Telaprevir

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

Key facts

Telaprevir 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 3A Inhibitors, HCV NS3/4A Protease Inhibitors and Organic Anion Transporting Polypeptide 1B1 Inhibitors. DrugCentral lists 15 molecular targets, including NS3 protease, CMA1 and CELA1. 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 3A Inhibitors; HCV NS3/4A Protease Inhibitors; Organic Anion Transporting Polypeptide 1B1 Inhibitors.
• Molecular targets: NS3 protease, CMA1, CELA1 and NS3 (15 listed in DrugCentral).
• Indications: Chronic hepatitis C.
• ATC code: J05AP02 (Antivirals for treatment of HCV infections).
• Molecular formula: C36H53N7O6; molecular weight 679.86 g/mol.

Indications & contraindications

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

Indications (1)

• Chronic hepatitis C

Contraindications (1)

• Anemia

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 3A Inhibitors; HCV NS3/4A Protease Inhibitors; Organic Anion Transporting Polypeptide 1B1 Inhibitors; Organic Anion Transporting Polypeptide 2B1 Inhibitors; P-Glycoprotein Inhibitors
• Established pharmacologic class: Hepatitis C Virus NS3/4A Protease Inhibitor

Molecular targets (15)

Target	Gene	Action	Activity
NS3 protease	—	unknown	Ki 8.41
Chymase	CMA1	unknown	IC50 7.59
Chymotrypsin-like elastase family member 1	CELA1	unknown	IC50 7.52
NS3 protease	NS3	unknown	Ki 7.09
Lysosomal protective protein	CTSA	inhibitor	IC50 7.00
NS3 protease	—	unknown	IC50 6.89
Cathepsin B	CTSB	unknown	IC50 6.68
Cathepsin S	CTSS	unknown	IC50 6.52
Cathepsin K	CTSK	unknown	IC50 6.20
Neutrophil elastase	ELANE	unknown	IC50 6.17
Cathepsin L2	CTSV	unknown	IC50 5.87
Cathepsin L1	CTSL	unknown	IC50 5.46
Plasminogen	PLG	unknown	IC50 5.06
Replicase polyprotein 1ab	REP	unknown	IC50 4.94
Hepatitis C virus serine protease, NS3/NS4A	NS3|NS4A	inhibitor	—

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2011-09-19	EMA	—	Janssen-Cilag International N.V.
2011-05-23	FDA	—	VERTEX PHARMS

ATC classification

ATC code	Therapeutic hierarchy
J05AP02	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 · Informative PGx
• FDA label: IFNL3 · Informative 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	1050.7
Rash	425.1
Thrombocytopenia	326.5
Anal pruritus	210.4
Pancytopenia	200.9
Neutropenia	185.6
Leukopenia	144.0
Pruritus	130.6
Anorectal discomfort	117.1
Hepatic failure	109.3
Drug reaction with eosinophilia and systemic symptoms	107.7
Influenza like illness	96.6

Chemical structure

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

• Molecular formula: C₃₆H₅₃N₇O₆
• Molecular weight: 679.86 g/mol
• CAS number: 402957-28-2
• InChIKey: BBAWEDCPNXPBQM-GDEBMMAJSA-N
• PubChem CID: 3010818

CCC[C@H](NC(=O)[C@@H]1[C@H]2CCC[C@H]2CN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)C1=CN=CC=N1)C1CCCCC1)C(C)(C)C)C(=O)C(=O)NC1CC1

Frequently asked questions

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

What is Telaprevir used for?

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

How does Telaprevir work?

Telaprevir is classified as Cytochrome P450 3A Inhibitors, HCV NS3/4A Protease Inhibitors and Organic Anion Transporting Polypeptide 1B1 Inhibitors; its molecular targets in DrugCentral include NS3 protease, CMA1, CELA1 and NS3.

When was Telaprevir first approved?

Telaprevir was first approved by the FDA in 2011.

What drug class does Telaprevir belong to?

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

What is the chemical formula of Telaprevir?

Telaprevir has the molecular formula C36H53N7O6 and a molecular weight of 679.86 g/mol.

Sources

• DrugCentral drug card 4173 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL231813 — compound record and bioactivity
• PubChem CID 3010818 — chemical identifiers
• DrugBank DB05521 — drug record
• FDA UNII 655M5O3W0U — substance identity
• DailyMed: FDA labels for Telaprevir — current prescribing information (label search)
• UniProt P23946 (CMA1) — target protein
• UniProt Q9UNI1 (CELA1) — target protein
• UniProt P10619 (CTSA) — target protein
• UniProt P07858 (CTSB) — target protein
• UniProt P25774 (CTSS) — target protein
• UniProt P43235 (CTSK) — 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.