IBALIZUMAB

(TROGARZO)
FDA APPROVED ON MARCH 6, 2018
Ibalizumab (trade name Trogarzo) :

• Is a non-immunosuppressive humanised monoclonal antibody.

• It binds CD4, the primary receptor for HIV and inhibits HIV from
entering cells.

• It is a post-attachment inhibitor, blocking HIV from binding to

the CCR5 and CXCR4 co-receptors after HIV binds to the CD4 receptor
on the surface of a CD4 cell.

• Post-attachment inhibitors are a sub-class of HIV drugs called entry

inhibitors.
 DOSE :150MG/ML (200MG/1.33ML SINGLE-DOSE VIAL).

INDICATIONS:
• INDICATED FOR HUMAN IMMUNODEFICIENCY VIRUS-1 (HIV-1) INFECTION
WITH MULTIDRUG-RESISTANT INFECTION FAILING CURRENT
ANTIRETROVIRAL THERAPY (ART) REGIMEN.

• USE IN COMBINATION WITH OTHER ART DRUGS.

• NO DOSE MODIFICATION NEEDED WHEN COMBINED WITH OTHER ART.

 DOSAGE SCHEDULE :

FIRST DOSE (SINGLE LOADING DOSE): 2000 MG IV INFUSED OVER AT LEAST

30 MIN.
•

MAINTENANCE DOSES: 800 MG IV Q 2WEEKS INFUSED OVER AT LEAST 15-30

MIN DILUTED IN 250 ML 0.9 % SODIUM CHLORIDE.

IF A MAINTENANCE DOSE (800 MG) IS MISSED BY ≥3 DAYS BEYOND THE

SCHEDULED DOSING DAY, ADMINISTER A LOADING DOSE (2000 MG) AS
EARLY AS POSSIBLE
• IT CAN BE GIVEN BY INTRAVENOUS OR SUBCUTANEOUS
ROUTES.
• BOTH ARE WELL TOLERATED.
• IT HAS A T1/2 OF 3 DAYS.
• IT SIGNIFICANTLY IMPROVES CD4 CELL COUNTS.
• IT IS LONG ACTING.
• SHOWS NO CROSS RESISTANCE WITH NRTI, NNRTI &
PROTEASE INHIBITORS.
 METABOLISM : “TARGET MEDIATED ELIMINATION”

• IT OCCURS VIA RECEPTOR MEDIATED ENDOCYTOSIS.

• IBALIZUMAB BINDS TO CD4 RECEPTORS

INTERNALISATION OCCURS VIA CLATHRIN COATED PITS

ENDOSOME FUSION AND LYSOSOMAL DEGRADATION

ADVERSE DRUG EFFECTS :
• HEADACHE
• DIARRHOEA (8%)
• DIZZINESS (8%)
• NAUSEA (5%)
• RASH (5%)
• UPPER RESPIRATORY TRACT INFECTION
• NASOPHARINGITIS
• ORAL CANDIDIASIS
• IT CAUSES IMMUNE RECONSTITUTION INFLAMMATORY SYNDROME ( IRIS )
WHEN COMBINED WITH OTHER ART.
CONTRAINDICATIONS :
• MONOCLONAL ANTIBODIES ARE TRANSPORTED ACROSS THE
PLACENTA AS PREGNANCY PROGRESSES.
• THEREFORE, IBALIZUMAB HAS THE POTENTIAL TO BE
TRANSMITTED FROM THE MOTHER TO THE DEVELOPING FETUS.
• OWING TO THE POTENTIAL FOR HIV TRANSMISSION AND
ADVERSE REACTIONS IN A BREASTFED INFANT, MOTHERS
ADVICED NOT TO BREASTFEED
 STORAGE :
• REFRIGERATE AT 2-8°C (36-46°F).
• DO NOT FREEZE.
• PROTECT FROM LIGHT.
ANNUAL COST OF THIS REGIMEN IS
$1,18,000