Enfuvirtide

Enfuvirtide Brand Name– Fuzeon

What is Enfuvirtide

Enfuvirtide also known as T-20, is the first medication in a class of anti-HIV drugs called fusion inhibitors.

It is a synthetic 36-amino-acid peptide derived from the HIV-1 envelope glycoprotein gp41 and it interferes with the entry of HIV-1 into cells by inhibiting the fusion of viral and cellular membranes.

The drug is indicated to treat HIV infection in antiretroviral-experienced patients with evidence of ongoing viral replication despite ongoing antiretroviral therapy (i.e., show resistance to current HIV treatments).

Enfuvirtide should be used in combination with an individualized antiretroviral regimen. It remains active against HIV strains in patients who have previously received and developed resistance to other classes of antiretroviral agents.

In clinical trials, patients receiving enfuvirtide in addition to an individualized antiretroviral regimen were less likely to experience virologic failure or relapse compared to those receiving an individualized antiretroviral regimen alone; patients whose virus was sensitive to a greater number of antiretroviral drugs did demonstrate a greater sensitivity to enfuvirtide.

During use, at least 98% of patients will develop injection site reactions to varying degrees, with almost 85% of patients developing the reactions within the first week of use. Patients should be appropriately counseled regarding injection site reactions before therapy is initiated.

Indications

  1. human immunodeficiency virus (HIV)
  2. human immunodeficiency virus (HIV) infection
  3. human immunodeficiency virus (HIV) prophylaxis

Side Effects

  1. abdominal pain
  2. acute respiratory distress syndrome (ARDS)
  3. angina
  4. anorexia
  5. antibody formation
  6. anxiety
  7. asthenia
  8. chills
  9. conjunctivitis
  10. constipation
  11. cough
  12. cranial nerve palsies
  13. cutaneous amyloidosis
  14. depression
  15. diarrhea
  16. dysgeusia
  17. dyspnea
  18. ecchymosis
  19. elevated hepatic enzymes
  20. eosinophilia
  21. erythema
  22. fatigue
  23. fever
  24. folliculitis
  25. glomerulonephritis
  26. Guillain-Barre syndrome
  27. hematoma
  28. hematuria
  29. hepatitis
  30. hyperglycemia
  31. hypertriglyceridemia
  32. hypotension
  33. infection
  34. influenza
  35. injection site reaction
  36. insomnia
  37. lymphadenopathy
  38. myalgia
  39. nausea
  40. neutropenia
  41. pancreatitis
  42. paresthesias
  43. peripheral edema
  44. peripheral neuropathy
  45. pruritus
  46. rash
  47. renal failure (unspecified)
  48. renal tubular necrosis
  49. sinusitis
  50. steatosis
  51. suicidal ideation
  52. thrombocytopenia
  53. vomiting
  54. weight loss
  55. xerostomia

Monitoring Parameters

  • blood glucose
  • CBC with differential
  • CD4+ T cell count
  • hepatitis B serology
  • LFTs
  • plasma hepatitis C RNA
  • plasma HIV RNA
  • pregnancy testing
  • serum bilirubin (total and direct)
  • serum cholesterol
  • serum lipid profile
  • urinalysis

Contraindications

  • anticoagulant therapy
  • autoimmune disease
  • breast-feeding
  • coagulopathy
  • Graves’ disease
  • Guillain-Barre syndrome
  • hemophilia
  • hepatitis B and HIV coinfection
  • hepatitis C and HIV coinfection
  • human immunodeficiency virus (HIV) infection resistance
  • immune reconstitution syndrome
  • pregnancy
  • pulmonary disease
  • respiratory infection
  • substance abuse
  • tobacco smoking

Interactions

  • Tipranavir

Tipranavir: (Moderate) Phase 3 trials showed that the coadministration of enfuvirtide increases tipranavir trough concentrations by 45%; however, the mechanism for this increase is unknown. The manufacturer of tipranavir states that tipranavir dosage adjustments are not recommended

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