RESCRIPTOR- delavirdine mesylate tablet

Kraj: Stany Zjednoczone

Język: angielski

Źródło: NLM (National Library of Medicine)

Składnik aktywny:

DELAVIRDINE MESYLATE (UNII: 421105KRQE) (DELAVIRDINE - UNII:DOL5F9JD3E)

Dostępny od:

ViiV Healthcare Company

INN (International Nazwa):

DELAVIRDINE MESYLATE

Skład:

DELAVIRDINE MESYLATE 100 mg

Droga podania:

ORAL

Typ recepty:

PRESCRIPTION DRUG

Wskazania:

RESCRIPTOR tablets are indicated for the treatment of HIV-1 infection in combination with at least 2 other active antiretroviral agents when therapy is warranted. The following should be considered before initiating therapy with RESCRIPTOR in treatment-naive patients. There are insufficient data directly comparing antiretroviral regimens containing RESCRIPTOR with currently preferred 3-drug regimens for initial treatment of HIV. In studies comparing regimens consisting of 2 nucleoside reverse transcriptase inhibitors (NRTIs) (currently considered suboptimal) to RESCRIPTOR plus 2 NRTIs, the proportion of patients receiving the regimen containing RESCRIPTOR who achieved and sustained an HIV-1 RNA level <400 copies/mL over 1 year of therapy was relatively low (see DESCRIPTION OF CLINICAL STUDIES). Resistant virus emerges rapidly when RESCRIPTOR is administered as monotherapy. Therefore, RESCRIPTOR should always be administered in combination with other antiretroviral agents. RESCRIPTOR tablets are contraindicate

Podsumowanie produktu:

RESCRIPTOR tablets are available as follows: 200-mg: white, capsule-shaped tablets marked with “RES200” Bottles of 180 tablets - NDC 49702-225-17. Store at controlled room temperature 20° to 25°C (68° to 77°F) [see USP]. Keep container tightly closed. Protect from high humidity.

Status autoryzacji:

New Drug Application

Charakterystyka produktu

RESCRIPTOR- DELAVIRDINE MESYLATE TABLET
VIIV HEALTHCARE COMPANY
---------- PRESCRIBING INFORMATION
RESCRIPTOR
(DELAVIRDINE MESYLATE)
TABLETS
DESCRIPTION
RESCRIPTOR tablets contain delavirdine mesylate, a synthetic
non-nucleoside reverse transcriptase
inhibitor (NNRTI) of the human immunodeficiency virus type 1 (HIV-1).
The chemical name of
delavirdine mesylate is piperazine, 1-[3-[(1-methyl-ethyl)amino]-2-
pyridinyl]-4-[[5-
[(methylsulfonyl)amino]-1H-indol-2-yl]carbonyl]-,
monomethanesulfonate. Its molecular formula is
C
H N O S•CH O S, and its molecular weight is 552.68. The structural
formula is:
Delavirdine mesylate is an odorless white-to-tan crystalline powder.
The aqueous solubility of
delavirdine free base at 23°C is 2,942 mcg/mL at pH 1.0, 295 mcg/mL
at pH 2.0, and 0.81 mcg/mL at pH
7.4.
Each RESCRIPTOR tablet, for oral administration, contains 200 mg of
delavirdine mesylate (henceforth
referred to as delavirdine). Inactive ingredients consist of carnauba
wax, colloidal silicon dioxide,
croscarmellose sodium, lactose, magnesium stearate, and
microcrystalline cellulose. In addition, the
200-mg tablet contains hypromellose and Opadry White YS-1-18202-A.
MICROBIOLOGY
MECHANISM OF ACTION:
Delavirdine is an NNRTI of HIV-1. Delavirdine binds directly to
reverse transcriptase (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 addition, HIV-1 group
O, a group of highly divergent strains
that are uncommon in North America, may not be inhibited by
delavirdine.
_IN VITRO HIV-1 SUSCEPTIBILITY: _In vitro anti-HIV-1 activity of
delavirdine was assessed by infecting cell
lines of lymphoblastic and monocytic origin and peripheral blood
lymphocytes with laboratory and
clinical isolates of HIV-1. IC
and IC
values (50% and 90% inhibitory concentrations) for laboratory
isolates (n = 5) ranged from 0.005 to 0.030 microM and