Tifuvirtide (also known as T 1249) is a synthetically designed hybrid retroviral envelope polypeptide patented by Trimeris, Inc. as fusion inhibitor useful for the treatment of HIV infection. Tifuvirtide binds to HIV glycoprotein 41 (gp41) and prevents its fusogenic conformation, inhibiting viral entry into host cells. Tifuvirtide is composed of sequences from HIV-1, HIV-2, and simian immunodeficiency virus. Tifuvirtide has greater potency in vitro, compared with enfuvirtide, and elicits activity against most enfuvirtide-resistant isolates in vitro and in vivo. A successful short-term phase 1/2 studies evaluation of antiretroviral activity and safety in humans proved the potential of this new drug, although further clinical development was discontinued.
Approval Year
PubMed
Title | Date | PubMed |
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Inhibition of HIV-1 group M and O isolates by fusion inhibitors. | 2005 Nov 4 |
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An anti-HIV microbicide engineered in commensal bacteria: secretion of HIV-1 fusion inhibitors by lactobacilli. | 2006 Oct 3 |
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Protein design of a bacterially expressed HIV-1 gp41 fusion inhibitor. | 2007 Apr 10 |
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Discovery and optimization of a natural HIV-1 entry inhibitor targeting the gp41 fusion peptide. | 2007 Apr 20 |
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Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus. | 2007 Jul 31 |
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Combinations of the first and next generations of human immunodeficiency virus (HIV) fusion inhibitors exhibit a highly potent synergistic effect against enfuvirtide- sensitive and -resistant HIV type 1 strains. | 2009 Aug |
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Novel recombinant engineered gp41 N-terminal heptad repeat trimers and their potential as anti-HIV-1 therapeutics or microbicides. | 2010 Aug 13 |
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HIV-1 fusion inhibitor peptides enfuvirtide and T-1249 interact with erythrocyte and lymphocyte membranes. | 2010 Mar 23 |
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Development of the next generation of HIV-1 integrase inhibitors: pyrazolone as a novel inhibitor scaffold. | 2010 Nov 15 |
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Antiviral strategies combining antiretroviral drugs with RNAi-mediated attack on HIV-1 and cellular co-factors. | 2013 Apr |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15747252
192 mg/day
Route of Administration:
Other
Substance Class |
Protein
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Protein Type | PEPTIDE |
Protein Sub Type | |
Sequence Type | COMPLETE |
Record UNII |
M6W86MD258
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Record Status |
Validated (UNII)
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C1660
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MOL_WEIGHT:NUMBER AVERAGE(CALCULATED) | CHEMICAL |
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Molecular Formula | CHEMICAL |
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