Saquinavir

Protease Inhibitor — ANTIINFECTIVES FOR SYSTEMIC USE

Key facts

Saquinavir is an ofm drug in the Protease Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 1995. Its mechanism of action is classified as Cytochrome P450 3A Inhibitors and HIV Protease Inhibitors. DrugCentral lists 23 molecular targets, including protease, pol and gag-pol. Recorded indications include Human immunodeficiency virus infection.

• Approval status: ofm (first approved 1995 by the FDA).
• Drug class: Protease Inhibitor.
• Mechanism of action: Cytochrome P450 3A Inhibitors; HIV Protease Inhibitors.
• Molecular targets: protease, pol, gag-pol and HIV-1 protease (23 listed in DrugCentral).
• Indications: Human immunodeficiency virus infection.
• ATC code: J05AE01 (Protease inhibitors).
• Molecular formula: C38H50N6O5; molecular weight 670.86 g/mol.

Indications & contraindications

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

Indications (1)

• Human immunodeficiency virus infection

Contraindications (22)

• Alcoholism
• Breastfeeding (mother)
• Chronic hepatitis C
• Chronic type B viral hepatitis
• Cirrhosis of liver
• Complete atrioventricular block
• Congenital long QT syndrome
• Diabetes mellitus
• Disease of liver
• Hepatic failure
• Hereditary factor IX deficiency disease
• Hereditary factor VIII deficiency disease
• Hypercholesterolemia
• Hyperglycemia
• Hypertriglyceridemia
• Hypokalemia
• Hypomagnesemia
• Liver function tests abnormal
• Prolonged QT interval
• Second degree atrioventricular block
• Torsades de pointes
• Viral hepatitis C

Mechanism & targets

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

Molecular targets (23)

Target	Gene	Action	Activity
Protease	protease	unknown	Ki 10.40
Pol polyprotein	pol	inhibitor	Ki 10.40
Gag-Pol polyprotein	gag-pol	unknown	Ki 10.19
Protease	HIV-1 protease	unknown	Ki 9.66
Protease	protease	unknown	IC50 9.30
Protease	HIV-1 protease	unknown	Ki 8.54
Cytochrome P450 3A4	CYP3A4	unknown	IC50 5.82
Substance-K receptor	TACR2	unknown	Ki 5.68
Thromboxane-A synthase	TBXAS1	unknown	IC50 5.66
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 5.61
Kappa-type opioid receptor	OPRK1	unknown	Ki 5.56
Mu-type opioid receptor	OPRM1	unknown	Ki 5.41
5-hydroxytryptamine receptor 1A	Htr1a	unknown	IC50 5.37
D(3) dopamine receptor	DRD3	unknown	Ki 5.28
Vasopressin V1a receptor	AVPR1A	unknown	Ki 5.15
Delta-type opioid receptor	OPRD1	unknown	Ki 5.00
Replicase polyprotein 1ab	REP	unknown	IC50 5.00
Multidrug resistance protein 1	ABCB1	unknown	IC50 4.92
Chloroquine resistance transporter	CRT	unknown	IC50 4.89
ATP-binding cassette sub-family G member 2	ABCG2	unknown	IC50 4.71

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
1996-10-03	EMA	—	ROCHE REGISTRATION GMBH
1995-12-06	FDA	—	HOFFMANN LA ROCHE

ATC classification

ATC code	Therapeutic hierarchy
J05AE01	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Protease inhibitors

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
Lipodystrophy acquired	951.5
Mitochondrial toxicity	862.2
Eyelid ptosis	672.6
Progressive external ophthalmoplegia	492.0
Viral mutation identified	462.0
Diplopia	457.2
Virologic failure	371.2
Pathogen resistance	320.9
Drug resistance	212.8
Foetal exposure during pregnancy	194.6
Ophthalmoplegia	184.1
Dysphagia	133.3

Chemical structure

• Molecular formula: C₃₈H₅₀N₆O₅
• Molecular weight: 670.86 g/mol
• CAS number: 127779-20-8
• InChIKey: QWAXKHKRTORLEM-UGJKXSETSA-N
• PubChem CID: 441243

CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CC(N)=O)NC(=O)C1=NC2=CC=CC=C2C=C1

Frequently asked questions

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

What is Saquinavir used for?

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

How does Saquinavir work?

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

When was Saquinavir first approved?

Saquinavir was first approved by the FDA in 1995.

What drug class does Saquinavir belong to?

Saquinavir is in the Protease Inhibitor class.

What is the chemical formula of Saquinavir?

Saquinavir has the molecular formula C38H50N6O5 and a molecular weight of 670.86 g/mol.

Sources

• DrugCentral drug card 2422 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL114 — compound record and bioactivity
• PubChem CID 441243 — chemical identifiers
• DrugBank DB01232 — drug record
• FDA UNII L3JE09KZ2F — substance identity
• DailyMed: FDA labels for Saquinavir — current prescribing information (label search)
• UniProt P08684 (CYP3A4) — target protein
• UniProt P21452 (TACR2) — target protein
• UniProt P24557 (TBXAS1) — target protein
• UniProt P08908 (HTR1A) — target protein
• UniProt P41145 (OPRK1) — target protein
• UniProt P35372 (OPRM1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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