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Table 5E. Characteristics of Fusion Inhibitors
Drug Formulation Dosing Recommendations Elimination
Serum
Half-life Storage Adverse Events
Enfuvirtide (T-20)
Fuzeon
®
▶ Injectable—supplied as
lyophilized powder
▶ Each vial contains 108 mg
of T-20; reconstitute with
1.1 mL of sterile water for
injection for delivery of
approximately 90 mg/1 mL
90 mg (1 mL) subcutaneously bid Expected
to undergo
catabolism to
its constituent
amino acids,
with
subsequent
recycling of the
amino acids in
the body pool
3.8 h Store at room
temperature
(up to 25
º
C
or 77
º
F)
Reconstituted
solution
should be
stored under
refrigeration
at 2
º
C-8
º
C
(36
º
F-46
º
F)
and used
within 24
hours
▶ Local injection site reactions in almost
100% of patients (pain, erythema,
induration, nodules and cysts,
pruritus, ecchymosis)
▶ Increased bacterial pneumonia
▶ Hypersensitivity reaction (<1%)—
symptoms may include rash, fever,
nausea, vomiting, chills, rigors,
hypotension, or elevated serum
transaminases; rechallenge is NOT
recommended
Table 5F. Characteristics of CCR5 Antagonists
Drug Formulation Dosing Recommendations Elimination Serum Half-life Adverse Events
Maraviroc (MVC)
Selzentry
®
150 mg, 300 mg tablets ▶ 150 mg bid when given with
strong CYP3A inhibitors (with
or without CYP3A inducers)
including PIs (except TPV/r)
▶ 300 mg bid when given with
NRTIs, T-20, TPV/r, NVP, and
other drugs that are not strong
CYP3A inhibitors or inducers
▶ 600 mg bid when given with
CYP3A inducers, including
EFV, ETR, etc (without a
CYP3A inhibitor)
▶ Take without regard to meals
CYP3A4
substrate
14–18 h
▶ Abdominal pain
▶ Cough
▶ Dizziness
▶ Musculoskeletal symptoms
▶ Pyrexia
▶ Rash
▶ Upper respiratory tract infections
▶ Hepatotoxicity
▶ Orthostatic hypotension
Table 5G. Characteristics of Non-Antiretroviral Pharmacoenhancers
Drug Formulation Dosing Recommendations Elimination Serum Half-life Adverse Events
Cobicistat (COBI)
Available only as
FTC/TDF/
EVG/COBI
Stribild
®
FTC 200 mg +
TDF 300 mg +
EVG 150 mg +
COBI 150 mg
Adults: One tablet once daily
with food
CYP3A
metabolism
(minor CYP2D6
metabolism)
3.5 h ▶ Nausea
▶ Diarrhea
▶ Inhibition of creatinine excretion
resulting in early increase in serum
creatinine (~0.14 mg/dL) and
decrease in eGFR; no effect on actual
GFR
▶ See also elvitegravir, tenofovir,
emtricitabine
