Lonafarnib

Farnesyltransferase Inhibitor — ALIMENTARY TRACT AND METABOLISM

Key facts

Lonafarnib is an ofp drug in the Farnesyltransferase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2020. Its mechanism of action is classified as Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 2C19 Inhibitors and Cytochrome P450 2C8 Inhibitors. DrugCentral lists 4 molecular targets, including HRAS, FNTA|FNTB and NRAS. Recorded indications include Hutchinson-Gilford syndrome and Processingdeficient progeroid laminopathies.

• Approval status: ofp (first approved 2020 by the FDA).
• Drug class: Farnesyltransferase Inhibitor.
• Mechanism of action: Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 2C19 Inhibitors; Cytochrome P450 2C8 Inhibitors.
• Molecular targets: HRAS, FNTA|FNTB, NRAS and KRAS (4 listed in DrugCentral).
• Indications: Hutchinson-Gilford syndrome and Processingdeficient progeroid laminopathies.
• ATC code: A16AX20 (Various alimentary tract and metabolism products).
• Molecular formula: C27H31Br2ClN4O2; molecular weight 638.83 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Hutchinson-Gilford syndrome
• Processingdeficient progeroid laminopathies

Contraindications (3)

• Drug induction of cytochrome p450 CYP3A enzyme
• Drug inhibition of cytochrome p450 CYP3A enzyme
• Severe hepatic impairment

Mechanism & targets

• Mechanism of action (MoA): Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 2C19 Inhibitors; Cytochrome P450 2C8 Inhibitors; Cytochrome P450 3A Inhibitors; Farnesyltransferase Inhibitors; Organic Anion Transporting Polypeptide 1B1 Inhibitors; Organic Anion Transporting Polypeptide 1B3 Inhibitors; P-Glycoprotein Inhibitors
• Established pharmacologic class: Farnesyltransferase Inhibitor

Molecular targets (4)

Target	Gene	Action	Activity
GTPase HRas	HRAS	inhibitor	IC50 8.72
Protein farnesyltransferase	FNTA|FNTB	inhibitor	IC50 8.72
GTPase NRas	NRAS	inhibitor	IC50 8.55
GTPase KRas	KRAS	inhibitor	IC50 8.28

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2022-07-18	EMA	—	EIGERBIO EUROPE LIMITED	Yes
2020-11-20	FDA	—	EIGER BIOPHARMACEUTICALS INC	Yes

ATC classification

ATC code	Therapeutic hierarchy
A16AX20	ALIMENTARY TRACT AND METABOLISM › OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS › OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS › Various alimentary tract and metabolism products

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: CYP3A4 · Actionable PGx
• EMA label: LMNA, ZMPSTE24 · Testing Required
• FDA label: LMNA, ZMPSTE24 · Testing Required
• HCSC label

Chemical structure

• Molecular formula: C₂₇H₃₁Br₂ClN₄O₂
• Molecular weight: 638.83 g/mol
• CAS number: —
• InChIKey: DHMTURDWPRKSOA-RUZDIDTESA-N
• PubChem CID: 148195

C1CN(CCC1CC(=O)N2CCC(CC2)[C@@H]3C4=C(CCC5=C3N=CC(=C5)Br)C=C(C=C4Br)Cl)C(=O)N

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Lonafarnib used for?

DrugCentral lists the following indications for Lonafarnib: Hutchinson-Gilford syndrome and Processingdeficient progeroid laminopathies.

How does Lonafarnib work?

Lonafarnib is classified as Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 2C19 Inhibitors and Cytochrome P450 2C8 Inhibitors; its molecular targets in DrugCentral include HRAS (inhibitor), FNTA|FNTB (inhibitor), NRAS (inhibitor) and KRAS (inhibitor).

When was Lonafarnib first approved?

Lonafarnib was first approved by the FDA in 2020.

What drug class does Lonafarnib belong to?

Lonafarnib is in the Farnesyltransferase Inhibitor class.

What is the chemical formula of Lonafarnib?

Lonafarnib has the molecular formula C27H31Br2ClN4O2 and a molecular weight of 638.83 g/mol.

Sources

• DrugCentral drug card 5414 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL298734 — compound record and bioactivity
• PubChem CID 148195 — chemical identifiers
• DrugBank DB06448 — drug record
• FDA UNII IOW153004F — substance identity
• DailyMed: FDA labels for Lonafarnib — current prescribing information (label search)
• UniProt P01112 (HRAS) — target protein
• UniProt P01111 (NRAS) — target protein
• UniProt P01116 (KRAS) — target protein
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.