Enfuvirtide

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Enfuvirtide
Clinical data
Trade namesFuzeon
AHFS/Drugs.comMonograph
MedlinePlusa603023
License data
Pregnancy
category
Subcutaneous
ATC code
Legal status
Legal status
JSmol)
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Enfuvirtide (

AIDS/HIV
.

Medical uses

Enfuvirtide is

indicated for the treatment of HIV-1 infection, in combination therapy with other antiretrovirals, in people where all other treatments have failed.[2]

Adverse effects

Common

rechallenge is not recommended.[2]

Pharmacology

Mechanism of action

Enfuvirtide works by disrupting the

fusion inhibitors.[citation needed
]

HIV binds to the host CD4+ cell receptor via the viral protein gp120; gp41, a viral transmembrane protein, then undergoes a conformational change that assists in the fusion of the viral membrane to the host cell membrane. Enfuvirtide binds to gp41 preventing the creation of an entry pore for the capsid of the virus, keeping it out of the cell.[3]

Enfuvirtide is also an activator of the chemotactic factor receptor, formyl peptide receptor 1, and thereby activates phagocytes and presumably other cells bearing this receptor (see

formyl peptide receptors).[4] The physiological significance of this activation is unknown.[citation needed
]

Microbiology

Enfuvirtide is considered to be active against HIV-1 only. Low activity against HIV-2 isolates has been demonstrated in vitro.[5]

Variable susceptibility to enfuvirtide has been observed in clinical isolates, with

acquired resistance the result of a mutated 10 amino acid motif in viral gp41. Primary resistance, however, has yet to be observed.[6]

Structural formula

Enfuvirtide is a 36-amino acid peptide with the following sequence:[7][8]

Asp-Lys-Trp-Ala-Ser-Leu-Trp-Asn-Trp-Phe-NH2
(Ac-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-NH2)

History

Enfuvirtide originated at

fusion inhibitor, a new class of antiretroviral drugs. It was approved on the basis of two studies which compared the effect of optimized regimens of antiretroviral medication with and without the addition of enfuvirtide on serum viral load.[citation needed
]

References

  1. ^ a b "Product". guildlink.com.au. Archived from the original on 8 January 2023. Retrieved 8 January 2023.
  2. ^
    ISBN 0-9757919-2-3
    .
  3. S2CID 32014873
    .
  4. PMID 10339497
    .
  5. ^ Roche Products Pty Ltd. Fuzeon (Australian Approved Product Information). Dee Why (NSW): Roche; 2005.
  6. PMID 15231762
    .
  7. PMID 7786578
    .
  8. PMID 7543152
    .
  9. ^ "Drugs@FDA: FDA Approved Drug Products – Fuzeon (Click on 'Approval Date(s) and History, Letters, Labels, Reviews for NDA 021481')". accessdata.fda.gov. United States Food and Drug Administration. Archived from the original on 28 June 2017. Retrieved 6 January 2019.
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