Enfuvirtide
Mechanism :
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 the conformational changes required for the fusion of viral and cellular membranes.
Indication :
- HIV-1 infection in treatment-experienced patients with evidence of HIV-1 replication despite ongoing antiretroviral therapy
Contraindications :
Contraindicated in patients with known hypersensitivity to any of its components.
Dosing :
<6 years:
Safety and efficacy not established.
6-16 years:
2 mg/kg twice daily up to a maximum dose of 90 mg twice daily SC.
>16 years:
90 mg SC, twice a day.
Adverse Effect :
Local injection site reactions, diarrhea, nausea, fatigue, peripheral neuropathy, insomnia, anorexia, myalgia, flu like symptoms, Guillain Barre syndrome, hypersensitivity.
Interaction :
CYP450 Metabolized Drugs: Enfuvirtide is unlikely to have significant drug interactions with concomitantly administered drugs metabolized by CYP450 enzymes.
Antiretroviral Agents: No drug interactions with other antiretroviral medications have been identified that would warrant alteration of either the enfuvirtide dose or the dose of the other antiretroviral medication.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 35-50 | Dose as in normal renal function |
| 10-35 | Dose as in normal renal function |
| <10 | Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
| HD | 13% dialysed. Dose as in GFR<10 mL/min |
| HDF/High flux | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
| CAV/VVHD | Unlikely to be dialysed. Dose as in GFR=10–35 mL/min |
Hepatic Dose :
No dosage adjustments are recommended.