VIRACEPT- nelfinavir mesylate tablet, film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

NELFINAVIR MESYLATE (UNII: 98D603VP8V) (NELFINAVIR - UNII:HO3OGH5D7I)

Available from:

State of Florida DOH Central Pharmacy

INN (International Name):

NELFINAVIR MESYLATE

Composition:

NELFINAVIR MESYLATE 625 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

VIRACEPT in combination with other antiretroviral agents is indicated for the treatment of HIV infection. In the clinical studies described below, efficacy was evaluated by the percent of patients with plasma HIV RNA < 400 copies/mL (Studies 511 and 542) or < 500 copies/mL (Study ACTG 364), using the Roche RT-PCR (Amplicor) HIV-1 Monitor or < 50 copies/mL, using the Roche HIV-1 Ultrasensitive assay (Study Avanti 3). In the analysis presented in each figure, patients who terminated the study early for any reason, switched therapy due to inadequate efficacy or who had a missing HIV-RNA measurement that was either preceded or followed by a measurement above the limit of assay quantification were considered to have HIV-RNA above 400 copies/mL, above 500 copies/mL, or above 50 copies/mL at subsequent time points, depending on the assay that was used. Study 511 was a double-blind, randomized, placebo controlled trial comparing treatment with zidovudine (ZDV; 200 mg TID) and lamivudine (3TC; 150 mg BID) plus 2 doses

Product summary:

VIRACEPT (nelfinavir mesylate) 250 mg: Light blue, capsule-shaped tablets with a clear film coating engraved with "VIRACEPT" on one side and "250 mg" on the other. VIRACEPT (nelfinavir mesylate) 625 mg: White oval tablet with a clear film coating engraved with "V" on one side and "625" on the other. VIRACEPT (nelfinavir mesylate) Oral Powder is available as a 50 mg/g off-white powder containing 50 mg (as nelfinavir free base) in each level scoopful (1 gram). They are supplied by State of Florida DOH Central Pharmacy as follows: Viracept tablets and oral powder should be stored at 15° to 30°C (59° TO 86°F). Keep container tightly closed. Dispense in original container.

Authorization status:

New Drug Application

Summary of Product characteristics

VIRACEPT - NELFINAVIR MESYLATE TABLET, FILM COATED
STATE OF FLORIDA DOH CENTRAL PHARMACY
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VIRACEPT
(NELFINAVIR MESYLATE)
TABLETS AND ORAL POWDER
DESCRIPTION
VIRACEPT (nelfinavir mesylate) is an inhibitor of the human
immunodeficiency virus (HIV)
protease. VIRACEPT Tablets are available for oral administration as a
light blue, capsule-shaped tablet
with a clear film coating in 250 mg strength (as nelfinavir free base)
and as a white oval tablet with a
clear film coating in 625 mg strength (as nelfinavir free base). Each
tablet contains the following
common inactive ingredients: calcium silicate, crospovidone, magnesium
stearate, hypromellose, and
triacetin. In addition, the 250 mg tablet contains FD&C blue #2 powder
and the 625 mg tablet contains
colloidal silicon dioxide. VIRACEPT Oral Powder is available for oral
administration in a 50 mg/g
strength (as nelfinavir free base) in bottles. The oral powder also
contains the following inactive
ingredients: microcrystalline cellulose, maltodextrin, dibasic
potassium phosphate, crospovidone,
hypromellose, aspartame, sucrose palmitate, and natural and artificial
flavor. The chemical name for
nelfinavir mesylate is [3_S_-[2(2_S*_,3_S*_),
3α,4aβ,8aβ]]-_N_-(1,1-dimethylethyl)decahydro-2-[2-hydroxy-3-
[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinoline
carboxamide mono-
methanesulfonate (salt) and the molecular weight is 663.90 (567.79 as
the free base). Nelfinavir
mesylate has the following structural formula:
Nelfinavir mesylate is a white to off-white amorphous powder, slightly
soluble in water at pH ≤4 and
freely soluble in methanol, ethanol, 2-propanol and propylene glycol.
MICROBIOLOGY
MECHANISM OF ACTION
Nelfinavir is an inhibitor of the HIV-1 protease. Inhibition of the
viral protease prevents cleavage of
the _gag _and _gag-pol _polyprotein resulting in the production of
immature, non-infectious virus.
ANTIVIRAL ACTIVITY IN VITRO
The antiviral activity of nelfinavir _in vitro_ has been demonstrated
in both acute and/or chronic HIV
i