saquinavir
Trade name: invirase
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
Earliest trial started Jun 1, 1997 (NCT00003008)
Timeline
Indications
Approved for
Studied for
- AIDS-Associated Nephropathy · Phase 3
- Cardiovascular Diseases · Phase 4
- Directly Observed Therapy · Phase 3
- Drug-Related Side Effects and Adverse Reactions · Phase 2
- Drugs, Investigational · Phase 2/Phase 3
- Healthy Volunteers · Phase 4
- HIV-Associated Lipodystrophy Syndrome · Phase 4
- HIV Infections · Phase 4
- Pregnancy · Phase 1
- Pulmonary Arterial Hypertension · Early Phase 1
- Sarcoma · Phase 2
Mechanism of action
Q72874 inhibitor
Approval history
- approvedPriority reviewAcceleratedDec 6, 1995
Chemistry & pharmacology
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
Sources
- ChEMBLCHEMBL114 ↗
- WikipediaSaquinavir ↗
- NCATSL3JE09KZ2F ↗
- ChEMBLCHEMBL282042 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03631732 | Phase 3 | Aug 28, 2018 | Gilead Sciences |
| NCT02556268 | Phase 1 | Feb 1, 2016 | Bayer |
| NCT02616783 | Phase 3 | Dec 22, 2015 | Gilead Sciences |
| NCT02605954 | Phase 3 | Nov 18, 2015 | Gilead Sciences |
| NCT02469246 | Phase 3 | Jun 29, 2015 | Gilead Sciences |
| NCT02858401 | Phase 1 | Jan 29, 2015 | Gilead Sciences |
| NCT02023450 | Early Phase 1 (Phase 1) | Dec 1, 2013 | Central South University |
| NCT01638650 | Phase 1 | Jan 1, 2012 | Roche |
| NCT00717067 | Phase 4 | Jul 1, 2008 | Pfizer, ViiV Healthcare |
| NCT00623597 | Phase 2 | Jun 1, 2008 | Roche |
| NCT00622141 | Phase 1/Phase 2 (Phase 2) | Feb 12, 2008 | The Government Pharmaceutical Organization, The HIV Netherlands Australia Thailand Research Collaboration |
| NCT00622206 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2008 | The HIV Netherlands Australia Thailand Research Collaboration |
| NCT00476983 | Phase 2/Phase 3 (Phase 3) | May 20, 2007 | The HIV Netherlands Australia Thailand Research Collaboration |
| NCT00445146 | Phase 2 | Feb 1, 2007 | Gilead Sciences |
| NCT00438152 | Phase 4 | Sep 1, 2006 | Roche, University of London |
| NCT00435929 | Phase 1 | Sep 1, 2006 | Roche |
| NCT00389402 | Phase 4 | Jul 1, 2006 | Gilead Sciences, International Antiviral Therapy Evaluation Center (IATEC), Roche, University of Amsterdam |
| NCT00379405 | Phase 4 | Jun 1, 2006 | Badalona Hospital Germans Trias i Pujol, Fundacio Lluita Contra la SIDA, Hospital de Sant Pau i Santa Tecla de Tarragona |
| NCT00122603 | Phase 2 | Dec 1, 2005 | Bristol-Myers Squibb, French National Agency for Research on AIDS and Viral Hepatitis, GlaxoSmithKline, Roche, University of Paris |
| NCT00145561 | Phase 1/Phase 2 (Phase 2) | Aug 1, 2005 | Radboud University, Roche |