lonafarnib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
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: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 20, 2020 FDA EIGER BIOPHARMACEUTICALS INC

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:35610 antineoplastic agents
CHEBI has role CHEBI:64133 farnesyltransferase inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hutchinson-Gilford syndrome indication 238870004 DOID:3911
Drug induction of cytochrome p450 CYP3A enzyme contraindication 423236002
Drug inhibition of cytochrome p450 CYP3A enzyme contraindication 423819001




🐶 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 EIGER BIOPHARMS N213969 Nov. 20, 2020 RX CAPSULE ORAL 8828356 Oct. 17, 2023 REDUCING THE RISK OF MORTALITY IN HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS)
75MG ZOKINVY EIGER BIOPHARMS N213969 Nov. 20, 2020 RX CAPSULE ORAL 8828356 Oct. 17, 2023 REDUCING THE RISK OF MORTALITY IN HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS)
50MG ZOKINVY EIGER BIOPHARMS N213969 Nov. 20, 2020 RX CAPSULE ORAL 7838531 July 26, 2024 REDUCING THE RISK OF MORTALITY IN HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS)
75MG ZOKINVY EIGER BIOPHARMS N213969 Nov. 20, 2020 RX CAPSULE ORAL 7838531 July 26, 2024 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 EIGER BIOPHARMS N213969 Nov. 20, 2020 RX CAPSULE ORAL Nov. 20, 2025 NEW CHEMICAL ENTITY
75MG ZOKINVY EIGER BIOPHARMS N213969 Nov. 20, 2020 RX CAPSULE ORAL Nov. 20, 2025 NEW CHEMICAL ENTITY
50MG ZOKINVY EIGER BIOPHARMS N213969 Nov. 20, 2020 RX CAPSULE ORAL Nov. 20, 2027 TREATMENT OF HUTCHINSON-GILFORD PROGERIA SYNDROME (HGPS) AND PROGEROID LAMINOPATHIES
75MG ZOKINVY EIGER BIOPHARMS 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
8024 IUPHAR_LIGAND_ID
2467553 RXNORM
341166 MMSL
39043 MMSL
d09683 MMSL
1137365008 SNOMEDCT_US
1137617003 SNOMEDCT_US
018565 NDDF
C115354 MESH_SUPPLEMENTAL_RECORD_UI
8191 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Zokinvy HUMAN PRESCRIPTION DRUG LABEL 1 73079-050 CAPSULE 50 mg ORAL NDA 29 sections
Zokinvy HUMAN PRESCRIPTION DRUG LABEL 1 73079-075 CAPSULE 75 mg ORAL NDA 29 sections