Summary
Saquinavir has reached the approved stage (maximum clinical phase 4) for at least one indication, so its use in HIV/AIDS would be drug repurposing rather than first-in-human development. This does not mean it is approved for HIV/AIDS. ClinicalTrials.gov lists 8 registered trials linking Saquinavir to HIV/AIDS: 7 have completed; 1 is terminated, withdrawn, suspended or of unknown status. The most advanced is Phase 3 (NCT00002334). It plans or enrolled 3000 participants. Registration activity spans 1999 to 2014. The literature layer holds 15 publications for this pair: 1 Cochrane review, 3 meta-analyses, 3 systematic reviews, 3 randomised controlled trial publications and 5 clinical trial publications. Publication years run from 1997 to 2023. Because at least one synthesis-level source exists (systematic review, meta-analysis or Cochrane review), this pair has been assessed beyond single studies, although the synthesis may concern a different indication.
The RepurpOS disease-intelligence file for HIV/AIDS ranks 249 candidate therapeutics from Open Targets, ChEMBL, DGIdb and PubMed; only a minority carry direct clinical evidence, and this page covers one of those. Spontaneous remission context recorded for the condition: Spontaneous elite control (natural viremic suppression without ART) in <1% of people living with HIV; untreated, median time to AIDS ~10 years; viral rebound within weeks of ART interruption in 99%+ of patients.
Evidence table
| Evidence tier | A · Strong |
|---|---|
| Evidence score | 76.0 (trials 26.0, literature 30.0, tier 15, approved bonus 5.0) |
| Registered trials | 8 total: 0 recruiting, 0 active / not yet recruiting, 7 completed, 1 other |
| Linked publications | 15 (5 clinical trial publications, 3 meta-analyses, 3 systematic reviews, 3 randomised controlled trial publications, 1 Cochrane review) |
| Agent type | Drug (Small molecule) |
| Development stage (any indication) | Approved |
| Mechanism / class | Not recorded |
| Data sources | Open Targets, ChEMBL |
How the evidence score is calculated
- Each registered trial scores by status (recruiting / active / enrolling 3, completed 2.5, not yet recruiting 2, unknown 1, terminated / withdrawn / suspended 0.5) plus a phase bonus (phase 3-4 +2, phase 2 +1, phase 1 +0.5). The trial component is capped at 30.
- Each literature item scores by design (Cochrane review 5, meta-analysis 4, systematic review 3, RCT 3, clinical trial publication 2, curated reference 1.5, other PubMed record 1). The literature component is capped at 30.
- The existing evidence tier adds 15 (A / Strong), 10 (B / Moderate), 5 (C / Preliminary) or 0 (D / Anecdotal).
- Agents approved for any indication (max clinical phase 4) add 5, because an approved agent has an established safety profile that lowers the barrier to repurposing trials.
- The score ranks what has been studied, not what works. It does not read effect sizes or directions of effect.
Registered clinical trials
| NCT ID | Title | Status | Phase | Enrolment |
|---|---|---|---|---|
| NCT00002334 | A Study of Zidovudine (AZT) Used Alone or in Combination With Other Anti-HIV Drugs in HIV-Infected Patients With Little or No Previous Treatment | completed | Phase 3 | 3,000 |
| NCT00002367 | A Study of Saquinavir Soft Gelatin Capsules Plus Zidovudine Plus Lamivudine in the Treatment of HIV-1 Infected Patients Who Have Never Taken Anti-HIV Drugs | completed | Phase 3 | 40 |
| NCT02302547 | Trial to Evaluate the Interest of a Reductive Anti Retroviral Strategy Using Dual Therapy Inspite of Triple Therapy 2014 | completed | Phase 3 | 224 |
| NCT00000848 | The Anti-HIV Effects of Saquinavir Soft Gelatin Capsules Versus Indinavir in Patients Who Have Used Saquinavir Hard Gelatin Capsules for One Year | completed | Phase 2 | 144 |
| NCT02239835 | Tipranavir and Ritonavir vs. Saquinavir and Ritonavir Used With Two Nucleoside Reverse Transcriptase Inhibitors in Single Protease Inhibitor-experienced HIV-1 Patients 1999 | terminated | Phase 2 | 79 |
| NCT00476502 | Study of Genetic Polymorphisms in Thai HIV-1 Infected Patients on SQV/r 2006 | completed | Not applicable | 250 |
| NCT00051831 | Effect of an Enfuvirtide-based Anti-HIV Drug Regimen on Latent HIV Reservoirs in Treatment Naive Adults 2003 | completed | Not applicable | 19 |
| NCT00192608 | A 48-Week, Randomised, Study to Describe the Pharmacokinetic Profile and Durability of Atazanavir-Saquinavir-Ritonavir Once Daily and Describe the Pharmacokinetic Profile of Saquinavir-Ritonavir Using Saquinavir 500mg Formulation: the ASK-500 Study 2004 | completed | Not applicable | 40 |
Published literature
- Meta-analysis Interactions of Antiretroviral Drugs with Food, Beverages, Dietary Supplements, and Alcohol: A Systematic Review and Meta-analysesWiesner A, Skrońska M, Gawlik G et al. · AIDS and behavior · 2023 · PMID 36318429
- Systematic review Influence of Malnutrition on the Pharmacokinetics of Drugs Used in the Treatment of Poverty-Related Diseases: A Systematic ReviewVerrest L, Wilthagen EA, Beijnen JH et al. · Clinical pharmacokinetics · 2021 · PMID 34060020
- Clinical trial publication Improved adipose tissue function with initiation of protease inhibitor-only ARTMaughan RT, Feeney ER, Capel E et al. · The Journal of antimicrobial chemotherapy · 2016 · PMID 27516476
- Clinical trial publication Effect of a modified saquinavir/ritonavir dosing regimen with lower dose lead-in phase on QTc interval, pharmacokinetics, antiviral activity and safety in treatment-naïve HIV-1-infected patientsBoffito M, Jackson A, Pozniak A et al. · Drugs in R&D · 2015 · PMID 25742730
- Clinical trial publication Provirus activation plus CD59 blockage triggers antibody-dependent complement-mediated lysis of latently HIV-1-infected cellsLan J, Yang K, Byrd D et al. · Journal of immunology (Baltimore, Md. : 1950) · 2014 · PMID 25149467
- Systematic review Protecting the fetus against HIV infection: a systematic review of placental transfer of antiretroviralsMcCormack SA, Best BM · Clinical pharmacokinetics · 2014 · PMID 25223699
- Clinical trial publication Discordant associations between SLCO1B1 521T→C and plasma levels of ritonavir-boosted protease inhibitors in AIDS clinical trials group study A5146Zhang X, Tierney C, Albrecht M et al. · Therapeutic drug monitoring · 2013 · PMID 23503447
- Cochrane review Abacavir-based triple nucleoside regimens for maintenance therapy in patients with HIVCruciani M, Mengoli C, Serpelloni G et al. · The Cochrane database of systematic reviews · 2013 · PMID 23740608
- Clinical trial publication Effectiveness and safety of saquinavir/ritonavir in HIV-infected pregnant women: INEMA cohortBrunet C, Reliquet V, Jovelin T et al. · Medecine et maladies infectieuses · 2012 · PMID 22938775
- Randomized controlled trial Randomized comparison of metabolic and renal effects of saquinavir/r or atazanavir/r plus tenofovir/emtricitabine in treatment-naïve HIV-1-infected patientsVrouenraets SM, Wit FW, Fernandez Garcia E et al. · HIV medicine · 2011 · PMID 21819530
- Randomized controlled trial Pharmacokinetic interaction of vicriviroc with other antiretroviral agents: results from a series of fixed-sequence and parallel-group clinical trialsKasserra C, O'Mara E · Clinical pharmacokinetics · 2011 · PMID 21348539
- Randomized controlled trial Saquinavir/ritonavir monotherapy as a new nucleoside-sparing maintenance strategy in long-term virologically suppressed HIV-infected patientsPatricia E, Domingo P, Gutierrez M et al. · Current HIV research · 2010 · PMID 20636275
- Meta-analysis Effects of first-line use of nucleoside analogues, efavirenz, and ritonavir-boosted protease inhibitors on lipid levelsHill A, Sawyer W, Gazzard B · HIV clinical trials · 2009 · PMID 19362991
- Meta-analysis Fosamprenavir clinical study meta-analysis in ART-naïve subjects: rare occurrence of virologic failure and selection of protease-associated mutationsRoss L, Vavro C, Wine B et al. · HIV clinical trials · 2006 · PMID 17197380
- Systematic review HIV-1 protease inhibitors. A review for cliniciansDeeks SG, Smith M, Holodniy M et al. · JAMA · 1997 · PMID 8990341
Mechanism and notes
No mechanism of action is recorded for this pair in the source databases.
OSMF's existing evidence tier for this pair is A (Strong), derived from the strength of the disease association recorded in Open Targets and ChEMBL. The tier describes how well the drug-disease link is documented, not how well the drug works.
Frequently asked questions
Is Saquinavir approved for HIV/AIDS?
Saquinavir has reached the approved stage (maximum clinical phase 4) for at least one indication, so its use in HIV/AIDS would be drug repurposing rather than first-in-human development. This does not mean it is approved for HIV/AIDS. Approval status for the specific indication should always be confirmed with the relevant regulator and prescribing information.
Is Saquinavir in clinical trials for HIV/AIDS?
ClinicalTrials.gov lists 8 registered trials linking Saquinavir to HIV/AIDS: 7 have completed; 1 is terminated, withdrawn, suspended or of unknown status. The most advanced is Phase 3 (NCT00002334). It plans or enrolled 3000 participants. Registration activity spans 1999 to 2014.
What does the evidence show for Saquinavir in HIV/AIDS?
Saquinavir has both completed registered trials and synthesis-level publications linked to HIV/AIDS. That is the strongest profile in this database, but the summaries here do not extract effect sizes, so read the linked reviews for direction and magnitude of benefit. OSMF's existing evidence tier for this pair is A (Strong), derived from the strength of the disease association recorded in Open Targets and ChEMBL. The tier describes how well the drug-disease link is documented, not how well the drug works.
Cite this page
Data: ClinicalTrials.gov, PubMed, Open Targets, ChEMBL, DGIdb and the OSMF therapeutic agent database. Last updated 2026-07-05. Page built 2026-10-07.