Journal: ACS Omega

Article Title: Development of an Analytical Method for Determination of Related Substances and Degradation Products of Cabotegravir Using Analytical Quality by Design Principles

doi: 10.1021/acsomega.1c07260

Figure Lengend Snippet: Chromatogram of cabotegravir and its related substances ( 2CBG , 4CBG , dFCBG , and HICBG ) as well as its degradation products ( DP1 , DP2 , DP3 , DP4 ) analyzed with initial chromatographic conditions (MP A: 0.5% formic acid:ACN (94:6, v/v); MP B: MeOH:ACN (94:6, v/v); Acquity UPLC BEH Phenyl column, 1.7 μm, 150 mm × 2.1 mm; T c = 35 °C; flow rate = 0.3 mL/min. Gradient: t = 0 min, 42% B; 18 min, 42% B; 20 min, 59% B; 22 min, 89% B; 29 min, 89% B; 29,5 min, 42% B; 5.5 min equilibration).

Article Snippet: Cabotegravir, chemically known as (3 S ,11 aR )- N -((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11 a -hexahydrooxazolo(3,2- a )pyrido(1,2- d )pyrazine-8-carboxamide ( Figure ) is a second-generation integrase inhibitor, developed by Viiv Healthcare for HIV treatment and pre-exposure prophylaxis.

Techniques:

Journal: ACS Omega

Article Title: Development of an Analytical Method for Determination of Related Substances and Degradation Products of Cabotegravir Using Analytical Quality by Design Principles

doi: 10.1021/acsomega.1c07260

Figure Lengend Snippet: Chromatogram of the best chromatographic conditions for separation of cabotegravir, its eight impurities, and one unknown impurity from method scouting. Chromatographic conditions: MP A, phosphate buffer, pH = 2.0; MP B, ACN; Acquity UPLC BEH Phenyl column, 1.7 μm, 150 mm × 2.1 mm; T c = 40 °C; flow rate = 0.3 mL/min. Gradient: t = 0 min, 30% B; 1 min, 30% B; 16 min, 90% B; 17 min, 30% B; 3 min equilibration.

Article Snippet: Cabotegravir, chemically known as (3 S ,11 aR )- N -((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11 a -hexahydrooxazolo(3,2- a )pyrido(1,2- d )pyrazine-8-carboxamide ( Figure ) is a second-generation integrase inhibitor, developed by Viiv Healthcare for HIV treatment and pre-exposure prophylaxis.

Techniques:

Journal: ACS Omega

Article Title: Development of an Analytical Method for Determination of Related Substances and Degradation Products of Cabotegravir Using Analytical Quality by Design Principles

doi: 10.1021/acsomega.1c07260

Figure Lengend Snippet: Trellis graphs from DoE study to establish CMA models and robustness testing. Graph is showing by white color an area where defined criteria are met, the design space. Other colors represent areas where the criteria are not met: dark blue = R DP4 , HICBG ≤ 2.0, purple = C pk ( R DP4 , HICBG ) ≤ 1.33; light blue = R 2CBG , 4CBG ≤ 2.0, orange = C pk ( R 2CBG , 4CBG ) ≤ 1.33; pink = R 4CBG , cabotegravir ≤ 2.0, lime = C pk ( R 4CBG , cabotegravir ) ≤ 1.33, x = pump flow rate (0.2–0.4 mL/min); y = final percent of acetonitrile in gradient (50–90%) at pH of 2.75 (top line), 3.25 (middle line), and 3.75 (bottom line); and column temperature of 30 (left column), 40 (middle column), and 50 °C (right column).

Article Snippet: Cabotegravir, chemically known as (3 S ,11 aR )- N -((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11 a -hexahydrooxazolo(3,2- a )pyrido(1,2- d )pyrazine-8-carboxamide ( Figure ) is a second-generation integrase inhibitor, developed by Viiv Healthcare for HIV treatment and pre-exposure prophylaxis.

Techniques:

Journal: ACS Omega

Article Title: Development of an Analytical Method for Determination of Related Substances and Degradation Products of Cabotegravir Using Analytical Quality by Design Principles

doi: 10.1021/acsomega.1c07260

Figure Lengend Snippet: Detection Limit Results from Analytical Method Validation

Article Snippet: Cabotegravir, chemically known as (3 S ,11 aR )- N -((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11 a -hexahydrooxazolo(3,2- a )pyrido(1,2- d )pyrazine-8-carboxamide ( Figure ) is a second-generation integrase inhibitor, developed by Viiv Healthcare for HIV treatment and pre-exposure prophylaxis.

Techniques:

Journal: ACS Omega

Article Title: Development of an Analytical Method for Determination of Related Substances and Degradation Products of Cabotegravir Using Analytical Quality by Design Principles

doi: 10.1021/acsomega.1c07260

Figure Lengend Snippet: Quantification Limit Results from Analytical Method Validation

Article Snippet: Cabotegravir, chemically known as (3 S ,11 aR )- N -((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11 a -hexahydrooxazolo(3,2- a )pyrido(1,2- d )pyrazine-8-carboxamide ( Figure ) is a second-generation integrase inhibitor, developed by Viiv Healthcare for HIV treatment and pre-exposure prophylaxis.

Techniques:

Journal: ACS Omega

Article Title: Development of an Analytical Method for Determination of Related Substances and Degradation Products of Cabotegravir Using Analytical Quality by Design Principles

doi: 10.1021/acsomega.1c07260

Figure Lengend Snippet: Linearity Results for Cabotegravir and All Eight Impurities from Analytical Method Validation

Article Snippet: Cabotegravir, chemically known as (3 S ,11 aR )- N -((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11 a -hexahydrooxazolo(3,2- a )pyrido(1,2- d )pyrazine-8-carboxamide ( Figure ) is a second-generation integrase inhibitor, developed by Viiv Healthcare for HIV treatment and pre-exposure prophylaxis.

Techniques:

Journal: International journal of antimicrobial agents

Article Title: Antibacterial and antivirulence activities of auranofin against Clostridium difficile

doi: 10.1016/j.ijantimicag.2018.09.018

Figure Lengend Snippet: The minimum inhibitory concentration (MIC, µg/mL) of auranofin and control drugs against vancomycin-resistant Enterococcus faecium isolates.

Article Snippet: Auranofin, linezolid (Chem-Impex International, Wood Dale, IL), vancomycin hydrochloride (Gold Biotechnology, St. Louis, MO) metronidazole (Beantown Chemical Corporation, Hudson, NH), sodium selenite (MP Biomedicals, Santa Ana, CA), and fidaxomicin (Apexbio, Houston, TX) were procured from commercial vendors.

Techniques: Concentration Assay