Updated: 2/28/2019

Fusion Inhibitors

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Snapshot
  • A 55-year-old man presents to the HIV clinic for a follow-up visit. He was recently diagnosed with HIV and was started on first-line highly active antiretroviral therapy (HAART). However, his CD4 count at his last visit remained low. Drug resistance analysis of the HIV strain was sent at that time and revealed 3 major mutations causing the virus to be resistant to many first-line agents. The analysis also revealed that the HIV strain was CCR5-tropic. The patient was started on maraviroc.
Introduction
  • Drugs
    • enfuvirtide
      • prevents penetration of HIV into CD4+ T-cells
    • maraviroc
      • prevents attachment of HIV into CD4+ T-cells
  • Clinical use
    • a class of highly active antiretroviral therapy (HAART)
    • often used as second-line in patients with drug resistance to first-line agents
Enfuvirtide
  • Mechanism of action
    • binds to gp41, which inhibits HIV entry into the cell
  • Adverse effects
    • injection site skin reaction
    • gastrointestinal upset
    • fatigue
Maraviroc
  • Mechanism of action
    • binds to CCR5, which is a protein on the surface of T-cells and monocytes
    • inhibits the interaction of CCR5 with gp120 on HIV, thus inhibiting docking
  • Clinical use
    • requires assay showing that the virus is CCR5-tropic, which indicates that the virus is infecting cells with CCR5 expression (vs CXCR4), making it susceptible to the drug
  • Adverse effects
    • rash
    • gastrointestinal upset
    • immunosuppression

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Questions (2)
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(M1.MC.15.75) A 25-year-old sexually active male presents to an internal medicine physician for a routine health check up after having several unprotected sexual encounters. After appropriate testing the physician discusses with the patient that he is HIV+ and must be started on anti-retroviral treatment. Which of the following medications prescribed acts on the gp41 subunit of the HIV envelope glycoprotein?

QID: 106845
1

Amantadine

3%

(8/235)

2

Rimantadine

1%

(3/235)

3

Zidovudine

20%

(48/235)

4

Saquinavir

7%

(16/235)

5

Enfuvirtide

67%

(158/235)

M 1 E

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