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

Stem definition	Drug id	CAS RN
peptides and glycopeptides	1010	159519-65-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: enfuvirtide fuzeon pentafuside	Enfuvirtide interferes with the entry of HIV-1 into cells by inhibiting fusion of viral and cellular membranes. Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes. Molecular weight: 4491.95 Formula: C204H301N51O64 CLOGP: LIPINSKI: None HAC: 115 HDO: 63 TPSA: 1902.89 ALOGS: ROTB: 151

Molecule

Description

Molfile Inchi Smiles

Synonyms:

enfuvirtide
fuzeon
pentafuside

Enfuvirtide interferes with the entry of HIV-1 into cells by inhibiting fusion of viral and cellular membranes. Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes.

Molecular weight: 4491.95
Formula: C204H301N51O64
CLOGP:
LIPINSKI: None
HAC: 115
HDO: 63
TPSA: 1902.89
ALOGS:
ROTB: 151

Drug dosage:

Dose	Unit	Route
0.18	g	P

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	4 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	1000 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.57 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	0.36 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.08 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.07 L/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
March 13, 2003	FDA	ROCHE
May 27, 2023	EMA	ROCHE REGISTRATION GMBH

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	544.48	90.84	110	2828	6220	63479864
Jaundice cholestatic	528.48	90.84	110	2828	7214	63478870
Schizophrenia	505.92	90.84	112	2826	9840	63476244
Psychotic disorder	395.73	90.84	111	2827	25601	63460483
Hepatotoxicity	368.38	90.84	114	2824	36927	63449157
Blood bilirubin increased	355.42	90.84	111	2827	37029	63449055
Cholelithiasis	337.10	90.84	111	2827	43814	63442270
Asthma-chronic obstructive pulmonary disease overlap syndrome	189.87	90.84	38	2900	2023	63484061
Total lung capacity increased	185.54	90.84	38	2900	2272	63483812
Hepatic enzyme increased	174.63	90.84	111	2827	202217	63283867

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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
Depression	1027.21	31.47	439	5585	96659	34854248
Drug interaction	719.83	31.47	456	5568	225490	34725417
Mitochondrial toxicity	621.16	31.47	133	5891	2566	34948341
Lipodystrophy acquired	598.24	31.47	134	5890	3210	34947697
Eyelid ptosis	510.89	31.47	131	5893	5635	34945272
Psychiatric decompensation	445.90	31.47	103	5921	2834	34948073
Depression suicidal	407.81	31.47	93	5931	2412	34948495
Tearfulness	396.69	31.47	92	5932	2575	34948332
Loss of personal independence in daily activities	377.42	31.47	159	5865	33020	34917887
Diplopia	360.88	31.47	128	5896	16715	34934192

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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
Depression	905.79	44.63	425	6924	216365	79520674
Drug interaction	706.72	44.63	449	6900	414734	79322305
Mitochondrial toxicity	672.64	44.63	131	7218	2983	79734056
Lipodystrophy acquired	664.73	44.63	137	7212	4188	79732851
Psychotic disorder	618.31	44.63	205	7144	41197	79695842
Eyelid ptosis	512.40	44.63	132	7217	10912	79726127
Psychiatric decompensation	473.56	44.63	102	7247	3861	79733178
Hypomania	448.55	44.63	110	7239	7434	79729605
Depression suicidal	420.45	44.63	92	7257	3750	79733289
Jaundice cholestatic	404.60	44.63	110	7239	11174	79725865

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J05AX07	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Other antivirals
CHEBI has role	CHEBI:59886	HIV fusion inhibitors
FDA EPC	N0000175616	Human Immunodeficiency Virus 1 Fusion Inhibitor
FDA MoA	N0000175615	Fusion Protein 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	D023581	HIV Fusion 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
Pneumonia	contraindication	233604007	DOID:552
Breastfeeding (mother)	contraindication	413712001
Smokes tobacco daily	contraindication	449868002

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.09	acidic
pKa10	12.17	acidic
pKa11	12.25	acidic
pKa12	12.34	acidic
pKa13	12.44	acidic
pKa14	12.6	acidic
pKa15	12.67	acidic
pKa16	12.74	acidic
pKa17	12.82	acidic
pKa18	12.92	acidic

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Orange Book patent data (new drug applications)

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Transmembrane glycoprotein gp41	Membrane other	O40239_9PLVG	INHIBITOR			CHEMBL	CHEMBL
Envelope glycoprotein	Viral envelope protein	Q53I07_9HIV1				WOMBAT-PK
GP41	Unclassified	Q76270_9HIV1		EC50	8	CHEMBL

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External reference:

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ID	Source
009919	NDDF
139896	RXNORM
16130199	PUBCHEM_CID
17175	MMSL
19OWO1T3ZE	UNII
398902008	SNOMEDCT_US
4021375	VUID
4021375	VANDF
409127007	SNOMEDCT_US
46376	MMSL

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Pharmaceutical products:

None