Boceprevir

Hepatitis C Virus NS3/4A Protease Inhibitor — ANTIINFECTIVES FOR SYSTEMIC USE

Key facts

Boceprevir is an ofm drug in the Hepatitis C Virus NS3/4A Protease Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2011. Its mechanism of action is classified as Cytochrome P450 3A4 Inhibitors, Cytochrome P450 3A5 Inhibitors and HCV NS3/4A Protease Inhibitors. DrugCentral lists 15 molecular targets, including NS3|NS4A, Nonstructural protein NS3-4A and NS3 protease. Recorded indications include Chronic hepatitis C.

• Approval status: ofm (first approved 2011 by the FDA).
• Drug class: Hepatitis C Virus NS3/4A Protease Inhibitor.
• Mechanism of action: Cytochrome P450 3A4 Inhibitors; Cytochrome P450 3A5 Inhibitors; HCV NS3/4A Protease Inhibitors.
• Molecular targets: NS3|NS4A, Nonstructural protein NS3-4A, NS3 protease and NS3 (15 listed in DrugCentral).
• Indications: Chronic hepatitis C.
• ATC code: J05AP03 (Antivirals for treatment of HCV infections).
• Molecular formula: C27H45N5O5; molecular weight 519.69 g/mol.

Indications & contraindications

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

Indications (1)

• Chronic hepatitis C

Contraindications (2)

• Anemia
• Neutropenic disorder

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 3A4 Inhibitors; Cytochrome P450 3A5 Inhibitors; HCV NS3/4A Protease Inhibitors
• Established pharmacologic class: Hepatitis C Virus NS3/4A Protease Inhibitor

Molecular targets (15)

Target	Gene	Action	Activity
Hepatitis C virus serine protease, NS3/NS4A	NS3|NS4A	inhibitor	Ki 8.96
Nonstructural protein NS3-4A	—	unknown	Ki 7.85
NS3 protease	—	unknown	Ki 7.85
Genome polyprotein	NS3	unknown	Ki 7.85
Chymase	CMA1	unknown	IC50 7.49
Cathepsin K	CTSK	unknown	IC50 7.40
Cathepsin L2	CTSV	unknown	IC50 7.12
Cathepsin S	CTSS	unknown	IC50 6.92
Cathepsin L1	CTSL	unknown	IC50 6.12
Replicase polyprotein 1a	—	inhibitor	IC50 6.02
Lysosomal protective protein	CTSA	inhibitor	IC50 6.00
Cathepsin F	CTSF	unknown	IC50 5.96
Replicase polyprotein 1ab	REP	unknown	IC50 5.38
Cathepsin B	CTSB	unknown	IC50 5.21
Neutrophil elastase	ELANE	unknown	IC50 4.77

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2011-05-13	FDA	—	MERCK SHARP DOHME

ATC classification

ATC code	Therapeutic hierarchy
J05AP03	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Antivirals for treatment of HCV infections

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: IFNL3 · No Clinical PGx
• FDA label: IFNL3 · No Clinical PGx
• HCSC label: IFNL3 · No Clinical PGx

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Anaemia	604.1
Neutropenia	199.6
Dysgeusia	139.3
Thrombocytopenia	109.1
Ascites	85.1
Leukopenia	79.4
Hepatic failure	58.6
Hepatic cirrhosis	56.0
Rash	55.3
Viral load increased	54.9
Pancytopenia	47.2
Hepatocellular carcinoma	47.0

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Boceprevir is on its molecule page.

• Molecular formula: C₂₇H₄₅N₅O₅
• Molecular weight: 519.69 g/mol
• CAS number: 394730-60-0
• InChIKey: LHHCSNFAOIFYRV-DOVBMPENSA-N
• PubChem CID: 10324367

CC(C)(C)NC(=O)N[C@H](C(=O)N1C[C@H]2[C@@H]([C@H]1C(=O)NC(CC1CCC1)C(=O)C(N)=O)C2(C)C)C(C)(C)C

Frequently asked questions

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

What is Boceprevir used for?

DrugCentral lists the following indications for Boceprevir: Chronic hepatitis C.

How does Boceprevir work?

Boceprevir is classified as Cytochrome P450 3A4 Inhibitors, Cytochrome P450 3A5 Inhibitors and HCV NS3/4A Protease Inhibitors; its molecular targets in DrugCentral include NS3|NS4A (inhibitor), Nonstructural protein NS3-4A, NS3 protease and NS3.

When was Boceprevir first approved?

Boceprevir was first approved by the FDA in 2011.

What drug class does Boceprevir belong to?

Boceprevir is in the Hepatitis C Virus NS3/4A Protease Inhibitor class.

What is the chemical formula of Boceprevir?

Boceprevir has the molecular formula C27H45N5O5 and a molecular weight of 519.69 g/mol.

Sources

• DrugCentral drug card 4172 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL218394 — compound record and bioactivity
• PubChem CID 10324367 — chemical identifiers
• DrugBank DB08873 — drug record
• FDA UNII 89BT58KELH — substance identity
• DailyMed: FDA labels for Boceprevir — current prescribing information (label search)
• UniProt P23946 (CMA1) — target protein
• UniProt P43235 (CTSK) — target protein
• UniProt O60911 (CTSV) — target protein
• UniProt P25774 (CTSS) — target protein
• UniProt P07711 (CTSL) — target protein
• UniProt P10619 (CTSA) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

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