reference:

IDSource
D10687 KEGG_DRUG
6UO390AMFB UNII
C4519258 UMLSCUI
CHEBI:192617 CHEBI
CHEMBL2205807 ChEMBL_ID
15664 PUBCHEM_CID
DB11932 DRUGBANK_ID
9829 INN_ID
926368006 SNOMEDCT_US
926389002 SNOMEDCT_US
EI3 PDB_CHEM_ID
38681 MMSL
018457 NDDF
2475532 RXNORM
6UO390AMFB INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Xeglyze HUMAN PRESCRIPTION DRUG LABEL 1 43598-921 LOTION 0.74 g TOPICAL NDA 25 sections