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 |
|---|---|---|
| Antiviral strategies combining antiretroviral drugs with RNAi-mediated attack on HIV-1 and cellular co-factors. | 2013-04 |
|
| Development of the next generation of HIV-1 integrase inhibitors: pyrazolone as a novel inhibitor scaffold. | 2010-11-15 |
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| Novel recombinant engineered gp41 N-terminal heptad repeat trimers and their potential as anti-HIV-1 therapeutics or microbicides. | 2010-08-13 |
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| HIV-1 fusion inhibitor peptides enfuvirtide and T-1249 interact with erythrocyte and lymphocyte membranes. | 2010-03-23 |
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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. | 2009-08 |
|
| Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus. | 2007-07-31 |
|
| Discovery and optimization of a natural HIV-1 entry inhibitor targeting the gp41 fusion peptide. | 2007-04-20 |
|
| Protein design of a bacterially expressed HIV-1 gp41 fusion inhibitor. | 2007-04-10 |
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| An anti-HIV microbicide engineered in commensal bacteria: secretion of HIV-1 fusion inhibitors by lactobacilli. | 2006-10-03 |
|
| Inhibition of HIV-1 group M and O isolates by fusion inhibitors. | 2005-11-04 |
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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| Record Version |
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Preferred Name | English | ||
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Official Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Code | English |
| Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C1660
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DTXSID70179833
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M6W86MD258
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300000025276
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DB05413
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16130644
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C152617
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CHEMBL2108654
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8467
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251562-00-2
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TARGET ORGANISM->INHIBITOR |
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| AMINO_ACID_SUBSTITUTION | [1_1] | N-TERMINUS | TRYPTOPHAN | N-ACETYL-L-TRYPTOPHAN | U9264T8OAE | |
| AMINO_ACID_SUBSTITUTION | [1_39] | C-TERMINUS | PHENYLALANINE |
Amount:
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PHENYLALANYLAMIDE | PV9T9B2S11 |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT:NUMBER AVERAGE(CALCULATED) | CHEMICAL |
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| Molecular Formula | CHEMICAL |
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