Darunavir

Protease Inhibitor — ANTIINFECTIVES FOR SYSTEMIC USE

Key facts

Darunavir is an ofp drug in the Protease Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2006. Its mechanism of action is classified as Cytochrome P450 2D6 Inhibitors, Cytochrome P450 3A Inhibitors and HIV Protease Inhibitors. DrugCentral lists 6 molecular targets, including HIV-1 protease, pol and HIV-1 protease. Recorded indications include Human immunodeficiency virus infection.

• Approval status: ofp (first approved 2006 by the FDA).
• Drug class: Protease Inhibitor.
• Mechanism of action: Cytochrome P450 2D6 Inhibitors; Cytochrome P450 3A Inhibitors; HIV Protease Inhibitors.
• Molecular targets: HIV-1 protease, pol, HIV-1 protease and protease (6 listed in DrugCentral).
• Indications: Human immunodeficiency virus infection.
• ATC code: J05AE10 (Protease inhibitors).
• Molecular formula: C27H37N3O7S; molecular weight 547.67 g/mol.

Indications & contraindications

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

Indications (1)

• Human immunodeficiency virus infection

Off-label uses (1)

• Coronavirus infection

Contraindications (13)

• Breastfeeding (mother)
• Chronic hepatitis C
• Chronic type B viral hepatitis
• Cirrhosis of liver
• Diabetes mellitus
• Disease of liver
• Hepatic failure
• Hereditary factor IX deficiency disease
• Hereditary factor VIII deficiency disease
• Hypercholesterolemia
• Hyperglycemia
• Hypertriglyceridemia
• Liver function tests abnormal

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 2D6 Inhibitors; Cytochrome P450 3A Inhibitors; HIV Protease Inhibitors
• Established pharmacologic class: Protease Inhibitor

Molecular targets (6)

Target	Gene	Action	Activity
Protease	HIV-1 protease	unknown	Ki 10.96
Pol polyprotein	pol	inhibitor	Ki 10.85
Protease	HIV-1 protease	unknown	Ki 10.82
Protease	protease	unknown	IC50 10.21
Gag-Pol polyprotein	gag-pol	unknown	Ki 9.66
Multidrug resistance protein 1	ABCB1	unknown	IC50 5.18

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2007-11-22	PMDA	—	Janssen Pharmaceutical K.K.	Yes
2007-02-12	EMA	—	Janssen-Cilag International NV
2006-06-23	FDA	—	JANSSEN PRODS

ATC classification

ATC code	Therapeutic hierarchy
J05AE10	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Protease inhibitors
J05AR14	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Antivirals for treatment of HIV infections, combinations
J05AR22	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Antivirals for treatment of HIV infections, combinations
J05AR26	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Antivirals for treatment of HIV infections, combinations

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: CYP3A4

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
Foetal exposure during pregnancy	2235.0
Virologic failure	1796.4
Drug interaction	950.9
Immune reconstitution inflammatory syndrome	856.2
Viral mutation identified	837.3
Lipodystrophy acquired	805.3
Exposure during pregnancy	745.1
Pathogen resistance	711.2
Abortion spontaneous	680.9
Drug resistance	604.2
Premature baby	505.3
Blood HIV RNA increased	444.5

Chemical structure

• Molecular formula: C₂₇H₃₇N₃O₇S
• Molecular weight: 547.67 g/mol
• CAS number: 206361-99-1
• InChIKey: CJBJHOAVZSMMDJ-HEXNFIEUSA-N
• PubChem CID: 213039

CC(C)CN(C[C@@H](O)[C@H](CC1=CC=CC=C1)NC(=O)O[C@H]1CO[C@H]2OCC[C@@H]12)S(=O)(=O)C1=CC=C(N)C=C1

Frequently asked questions

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

What is Darunavir used for?

DrugCentral lists the following indications for Darunavir: Human immunodeficiency virus infection.

How does Darunavir work?

Darunavir is classified as Cytochrome P450 2D6 Inhibitors, Cytochrome P450 3A Inhibitors and HIV Protease Inhibitors; its molecular targets in DrugCentral include HIV-1 protease, pol (inhibitor), HIV-1 protease and protease.

When was Darunavir first approved?

Darunavir was first approved by the FDA in 2006.

What drug class does Darunavir belong to?

Darunavir is in the Protease Inhibitor class.

What is the chemical formula of Darunavir?

Darunavir has the molecular formula C27H37N3O7S and a molecular weight of 547.67 g/mol.

Sources

• DrugCentral drug card 4143 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201127 — compound record and bioactivity
• PubChem CID 213039 — chemical identifiers
• DrugBank DB01264 — drug record
• FDA UNII YO603Y8113 — substance identity
• DailyMed: FDA labels for Darunavir — current prescribing information (label search)
• UniProt P08183 (ABCB1) — 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.