Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C38H50N6O5 |
Molecular Weight | 670.8408 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[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=QWAXKHKRTORLEM-UGJKXSETSA-N
InChI=1S/C38H50N6O5/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/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)/t26-,27+,30-,31-,32-,33+/m0/s1
Molecular Formula | C38H50N6O5 |
Molecular Weight | 670.8408 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
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 Date8.7886083E11 |
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 |
---|---|---|
Unexplained thrombosis in HIV-infected patients receiving protease inhibitors: report of seven cases. | 1999 Dec |
|
Structural and kinetic analyses of the protease from an amprenavir-resistant human immunodeficiency virus type 1 mutant rendered resistant to saquinavir and resensitized to amprenavir. | 2000 Aug |
|
BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents. | 2000 Aug |
|
Inhibitory effect of human immunodeficiency virus protease inhibitors on multidrug resistance transporter P-glycoproteins. | 2000 Dec |
|
Increasing cerebrospinal fluid chemokine concentrations despite undetectable cerebrospinal fluid HIV RNA in HIV-1-infected patients receiving antiretroviral therapy. | 2000 Dec 15 |
|
In-vitro tipranavir susceptibility of HIV-1 isolates with reduced susceptibility to other protease inhibitors. | 2000 Jan 7 |
|
Drug resistance and drug combination features of the human immunodeficiency virus inhibitor, BCH-10652 [(+/-)-2'-deoxy-3'-oxa-4'-thiocytidine, dOTC]. | 2000 Jul |
|
In vitro activity of human immunodeficiency virus protease inhibitors against Pneumocystis carinii. | 2000 May |
|
A mutation in human immunodeficiency virus type 1 protease, N88S, that causes in vitro hypersensitivity to amprenavir. | 2000 May |
|
Inhibition of HIV-1 protease by a boron-modified polypeptide. | 2000 Oct 1 |
|
In vitro resistance profile of the human immunodeficiency virus type 1 protease inhibitor BMS-232632. | 2000 Sep |
|
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors. | 2000 Sep 7 |
|
Tipranavir inhibits broadly protease inhibitor-resistant HIV-1 clinical samples. | 2000 Sep 8 |
|
Comparison of P-triglyceride levels among patients with human immunodeficiency virus on randomized treatment with ritonavir, indinavir or ritonavir/saquinavir. | 2001 |
|
Analysis of HIV-1 mutation patterns in patients failing antiretroviral therapy. | 2001 |
|
Generation of a flexible cell line with regulatable, high-level expression of HIV Gag/Pol particles capable of packaging HIV-derived vectors. | 2001 Apr |
|
P-glycoprotein limits oral availability, brain, and fetal penetration of saquinavir even with high doses of ritonavir. | 2001 Apr |
|
Determination of serum levels of thirteen human immunodeficiency virus-suppressing drugs by high-performance liquid chromatography. | 2001 Apr 13 |
|
[Improving the pharmacokinetics of protease inhibitors in a more innovative manner. HIV drugs administered in a more clever way]. | 2001 Apr 2 |
|
Antiviral drugs: current state of the art. | 2001 Aug |
|
Pharmacology and clinical experience with saquinavir. | 2001 Feb |
|
Pharmacokinetics of ritonavir and saquinavir in a haemodialysis patient. | 2001 Feb |
|
Ritonavir, efavirenz, and nelfinavir inhibit CYP2B6 activity in vitro: potential drug interactions with bupropion. | 2001 Feb |
|
Progressive human immunodeficiency virus-specific immune recovery with prolonged viral suppression. | 2001 Feb 15 |
|
Large hepatic mitochondrial DNA deletions associated with L-lactic acidosis and highly active antiretroviral therapy. | 2001 Feb 16 |
|
Ritonavir-induced carbamazepine toxicity. | 2001 Jan |
|
Effect of alpha1-acid glycoprotein on the intracellular accumulation of the HIV protease inhibitors saquinavir, ritonavir and indinavir in vitro. | 2001 Jan |
|
Pilot study of a combination of highly active antiretroviral therapy and cytokines to induce HIV-1 remission. | 2001 Jan 1 |
|
Patterns of resistance mutations to antiretroviral drugs in extensively treated HIV-1-infected patients with failure of highly active antiretroviral therapy. | 2001 Jan 1 |
|
Efficacy, tolerance, and pharmacokinetics of the combination of stavudine, nevirapine, nelfinavir, and saquinavir as salvage regimen after ritonavir or indinavir failure. | 2001 Jan 20 |
|
The use of and response to second-line protease inhibitor regimens: results from the EuroSIDA study. | 2001 Jan 26 |
|
Predictors of protease inhibitor-associated adverse events. | 2001 Jul |
|
Combination therapy with saquinavir soft gelatin capsules in children with human immunodeficiency virus infection. | 2001 Jul |
|
CMVR diagnoses and progression of CD4 cell counts and HIV viral load measurements in HIV patients on HAART. | 2001 Jul |
|
Synthesis of a chiral aziridine derivative as a versatile intermediate for HIV protease inhibitors. | 2001 Jul 26 |
|
The effect of fluconazole on ritonavir and saquinavir pharmacokinetics in HIV-1-infected individuals. | 2001 Jun |
|
Prognostic factors of combined viral load and CD4+ cell count responses under triple antiretroviral therapy, Aquitaine cohort, 1996-1998. | 2001 Jun 1 |
|
Effect of ritonavir/saquinavir on stereoselective pharmacokinetics of methadone: results of AIDS Clinical Trials Group (ACTG) 401. | 2001 Jun 1 |
|
The effect of nevirapine in combination with nelfinavir in heavily pretreated HIV-1-infected patients: a prospective, open-label, controlled, randomized study. | 2001 Jun 1 |
|
A comprehensive account on the role of efflux transporters in the gastrointestinal absorption of 13 commonly used substrate drugs in humans. | 2001 Mar |
|
The safety and antiviral effect of protease inhibitors in children. | 2001 Mar |
|
Elevated alpha-1-acid glycoprotein reduces the volume of distribution and systemic clearance of saquinavir. | 2001 Mar |
|
Sequencing of protease inhibitor therapy: insights from an analysis of HIV phenotypic resistance in patients failing protease inhibitors. | 2001 Mar 30 |
|
Structure-activity studies of FIV and HIV protease inhibitors containing allophenylnorstatine. | 2001 May |
|
Secreted aspartic proteases of Candida albicans, Candida tropicalis, Candida parapsilosis and Candida lusitaniae. Inhibition with peptidomimetic inhibitors. | 2001 May |
|
Regulation of expression of 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue: tissue-specific induction by cytokines. | 2001 May |
|
Simultaneous determination of the HIV protease inhibitors indinavir, amprenavir, saquinavir, ritonavir and nelfinavir in human plasma by high-performance liquid chromatography. | 2001 May 5 |
|
Combined hydroxypropyl-beta-cyclodextrin and poly(alkylcyanoacrylate) nanoparticles intended for oral administration of saquinavir. | 2001 May 7 |
|
[Drug interactions with antiretroviral agents]. | 2001 May-Jun |
|
Mismatched double-stranded RNA (polyI-polyC(12)U) is synergistic with multiple anti-HIV drugs and is active against drug-sensitive and drug-resistant HIV-1 in vitro. | 2001 Sep |
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.
Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Jul 05 23:07:37 UTC 2023
by
admin
on
Wed Jul 05 23:07:37 UTC 2023
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Record UNII |
L3JE09KZ2F
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Record Status |
Validated (UNII)
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Record Version |
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Common Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
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NDF-RT |
N0000175889
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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NDF-RT |
N0000000246
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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WHO-VATC |
QJ05AE01
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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EMA ASSESSMENT REPORTS |
INVIRASE (AUHTORIZED: HIV INFECTIONS)
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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EMA ASSESSMENT REPORTS |
FORTOVASE (WITHDRAWN: HIV INFECTIONS)
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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WHO-ESSENTIAL MEDICINES LIST |
6.4.2.3
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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WHO-ATC |
J05AE01
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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NCI_THESAURUS |
C97366
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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LIVERTOX |
NBK548019
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
7098
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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C29444
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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4813
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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DB01232
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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SAQUINAVIR
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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SAQUINAVIR
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
|
PRIMARY | Description: A white or almost white powder. Solubility: Practically insoluble in water and soluble in methanol. Category: Antiretroviral (Protease Inhibitor). Storage: Saquinavir should be kept at 2-8?C in a tightly closed container, protected from light. Additional information: Saquinavir is slightly hygroscopic. Requirements: Saquinavir contains not less than 98.5 % and not more than 101.0 % of C38H50N6O5, calculated with reference to the dried substance. | ||
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L3JE09KZ2F
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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CHEMBL114
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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N0000190114
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | Cytochrome P450 3A Inhibitors [MoA] | ||
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JJ-79
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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2422
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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63621
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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SUB10446MIG
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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83395
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | RxNorm | ||
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441243
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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Saquinavir
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
|
PRIMARY | |||
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M9776
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | Merck Index | ||
|
L3JE09KZ2F
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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D019258
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
|
PRIMARY | |||
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DTXSID6044012
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY | |||
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100000089169
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
|
PRIMARY | |||
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7161
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
|
PRIMARY | |||
|
127779-20-8
Created by
admin on Wed Jul 05 23:07:37 UTC 2023 , Edited by admin on Wed Jul 05 23:07:37 UTC 2023
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PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TRANSPORTER -> INHIBITOR | |||
|
TRANSPORTER -> INHIBITOR |
SUBSTRATE USED: ESTRONE-3-SULFATE
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TRANSPORTER -> SUBSTRATE | |||
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BINDER->LIGAND |
BINDING
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METABOLIC ENZYME -> SUBSTRATE | |||
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TRANSPORTER -> INHIBITOR | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TRANSPORTER -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT | |||
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TRANSPORTER -> INHIBITOR | |||
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TRANSPORTER -> INHIBITOR |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Volume of Distribution | PHARMACOKINETIC |
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