RESCRIPTOR TABLET

Država: Kanada

Jezik: engleski

Izvor: Health Canada

Aktivni sastojci:

DELAVIRDINE MESYLATE

Dostupno od:

VIIV HEALTHCARE ULC

ATC koda:

J05AG02

INN (International ime):

DELAVIRDINE

Doziranje:

100MG

Farmaceutski oblik:

TABLET

Sastav:

DELAVIRDINE MESYLATE 100MG

Administracija rute:

ORAL

Jedinice u paketu:

360

Tip recepta:

Prescription

Područje terapije:

NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS

Proizvod sažetak:

Active ingredient group (AIG) number: 0134000001; AHFS:

Status autorizacije:

CANCELLED POST MARKET

Datum autorizacije:

2018-11-01

Svojstava lijeka

1
PRODUCT MONOGRAPH
RESCRIPTOR
®
(DELAVIRDINE MESYLATE)
TABLETS - 100 MG
ANTIRETROVIRAL AGENT
ViiV Healthcare ULC
Date of Preparation:
8455 route Transcanadienne
December 15, 2009
Montreal, Quebec
H4S 1Z1
Control No. 134878
©
2009 ViiV Healthcare ULC. All Rights Reserved.
®
RESCRIPTOR is a registered trademark, used under license by ViiV
Healthcare ULC
2
RESCRIPTOR
®
(DELAVIRDINE MESYLATE)
TABLETS - 100 MG
ANTIRETROVIRAL AGENT
ACTION AND CLINICAL PHARMACOLOGY
RESCRIPTOR (delavirdine mesylate) is a non-nucleoside reverse
transcriptase inhibitor (NNRTI) of
the human immunodeficiency virus-type 1 (HIV-1). Reverse transcriptase
(RT) is located in the core
of the HIV-1 virus and is released upon entry into the host cell. It
uses the viral RNA as a template to
form DNA. This is a pivotal step in the HIV-1 infection process.
Delavirdine mesylate (henceforth referred to as delavirdine) is a
selective inhibitor of RT. It binds
directly to RT and blocks RNA-dependent and DNA-dependent DNA
polymerase activities.
Delavirdine does not compete with template: primer or deoxynucleoside
triphosphates. HIV-2 RT
and human cellular DNA polymerases α, γ, or δ are not inhibited by
delavirdine.
_IN VITRO_ HIV-1 SUSCEPTIBILITY
The antiviral activity of delavirdine
_in vitro_
has been demonstrated in both acute and chronic HIV
infections in lymphoblastic and monocytic cell lines and peripheral
blood lymphocytes with
laboratory and clinical isolates of HIV-1. IC
50
and IC
90
values (50% and 90% inhibitory
concentrations) for laboratory isolates (N=5) ranged from 0.005 to
0.030 µM and 0.04 to 0.10 µM,
respectively. Mean IC
50
of clinical isolates (N=74) was 0.038 µM (range 0.001 to 0.69 µM);
73 of 74
clinical isolates had an IC
50
≤
0.18 µM. The IC
90
of 24 of these clinical isolates ranged from 0.05 to
0.10 µM. In drug combination studies of delavirdine with zidovudine,
didanosine, zalcitabine,
lamivudine, interferon- α and protease inhibitors, additive to
synergistic anti-HIV-1 activity was
3
observed in cell culture. The