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
CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(N)=O)NC(=O)C4=CC=C5C=CC=CC5=N4
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 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult 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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 Sources: |
unhealthy, adult |
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 |
---|---|---|
Saquinavir soft gelatin capsule: a comparative safety review. | 2001 |
|
Comparison of P-triglyceride levels among patients with human immunodeficiency virus on randomized treatment with ritonavir, indinavir or ritonavir/saquinavir. | 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 |
|
Impact of HIV type 1 protease, reverse transcriptase, cleavage site, and p6 mutations on the virological response to quadruple therapy with saquinavir, ritonavir, and two nucleoside analogs. | 2001 Apr 10 |
|
Differences in the intracellular accumulation of HIV protease inhibitors in vitro and the effect of active transport. | 2001 Apr 13 |
|
Determination of serum levels of thirteen human immunodeficiency virus-suppressing drugs by high-performance liquid chromatography. | 2001 Apr 13 |
|
Determination of interaction kinetic constants for HIV-1 protease inhibitors using optical biosensor technology. | 2001 Apr 15 |
|
High prevalence of genotypic and phenotypic HIV-1 drug-resistant strains among patients receiving antiretroviral therapy in Abidjan, Côte d'Ivoire. | 2001 Apr 15 |
|
A phase II trial of dual protease inhibitor therapy: amprenavir in combination with indinavir, nelfinavir, or saquinavir. | 2001 Apr 15 |
|
[Improving the pharmacokinetics of protease inhibitors in a more innovative manner. HIV drugs administered in a more clever way]. | 2001 Apr 2 |
|
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 |
|
Pharmacokinetics and resistance mutations affect virologic response to ritonavir/saquinavir-containing regimens. | 2001 Aug |
|
Antiviral drugs: current state of the art. | 2001 Aug |
|
Comparison of virologic, immunologic, and clinical response to five different initial protease inhibitor-containing and nevirapine-containing regimens. | 2001 Aug 1 |
|
Steady-state pharmacokinetics of twice-daily dosing of saquinavir plus ritonavir in HIV-1-infected individuals. | 2001 Aug 1 |
|
HIV-protease inhibitors contribute to P-glycoprotein efflux function defect in peripheral blood lymphocytes from HIV-positive patients receiving HAART. | 2001 Aug 1 |
|
[Resistance to protease inhibitors]. | 2001 Feb |
|
Pharmacology and clinical experience with saquinavir. | 2001 Feb |
|
New developments in anti-HIV chemotherapy. | 2001 Jan-Feb |
|
Structure-based design of non-peptide HIV protease inhibitors. | 2001 Jan-Feb |
|
Maternal-fetal transfer of saquinavir studied in the ex vivo placental perfusion model. | 2001 Jul |
|
Predictors of protease inhibitor-associated adverse events. | 2001 Jul |
|
HIV protease inhibitors attenuate adherence of Candida albicans to epithelial cells in vitro. | 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 |
|
Capillary electrophoretic separation of protease inhibitors used in human immunodeficiency virus therapy. | 2001 Jul 13 |
|
High-performance liquid chromatographic assay to determine the plasma levels of HIV-protease inhibitors (amprenavir, indinavir, nelfinavir, ritonavir and saquinavir) and the non-nucleoside reverse transcriptase inhibitor (nevirapine) after liquid-liquid extraction. | 2001 Jul 15 |
|
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 |
|
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 |
|
Design and synthesis of a conformationally restricted trans peptide isostere based on the bioactive conformations of saquinavir and nelfinavir. | 2001 Jun 1 |
|
Selection by AZT and rapid replacement in the absence of drugs of HIV type 1 resistant to multiple nucleoside analogs. | 2001 Jun 10 |
|
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 binding energetics of first- and second-generation HIV-1 protease inhibitors: implications for drug design. | 2001 Jun 15 |
|
A comprehensive account on the role of efflux transporters in the gastrointestinal absorption of 13 commonly used substrate drugs in humans. | 2001 Mar |
|
Sequencing of protease inhibitor therapy: insights from an analysis of HIV phenotypic resistance in patients failing protease inhibitors. | 2001 Mar 30 |
|
The interaction of saquinavir (soft gelatin capsule) with ketoconazole, erythromycin and rifampicin: comparison of the effect in healthy volunteers and in HIV-infected patients. | 2001 May |
|
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 |
|
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 |
|
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 |
|
Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5. | 2001 Sep 14 |
|
Peptide mimetic HIV protease inhibitors are ligands for the orphan receptor SXR. | 2001 Sep 7 |
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
Mon Mar 31 18:03:54 GMT 2025
by
admin
on
Mon Mar 31 18:03:54 GMT 2025
|
Record UNII |
L3JE09KZ2F
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Preferred Name | English | ||
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NDF-RT |
N0000175889
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
||
|
NDF-RT |
N0000000246
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
||
|
WHO-VATC |
QJ05AE01
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
||
|
EMA ASSESSMENT REPORTS |
INVIRASE (AUHTORIZED: HIV INFECTIONS)
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
||
|
EMA ASSESSMENT REPORTS |
FORTOVASE (WITHDRAWN: HIV INFECTIONS)
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
||
|
WHO-ESSENTIAL MEDICINES LIST |
6.4.2.3
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
||
|
WHO-ATC |
J05AE01
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
||
|
NCI_THESAURUS |
C97366
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
||
|
LIVERTOX |
NBK548019
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
7098
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
C29444
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
4813
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
DB01232
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
SAQUINAVIR
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
SAQUINAVIR
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
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. | ||
|
L3JE09KZ2F
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
CHEMBL114
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
N0000190114
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | Cytochrome P450 3A Inhibitors [MoA] | ||
|
JJ-79
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
2422
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
63621
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
SUB10446MIG
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
83395
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | RxNorm | ||
|
441243
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
Saquinavir
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
m9776
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | Merck Index | ||
|
L3JE09KZ2F
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
D019258
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
DTXSID6044012
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
100000089169
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
7161
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY | |||
|
127779-20-8
Created by
admin on Mon Mar 31 18:03:54 GMT 2025 , Edited by admin on Mon Mar 31 18:03:54 GMT 2025
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TRANSPORTER -> INHIBITOR | |||
|
TRANSPORTER -> INHIBITOR | |||
|
BINDER->LIGAND |
BINDING
|
||
|
TARGET -> INHIBITOR |
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
TRANSPORTER -> SUBSTRATE | |||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
TARGET ORGANISM->INHIBITOR |
IC50
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
SALT/SOLVATE -> PARENT |
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
TRANSPORTER -> INHIBITOR | |||
|
METABOLIC ENZYME -> SUBSTRATE |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Volume of Distribution | PHARMACOKINETIC |
|
|
|||