Land: Kanada
Språk: engelska
Källa: Health Canada
DELAVIRDINE MESYLATE
VIIV HEALTHCARE ULC
J05AG02
DELAVIRDINE
100MG
TABLET
DELAVIRDINE MESYLATE 100MG
ORAL
360
Prescription
NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
Active ingredient group (AIG) number: 0134000001; AHFS:
CANCELLED POST MARKET
2018-11-01
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 Läs hela dokumentet