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

Stem definition	Drug id	CAS RN
HIV protease inhibitors	1437	150378-17-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: indinavir indinavir sulphate crixivan indinavir sulfate	A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. Molecular weight: 613.80 Formula: C36H47N5O4 CLOGP: 3.68 LIPINSKI: 1 HAC: 9 HDO: 4 TPSA: 118.03 ALOGS: -4.11 ROTB: 12 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

indinavir
indinavir sulphate
crixivan
indinavir sulfate

A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.

Molecular weight: 613.80
Formula: C36H47N5O4
CLOGP: 3.68
LIPINSKI: 1
HAC: 9
HDO: 4
TPSA: 118.03
ALOGS: -4.11
ROTB: 12

Status: OFM

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

Drug dosage:

Dose	Unit	Route
2.40	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	65 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	27.21 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	18 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.82 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.36 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.02 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
March 13, 1996	FDA	MERCK SHARP DOHME

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
Viral mutation identified	205.68	54.05	32	652	1778	63486560
Drug resistance	139.52	54.05	35	649	22898	63465440
Virologic failure	84.44	54.05	15	669	1847	63486491
Pathogen resistance	76.91	54.05	17	667	6381	63481957

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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
Lipodystrophy acquired	914.30	42.68	164	2313	3180	34951274
Mitochondrial toxicity	774.34	42.68	138	2339	2561	34951893
Eyelid ptosis	669.79	42.68	138	2339	5628	34948826
Diplopia	517.80	42.68	137	2340	16706	34937748
Progressive external ophthalmoplegia	434.80	42.68	77	2400	1358	34953096
Ophthalmoplegia	155.53	42.68	34	2443	1806	34952648
Virologic failure	129.05	42.68	33	2444	3447	34951007
Blood lactic acid increased	111.79	42.68	34	2443	6694	34947760
Dysphagia	101.54	42.68	60	2417	62321	34892133
Pathogen resistance	100.31	42.68	34	2443	9448	34945006

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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
Lipodystrophy acquired	975.88	42.36	162	2581	4163	79737482
Mitochondrial toxicity	846.66	42.36	137	2606	2977	79738668
Eyelid ptosis	673.48	42.36	137	2606	10907	79730738
Diplopia	517.50	42.36	136	2607	33330	79708315
Progressive external ophthalmoplegia	489.74	42.36	77	2666	1368	79740277
Viral mutation identified	241.23	42.36	49	2694	3809	79737836
Virologic failure	163.11	42.36	36	2707	4155	79737490
Ophthalmoplegia	158.61	42.36	33	2710	2879	79738766
Drug resistance	154.21	42.36	57	2686	42156	79699489
Pathogen resistance	127.83	42.36	38	2705	14304	79727341

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J05AE02	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Protease inhibitors
CHEBI has role	CHEBI:35660	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
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D017320	HIV Protease Inhibitors
MeSH PA	D011480	Protease Inhibitors
MeSH PA	D000084762	Viral Protease Inhibitors

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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
Prevention of HIV Infection after Exposure	off-label use
Pyuria	contraindication	4800001	DOID:1439
Hypercholesterolemia	contraindication	13644009
Hyperbilirubinemia	contraindication	14783006	DOID:2741
Cirrhosis of liver	contraindication	19943007	DOID:5082
Blood in urine	contraindication	34436003
Hemolytic anemia	contraindication	61261009	DOID:583
Diabetes mellitus	contraindication	73211009	DOID:9351
Hyperglycemia	contraindication	80394007	DOID:4195

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.82	acidic
pKa2	12.01	acidic
pKa3	6.96	Basic
pKa4	3.56	Basic
pKa5	2.83	Basic

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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
Thromboxane-A synthase	Enzyme	P24557	THAS_HUMAN		IC50	5.73	DRUG MATRIX
Substance-K receptor	GPCR	P21452	NK2R_HUMAN		Ki	5.77	DRUG MATRIX
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	5.77	CHEMBL
Multidrug and toxin extrusion protein 2	Transporter	Q86VL8	S47A2_HUMAN		IC50	5.11	CHEMBL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	6.40	DRUG MATRIX
Pol polyprotein	Enzyme		Q72874_9HIV1	INHIBITOR	Ki	10.15	CHEMBL	CHEMBL
Gag-Pol polyprotein	Polyprotein		POL_HV1BR		IC50	9.22	WOMBAT-PK
Protease	Enzyme		Q4U254_9ENTO		Ki	8.48	CHEMBL
Protease	Enzyme		Q9YQ12_9HIV1		Ki	9.27	CHEMBL
Protease	Unclassified		O90781_9PLVG		Ki	9.06	CHEMBL

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External reference:

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ID	Source
MK1	PDB_CHEM_ID
005733	NDDF
005734	NDDF
108695003	SNOMEDCT_US
108696002	SNOMEDCT_US
114289	RXNORM
12684	IUPHAR_LIGAND_ID
157810-81-6	SECONDARY_CAS_RN
180683-37-8	SECONDARY_CAS_RN
372529006	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
CRIXIVAN	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0570	CAPSULE	100 mg	ORAL	NDA	28 sections
CRIXIVAN	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0571	CAPSULE	200 mg	ORAL	NDA	28 sections
CRIXIVAN	HUMAN PRESCRIPTION DRUG LABEL	1	0006-0573	CAPSULE	400 mg	ORAL	NDA	28 sections
CRIXIVAN	HUMAN PRESCRIPTION DRUG LABEL	1	16590-064	CAPSULE	400 mg	ORAL	NDA	28 sections
CRIXIVAN	HUMAN PRESCRIPTION DRUG LABEL	1	21695-366	CAPSULE	400 mg	ORAL	NDA	27 sections
CRIXIVAN	HUMAN PRESCRIPTION DRUG LABEL	1	53808-0661	CAPSULE	400 mg	ORAL	NDA	27 sections

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