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

Stem definitionDrug idCAS RN
farnesyl transferase inhibitors 5414 193275-84-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lonafarnib
  • zokinvy
  • SCH 66336
  • SCH66336
Lonafarnib inhibits farnesyltransferase to prevent farnesylation and subsequent accumulation of progerin and progerin-like proteins in the inner nuclear membrane.
  • Molecular weight: 638.83
  • Formula: C27H31Br2ClN4O2
  • CLOGP: 3.49
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 1
  • TPSA: 79.53
  • ALOGS: -5.89
  • ROTB: 3
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ
BA (Bioavailability) 40 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKDC,STK33,SYK,TEK,TTK 37
kinase-selectivity-class AXL,PDK1 2
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Nov. 20, 2020 FDA EIGER BIOPHARMACEUTICALS INC
July 18, 2022 EMA EIGERBIO EUROPE LIMITED

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 A16AX20 ALIMENTARY TRACT AND METABOLISM
OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS
OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS
Various alimentary tract and metabolism products
MeSH PA D004791 Enzyme Inhibitors
FDA MoA N0000182140 Cytochrome P450 2C19 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000187062 Cytochrome P450 2C8 Inhibitors
FDA MoA N0000190107 Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA N0000190108 Organic Anion Transporting Polypeptide 1B3 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
FDA EPC N0000193938 Farnesyltransferase Inhibitor
FDA MoA N0000193939 Farnesyltransferase Inhibitors
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:64133 EC 2.5.1.58 (protein farnesyltransferase) inhibitor

Related Drugs by ATC class:

A16AX Various alimentary tract and metabolism products 23 drugs
anethole trithionedoxecitinedoxribtimineeliglustatfosdenopteringivosiranglycerol phenylbutyratelumasiranmigalastatmiglustatnedosirannitisinone show all 23 →

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

DiseaseRelationSNOMED_IDDOID
Hutchinson-Gilford syndrome indication 238870004 DOID:3911
Processingdeficient progeroid laminopathies indication
Drug induction of cytochrome p450 CYP3A enzyme contraindication 423236002
Drug inhibition of cytochrome p450 CYP3A enzyme contraindication 423819001
Severe hepatic impairment contraindication 710067001




🐶 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
50MG ZOKINVY SENTYNL THERAPS INC N213969 Nov. 20, 2020 RX CAPSULE ORAL 7838531 July 26, 2029 REDUCING THE RISK OF MORTALITY IN HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS)
75MG ZOKINVY SENTYNL THERAPS INC N213969 Nov. 20, 2020 RX CAPSULE ORAL 7838531 July 26, 2029 REDUCING THE RISK OF MORTALITY IN HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
50MG ZOKINVY SENTYNL THERAPS INC N213969 Nov. 20, 2020 RX CAPSULE ORAL Nov. 20, 2027 TREATMENT OF HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS) AND PROGEROID LAMINOPATHIES
75MG ZOKINVY SENTYNL THERAPS INC N213969 Nov. 20, 2020 RX CAPSULE ORAL Nov. 20, 2027 TREATMENT OF HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS) AND PROGEROID LAMINOPATHIES

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Protein farnesyltransferase Enzyme INHIBITOR IC50 8.72 SCIENTIFIC LITERATURE DRUG LABEL
GTPase HRas Cytosolic other INHIBITOR IC50 8.72 IUPHAR
GTPase KRas Enzyme INHIBITOR IC50 8.28 IUPHAR
GTPase NRas Enzyme INHIBITOR IC50 8.55 IUPHAR

External reference:

IDSource
D04768 KEGG_DRUG
IOW153004F UNII
C1257385 UMLSCUI
CHEBI:47097 CHEBI
336 PDB_CHEM_ID
CHEMBL298734 ChEMBL_ID
148195 PUBCHEM_CID
DB06448 DRUGBANK_ID
8191 INN_ID
C115354 MESH_SUPPLEMENTAL_RECORD_UI
8024 IUPHAR_LIGAND_ID
1137365008 SNOMEDCT_US
1137617003 SNOMEDCT_US
4041665 VANDF
341166 MMSL
39043 MMSL
d09683 MMSL
018565 NDDF
2467553 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Zokinvy HUMAN PRESCRIPTION DRUG LABEL 1 42358-450 CAPSULE 50 mg ORAL NDA 28 sections
Zokinvy HUMAN PRESCRIPTION DRUG LABEL 1 42358-475 CAPSULE 75 mg ORAL NDA 28 sections
Zokinvy HUMAN PRESCRIPTION DRUG LABEL 1 73079-050 CAPSULE 50 mg ORAL NDA 30 sections
Zokinvy HUMAN PRESCRIPTION DRUG LABEL 1 73079-075 CAPSULE 75 mg ORAL NDA 30 sections