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1. Dp 178
2. Dp-178
3. Dp178
4. Fuzeon
5. Pentafuside
6. Peptide T20
7. T20 Peptide
8. T20, Peptide
1. Pentafuside
2. Fuzeon
3. Dp178
4. Dp-178
5. T-20
6. Chebi:608828
7. T 20
8. Ac-ytslihslieesqnqqekneqelleldkwaslwnwf-nh2
9. T20
10. Dp 178
11. Fuzeon (tm)
12. Fuzeon T-20
13. T 20 (peptide)
14. Enfurvitide (t-20)
15. Enfuvirtide+pro 140
16. Enfuvirtide + T1144
17. Tnx-355 & Efuvirtide
18. Unii-19owo1t3ze
19. 19owo1t3ze
20. T20-lai
21. Enfuvirtide [usan:inn:ban]
22. Chembl525076
23. Hsdb 7341
24. Dtxsid20166672
25. Gna & G-20
26. Hha & T-20
27. Pentafuside (trivial Name)
28. Bdbm50023615
29. T-20+pro 140
30. Gp41 127-162 Aa
31. 5a8 & T-20
32. R-698
33. T20 + T1144
34. Ac-ytslihslieesqnqqekneqelleldkwaslwnwf-nh2 & Pro 140 (anti-ccr5 Monoclonal Antibody)
35. Humanized Monoclonal Antibody To Cd4 & Ac-ytslihslieesqnqqekneqelleldkwaslwnwf-nh2
36. Ac-tyr-thr-ser-leu-ile-his-ser-leu-ile-glu-glu-ser-gln-asn-gln-gln-glu-lys-asn-glu-gln-glu-leu-leu-glu-leu-asp-lys-trp-ala-ser-leu-trp-asn-trp-phe-nh2 & Galanthus Nivalis Agglutinin (gna)
37. Ac-tyr-thr-ser-leu-ile-his-ser-leu-ile-glu-glu-ser-gln-asn-gln-gln-glu-lys-asn-glu-gln-glu-leu-leu-glu-leu-asp-lys-trp-ala-ser-leu-trp-asn-trp-phe-nh2 & Hippeastrum Hybrid Agglutinin( Hha)
38. Acetyl-tyr-thr-ser-leu-ile-his-ser-leu-ile-glu-glu-ser-gln-asn-gln-gln-glu-lys-asn-glu-gln-glu-leu-leu-glu-leu-asp-lys-trp-ala-ser-leu-trp-asn-trp-phe-nh2
39. Actyrthrserleuilehisserleuileglugluserglnasnglnglnglulysasngluglngluleuleugluleuasplystrpalaserleutrpasntrpphenh2
40. T-20-lai [ac-tyr-thr-ser-leu-ile-his-ser-leu-ile-glu-glu-ser-gln-asn-gln-gln-glu-lys-asn-glu-gln-glu-leu-leu-glu-leu-asp-lys-trp-ala-ser-leu-trp-asn-trp-phe-nh2]
| Molecular Weight | 4492 g/mol |
|---|---|
| Molecular Formula | C204H301N51O64 |
| XLogP3 | -14.7 |
| Hydrogen Bond Donor Count | 63 |
| Hydrogen Bond Acceptor Count | 67 |
| Rotatable Bond Count | 151 |
| Exact Mass | 4491.1933541 g/mol |
| Monoisotopic Mass | 4489.1866445 g/mol |
| Topological Polar Surface Area | 1900 Ų |
| Heavy Atom Count | 319 |
| Formal Charge | 0 |
| Complexity | 11200 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 39 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
| 1 of 2 | |
|---|---|
| Drug Name | Fuzeon |
| PubMed Health | Enfuvirtide (Injection) |
| Drug Classes | Antiretroviral Agent |
| Active Ingredient | Enfuvirtide |
| Dosage Form | Injectable |
| Route | Subcutaneous |
| Strength | 90mg/vial |
| Market Status | Prescription |
| Company | Roche |
| 2 of 2 | |
|---|---|
| Drug Name | Fuzeon |
| PubMed Health | Enfuvirtide (Injection) |
| Drug Classes | Antiretroviral Agent |
| Active Ingredient | Enfuvirtide |
| Dosage Form | Injectable |
| Route | Subcutaneous |
| Strength | 90mg/vial |
| Market Status | Prescription |
| Company | Roche |
Enfuvirtide is used in combination with other antiretroviral agents for the treatment of HIV-1 infection in treatment-experienced patients with evidence of HIV-1 replication despite ongoing antiretroviral therapy. Enfuvirtide must be paired with at least one other antiretroviral agent that is active in vitro according to HIV resistance tests and drug history. This indication is based on analyses of plasma HIV-1 RNA levels and CD4 cell counts in controlled studies of /enfuvirtide/ of 24 weeks duration. Subjects enrolled were treatment-experienced adults; many had advanced disease. There are no studies of /enfutide/ in antiretroviral naive patients. There are no results from controlled trials evaluating the effect of /enfuvirtide/ on clinical progression of HIV-1. /Included in US product labeling/
Thomson.Micromedex. Drug Information for the Health Care Professional. 25th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2005., p. 1269
Hypersensitivity reactions, including rash, fever, nausea and vomiting, chills, rigors, hypotension, and elevated serum liver transaminase concentrations, have been reported in up to 1% of patients receiving enfuvirtide; these hypersensitivity reactions have recurred on rechallenge. Other adverse events reported in patients receiving enfuvirtide that may be immune mediated include primary immune complex reactions, respiratory distress, glomerulonephritis, and Guillain-Barre syndrome. Patients experiencing signs and symptoms suggestive of a systemic hypersensitivity reaction should discontinue enfuvirtide and seek immediate medical evaluation. Enfuvirtide therapy should not be reinitiated in patients who have experienced systemic signs and symptoms consistent with a hypersensitivity reaction while receiving the drug.
McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 618
The incidence of bacterial pneumonia in patients receiving enfuvirtide in phase III clinical studies was higher than the incidence in control patients (4.68 pneumonia events per 100 patient-years versus 0.61 events per 100 patient years, respectively). Risk factors for pneumonia included low initial CD4+ T-cell count, high initial viral load, IV drug abuse, smoking, and history of lung disease. Although the increased incidence of pneumonia has not been directly attributed to the drug, HIV-infected patients receiving enfuvirtide (especially those with underlying conditions that may predispose them to pneumonia) should be monitored carefully for signs and symptoms of pneumonia.
McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 618
Subcutaneous injection of enfuvirtide has been associated with reactions at the site of administration, including mild to moderate pain/discomfort, induration, erythema, presence of nodules or cysts, pruritus, and ecchymosis, in up to 98% of patients. In clinical studies, injection site reactions occurred during the first week of therapy in 86% of patients; in most patients, the severity of these reactions did not change during the 24-week study. Individual injection site reactions persisted for longer than 7 days in 17% of patients. Because of the frequency and duration of these reactions, injection site reactions often were present at more than one site. Ongoing reactions at 6 or more sites were present in 23% of patients enrolled in clinical studies.
McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 618
The most common adverse effects reported with enfuvirtide are injection site reactions. Other adverse effects reported in 2% or more of patients receiving enfuvirtide in conjunction with other antiretrovirals include abdominal pain, anorexia, anxiety, asthenia, conjunctivitis, constipation, cough, decreased weight, decreased appetite, depression, herpes simplex, influenza or influenza-like illness, insomnia, lymphadenopathy, myalgia, pancreatitis, peripheral neuropathy, pruritus, sinusitis, skin papilloma, and taste disturbance.
McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 619
For more Drug Warnings (Complete) data for ENFUVIRTIDE (10 total), please visit the HSDB record page.
Enfuvirtide is an antiretroviral drug used in combination therapy for the treatment of HIV-1/AIDS.
FDA Label
Fuzeon is indicated in combination with other antiretroviral medicinal products for the treatment of HIV-1-infected patients who have received treatment with and failed on regimens containing at least one medicinal product from each of the following antiretroviral classes: protease inhibitors, non-nucleoside reverse-transcriptase inhibitors and nucleoside reverse-transcriptase inhibitors, or who have intolerance to previous antiretroviral regimens.
In deciding on a new regimen for patients who have failed an antiretroviral regimen, careful consideration should be given to the treatment history of the individual patient and the patterns of mutations associated with different medicinal products. Where available, resistance testing may be appropriate.
HIV Fusion Inhibitors
Inhibitors of the fusion of HIV to host cells, preventing viral entry. This includes compounds that block attachment of HIV ENVELOPE PROTEIN GP120 to CD4 RECEPTORS. (See all compounds classified as HIV Fusion Inhibitors.)
J05AX07
J - Antiinfectives for systemic use
J05 - Antivirals for systemic use
J05A - Direct acting antivirals
J05AX - Other antivirals
J05AX07 - Enfuvirtide
Absorption
After a 90 mg single subcutaneous injection of Enfuvirtide into the abdomen in 12 HIV-1 infected subjects, the mean peak concentration is 4.59+/-1.5 ug/ml and the median time to peak concentration was 8 hours (ranged from 3 to12 hours).
Volume of Distribution
5.5 1.1 L
Clearance
24.8 +/- 4.1 mL/h/kg [HIV-1 infected adult and pediatric subjects following a 90-mg single SC dose of enfuvirtide]
30.6 +/- 10.6 mL/h/kg [Following 90-mg twice daily dosing of FUZEON SC in combination with other antiretroviral agents in HIV-1 infected subjects]
40 +/- 17 mL/h/kg [pediatric patients in the presence of concomitant medications including antiretroviral agents receiving the 2 mg/kg twice daily dose]
Enfuvirtide is almost completely absorbed following subcutaneous injection (absolute bioavailability: 84.3%), and systemic absorption is comparable following subcutaneous injection of a ... dose into the abdomen, thigh, or arm. ...
McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 619
Following a 90-mg single subcutaneous injection of /enfuvirtide/ into the abdomen in 12 HIV-1 infected subjects, the mean (+/-SD) Cmax was 4.59 +/- 1.5 ug/mL, AUC was 55.8 +/- 12.1 ughr/mL and the median Tmax was 8 hours (ranged from 3 to 12 hr).
Physicians Desk Reference. 59th ed. Thomson PDR. Montvale, NJ 2005., p. 2882
Protein binding: 92% bound to plasma proteins over a concentration range of 2 to 10 ug/mL; predominantly bound to albumin and somewhat bound to alpha-1 acid glycoprotein.
Thomson.Micromedex. Drug Information for the Health Care Professional. 25th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2005., p. 1269
Volume of Distribution: (VolD): 5.5 + or - 1.1 L.
Thomson.Micromedex. Drug Information for the Health Care Professional. 25th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2005., p. 1269
For more Absorption, Distribution and Excretion (Complete) data for ENFUVIRTIDE (8 total), please visit the HSDB record page.
Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool.
In vitro studies with human microsomes and hepatocytes indicate that enfuvirtide undergoes hydrolysis to form a deamidated metabolite at the C-terminal phenylalanine residue, M3. The hydrolysis reaction is not NADPH dependent. The M3 metabolite is detected in human plasma following administration of enfuvirtide, with an AUC ranging from 2.4% to 15% of the enfuvirtide AUC.
Physicians Desk Reference. 59th ed. Thomson PDR. Montvale, NJ 2005., p. 2882
3.8 +/- 0.6 hrs
Following a 90-mg single subcutaneous dose of enfuvirtide (N=12) the mean +/-SD elimination half-life of enfuvirtide is 3.8 +/- 0.6 hr...
Physicians Desk Reference. 59th ed. Thomson PDR. Montvale, NJ 2005., p. 2882
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. By disrupting the HIV-1 molecular machinery during its final stage of fusion with the target cell, enfuvirtide limits the spread of further infection. Enfuvirtide is a biomimetic peptide that was rationally designed to mimic components of the HIV-1 fusion machinery and displace them, preventing normal fusion.
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 conformational changes required for fusion of viral and cellular membranes.
Thomson.Micromedex. Drug Information for the Health Care Professional. 25th ed. Volume 1. Plus Updates. Content Reviewed by the United States Pharmacopeial Convention, Inc. Greenwood Village, CO. 2005., p. 1269
Enfuvirtide, a synthetic antiretroviral agent, is a human immunodeficiency virus (HIV) fusion inhibitor. Enfuvirtide is a synthetic 36-amino acid peptide that interferes with entry of HIV type 1 (HIV-1) into target cells by inhibiting fusion of the viral and cellular membranes. Enfuvirtide binds to heptad repeat 1 (HR1) in the envelope glycoprotein 41 (gp41) of HIV-1 that is involved in fusion of the virus with the membrane of the host CD4+ T-cell. Binding of enfuvirtide to gp41 blocks conformational changes in the HIV-1 glycoprotein that are required for fusion of the viral and cell membranes, thereby preventing entry of the viral genome into the healthy CD4+ T-cell.
McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 619
In vitro studies indicate that enfuvirtide is active against HIV-1, but is inactive against HIV-2. HIV-1 strains with reduced susceptibility to enfuvirtide can be produced in vitro and strains with reduced susceptibility to enfuvirtide have emerged during therapy with the drug. These strains have contained mutations in the HR1 domain of gp41 within the region of amino acids 36-45.
McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplements)., p. 619
To define the role of the human immunodeficiency virus type 1 (HIV-1) envelope proteins in virus infection, a series of peptides were synthesized based on various regions of the HIV-1 transmembrane protein gp41. One of these peptides, DP-178, corresponding to a region predictive of alpha-helical secondary structure (residues 643-678 of the HIV-1LAI isolate), has been identified as a potent antiviral agent. This peptide consistently blocked 100% of virus-mediated cell-cell fusion at < 5 ng/mL (IC90 approximately 1.5 ng/mL) and gave an approximately 10 times reduction in infectious titer of cell-free virus at approximately 80 ng/mL. The inhibitory activity was observed at peptide concentrations approximately 10(4) to 10(5) times lower than those at which cytotoxicity and cytostasis were detected. Peptide-mediated inhibition is HIV-1 specific in that approximately 10(2) to 10(3) times more peptide was required for inhibition of a human immunodeficiency virus type 2 isolate. Further experiments showed that DP-178 exhibited antiviral activity against both prototypic and primary HIV-1 isolates. As shown by PCR analysis of newly synthesized proviral DNA, DP-178 blocks an early step in the virus life cycle prior to reverse transcription. Finally, we discuss possible mechanisms by which DP-178 may exert its inhibitory activity.
PMID:7937889 Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC44898 Wild CT et al; Proc Natl Acad Sci U S A 91(21): 9770-4 (1994)
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