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Showing drug card for Tipranavir (DB00932)

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Creation Date 2005-06-13 13:24:05
Update Date 2009-02-19 16:03:44
Primary Accession Number DB00932
Secondary Accession Number
  • APRD01306
Name Tipranavir
Drug Type
  • Approved
  • Investigational
  • Small Molecule
Description Tipranavir is a nonpeptidic protease inhibitor that targets the HIV protease. It is administered with ritonavir in combination therapy to treat HIV infections.
Synonyms
  1. TPV
  2. tipranavir
Brand Names
  1. Aptivus
  2. Aptivus (Boehringer Ingelheim)
Brand Mixtures Not Available
Chemical IUPAC Name N-[3-[(1R)-1-[(6R)-2-hydroxy-4-oxo-6-(2-phenylethyl)-6-propyl-5H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)pyridine-2-sulfonamide
Chemical Formula C31H33F3N2O5S
Chemical Structure Structure
CAS Registry Number 174484-41-4
InChI Identifier InChI=1/C31H33F3N2O5S/c1-3-16-30(17-15-21-9-6-5-7-10-21)19-26(37)28(29(38)41-30)25(4-2)22-11-8-12-24(18-22)36-42(39,40)27-14-13-23(20-35-27)31(32,33)34/h5-14,18,20,25,36,38H,3-4,15-17,19H2,1-2H3/t25-,30-/m1/s1
InChI Key NZPXPXAGXYTROM-FYBSXPHGBK
KEGG Drug Not Available
KEGG Compound Not Available
PubChem Compound 65027 Link Image
PubChem Substance 206974 Link Image
ChEBI ID Not Available
PharmGKB ID Not Available
HET ID TPV Link Image
GenBank ID Not Available
Drug ID Number [DIN] 02273322 Link Image
RxList Link http://www.rxlist.com/cgi/generic/aptivus.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Tipranavir Link Image
FDA Label
Material Safety Data Sheet (MSDS) Not Available
Synthesis Reference Not Available
Average Molecular Weight 602.6640
Monoisotopic Molecular Weight 602.2062
State Solid
Melting Point Not Available
Experimental Water Solubility Insoluble Source: PhysProp
Predicted Water Solubility 2.07e-04 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 6.9 Source: PhysProp
Predicted LogP 5.71 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -6.46 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES CCC[C@@]1(CCC2=CC=CC=C2)CC(=O)C([C@H](CC)C2=CC(NS(=O)(=O)C3=NC=C(C=C3)C(F)(F)F)=CC=C2)=C(O)O1
Canonical SMILES CCCC1(CCC2=CC=CC=C2)CC(=O)C(C(CC)C2=CC(NS(=O)(=O)C3=NC=C(C=C3)C(F)(F)F)=CC=C2)=C(O)O1
Drug Category
  • Anti-HIV Agents
  • HIV Protease Inhibitors
ATC Codes
AHFS Codes
  • 08:18.08.08
Indication For combination antiretroviral treatment of HIV-1 infected adult patients with evidence of viral replication, who are highly treatment-experienced or have HIV-1 strains resistant to multiple protease inhibitors.
Pharmacology Tipranavir is a non-peptidic protease inhibitor (PI) of HIV. Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Nelfinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.
Mechanism of Action Tipranavir (TPV) is a non-peptidic HIV-1 protease inhibitor that inhibits the virus-specific processing of the viral Gag and Gag-Pol polyproteins in HIV-1 infected cells, thus preventing formation of mature virions.
Absorption Absorption is limited, although no absolute quantification of absorption is available.
Toxicity Oral LD50 in rat is over 5,000 mg/kg. Side effects include thirst and hunger, unexplained weight loss, increased urination, fatigue, and dry, itchy skin.
Protein Binding Extensive (> 99.9%), to both human serum albumin and α-1-acid glycoprotein.
Biotransformation Hepatic. In vitro metabolism studies with human liver microsomes indicated that CYP 3A4 is the predominant CYP enzyme involved in tipranavir metabolism.
Half Life 5-6 hours
Dosage Forms
Form Route
Capsule Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Abacavir Tipranavir decreases the concentration of Abacavir.
Alprazolam Tipranavir may decrease the metabolism and clearance of Alprazolam. Consider alternate therapy or monitor for Alprazolam toxic effects if Tipranavir is initiated or dose increased.
Amiodarone Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Amiodarone. Concomitant therapy is contraindicated.
Amlodipine Tipranavir may decrease the metabolism and clearance of the calcium channel blocker, Amlopidine. Monitor for changes in Amlopidine therapeutic and toxic effects if Tipranavir is initiated, discontinued or dose changed.
Astemizole Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Astemizole. Concomitant therapy is contraindicated.
Atazanavir Tipranavir, co-administered with Ritonavir, may decrease the plasma concentration of Atazanavir. Consider alternate therapy.
Atorvastatin Tipranavir, co-administered with Ritonavir, increases the adverse/toxic effects of Atorvastatin. Concomitant therapy should be avoided.
Bepridil Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Bepridil. Concomitant therapy is contraindicated.
Bromazepam Tipranavir may decrease the metabolism and clearance of Bromazepam. Consider alternate therapy or monitor for Bromazepam toxic effects if Tipranavir is initiated or dose increased.
Bromocriptine Tipranavir may increase the plasma concentration of Bromocriptine. Concomitant therapy should be avoided.
Budesonide Tipranavir may increase the plasma concentration of Budesonide. Monitor for toxic Budesonide effects during concomitant administration.
Carbamazepine Concomitant use may result in decreased Tipranavir and increased Carbamazepine concentrations.
Chlordiazepoxide Tipranavir may decrease the metabolism and clearance of Chlordiazepoxide. Consider alternate therapy or monitor for Alprazolam toxic effects if Tipranavir is initiated or dose increased.
Cisapride Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Cisapride. Concomitant therapy is contraindicated.
Clarithromycin The concentrations of Tipranavir and Clarithromycin increase during concomitant therapy. Dose adjustments are required for patients with renal impairment.
Clobazam Tipranavir may decrease the metabolism and clearance of Clobazam. Consider alternate therapy or monitor for Clobazam toxic effects if Tipranavir is initiated or dose increased.
Clonazepam Tipranavir may decrease the metabolism and clearance of Clonazepam. Consider alternate therapy or monitor for Clonazepam toxic effects if Tipranavir is initiated or dose increased.
Clorazepate Tipranavir may decrease the metabolism and clearance of Clorazepate. Consider alternate therapy or monitor for Clorazepate toxic effects if Tipranavir is initiated or dose increased.
Conjugated Estrogens Conjugated estrogens may increase the adverse dermatological effects (i.e. skin rash) of Tipranavir. Tipranavir may decrease the serum concentration Conjugated estrogens. Monitor for estrogen deficiency during concomitant therapy.
Cyclosporine Tipranavir may affect the efficacy/toxicity of Cyclosporine.
Delavirdine Concomitant use may result in increased Tipranavir and decreased Delavirdine concentrations. Monitor for altered therapeutic and adverse effects of both agents if either agent is initiated, discontinued or dose changed.
Desipramine Tipranavir, co-administered with Ritonavir, may increase the concentration of Desipramine. Monitor Desipramine concentration and efficacy/toxicity and adjust dose as required.
Diazepam Tipranavir may decrease the metabolism and clearance of Diazepam. Consider alternate therapy or monitor for Diazepam toxic effects if Tipranavir is initiated or dose increased.
Didanosine Tipranavir decreases the concentration of Didanosine.
Diethylstilbestrol Diethylstilbestrol may increase the adverse dermatological effects (i.e. skin rash) of Tipranavir. Tipranavir may decrease the serum concentration Diethylstilbestrol. Monitor estrogen levels during concomitant therapy.
Dihydroergotamine Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Dihydroergotamine. Concomitant therapy is contraindicated.
Diltiazem Tipranavir, co-administered with Ritonavir, may alter the concentration of Diltiazem. Monitor for efficacy and adverse/toxic effects of Diltiazem.
Disulfiram Disulfiram may cause Tipranavir (Aptivus brand) toxicity by inhibiting alcohol metabolism. Aptivus capsules contain alcohol.
Efavirenz Efavirenz may alter the serum concentration Tipranavir. Monitor for changes in Tipranavir therapeutic and adverse effects if Efavirenz is initiated, discontinued or dose changed.
Ergoloid mesylate Tipranavir may increase the plasma concentration of Ergoloid mesylates. Concomitant therapy should be avoided.
Ergonovine Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Ergonovine. Concomitant therapy is contraindicated.
Ergotamine Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Ergotamine. Concomitant therapy is contraindicated.
Esomeprazole Tipranavir, co-administered with Ritonavir, may decrease the plasma concentration of Esomeprazole. Consider alternate therapy or increase the dose of Esomeprazole based on the therapeutic response.
Estazolam Tipranavir may decrease the metabolism and clearance of Estazolam. Consider alternate therapy or monitor for Estazolam toxic effects if Tipranavir is initiated or dose increased.
Estradiol Estradiol may increase the adverse dermatological effects (i.e. skin rash) of Tipranavir. Tipranavir may decrease the serum concentration Estradiol. Use an alternate form of contraception or monitor for estrogen deficiency if Estradiol is used for hormone replacement therapy.
Estrone Estropipate may increase the adverse dermatological effects (i.e. skin rash) of Tipranavir. Tipranavir may decrease the serum concentration Estropipate. Monitor for estrogen deficiency during concomitant therapy.
Ethinyl Estradiol Tipranavir, co-administered with Ritonavir, decreases Ethinyl estradiol concentrations. Ethinyl estradiol may increase the adverse dermatological effects (i.e. skin rash) of Tipranavir. Use an alternate form of contraception or monitor for estrogen deficiency if Ethinyl estradiol is used for hormone replacement therapy.
Etravirine Tipranavir, co-administered with Ritonavir, may decrease the effect of Etravirene by decreasing Etravirene serum concentration. Concomitant therapy should be avoided.
Felodipine Tipranavir, co-administered with Ritonavir, may alter the concentration of Felopidine. Monitor for efficacy and adverse/toxic effects of Felopidine.
Flecainide Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Flecainide. Concomitant therapy is contraindicated.
Fluconazole Fluconazole may increase the serum concentration of Tipranavir. Dose adjustments are not required.
Fluoxetine Tipranavir increases the concentration of Fluoxetine. The Fluoxetine dose may require an adjustment.
Flurazepam Tipranavir may decrease the metabolism and clearance of Flurazepam. Consider alternate therapy or monitor for Flurazepam toxic effects if Tipranavir is initiated or dose increased.
Fluticasone Propionate Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Fluticasone propionate. Concomitant therapy should be avoided if possible.
Fosamprenavir Tipranavir, co-administered with Ritonavir, may decrease the plasma concentration of Fosamprenavir. Consider alternate therapy.
Fusidic Acid Concomitant therapy of Tipranavir with Fusidic acid may result in increased serum concentrations of both agents. Consider alternate therapy or monitor for increased serum concentrations and toxocity of both agents.
Isradipine Tipranavir may decrease the metabolism and clearance of the calcium channel blocker, Isradipine. Monitor for changes in Isradipine therapeutic and adverse effects if Tipranavir is initiated, discontinued or dose changed.
Itraconazole Tipranavir may increase the serum concentration of Itraconazole.
Ketoconazole Tipranavir may increase the serum concentration of Ketoconazole.
Lopinavir Tipranavir, co-administered with Ritonavir, may decrease the plasma concentration of Lopinavir. Consider alternate therapy.
Lovastatin Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Lovastatin. Concomitant therapy is contraindicated.
Meperidine Tipranavir may increase the adverse/toxic effects of Meperidine. Consider alternate therapy or monitor for Meperidine toxicity during concomitant use.
Mestranol Mestranol may increase the adverse dermatological effects (i.e. skin rash) of Tipranavir. Tipranavir may decrease the serum concentration Mestranol. Use an alternate form of contraception or monitor for estrogen deficiency if Mestranol is used for hormone replacement therapy.
Methadone Tipranavir, co-administered with Ritonavir, decreases the Methadone concentration. Monitor for symptoms of opiate withdrawal.
Methylergonovine Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Methylergonovine. Concomitant therapy is contraindicated.
Midazolam Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Midazolam. Concomitant therapy is contraindicated.
Nevirapine Nevirapine, a CYP3A4 inducer, may decrease the serum concentration of Tipranavir, a CYP3A4 substrate. Monitor for changesin Tipranavir effect if Nevirapine is initiated, discontinued or dose changed.
Nicardipine Tipranavir, co-administered with Ritonavir, may alter the concentration of Nicardipine. Monitor for efficacy and adverse/toxic effects of Nicardipine.
Nifedipine Tipranavir may decrease the metabolism and clearance of the calcium channel blocker, Nifedipine. Monitor for changes in Nifedipine therapeutic and adverse effects if Tipranavir is initiated, discontinued or dose changed.
Nimodipine Tipranavir may decrease the metabolism and clearance of the calcium channel blocker, Nimodipine. Monitor for changes in Nimodipine therapeutic and adverse effects if Tipranavir is initiated, discontinued or dose changed.
Nisoldipine Tipranavir, co-administered with Ritonavir, may alter the concentration of Nisoldipine. Monitor for efficacy and adverse/toxic effects of Nisoldipine.
Nitrendipine Tipranavir may decrease the metabolism and clearance of the calcium channel blocker, Nitrendipine. Monitor for changes in Nitrendipine therapeutic and adverse effects if Tipranavir is initiated, discontinued or dose changed.
Omeprazole Tipranavir, co-administered with Ritonavir, may decrease the plasma concentration of Omeprazole. Consider alternate therapy or increase the dose of Omeprazole based on the therapeutic response.
Paroxetine Tipranavir increases the concentration of Paroxetine. The Paroxetine dose may require an adjustment.
Pergolide Tipranavir may increase the plasma concentration of Pergolide. Concomitant therapy should be avoided.
Phenobarbital Phenobarbial decreases the concentration of Tipranavir. Monitor for decreased Tipranavir efficacy.
Phenytoin Phenytoin decreases the concentration of Tipranavir. Monitor for decreased Tipranavir efficacy.
Pimozide Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Pimozide. Concomitant therapy is contraindicated.
Posaconazole Tipranavir may increase the serum concentration of Posaconazole. Posaconazole may increase the serum concentration of Tipranavir.
Pravastatin Tipranavir may increase the plasma concentration of Pravastatin. Consider alternate therapy.
Prazepam Tipranavir may decrease the metabolism and clearance of Prazepam. Consider alternate therapy or monitor for Prazepam toxic effects if Tipranavir is initiated or dose increased.
Propafenone Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Propafenone. Concomitant therapy is contraindicated.
Quazepam Tipranavir may decrease the metabolism and clearance of Quazepam. Consider alternate therapy or monitor for Quazepam toxic effects if Tipranavir is initiated or dose increased.
Quinidine Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Quinidine. Concomitant therapy is contraindicated.
Rifabutin Tipranavir increases the concentration of Rifabutin. Adjust Rifabutin dose and monitor for adverse/toxic effects.
Rifampin Rifampin may decrease the plasma concentration of Tipranavir. Concomitant use is not recommended.
Rifapentine Concomitant therapy may cause decreased Tipranavir and increased Rifapentine plasma concentrations.
Rosuvastatin Concomitant therapy of Rosuvastatin and Tipranavir/Ritonavir may increase Rosuvastatin and Tipranavir concentrations. Consider alternate therapy.
Saquinavir Tipranavir, co-administered with Ritonavir, may decrease the plasma concentration of Saquinavir. Consider alternate therapy.
Sertraline Tipranavir increases the concentration of Sertraline. The Sertraline dose may require an adjustment.
Sildenafil Tipranavir, co-administered with Ritonavir, may increase the concentration of Sildenafil. Alternate therapy should be considered.
Simvastatin Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Simvastatin. Concomitant therapy is contraindicated.
Sirolimus Tipranavir may affect the efficacy/toxicity of Sirolimus.
Sodium bicarbonate Sodium bicarbonate may decrease the absorption of Tipranavir. Separate administration of the agents and monitor for decreased efficacy of Tipranavir.
St. John's Wort St. John's Wort may decrease the concentration and efficacy of Tipranavir. Concomitant therapy should be avoided.
Tacrolimus Tipranavir may decrease the metabolism and clearance of Tacrolimus. Dose adjustments may be required. Monitor for Tacrolimus efficacy and toxicity during concomitant therapy.
Tadalafil Tipranavir, co-administered with Ritonavir, may increase the concentration of Tadalafil. Alternate therapy should be considered.
Temsirolimus Tipranavir may affect the efficacy/toxicity of Temsirolimus.
Terfenadine Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Terfenadine. Concomitant therapy is contraindicated.
Theophylline Tipranavir, co-administered with Ritonavir, may decrease the concentration of Theophylline.
Trazodone Tipranavir increases the concentration of Trazodone. Monitor for adverse/toxic effects of Trazodone. Trazodone dose adjustment may be necessary.
Triazolam Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Triazolam. Concomitant therapy is contraindicated.
Valproic Acid Tipranavir decreases the concentration of Valproic acid. Monitor Valproid acid efficacy.
Vardenafil Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Vardenafil. Concomitant therapy is contraindicated.
Verapamil Tipranavir, co-administered with Ritonavir, may alter the concentration of Verapamil. Monitor for efficacy and adverse/toxic effects of Verapamil.
Voriconazole Tipranavir may alter the serum concentration of Voriconazole.
Zidovudine Tipranavir decreases the concentration of Zidovudine.
Food Interactions Not Available
Pathways Not Available
General References
  1. Doyon L, Tremblay S, Bourgon L, Wardrop E, Cordingley MG: Selection and characterization of HIV-1 showing reduced susceptibility to the non-peptidic protease inhibitor tipranavir. Antiviral Res. 2005 Oct;68(1):27-35. [PubMed Link Image]
  2. Wikipedia Link Image
  3. RxList Link Image
Organisms Affected
  • Human Immunodeficiency Virus
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 3A4 (CYP3A4)
Targets
  1. HIV-1 protease
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 3A4 (CYP3A4)
Enzyme 1 Gene Name CYP3A4
Enzyme 1 SwissProt ID P08684 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P08684|CP3A4_HUMAN Cytochrome P450 3A4 (EC 1.14.13.67) 
ALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMFD
MECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISIA
EDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYSM
DVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICVF
PREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSII
FIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVVN
ETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERFSK
KNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLGG
LLQPEKPVVLKVESRDGTVSGA
Drug Target 1 [top]
Target 1 ID 731
Target 1 Name HIV-1 protease
Target 1 Synonyms
  1. Fragment
Target 1 Gene Name HIV-1 protease
Target 1 Protein Sequence >HIV-1 protease 
PQVTLWQRPIVTIKIGGQLKEALLDTGADDTVLEEMSLPGKWKPKMIGGIGGFIKVRQYD
QVSIEICGHKAIGTVLIGPTPVNIIGRNLLTQLGCTLNF
Target 1 Number of Residues 100
Target 1 Molecular Weight 10725
Target 1 Theoretical pI 8.77
Target 1 GO Classification
Function
catalytic activity
hydrolase activity
peptidase activity
endopeptidase activity
aspartic-type endopeptidase activity
Process
physiological process
metabolism
macromolecule metabolism
protein metabolism
cellular protein metabolism
proteolysis
Component
Not Available
Target 1 General Function Involved in aspartic-type endopeptidase activity
Target 1 Specific Function Not Available
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • None
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 4377614 Link Image
Target 1 UniProtKB/Swiss-Prot ID O90777 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name O90777_9PLVG Link Image
Target 1 PDB ID 1ODW Link Image
Target 1 PDB File Show
Target 1 3D Structure
Target 1 Cellular Location
  • Cytoplasmic
Target 1 Gene Sequence >297 bp 
CCTCAGGTCACTCTTTGGCAACGACCCATAGTCACAATAAAGATAGGGGGGCAACTAAAG
GAAGCTCTATTAGATACAGGAGCAGATGATACAGTATTAGAAGAAATGAGTTTGCCAGGA
AAATGGAAACCAAAAATGATAGGGGGAATTGGAGGTTTTATCAAAGTAAGACAGTATGAT
CAGGTATCCATAGAAATCTGCGGACATAAAGCTATAGGTACAGTATTAATAGGACCTACA
CCTGTCAACATAATTGGAAGGAATCTGTTGACTCAGCTTGGCTGCACTTTAAATTTT
Target 1 GenBank Gene ID
Target 1 GeneCard ID Not Available
Target 1 GenAtlas ID Not Available
Target 1 HGNC ID Not Available
Target 1 Chromosome Location Not Available
Target 1 Locus Not Available
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Servais J, Lambert C, Fontaine E, Plesseria JM, Robert I, Arendt V, Staub T, Schneider F, Hemmer R, Burtonboy G, Schmit JC: Comparison of DNA sequencing and a line probe assay for detection of human immunodeficiency virus type 1 drug resistance mutations in patients failing highly active antiretroviral therapy. J Clin Microbiol. 2001 Feb;39(2):454-9. [PubMed Link Image]
  2. Servais J, Lambert C, Fontaine E, Plesseria JM, Robert I, Arendt V, Staub T, Schneider F, Hemmer R, Burtonboy G, Schmit JC: Variant human immunodeficiency virus type 1 proteases and response to combination therapy including a protease inhibitor. Antimicrob Agents Chemother. 2001 Mar;45(3):893-900. [PubMed Link Image]
Target 1 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
  3. Koh Y, Matsumi S, Das D, Amano M, Davis DA, Li J, Leschenko S, Baldridge A, Shioda T, Yarchoan R, Ghosh AK, Mitsuya H: Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization. J Biol Chem. 2007 Sep 28;282(39):28709-20. Epub 2007 Jul 17. [PubMed Link Image]
  4. Dierynck I, De Wit M, Gustin E, Keuleers I, Vandersmissen J, Hallenberger S, Hertogs K: Binding kinetics of darunavir to HIV-1 protease explain the potent antiviral activity and high genetic barrier. J Virol. 2007 Oct 10;. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.