Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C38H50N6O5.CH4O3S |
Molecular Weight | 766.946 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(O)(=O)=O.[H][C@@]12CCCC[C@]1([H])CN(C[C@@H](O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(N)=O)NC(=O)C4=CC=C5C=CC=CC5=N4)[C@@H](C2)C(=O)NC(C)(C)C
InChI
InChIKey=IRHXGOXEBNJUSN-YOXDLBRISA-N
InChI=1S/C38H50N6O5.CH4O3S/c1-38(2,3)43-37(49)32-20-26-14-7-8-15-27(26)22-44(32)23-33(45)30(19-24-11-5-4-6-12-24)41-36(48)31(21-34(39)46)42-35(47)29-18-17-25-13-9-10-16-28(25)40-29;1-5(2,3)4/h4-6,9-13,16-18,26-27,30-33,45H,7-8,14-15,19-23H2,1-3H3,(H2,39,46)(H,41,48)(H,42,47)(H,43,49);1H3,(H,2,3,4)/t26-,27+,30-,31-,32-,33+;/m0./s1
DescriptionSources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/021785s001,002,020828s019,020,020628s022,023lbl.pdfCurator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB01232 | http://reference.medscape.com/drug/invirase-saquinavir-342628 | https://www.drugs.com/cdi/saquinavir.html | https://www.ncbi.nlm.nih.gov/pubmed/20950334
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/021785s001,002,020828s019,020,020628s022,023lbl.pdf
Curator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB01232 | http://reference.medscape.com/drug/invirase-saquinavir-342628 | https://www.drugs.com/cdi/saquinavir.html | https://www.ncbi.nlm.nih.gov/pubmed/20950334
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.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL5074 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8360874 |
0.5 nM [IC50] | ||
Target ID: CHEMBL2366517 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20108932 |
0.4 nM [IC50] | ||
Target ID: CHEMBL243 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17964171 |
0.4 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | FORTOVASE Approved UseINDICATIONS & USAGE INVIRASE in combination with ritonavir and other antiretroviral agents is indicated for the treatment of HIV-1 infection in adults (over the age of 16 years). The following points should be considered when initiating therapy with INVIRASE: – The twice daily administration of INVIRASE in combination with ritonavir is supported by safety data from the MaxCmin 1 trial [see Adverse Reactions (6.1) Launch Date1997 |
Doses
Dose | Population | Adverse events |
---|---|---|
1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Other AEs: Diabetes mellitus, Lipodystrophy... Other AEs: Diabetes mellitus (3%) Sources: Lipodystrophy (5%) Nausea (11%) Vomiting (7%) Diarrhea (8%) Abdominal pain (6%) Constipation (2%) Fatigue (6%) Fever (3%) Back pain (2%) Pneumonia (5%) Bronchitis (3%) Influenza (3%) Sinusitis (3%) Rash (3%) Pruritus (3%) Dry lips (2%) Eczema (2%) |
1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Other AEs: Nausea, Vomiting... Other AEs: Nausea (22.2%) Sources: Vomiting (6.2%) Diarrhea (4.9%) Abdominal pain (2.5%) Diarrhea aggravated (2.5%) Esophageal reflux (2.5%) Fatigue (2.5%) Dizziness (excl vertigo) (1.2%) Dermatitis (1.2%) Decreased appetite (3.7%) Headache (2.5%) Insomnia (1.2%) Weakness (2.5%) Depression (2.5%) Anxiety (1.2%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Nausea | 11% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Back pain | 2% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Constipation | 2% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Dry lips | 2% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Eczema | 2% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Bronchitis | 3% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Diabetes mellitus | 3% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Fever | 3% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Influenza | 3% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Pruritus | 3% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Rash | 3% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Sinusitis | 3% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Lipodystrophy | 5% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Pneumonia | 5% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Abdominal pain | 6% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Fatigue | 6% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Vomiting | 7% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Diarrhea | 8% | 1000 mg 2 times / day multiple, oral Recommended Dose: 1000 mg, 2 times / day Route: oral Route: multiple Dose: 1000 mg, 2 times / day Co-administed with:: ritonavir(100 mg; 2/day) Sources: |
unhealthy, adult n = 148 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Population Size: 148 Sources: |
Anxiety | 1.2% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Dermatitis | 1.2% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Dizziness (excl vertigo) | 1.2% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Insomnia | 1.2% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Abdominal pain | 2.5% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Depression | 2.5% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Diarrhea aggravated | 2.5% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Esophageal reflux | 2.5% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Fatigue | 2.5% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Headache | 2.5% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Weakness | 2.5% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Nausea | 22.2% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Decreased appetite | 3.7% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Diarrhea | 4.9% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Vomiting | 6.2% | 1600 mg 1 times / day multiple, oral Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Co-administed with:: ritonavir(100 mg; 1/day) Sources: |
unhealthy, adult n = 81 Health Status: unhealthy Condition: HIV-1 infection Age Group: adult Sex: M+F Population Size: 81 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/16118329/ Page: 5.0 |
little [IC50 >100 uM] | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/16118329/ Page: 5.0 |
little [IC50 >100 uM] | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/16118329/ Page: 5.0 |
little [IC50 >100 uM] | |||
Page: 3.0 |
negligible [IC50 >100 uM] | |||
Page: 3.0 |
negligible [IC50 >100 uM] | |||
weak [Ki 1.8 uM] | ||||
yes [IC50 1.8 uM] | ||||
Sources: https://pubmed.ncbi.nlm.nih.gov/16118329/ Page: 5.0 |
yes [IC50 13 uM] | |||
Sources: https://www.zora.uzh.ch/id/eprint/32186/ Page: 5.0 |
yes [IC50 2.1 uM] | |||
Page: 3.0 |
yes [IC50 2.14 uM] | |||
yes [IC50 27.4 uM] | ||||
Sources: https://www.zora.uzh.ch/id/eprint/32186/ Page: 5.0 |
yes [IC50 4.1 uM] | |||
Sources: https://www.zora.uzh.ch/id/eprint/32186/ Page: 12.0 |
yes [IC50 5.3 uM] | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/16118329/ Page: 5.0 |
yes [IC50 5.5 uM] | |||
Page: 3.0 |
yes [IC50 54 uM] | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/16118329/ Page: 5.0 |
yes [IC50 8 uM] | |||
yes [IC50 8.3 uM] | ||||
yes [Ki 0.6 uM] | ||||
Sources: https://pubmed.ncbi.nlm.nih.gov/9758674/ Page: 3.0 |
yes [Ki 24 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes [IC50 <10 uM] | ||||
yes | ||||
yes | ||||
yes | yes (co-administration study) Comment: Coadministration with ritonavir (CYP3A4 inhibitor): mean saquinavir AUC value was seven fold greater than mean value observed after administration of saquinavir alone. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/021785s001,002,020828s019,020,020628s022,023lbl.pdf#page=13 Page: 13,19 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/15721475/ Page: 3.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Anti-HIV activity and mechanism of action of macrocyclic diamide SRR-SB3. | 1998 Dec |
|
Hydroxyurea-induced neurotoxicity in HIV disease. | 1999 Aug 20 |
|
Non-active site changes elicit broad-based cross-resistance of the HIV-1 protease to inhibitors. | 1999 Aug 20 |
|
Cage dimeric 4-aryl-1,4-dihydropyridines as promising lead structures for the development of a novel class of HIV-1 protease inhibitors. | 1999 Jan |
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Pyrido [1,2a] indole derivatives identified as novel non-nucleoside reverse transcriptase inhibitors of human immunodeficiency virus type 1. | 1999 Mar |
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Synthesis and anti-HIV activity of prodrugs derived from saquinavir and indinavir. | 2000 Mar |
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Inhibition of HIV-1 protease by a boron-modified polypeptide. | 2000 Oct 1 |
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Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors. | 2000 Sep 7 |
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Saquinavir soft gelatin capsule: a comparative safety review. | 2001 |
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Comparison of P-triglyceride levels among patients with human immunodeficiency virus on randomized treatment with ritonavir, indinavir or ritonavir/saquinavir. | 2001 |
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Determination of serum levels of thirteen human immunodeficiency virus-suppressing drugs by high-performance liquid chromatography. | 2001 Apr 13 |
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[Improving the pharmacokinetics of protease inhibitors in a more innovative manner. HIV drugs administered in a more clever way]. | 2001 Apr 2 |
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Antiretrovirals: simultaneous determination of five protease inhibitors and three nonnucleoside transcriptase inhibitors in human plasma by a rapid high-performance liquid chromatography--mass spectrometry assay. | 2001 Aug |
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Pharmacokinetics and resistance mutations affect virologic response to ritonavir/saquinavir-containing regimens. | 2001 Aug |
|
Antiviral drugs: current state of the art. | 2001 Aug |
|
Pharmacokinetics of ritonavir and saquinavir in a haemodialysis patient. | 2001 Feb |
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Switch of protease inhibitor-containing HAART in routine clinical practice: a four-year prospective observational study. | 2001 Feb |
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Ritonavir, efavirenz, and nelfinavir inhibit CYP2B6 activity in vitro: potential drug interactions with bupropion. | 2001 Feb |
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Progressive human immunodeficiency virus-specific immune recovery with prolonged viral suppression. | 2001 Feb 15 |
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Large hepatic mitochondrial DNA deletions associated with L-lactic acidosis and highly active antiretroviral therapy. | 2001 Feb 16 |
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Effect of alpha1-acid glycoprotein on the intracellular accumulation of the HIV protease inhibitors saquinavir, ritonavir and indinavir in vitro. | 2001 Jan |
|
Patterns of resistance mutations to antiretroviral drugs in extensively treated HIV-1-infected patients with failure of highly active antiretroviral therapy. | 2001 Jan 1 |
|
Structure-based design of non-peptide HIV protease inhibitors. | 2001 Jan-Feb |
|
Synergistic antiviral effect of PEG-asparaginase (ONCASPAR), with protease inhibitor alone and in combination with RT inhibitors against HIV-1 infected T-cells: a model of HIV-1-induced T-cell lymphoma. | 2001 Jan-Feb |
|
HIV protease inhibitors attenuate adherence of Candida albicans to epithelial cells in vitro. | 2001 Jul |
|
CMVR diagnoses and progression of CD4 cell counts and HIV viral load measurements in HIV patients on HAART. | 2001 Jul |
|
Capillary electrophoretic separation of protease inhibitors used in human immunodeficiency virus therapy. | 2001 Jul 13 |
|
Synthesis of a chiral aziridine derivative as a versatile intermediate for HIV protease inhibitors. | 2001 Jul 26 |
|
The effects of antiretroviral protease inhibitors on serum lipid levels in HIV-infected patients. | 2001 Jun |
|
Simultaneous determination of the HIV-protease inhibitors indinavir, amprenavir, ritonavir, saquinavir and nelfinavir in human plasma by reversed-phase high-performance liquid chromatography. | 2001 Jun 15 |
|
The safety and antiviral effect of protease inhibitors in children. | 2001 Mar |
|
Clinical outcome among HIV-infected patients starting saquinavir hard gel compared to ritonavir or indinavir. | 2001 May 25 |
|
Increased risk of lipodystrophy when nucleoside analogue reverse transcriptase inhibitors are included with protease inhibitors in the treatment of HIV-1 infection. | 2001 May 4 |
|
Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5. | 2001 Sep 14 |
Patents
Sample Use Guides
1000 mg (with ritonavir 100 mg) PO q12hr, or in combination with ritonavir-enhanced lopinavir
Treatment-naïve patients: Initial dose: 500 mg PO BID plus ritonavir 100 mg BID x 7 days, THEN increase to 1000mg/100mg PO BID
Route of Administration:
Oral
In vitro antiviral activity of saquinavir was assessed in lymphoblastoid and monocytic cell lines and in peripheral blood lymphocytes. Saquinavir inhibited HIV activity in both acutely and chronically infected cells. IC50 and IC90 values (50% and 90% inhibitory concentrations) were in the range of 1 to 30 nM and 5 to 80 nM, respectively. In the presence of 40% human serum, the mean IC50 of saquinavir against laboratory strain HIV-1 RF in MT4 cells was 37.7± 5nM representing a 4-fold increase in the IC50 value. In cell culture, saquinavir demonstrated additive to synergistic effects against HIV-1 in combination with reverse transcriptase inhibitors (didanosine, lamivudine, nevirapine, stavudine, zalcitabine and zidovudine) without enhanced cytotoxicity. Saquinavir in combination with the protease inhibitors amprenavir, atazanavir, or lopinavir resulted in synergistic antiviral activity. Saquinavir displayed antiviral activity in vitro against HIV-1 clades A-H (IC50 ranged from 0.9 to 2.5 nM). The IC50 and IC90 values of saquinavir against HIV-2 isolates in vitro ranged from 0.25 nM to 14.6 nM and 4.65 nM to 28.6 nM respectively.
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Classification Tree | Code System | Code | ||
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EMA ASSESSMENT REPORTS |
INVIRASE (AUTHORIZED: HIV INFECTIONS)
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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NCI_THESAURUS |
C97366
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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Code System | Code | Type | Description | ||
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SAQUINAVIR MESYLATE
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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PRIMARY | Description: A white or almost white powder. Solubility: Very slightly soluble in water and sparingly soluble in methanol R. Category: Antiretroviral (Protease Inhibitor). Storage: Saquinavir mesilate should be kept in a tightly-closed container, protected from light. Additional information: Saquinavir mesilate is slightly hygroscopic. Definition: Saquinavir mesilate contains not less than 98.5 % and not more than 101.0 % of C38H50N6O5.CH4O3S calculated with reference to the dried substance. Manufacture: The production method must be evaluated to determine the potential for formation of alkyl mesilates, which is particularly likely to occur if the reaction medium contains lower alcohols. Where necessary, the production method is validated to demonstrate that alkyl mesilates are not detectable in the final product. | ||
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859857
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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PRIMARY | RxNorm | ||
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UHB9Z3841A
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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1609829
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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100000091808
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admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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149845-06-7
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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C1602
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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GG-17
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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UHB9Z3841A
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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60934
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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SUB12572MIG
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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DTXSID9023835
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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m9776
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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DBSALT002836
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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CHEMBL114
Created by
admin on Fri Dec 15 15:41:37 GMT 2023 , Edited by admin on Fri Dec 15 15:41:37 GMT 2023
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