FORTOVASE ROCHE CAPSULE

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

SAQUINAVIR

Available from:

HOFFMANN-LA ROCHE LIMITED

ATC code:

J05AE01

INN (International Name):

SAQUINAVIR

Dosage:

200MG

Pharmaceutical form:

CAPSULE

Composition:

SAQUINAVIR 200MG

Administration route:

ORAL

Units in package:

180

Prescription type:

Prescription

Therapeutic area:

HIV PROTEASE INHIBITORS

Product summary:

Active ingredient group (AIG) number: 0128571001; AHFS:

Authorization status:

CANCELLED POST MARKET

Authorization date:

2007-03-06

Summary of Product characteristics

PRODUCT MONOGRAPH
PR
FORTOVASE
®
ROCHE
®
(saquinavir)
Soft Gelatin Capsules - 200 mg
HIV Protease Inhibitor / Antiretroviral Agent
Hoffmann-La Roche Limited
Date of Preparation:
2455 Meadowpine Boulevard
November 13, 1998
Mississauga, Ontario
L5N 6L7
Date of Revision:
June 14, 2005
®
Registered Trademark of Hoffmann-La Roche Limited
©
Copyright 2002 - 2005 Hoffmann-La Roche Limited
CDS Version 1.6
Control Number: 098501
PRODUCT MONOGRAPH
PR
FORTOVASE
®
ROCHE
®
(saquinavir)
Soft Gelatin Capsules - 200 mg
PHARMACOLOGIC / THERAPEUTIC CLASSIFICATION
HIV Protease Inhibitor / Antiretroviral Agent
ACTION AND CLINICAL PHARMACOLOGY
Action: Saquinavir is a selective inhibitor of the human
immunodeficiency virus (HIV) protease
(IC
50
1 to 30 nM). This enzyme is required for cleavage of precursor
molecules into the
structural proteins of the mature virion core, and for activation of
reverse transcriptase during
the HIV growth cycle. Saquinavir therefore blocks these functions
which are essential for the
release of infectious virus.
No inhibition of human aspartyl or other proteases has been seen even
at a concentration of
10
:
M, indicating high selectivity (at least 50,000 fold). Experiments in
cell culture indicate that
saquinavir produces an additive to synergistic effect against HIV in
double and triple
combination with various reverse transcriptase inhibitors (including
zidovudine [ZDV],
didanosine [ddI], zalcitabine [ddC], lamivudine [3TC], stavudine
[d4T], and nevirapine), without
enhanced cytotoxicity.
Two key mutations have been identified in the protease gene which
contribute to genotypic
saquinavir resistance (G48V and L90M). This is the same pattern of
resistance which was
previously reported in patients treated with INVIRASE (saquinavir
mesylate, 600 mg TID).
Varying degrees of cross-resistance among protease inhibitors have
been observed.
- 3 -
Absorption: The absolute bioavailability of FORTOVASE (saquinavir) has
not been assessed.
However, following a single 600 mg dose, the relative bioavailability
of