saquinavir

Trade name: invirase

Small moleculeapproved

Approved

Dec 6, 1995

Saquinavir (brand names Invirase and Fortovase) is an antiretroviral drug used together with other medications to treat or prevent HIV/AIDS. Saquinavir is an inhibitor of HIV protease. HIV protease is an enzyme required for the proteolytic cleavage of viral polyprotein precursors into individual functional proteins found in infectious HIV. Saquinavir is a peptide-like substrate analog that binds to the protease active site and inhibits the activity of the enzyme. Saquinavir inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature noninfectious virus particles. The most frequent adverse events with saquinavir in either formulation are mild gastrointestinal symptoms, including diarrhea, nausea, loose stools & abdominal discomfort. Invirase is better tolerated than Fortovase. — NCATS

Clinical trial activity

80 trials · 47 clinical orgs · 1 marketing orgs

Phase 1
19
Phase 2
47
Phase 3
19
Phase 4
10

Earliest trial started Jun 1, 1997 (NCT00003008)

Timeline

1990s

  1. Dec 6, 1995

    Roche — Earliest FDA Approval

  2. Dec 6, 1995

    Roche — NDA Organization

  3. Jan 1, 1997

    Earliest Phase 2 Sponsor(trial)

  4. Jan 1, 1999

    Earliest Phase 1 Sponsor(trial)

  5. Jan 1, 1999

    Roche — Earliest Phase 3 Sponsor(trial)

Indications

Mechanism of action

Approval history

  • approvedPriority reviewAcceleratedDec 6, 1995

Chemistry & pharmacology

Loading structure…

SMILES

CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)c1ccc2ccccc2n1
Mol. weight
670.86 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Discontinued

Oral

Yes

Parenteral

No

Topical

No

Black box warning

Sources

Also known as

  • fortovase
  • fortovase
  • fortovase
  • invirase
  • invirase
  • invirase
  • invirase
  • invirase
  • invirase
  • invirase
  • invirase
  • ro-31-8959
  • ro-31-8959
  • ro-318959000
  • ro-318959000
  • ro-318959003
  • ro-318959003
  • ro-31-8959-003
  • ro-31-8959-003
  • saquinavir
  • saquinavir
  • saquinavir
  • saquinavir
  • saquinavir
  • saquinavir
  • saquinavir
  • saquinavir
  • saquinavir
  • saquinavir
  • saquinavir
  • saquinavir mesilate
  • saquinavir mesylate
  • saquinavir mesylate
  • saquinavir mesylate
  • saquinavir mesylate
  • saquinavir mesylate
  • saquinavir methanesulfonate
  • sequinavir
  • sqv
  • sqv

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT03631732Phase 3Aug 28, 2018Gilead Sciences
NCT02556268Phase 1Feb 1, 2016Bayer
NCT02616783Phase 3Dec 22, 2015Gilead Sciences
NCT02605954Phase 3Nov 18, 2015Gilead Sciences
NCT02469246Phase 3Jun 29, 2015Gilead Sciences
NCT02858401Phase 1Jan 29, 2015Gilead Sciences
NCT02023450Early Phase 1 (Phase 1)Dec 1, 2013Central South University
NCT01638650Phase 1Jan 1, 2012Roche
NCT00717067Phase 4Jul 1, 2008Pfizer, ViiV Healthcare
NCT00623597Phase 2Jun 1, 2008Roche
NCT00622141Phase 1/Phase 2 (Phase 2)Feb 12, 2008The Government Pharmaceutical Organization, The HIV Netherlands Australia Thailand Research Collaboration
NCT00622206Phase 1/Phase 2 (Phase 2)Jan 1, 2008The HIV Netherlands Australia Thailand Research Collaboration
NCT00476983Phase 2/Phase 3 (Phase 3)May 20, 2007The HIV Netherlands Australia Thailand Research Collaboration
NCT00445146Phase 2Feb 1, 2007Gilead Sciences
NCT00438152Phase 4Sep 1, 2006Roche, University of London
NCT00435929Phase 1Sep 1, 2006Roche
NCT00389402Phase 4Jul 1, 2006Gilead Sciences, International Antiviral Therapy Evaluation Center (IATEC), Roche, University of Amsterdam
NCT00379405Phase 4Jun 1, 2006Badalona Hospital Germans Trias i Pujol, Fundacio Lluita Contra la SIDA, Hospital de Sant Pau i Santa Tecla de Tarragona
NCT00122603Phase 2Dec 1, 2005Bristol-Myers Squibb, French National Agency for Research on AIDS and Viral Hepatitis, GlaxoSmithKline, Roche, University of Paris
NCT00145561Phase 1/Phase 2 (Phase 2)Aug 1, 2005Radboud University, Roche
Showing 20 of 80 trials
Page 1 / 4

Organizations

Research & Development (47)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
RocheFor profit312251999
National Institute of Allergy and Infectious Diseases (NIAID)Government191941999
Gilead SciencesFor profit8741999
National Institutes of Health (NIH)Government6141999
The HIV Netherlands Australia Thailand Research CollaborationAcademic/Hospital6632003
AbbottFor profit3322001
Boehringer IngelheimFor profit3321999
Bristol-Myers SquibbFor profit3221999
University of New South WalesAcademic/Hospital3232003
Badalona Hospital Germans Trias i PujolAcademic/Hospital2222005
Fundacio Lluita Contra la SIDAAcademic/Hospital2022005
Glaxo WellcomeFor profit2221999
International Antiviral Therapy Evaluation Center (IATEC)Academic/Hospital2122004
National Cancer Institute (NCI)Government2021997
Radboud UniversityAcademic/Hospital2112004
University of AmsterdamAcademic/Hospital2022004
University of WashingtonAcademic/Hospital2022002
AIDS Clinical Trials GroupAcademic/Hospital1012003
AIDS Malignancy ConsortiumAcademic/Hospital1011997
BayerFor profit1112016
47 organizations
Page 1 / 3

Marketing (2)

OrganizationOrg typeRelationshipDate
RocheFor profitSYNDec 17, 2004
RocheFor profitNDADec 6, 1995