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tipranavir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
HIV protease inhibitors	3609	174484-41-4

Description:

Molecule	Description
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. There was some evidence of in vitro activity against SARS-CoV-2, but no clinical trial data was found to support use in the treatment of COVID-19. Molecular weight: 602.67 Formula: C31H33F3N2O5S CLOGP: 7.76 LIPINSKI: 2 HAC: 7 HDO: 2 TPSA: 105.59 ALOGS: -6.47 ROTB: 11 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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. There was some evidence of in vitro activity against SARS-CoV-2, but no clinical trial data was found to support use in the treatment of COVID-19.

Molecular weight: 602.67
Formula: C31H33F3N2O5S
CLOGP: 7.76
LIPINSKI: 2
HAC: 7
HDO: 2
TPSA: 105.59
ALOGS: -6.47
ROTB: 11

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
1	g	O

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	23.70 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
June 22, 2005	FDA	BOEHRINGER INGELHEIM

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypomania	499.87	263.68	98	2159	6232	63480533
Jaundice cholestatic	485.61	263.68	98	2159	7226	63479539
Schizophrenia	461.33	263.68	99	2158	9853	63476912
Psychotic disorder	358.45	263.68	97	2160	25615	63461150
Hepatotoxicity	349.68	263.68	103	2154	36938	63449827
Blood bilirubin increased	327.52	263.68	98	2159	37042	63449723
Cholelithiasis	315.49	263.68	99	2158	43826	63442939

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Virologic failure	88.52	41.68	20	878	3460	34952573
Acquired immunodeficiency syndrome	83.54	41.68	14	884	504	34955529
Dyschromatopsia	58.60	41.68	10	888	401	34955632
Viral mutation identified	54.04	41.68	13	885	2941	34953092
Drug resistance	52.37	41.68	21	877	25906	34930127
Multiple-drug resistance	51.27	41.68	14	884	5225	34950808
HIV infection	46.81	41.68	10	888	1329	34954704
Viral load increased	45.59	41.68	11	887	2516	34953517

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypomania	498.74	90.75	98	2305	7446	79734539
Jaundice cholestatic	459.39	90.75	98	2305	11186	79730799
Schizophrenia	434.18	90.75	99	2304	15341	79726644
Psychotic disorder	337.28	90.75	99	2304	41303	79700682
Hepatotoxicity	333.13	90.75	103	2300	51249	79690736
Cholelithiasis	317.97	90.75	100	2303	52564	79689421
Blood bilirubin increased	295.44	90.75	100	2303	66132	79675853
Hepatic enzyme increased	209.23	90.75	104	2299	182506	79559479
Total lung capacity increased	202.06	90.75	38	2365	2260	79739725
Asthma-chronic obstructive pulmonary disease overlap syndrome	189.26	90.75	38	2365	3183	79738802

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J05AE09	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Protease inhibitors
CHEBI has role	CHEBI:35660	HIV protease inhibitors
CHEBI has role	CHEBI:36044	antiviral drugs
FDA EPC	N0000175889	Protease Inhibitor
FDA MoA	N0000000246	HIV Protease Inhibitors
MeSH PA	D019380	Anti-HIV Agents
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D044966	Anti-Retroviral Agents
MeSH PA	D000998	Antiviral Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Pepsin A-5	Enzyme	P0DJD9	PEPA5_HUMAN		Ki	5.70	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN				WOMBAT-PK
Cathepsin D	Enzyme	P07339	CATD_HUMAN		Ki	4.82	CHEMBL
Cathepsin E	Enzyme	P14091	CATE_HUMAN		Ki	5.05	CHEMBL
Pol polyprotein	Enzyme		Q72874_9HIV1	INHIBITOR	IC50	7.52	CHEMBL	CHEMBL
CAAX prenyl protease 1 homolog	Enzyme		FACE1_MOUSE		IC50	5.92	CHEMBL

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External reference:

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ID	Source
TPV	PDB_CHEM_ID
010844	NDDF
12685	IUPHAR_LIGAND_ID
190548	RXNORM
20182	MMSL
4024917	VUID
4024917	VANDF
418721002	SNOMEDCT_US
419409009	SNOMEDCT_US
54682461	PUBCHEM_CID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Aptivus	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0002	SOLUTION	100 mg	ORAL	NDA	32 sections
Aptivus	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0002	SOLUTION	100 mg	ORAL	NDA	32 sections
Aptivus	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0003	CAPSULE, LIQUID FILLED	250 mg	ORAL	NDA	32 sections
Aptivus	HUMAN PRESCRIPTION DRUG LABEL	1	0597-0003	CAPSULE, LIQUID FILLED	250 mg	ORAL	NDA	32 sections

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