Страна: САЩ
Език: английски
Източник: NLM (National Library of Medicine)
DELAVIRDINE MESYLATE (UNII: 421105KRQE) (DELAVIRDINE - UNII:DOL5F9JD3E)
KAISER FOUNDATION HOSPITALS
DELAVIRDINE MESYLATE
DELAVIRDINE MESYLATE 200 mg
PRESCRIPTION DRUG
New Drug Application
RESCRIPTOR- DELAVIRDINE MESYLATE TABLET KAISER FOUNDATION HOSPITALS ---------- 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, Opadry White YS-1-18202-A, and Pharmaceutical Ink Black. 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 μM Прочетете целия документ