Detailed description page of ThPDB2
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10480 details |
| Primary information | |
|---|---|
| ID | 10480 |
| Therapeutic ID | Th1088 |
| Protein Name | Enfuvirtide |
| Sequence | >Th1088_Enfuvirtide YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF |
| Molecular Weight | 4491.876 |
| Chemical Formula | C204H301N51O64 |
| Isoelectric Point | 4.3 |
| Hydrophobicity | -0.875 |
| Melting point | NA |
| Half-life | 3.8 ± 0.6 hrs |
| Description | 36 residue, synthetically prepared peptide with N-terminal acetylation and C-terminal amidation. It blocks the fusion of HIV-1 with CD4 cells. |
| Indication/Disease | Enfuvirtide is an antiretroviral drug used in combination therapy for the treatment of HIV-1/AIDS. |
| Pharmacodynamics | NA |
| Mechanism of Action | 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. It works by disrupting the HIV-1 molecular machinery at the final stage of fusion with the target cell, preventing uninfected cells from becoming infected. Enfuvirtide is a biomimetic peptide that was rationally designed to mimic components of the HIV-1 fusion machinery and displace them, preventing normal fusion. |
| Toxicity | NA |
| Metabolism | Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool. |
| 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). |
| 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] |
| Categories | Amino Acids, Peptides, and Proteins,Anti-HIV Agents,Anti-Infective Agents,Anti-Retroviral Agents,Antigens,Antigens, Viral,Antiinfectives for Systemic Use,Antiviral Agents,Antivirals for Systemic Use,Biological Factors,Cytochrome P-450 CYP2C19 Substrates,Cytochrome P-450 CYP2E1 Substrates,Cytochrome P-450 Substrates,Direct Acting Antivirals,env Gene Products, Human Immunodeficiency Virus,Fusion Protein Inhibitors,Gene Products, env,HIV Antigens,HIV Envelope Protein gp41,HIV Fusion Inhibitors,Human Immunodeficiency Virus 1 Fusion Inhibitor,Human Immunodeficiency Virus Proteins,Membrane Fusion Proteins,Membrane Proteins,Peptide Fragments,Peptides,Polyproteins,Proteins,Retroviridae Proteins,Viral Envelope Proteins,Viral Fusion Protein Inhibitors,Viral Fusion Proteins,Viral Proteins,Viral Structural Proteins |
| Patents Number | CA2224008 |
| Date of Issue | 18-Aug-2009 |
| Date of Expiry | 6-Jun-2016 |
| Drug Interaction | NA |
| Target | Envelope glycoprotein |
| Brand Name | NA |
| Company | NA |
| Brand Description | NA |
| Prescribed For | NA |
| Chemical Name | NA |
| Formulation | NA |
| Physical Appearance | NA |
| Route of Administration | NA |
| Recommended Dosage | NA |
| Contraindication | NA |
| Side Effects | NA |
| Useful Link 1 | NA |
| Useful Link 2 | NA |
| Remarks | NA |