tipranavir Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
HIV protease inhibitors 3609 174484-41-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tipranavir
  • aptivus
  • PNU-140690
  • PNU 140690
Tipranavir is an 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.
  • Molecular weight: 602.67
  • Formula: C31H33F3N2O5S
  • CLOGP: 7.76
  • LIPINSKI: 2
  • HAC: 7
  • HDO: 2
  • TPSA: 105.59
  • ALOGS: -6.47
  • ROTB: 11

Drug dosage:

DoseUnitRoute
1 g O

Approvals:

DateAgencyCompanyOrphan
June 22, 2005 FDA BOEHRINGER INGELHEIM

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cloacal exstrophy 231.68 98.24 23 367 5 4638597
Bladder agenesis 215.07 98.24 22 368 14 4638588
Lipodystrophy acquired 201.86 98.24 29 361 771 4637831
Genitalia external ambiguous 195.65 98.24 22 368 65 4638537
Tethered cord syndrome 188.60 98.24 21 369 55 4638547
Caudal regression syndrome 187.26 98.24 21 369 60 4638542
Meconium stain 185.28 98.24 21 369 68 4638534
Gastrointestinal disorder congenital 179.95 98.24 19 371 23 4638579
Meningomyelocele 178.97 98.24 23 367 254 4638348
Umbilical cord abnormality 173.98 98.24 22 368 211 4638391
Exomphalos 171.66 98.24 22 368 237 4638365
Drug resistance 151.89 98.24 32 358 8104 4630498
Congenital genital malformation 142.75 98.24 16 374 45 4638557
Viral mutation identified 138.70 98.24 22 368 1137 4637465
Anal atresia 128.41 98.24 17 373 238 4638364
Blood iron decreased 127.50 98.24 22 368 1907 4636695
Spine malformation 118.47 98.24 15 375 144 4638458
Gastrointestinal malformation 115.94 98.24 14 376 87 4638515

Pharmacologic Action:

SourceCodeDescription
ATC J05AE09 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Protease inhibitors
FDA MoA N0000000246 HIV Protease Inhibitors
FDA EPC N0000175889 Protease Inhibitor
MeSH PA D019380 Anti-HIV Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D044966 Anti-Retroviral Agents
MeSH PA D000998 Antiviral Agents
CHEBI has role CHEBI:36044 antiviral drug

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Human immunodeficiency virus infection indication 86406008 DOID:526
Intracranial hemorrhage contraindication 1386000
Hypercholesterolemia contraindication 13644009
Hyperbilirubinemia contraindication 14783006 DOID:2741
Hereditary factor VIII deficiency disease contraindication 28293008 DOID:12134
Hereditary factor IX deficiency disease contraindication 41788008 DOID:12259
Hepatic failure contraindication 59927004
Chronic type B viral hepatitis contraindication 61977001
Blood coagulation disorder contraindication 64779008 DOID:1247
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Procedure on central nervous system contraindication 118679007
Neoplasm of brain contraindication 126952004 DOID:1319
Inflammatory disease of liver contraindication 128241005
Chronic hepatitis C contraindication 128302006
Liver function tests abnormal contraindication 166603001
Disease of liver contraindication 235856003 DOID:409
Lesion of brain contraindication 301766008
Hypertriglyceridemia contraindication 302870006
Surgical procedure contraindication 387713003
Breastfeeding (mother) contraindication 413712001
Traumatic injury contraindication 417746004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.13 acidic
pKa2 6.12 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Multidrug resistance protein 1 Transporter WOMBAT-PK
Cathepsin D Enzyme Ki 4.82 CHEMBL
Pepsin A-5 Enzyme Ki 5.70 CHEMBL
Cathepsin E Enzyme Ki 5.05 CHEMBL
Pol polyprotein Enzyme INHIBITOR IC50 7.52 CHEMBL CHEMBL
CAAX prenyl protease 1 homolog Enzyme IC50 5.92 CHEMBL

External reference:

IDSource
4024917 VUID
N0000171602 NUI
C0663733 UMLSCUI
D08605 KEGG_DRUG
418721002 SNOMEDCT_US
190548 RXNORM
20182 MMSL
d05538 MMSL
419409009 SNOMEDCT_US
4024917 VANDF
010844 NDDF
CHEMBL222559 ChEMBL_ID
DB00932 DRUGBANK_ID
TPV PDB_CHEM_ID
CHEBI:63628 CHEBI
ZZT404XD09 UNII
7774 INN_ID
54682461 PUBCHEM_CID
C107201 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Aptivus HUMAN PRESCRIPTION DRUG LABEL 1 0597-0002 SOLUTION 100 mg ORAL NDA 19 sections
Aptivus HUMAN PRESCRIPTION DRUG LABEL 1 0597-0003 CAPSULE, LIQUID FILLED 250 mg ORAL NDA 19 sections