Drugs / Saquinavir
last change Aug 2023 re-read 2 minutes ago

Saquinavir

Small molecule

Developed for
HIV infectious disease · poisoning · pulmonary arterial hypertension
Investigated by
Hoffmann-La Roche · National Institute of Allergy and Infectious Diseases (NIAID) · Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) · The HIV Netherlands Australia Thailand Research Collaboration · Abbott · Kirby Institute
+27 more · Boehringer Ingelheim · Fight AIDS and Infectious Diseases Foundation · Germans Trias i Pujol Hospital · Gilead Sciences · Glaxo Wellcome · International Antiviral Therapy Evaluation Center · National Cancer Institute (NCI) · Roche Pharma AG · AIDS Associated Malignancies Clinical Trials Consortium · Bristol-Myers Squibb · Eastern Cooperative Oncology Group · French National Agency for Research on AIDS and Viral Hepatitis · GlaxoSmithKline · Ministry of Health, Thailand · National Heart, Lung, and Blood Institute (NHLBI) · National Institute of Mental Health (NIMH) · National Institutes of Health (NIH) · National Institutes of Health Clinical Center (CC) · PENTA Foundation · Parexel · Radboud University Medical Center · Roche for trial and Saquinavir,and Abbott for Kaletra · St Vincent's Hospital, Sydney · Stanford University · The Third Xiangya Hospital of Central South University · University of California, San Diego · Xiangya Hospital of Central South University

Regulatory milestones approvals, filings & regulatory actions · 6 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Withdrawn EU (EMA) Invirase 2023-08-16 europa.eu
Label expansions (2) US (FDA) INVIRASE 1996-09-27 – 2012-11-30 fda.gov
Label expansion US (FDA) FORTOVASE 2003-12-24 fda.gov
Approved EU (EMA) Invirase 1996-10-03 europa.eu
Approved US (FDA) INVIRASE 1995-12-06 fda.gov

Trials 63 · a red edge is where a trial was stopped

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 01 trial
Phase 0 NCT02023450 Dec 2013 → Dec 2014 pulmonary arterial hypertension The Third Xiangya Hospital of Central South University Unknown No outcome recorded
Phase 113 trials
Phase 1 NCT01638650 Jan → Jun 2012 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 1 NCT00435929 Sep 2006 → Nov 2009 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 1 NCT00307502 Jan 2005 → Dec 2009 HIV infectious disease Germans Trias i Pujol Hospital Completed No outcome recorded
Phase 1 NCT00032669 Mar 2002 → Apr 2006 HIV infectious disease National Cancer Institute (NCI) Completed No outcome recorded
Phase 1 NCT02184286 May 1999 → Feb 2000 HIV infectious disease Boehringer Ingelheim Terminated No outcome recorded
Phase 1 NCT00001108 ? → Jun 2000 HIV infectious disease National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 1 NCT00002372 HIV infectious disease Glaxo Wellcome Completed No outcome recorded
Phase 1 NCT00002111 HIV infectious disease Stanford University Completed No outcome recorded
Phase 1 NCT00000920 ? → Apr 2003 HIV infectious disease, pregnancy disorder National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 1 NCT00002380 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 1/22 trials
Phase 1/2 NCT00145561 Aug 2005 → Jan 2008 HIV infectious disease Radboud University Medical Center Completed No outcome recorded
Phase 1/2 NCT00084058 ? → Dec 2006 HIV infectious disease National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 223 trials
Phase 2 NCT00623597 Jun 2008 → Mar 2010 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 2 NCT00122603 Dec 2005 → Aug 2007 HIV infectious disease French National Agency for Research on AIDS and Viral Hepatitis Completed No outcome recorded
Phase 2 NCT00477048 May 2004 → May 2008 poisoning The HIV Netherlands Australia Thailand Research Collaboration Completed No outcome recorded
Phase 2 NCT00400738 Mar 2004 → Dec 2006 HIV infectious disease The HIV Netherlands Australia Thailand Research Collaboration Completed No outcome recorded
Phase 2 NCT00056641 Feb 2003 → Jan 2004 HIV infectious disease Boehringer Ingelheim Completed No outcome recorded
Phase 2 NCT00043953 Aug 2002 → ? HIV infectious disease Abbott Completed No outcome recorded
Phase 2 NCT00038532 Apr 2001 → ? HIV infectious disease Abbott Completed No outcome recorded
Phase 2 NCT00003008 Dec 1997 → Jun 2006 sarcoma Eastern Cooperative Oncology Group Completed No outcome recorded
Phase 2 NCT00000913 ? → Apr 2001 HIV infectious disease National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 2 NCT00001087 ? → Jul 2000 HIV infectious disease National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 2/34 trials
Phase 2/3 NCT00624195 Mar 2007 → Feb 2012 HIV infectious disease University of California, San Diego Completed No outcome recorded
Phase 2/3 NCT00039741 Aug 2002 → Aug 2009 HIV infectious disease National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 2/3 NCT00038519 Apr 2001 → ? HIV infectious disease Abbott Completed No outcome recorded
Phase 2/3 NCT00476983 The HIV Netherlands Australia Thailand Research Collaboration Withdrawn No outcome recorded
Phase 39 trials
Phase 3 NCT00105079 Apr 2005 → Aug 2007 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT00002448 Oct 1999 → ? HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT00002447 Oct 1999 → ? HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT00002374 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT00002378 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT00002382 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT00002367 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT00002178 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT00002334 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 47 trials
Phase 4 NCT00389402 Jul 2006 → Jul 2008 HIV infectious disease International Antiviral Therapy Evaluation Center Completed No outcome recorded
Phase 4 NCT00379405 Jun 2006 → May 2008 HIV infectious disease Germans Trias i Pujol Hospital Completed No outcome recorded
Phase 4 NCT00476359 Oct 2003 → Nov 2008 HIV infectious disease The HIV Netherlands Australia Thailand Research Collaboration Completed No outcome recorded
Phase 4 NCT00192660 Feb 2003 → Oct 2006 cardiovascular disorder, lipodystrophy Kirby Institute Completed No outcome recorded
Phase 4 NCT00050180 Nov 2002 → Aug 2007 HIV infectious disease National Institutes of Health Clinical Center (CC) Completed No outcome recorded
Phase 4 NCT00002425 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase 4 NCT00002229 HIV infectious disease Hoffmann-La Roche Completed No outcome recorded
Phase not applicable4 trials
NCT00192608 Nov 2004 → May 2006 HIV infectious disease Kirby Institute Completed No outcome recorded
NCT00005762 Mar 2001 → May 2004 HIV infectious disease National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
NCT00000892 ? → Aug 1999 HIV infectious disease National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
NCT00000898 ? → May 2000 HIV infectious disease National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Also used as a comparator or background therapy in 18 trials
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 11 trial
Phase 1 NCT02556268 Background Feb → Dec 2016 Bayer Completed No outcome recorded
Phase 1/21 trial
Phase 1/2 NCT00622206 Comparator Jan → Apr 2008 HIV infectious disease The HIV Netherlands Australia Thailand Research Collaboration Completed No outcome recorded
Phase 24 trials
Phase 2 NCT00665847 Background Nov 2008 → May 2011 Tibotec Pharmaceuticals, Ireland Completed No outcome recorded
Phase 2 NCT00004584 Background Dec 1999 → Jan 2002 HIV infectious disease Bristol-Myers Squibb Completed No outcome recorded
Phase 2 NCT02239835 Comparator Dec 1999 → Nov 2001 HIV infectious disease Boehringer Ingelheim Terminated No outcome recorded
Phase 2 NCT00046033 Background ? → Mar 2003 HIV infectious disease National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 39 trials
Phase 3 NCT03631732 Comparator Aug 2018 → Aug 2019 HIV infectious disease Gilead Sciences Completed No outcome recorded
Phase 3 NCT02616783 Comparator Dec 2015 → Feb 2018 HIV infectious disease Gilead Sciences Completed No outcome recorded
Phase 3 NCT02605954 Comparator Nov 2015 → Jun 2017 HIV infectious disease Gilead Sciences Completed No outcome recorded
Phase 3 NCT02302547 Comparator Dec 2014 → Aug 2017 HIV infectious disease University Hospital, Tours Completed No outcome recorded
Phase 3 NCT01475838 Comparator Nov 2011 → Nov 2013 AIDS Gilead Sciences Completed No outcome recorded
Phase 42 trials
Phase 4 NCT00717067 Background Jul → Nov 2008 HIV infectious disease ViiV Healthcare Completed No outcome recorded
Phase 4 NCT00438152 Comparator Sep 2006 → Feb 2009 HIV infectious disease Royal Free Hampstead NHS Trust Completed No outcome recorded
Phase not applicable1 trial
NCT00051831 Background Oct 2003 → Dec 2007 HIV infectious disease National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded

Evidence & citations 20 cited values

Every value below carries the sentence it was read from. 87 sources stand behind the page.

FieldValueCited text
Known as Saquinavir “Generic names: Efavirenz/Emtricitabine/Tenofovir, Lamivudine/Zidovudine, Emtricitabine, Lamivudine, Abacavir/Lamivudine, Zidovudine, Abacavir/Lamivudine/Zidovudine,...” NCT00624195
79

“It may include one or two nucleoside reverse transcriptase inhibitors, such as zidovudine, didanosine, lamuvidine, zalcitabine, stavudine), a non- nucleoside reverse...” NCT00032669

“Any approved antiretroviral protease inhibitor such as atazanavir, darunavir, indinavir, ritonavir, and saquinavir ; consistent with the most recent prescribing information documents” NCT02556268

“Tenofovir+Emtricitabine+Third agent (Including a ritonavir-boosted protease inhibitor : saquinavir or indinavir or fosamprenavir or tipranavir or darunavir or atazanavir or lopinavir” NCT02302547

“Protease inhibitors (PIs) included amprenavir, atazanavir, darunavir, fosamprenavir, Kaletra (lopinavir/ritonavir, coformulated), ritonavir, and saquinavir.” NCT01252940

“allowed PIs include atazanavir (ATV), darunavir (DRV), fosamprenavir (FPV), lopinavir (LPV), or saquinavir (SQV)” NCT01475838

saquinavir (SQV; Invirase®; Fortovase®) + RTV” NCT02616783

“nelfinavir mesylate (NFV), saquinavir (SQV)” NCT00039741

saquinavir (SQV; Invirase®) + RTV” NCT02605954

saquinavir [SQV]” NCT00665847

saquinavir (SQV)” NCT03631732

NCT00002380

NCT01638650

NCT00001040

NCT00002184

NCT00000920

NCT00307502

NCT02023450

NCT00035932

NCT00002333

NCT00003008

NCT00043953

NCT02239835

NCT00002334

NCT00623597

NCT00002347

NCT00046033

NCT00122603

NCT00002372

NCT00002374

NCT00002378

NCT00192608

NCT00002382

NCT00002383

NCT00400738

NCT00379405

NCT00000898

NCT00002190

NCT00002397

NCT00622206

NCT00001087

NCT00477048

NCT00056641

NCT00002425

NCT00050180

NCT00002440

NCT00002178

NCT00002447

NCT00004584

NCT00002448

NCT00002162

NCT00000892

NCT00005762

NCT00002367

NCT00000941

NCT00002111

NCT00102206

NCT00002229

NCT00435929

NCT00717067

NCT00105079

NCT00438152

NCT00038519

NCT00038532

NCT00145561

NCT00051831

NCT00000891

NCT00000918

NCT00001094

NCT00192660

NCT00476983

NCT00000913

NCT00389402

NCT00000912

NCT00001108

NCT00000848

NCT02184286

NCT00476359

NCT00000906

NCT00084058

Known as Fortovase “An Exploratory Study of Fortovase (Saquinavir) Soft Gelatin Capsules (SGC) Plus d4T and 3TC or Fortovase (Saquinavir) SGC Plus Nelfinavir and d4T in Patients With HIV-1...” NCT00002397
7

“Evaluation of Immune Reconstitution in HIV Infected Patients Treated With Fortovase (Saquinavir) SGC QD Plus Ritonavir QD Plus 2 NRTIs Vs Efavirenz QD Plus 2 NRTIs” NCT00002448

Fortovase (Saquinavir) Given With Low-Dose Ritonavir, Zidovudine, and Lamivudine to HIV-Positive Pregnant Women During and After Pregnancy and to Their Newborns” NCT00000920

Fortovase (FTV) (Saquinavir) Soft Gel Capsule (SGC)” NCT00002378

“saquinavir (SQV; Invirase®; Fortovase®) + RTV” NCT02616783

FORTOVASE (Saquinavir) Soft Gel Capsule (SGC)” NCT00002229

“Saquinavir-sgc (Fortovase®)” NCT02184286

Fortovase (Saquinavir)” NCT00002447

Known as FTV “Fortovase (FTV) (Saquinavir) Soft Gel Capsule (SGC)” NCT00002378
Known as INV “saquinavir mesylate (INV)” NCT00043953
Known as Invirase “The Pharmacokinetics of SAquinavir (Invirase New Tablet Formulation) 1,000mg + Ritonavir (Norvir) 100mg q12h in HIV-infected Pregnant Women (SARA)” NCT00145561
5

“saquinavir (SQV; Invirase®; Fortovase®) + RTV” NCT02616783

“saquinavir (SQV; Invirase®) + RTV” NCT02605954

“saquinavir [Invirase]” NCT01638650

“saquinavir [Invirase]” NCT00623597

NCT00285883

Known as Ro 31-8959 “To compare the safety, tolerance, and efficacy of saquinavir mesylate (Ro 31-8959) alone, zalcitabine (dideoxycytidine; ddC) alone, and both in combination, in patients...” NCT00002333
5

“To investigate the toxicity, antiviral activity, and pharmacokinetics in HIV-infected patients receiving 16 weeks of oral saquinavir mesylate ( Ro 31-8959 ) at one of two doses.” NCT00002111

“Specifically, to evaluate zidovudine/zalcitabine ( AZT / ddC ) alone or in combination with either nevirapine or saquinavir ( Ro 31-8959 ).” NCT00002347

“Saquinavir Mesylate (Ro 31-8959 ; HIV Proteinase Inhibitor)” NCT00002334

“saquinavir mesylate (Ro 31-8959)” NCT00001040

“Saquinavir HGC (Ro 31-8959)” NCT00002374

Known as RO 31-8959/000 ChEMBL registry synonym — accepted as the source's own label CHEMBL114
Known as RO 31-8959/003 ChEMBL registry synonym — accepted as the source's own label CHEMBL114
Known as Saquinavir HGC saquinavir HGC (hard gel capsules)” NCT00002374
Known as Saquinavir mesilate ChEMBL registry synonym — accepted as the source's own label CHEMBL114
Known as Saquinavir Mesylate “To compare the safety, tolerance, and efficacy of saquinavir mesylate (Ro 31-8959) alone, zalcitabine (dideoxycytidine; ddC) alone, and both in combination, in patients...” NCT00002333
3

“To investigate the toxicity, antiviral activity, and pharmacokinetics in HIV-infected patients receiving 16 weeks of oral saquinavir mesylate ( Ro 31-8959 ) at one of two doses.” NCT00002111

Saquinavir Mesylate (Ro 31-8959 ; HIV Proteinase Inhibitor)” NCT00002334

saquinavir mesylate (Ro 31-8959)” NCT00001040

Known as Saquinavir methanesulfonate salt ChEMBL registry synonym — accepted as the source's own label CHEMBL114
Known as saquinavir-SGC “The purpose of this study is to see if it is safe to give saquinavir-SGC (SQV) combined with low-dose ritonavir (RTV) plus zidovudine (ZDV) and lamivudine (3TC) to HIV-positive...” NCT00000920
3

“An Open-Label, Non-Comparative Study of Saquinavir-SGC in Combination With Zidovudine (AZT) and Lamivudine (3TC) in the Treatment of HIV-1 Infected Patients With No Previous...” NCT00002367

“saquinavir SGC (soft gel capsules)” NCT00002374

Saquinavir-sgc (Fortovase®)” NCT02184286

Known as Saquinavirum ChEMBL registry synonym — accepted as the source's own label CHEMBL114
Known as SCH-52852 ChEMBL registry synonym — accepted as the source's own label CHEMBL114
Known as SQV “This study aimed to assess the long-term efficacy, safety and use of therapeutic drug monitoring (TDM) of a double-boosted protease inhibitor (PI) combination, saquinavir (SQV)...” PMID 19430099 2009
23

“The purpose of this study is to see if it is safe to give saquinavir-SGC (SQV) combined with low-dose ritonavir (RTV) plus zidovudine (ZDV) and lamivudine (3TC) to HIV-positive...” NCT00000920

“This 48-week randomized study examined the safety and efficacy of a switch in CART to a once-daily regimen of saquinavir (SQV), ritonavir (RTV), and atazanavir (ATV) that did...” PMID 17479946 Apr 2007

“Adult AIDS Clinical Trials Group 5043 examined pharmacokinetic (PK) interactions between amprenavir (APV) and efavirenz (EFV) both by themselves and when nelfinavir (NFV),...” PMID 16048950 Aug 2005

“saquinavir/ritonavir 1500/100 mg or 1500/50 mg Twenty HIV-infected volunteers on stable doses of SQV/RTV 1500/100 mg OD for at least 3 months with an NRTI backbone and...” NCT00622206

“The 7 drugs that will be given in this study are stavudine (d4T), didanosine (ddI), lamivudine (3TC), nelfinavir (NFV), ritonavir (RTV), saquinavir (SQV), and nevirapine (NVP).” NCT00001108

“the combination of the HIV protease inhibitors (HIV-PIs) saquinavir and ritonavir (SQV+RIT) in patients with idiopathic pulmonary arterial hypertension (IPAH)” PMID 26401255 Sep 2015

“Efficacy and safety of a saquinavir (SQV) based regimen in HIV-1 infected Thai patients who have chronic indinavir (IDV) associated nephrotoxicity.” NCT00477048

“allowed PIs include atazanavir (ATV), darunavir (DRV), fosamprenavir (FPV), lopinavir (LPV), or saquinavir (SQV)” NCT01475838

“lopinavir/ritonavir (LPV/r), saquinavir (SQV), and the NRTIs emtricitabine (FTC) and abacavir sulfate (ABC)” NCT00102206

“Arm A: Saquinavir (SQV) plus ritonavir (RTV) plus delavirdine (DLV) plus adefovir dipivoxil placebo.” NCT00000892

“the protease inhibitor saquinavir (SQV) that has already been available for several years” NCT00389402

“Saquinavir (SQV) soft gel capsules (sgc) plus 2 reverse transcriptase inhibitors (RTIs)” NCT00002178

“when the IQ was <15, saquinavir (SQV) 750 mg/m(2) p.o. q12h was added to the regimen.” PMID 18625762 Jul 2008

“Saquinavir (SQV) sgc plus 2 new reverse transcriptase inhibitors (RTIs)” NCT00002378

“standard dual PI combination of saquinavir (SQV) and ritonavir (RTV)” NCT02239835

“saquinavir (SQV; Invirase®; Fortovase®) + RTV” NCT02616783

“nelfinavir mesylate (NFV), saquinavir (SQV)” NCT00039741

“saquinavir (SQV) or amprenavir (APV)” NCT00046033

“saquinavir (SQV; Invirase®) + RTV” NCT02605954

“Saquinavir (SQV)Sgc” NCT00001094

“saquinavir (SQV)” NCT00000906

“saquinavir (SQV)” NCT03631732

“saquinavir [SQV]” NCT00665847

Known as SQVsgc “Arm A: APV plus saquinavir soft gel capsule (SQVsgc) plus abacavir (ABC) plus efavirenz (EFV) plus adefovir (ADV).” NCT00000912
1

“saquinavir soft gelatin capsule formulation (SQV-SGC)” NCT00002425

Action Inhibit “other protease inhibitors (saquinavir/nelfinavir or saquinavir/ritonavir)” NCT00000892
Modality Small molecule CHEMBL114
Route Oral oral saquinavir mesylate” NCT00002111