Overview

Saquinavir is an HIV-1 protease inhibitor used in combination with ritonavir and other antiretrovirals for the treatment of human immunodeficiency virus-1 (HIV-1) infection. In 1995 it became the first protease inhibitor approved by the FDA, followed shortly by ritonavir in 1996, and remains in clinical use today due to a relatively benign adverse effect profile as compared to other antiretroviral therapies. While its efficacy was initially limited by exceptionally poor oral bioavailability (approximately 4%), its current indications require the co-administration of ritonavir - a potent enzyme inhibitor - that increases the bioavailability and subsequent serum concentrations of saquinavir, thus dramatically improving antiviral activity.

Indication

Saquinavir is indicated, in combination with ritonavir and other antiretroviral agents, for the treatment of HIV-1 infection in patients 16 years of age and older.

Associated Conditions

Human Immunodeficiency Virus Type 1 (HIV-1) Infection

Research Report

Published: Aug 7, 2025

Saquinavir (DB01232): A Comprehensive Pharmacological and Clinical Monograph

Executive Summary

Saquinavir represents a landmark compound in the history of medicine, being the first-in-class Human Immunodeficiency Virus (HIV) protease inhibitor approved for clinical use.[1] Its introduction in 1995 heralded the era of Highly Active Antiretroviral Therapy (HAART), fundamentally transforming the prognosis of HIV infection from a terminal illness to a manageable chronic condition.[2] The primary indication for Saquinavir is the treatment of HIV-1 infection, where it is used as a component of combination antiretroviral regimens.[3]

The entire clinical and commercial narrative of Saquinavir is dominated by a single, profound challenge: its exceptionally poor and variable oral bioavailability. The initial hard-gel capsule formulation, marketed as Invirase®, exhibited an average bioavailability of only 4% when administered alone.[3] This critical flaw, stemming from a combination of poor aqueous solubility and extensive first-pass metabolism, rendered the drug clinically suboptimal and drove all subsequent development and therapeutic strategies.[5]

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Clinical Trials

Title	Posted	Study ID	Phase	Status	Sponsor
Tipranavir and Ritonavir vs. Saquinavir and Ritonavir Used With Two Nucleoside Reverse Transcriptase Inhibitors in Single Protease Inhibitor-experienced HIV-1 Patients	2014/09/15	NCT02239835	Phase 2	Terminated	Boehringer Ingelheim
Testing of HIV Protease Inhibitors to Suppress Inflammation and Improve Cardio Pulmonary Hemodynamics in Subjects With Pulmonary Arterial Hypertension	2013/12/30	NCT02023450	Early Phase 1	UNKNOWN	The Third Xiangya Hospital of Central South University
A Study of Ritonavir-Boosted Invirase (Saquinavir) in Treatment-Naïve HIV-1 Infected Patients	2012/07/12	NCT01638650	Phase 1	Completed	Hoffmann-La Roche
Pharmacokinetics, Safety And Toleration Of Maraviroc Administered To Subjects With Various Degrees Of Renal Impaired And Normal Renal Function	2008/07/16	NCT00717067	Phase 4	Completed	ViiV Healthcare
A Study of Invirase (Saquinavir)/Ritonavir in HIV-Infected Infants and Children.	2008/02/26	NCT00623597	Phase 2	Completed	Hoffmann-La Roche
Efficacy and Safety of SQV in Patients Who Have Chronic IDV Nephrotoxicity	2007/05/22	NCT00477048	Phase 2	Completed	The HIV Netherlands Australia Thailand Research Collaboration
A PK and Salvage Study for Children With HIV-infection	2007/05/22	NCT00476359	Phase 4	Completed	The HIV Netherlands Australia Thailand Research Collaboration
Lopinavir Capsules to Kaletra or Invirase Tablets	2007/02/21	NCT00438152	Phase 4	Completed	Royal Free Hampstead NHS Trust
A Study of Saquinavir/Ritonavir in Liver-Impaired Patients With HIV Infection.	2007/02/16	NCT00435929	Phase 1	Completed	Hoffmann-La Roche
Directly Observed Therapy in High Risk Populations in Newark, NJ	2006/02/02	NCT00285883	Phase 3	Completed	Saint Michael's Medical Center

FDA Drug Approvals

Approved Product	Manufacturer	NDC Code	Route	Strength	Effective Date
Invirase	Genentech, Inc.	0004-0244	ORAL	500 mg in 1 1	12/26/2019
Invirase	State of Florida DOH Central Pharmacy	53808-0674	ORAL	500 mg in 1 1	9/20/2010

EMA Drug Approvals

Approved Product	Authorization Holder	Status	Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product	Manufacturer	Approval Number	Dosage Form	Strength	Approval Date
No HSA approvals found for this drug.

NMPA Drug Approvals

Approved Product	Company	Approval Number	Drug Type	Dosage Form	Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product	Registration No.	Company	Licence No.	Strength	Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product	ARTG ID	Sponsor	Registration Type	Status	Registration Date
No TGA approvals found for this drug.

Health Canada Drug Approvals

Approved Product	Company	DIN	Dosage Form	Strength	Market Date
FORTOVASE ROCHE	Hoffmann-La Roche Limited	02239083	Capsule - Oral	200 MG	11/26/1998

CIMA AEMPS Drug Approvals

Approved Product	Company	Registration Number	Pharmaceutical Form	Prescription Type	Status
INVIRASE 500 mg COMPRIMIDOS RECUBIERTOS CON PELICULA	Roche Registration Gmbh	96026002	COMPRIMIDO RECUBIERTO CON PELÍCULA	Uso Hospitalario	Not Commercialized

Philippines FDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product	Company	Registration Number	Dosage Form	Strength	Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name	MA Holder	MA Number	Pharmaceutical Form	Active Ingredient	Authorization Date
No UK EMC drug information found for this drug.

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