HIV drugs (fusion inhibitors)

Question 1

Binding and fusion inhibitors (drugs)

Answer 1

Maraviroc (MRC)
Enfuvirtide (T-20)
Ibalizumab (IBA)

Question 2

Maraviroc (MOA)

Answer 2

CCR5 inhibitor

binds to CCR5 receptor on the host cell and prevents HIV from binding to it

Question 3

Enfuvirtide (MOA)

Answer 3

Fusion inhibitor

binds to gp41 on virus and prevents fusion with host cell membrane

Question 4

Enfuvirtide (adverse effects)

Answer 4

injection site reaction (subcutaneous nodules secondary to IV site inflammatory response)
hypersensitivity reactions
increased risk of bacterial pneumonia

Question 5

Maraviroc (indication)

Answer 5

active ONLY against CCR5 strains of HIV
(has no activity against CXCR4)
active against viruses that have become resistant to other anti-retroviral agents (UNIQUE MOA)

Question 6

is Maraviroc dual tropic?

Answer 6

No

it only works on CCR5, has no effect on CXCR4 strains

Question 7

Maraviroc (adverse effects)

Answer 7

drug interaction (3A4 pathway)
upper respiratory tract infection
abdominal pain
hepatoxicity