All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
farnesyl transferase inhibitors	5414	193275-84-2

Description:

Molecule	Description
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:

Property	Value	Reference
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

Approvals:

Date	Agency	Company	Orphan
July 18, 2022	EMA	EIGERBIO EUROPE LIMITED
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:

Source	Code	Description
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
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:64133	farnesyltransferase inhibitors
FDA EPC	N0000193938	Farnesyltransferase Inhibitor
FDA MoA	N0000193939	Farnesyltransferase Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Protein farnesyltransferase	Enzyme	P49354 P49356	FNTA_HUMAN FNTB_HUMAN	INHIBITOR	IC50	8.72		SCIENTIFIC LITERATURE	DRUG LABEL
GTPase HRas	Cytosolic other	P01112	RASH_HUMAN	INHIBITOR	IC50	8.72		IUPHAR
GTPase KRas	Enzyme	P01116	RASK_HUMAN	INHIBITOR	IC50	8.28		IUPHAR
GTPase NRas	Enzyme	P01111	RASN_HUMAN	INHIBITOR	IC50	8.55		IUPHAR

External reference:

ID	Source
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
018565	NDDF
1137365008	SNOMEDCT_US
1137617003	SNOMEDCT_US
4041665	VANDF
2467553	RXNORM
341166	MMSL
39043	MMSL
d09683	MMSL
C115354	MESH_SUPPLEMENTAL_RECORD_UI
8191	INN_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Zokinvy	HUMAN PRESCRIPTION DRUG LABEL	1	73079-050	CAPSULE	50 mg	ORAL	NDA	29 sections
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
Zokinvy	HUMAN PRESCRIPTION DRUG LABEL	1	73079-075	CAPSULE	75 mg	ORAL	NDA	29 sections