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Multiple sources of anticipated degradation and process impurities of raltegravir potassium drug substance observed during the laboratory optimization and later during its bulk synthesis are described in this article. The impurities were monitored by UPLC, and their structures are tentatively assigned on the basis of fragmentation patterns in LC–MS and
Gulabrao D. Patil +8 more
semanticscholar +3 more sources
Crystal structure of raltegravir potassium, C20H20FKN6O5
The crystal structure of the potassium salt of raltegravir has been solved and refined using synchrotron X-ray powder diffraction data, and optimized using density functional techniques. Raltegravir potassium crystallizes in space groupP21/c(#14) witha= 15.610 59(9),b= 8.148 19(3),c= 16.125 97(6) Å,β= 94.1848(5)°,V= 2045.72(1) Å3, andZ= 4.
James A. Kaduk +3 more
semanticscholar +3 more sources
Biowaiver monograph for immediate-release solid oral dosage forms: Raltegravir potassium
The present monograph discusses the possibility of BCS-based biowaivers for immediate release pharmaceutical products containing raltegravir potassium, which is used to treat human immunodeficiency virus (HIV) infections. Raltegravir potassium can be assigned to BCS class II or IV since this compound has low solubility and uncertain permeability ...
Atsushi Kambayashi +12 more
semanticscholar +4 more sources
A manufacturing route for the synthesis of raltegravir potassium 1 was developed via a thermal rearrangement of amidoxime DMAD adducts 6 to construct the key, highly functionalized hydroxypyrimidin...
Guy R. Humphrey +10 more
semanticscholar +3 more sources
Synthesis of the HIV Integrase Inhibitor Raltegravir Potassium
Contributor Philip Kocienski +2 more
semanticscholar +3 more sources
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Clinical Infectious Diseases, 2020
BACKGROUND Although some integrase strand transfer inhibitors (INSTIs) promote peripheral and central adipose tissue/weight gain in HIV-infected individuals, the underlying mechanism has not been identified.
Jennifer Gorwood +16 more
semanticscholar +3 more sources
BACKGROUND Although some integrase strand transfer inhibitors (INSTIs) promote peripheral and central adipose tissue/weight gain in HIV-infected individuals, the underlying mechanism has not been identified.
Jennifer Gorwood +16 more
semanticscholar +3 more sources

