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https://www.readbyqxmd.com/read/27902508/cabotegravir-long-acting-injection-protects-macaques-against-intravenous-challenge-with-sivmac251
#1
Chasity D Andrews, Leslie S T Bernard, Amanda Yee Poon, Hiroshi Mohri, Natanya Gettie, William R Spreen, Agegnehu Gettie, Kasi Russell-Lodrigue, James Blanchard, Zhi Hong, David D Ho, Martin Markowitz
OBJECTIVE: We evaluated the effectiveness of cabotegravir (CAB; GSK1265744 or GSK744) long-acting (LA) as pre-exposure prophylaxis (PrEP) against intravenous SIV challenge in a model that mimics blood transfusions based on the per-act probability of infection. DESIGN: CAB LA is an InSTI formulated as a 200 mg/mL injectable nanoparticle suspension that is an effective pre-exposure prophylaxis (PrEP) agent against rectal and vaginal SHIV transmission in macaques...
November 29, 2016: AIDS
https://www.readbyqxmd.com/read/27799824/profile-of-cabotegravir-and-its-potential-in-the-treatment-and-prevention-of-hiv-1-infection-evidence-to-date
#2
REVIEW
Thomas Whitfield, Adele Torkington, Clare van Halsema
Modern antiretroviral therapy has demonstrated effectiveness in preexposure prophylaxis (PrEP) and treatment of HIV infection. There is a demand for prevention and treatment regimens that could overcome challenges of improving adherence, toxicity, and dosing convenience. Cabotegravir is an integrase strand transfer inhibitor and an analog of dolutegravir. Unlike dolutegravir, cabotegravir has a long half-life and can be formulated into a long-acting nanosuspension for parenteral administration. Initial pharmokinetic studies in humans have demonstrated adequate drug levels with intramuscular (IM) administration at 4 weekly and 8 weekly intervals, with few interactions with commonly used concomitant medications...
2016: HIV/AIDS: Research and Palliative Care
https://www.readbyqxmd.com/read/27162089/effect-of-cabotegravir-on-cardiac-repolarization-in-healthy-subjects
#3
Yu Lou, Ann M Buchanan, Shuguang Chen, Susan L Ford, Elizabeth Gould, David Margolis, William R Spreen, Parul Patel
A randomized, partial-blind, repeat-dose, 3-period crossover study (NCT02027454) assessed the effect of cabotegravir on QT interval in healthy subjects. To achieve a supratherapeutic dose, each subject received cabotegravir 150 mg (30 mg × 5 tablets) every 12 hours for a total of 3 doses over 2 days, matching placebo (every 12 hours) over 2 days, or a single open-label 400-mg dose of the positive control moxifloxacin, with a 21-day washout between treatments. Blood samples for pharmacokinetic analyses were collected up to 24 hours after the third dose on day 2...
November 2016: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/26713502/choosing-initial-antiretroviral-therapy-current-recommendations-for-initial-therapy-and-newer-or-investigational-agents
#4
Roy M Gulick
There is general consistency among US and European guidelines regarding the initiation of antiretroviral therapy for HIV-infected individuals. Recent and ongoing trials comparing regimens may lead to reevaluation of initial treatment choices. The choice of antiretroviral regimen will also likely be affected by development, evaluation, and availability of newer drugs. This article reviews currently recommended regimens and characteristics of selected current investigational drugs, including the nucleotide analogue reverse transcriptase inhibitor tenofovir alafenamide, the nonnucleoside reverse transcriptase inhibitor doravirine, the integrase strand transfer inhibitor cabotegravir, the HIV entry inhibitor BMS-663068, and the HIV maturation inhibitor BMS-955176...
October 2015: Topics in Antiviral Medicine
https://www.readbyqxmd.com/read/26711252/interspecies-scaling-of-excretory-amounts-using-allometry-retrospective-analysis-with-rifapentine-aztreonam-carumonam-pefloxacin-miloxacin-trovafloxacin-doripenem-imipenem-cefozopran-ceftazidime-linezolid-for-urinary-excretion-and-rifapentine-cabotegravir-and
#5
Nuggehally R Srinivas
1. Interspecies allometry scaling for prediction of human excretory amounts in urine or feces was performed for numerous antibacterials. Antibacterials used for urinary scaling were: rifapentine, pefloxacin, trovafloxacin (Gr1/low; <10%); miloxacin, linezolid, PNU-142300 (Gr2/medium; 10-40%); aztreonam, carumonam, cefozopran, doripenem, imipenem, and ceftazidime (Gr3/high; >50%). Rifapentine, cabotegravir, and dolutegravir was used for fecal scaling (high; >50%). 2. The employment of allometry equation: Y = aW(b) enabled scaling of urine/fecal amounts from animal species...
September 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/26633643/the-promise-and-pitfalls-of-long-acting-injectable-agents-for-hiv-prevention
#6
REVIEW
Raphael J Landovitz, Ryan Kofron, Marybeth McCauley
PURPOSE OF REVIEW: Preexposure prophylaxis for HIV prevention is highly effective when taken as prescribed. Adherence to required dosing regimens for protection may pose challenges. Long-acting agents for HIV prevention may have the potential to improve adherence via favorable pharmacokinetics supportive of infrequent dosing. This review focuses on the potential benefits and considerations for the study and use of 2 long-acting injectable agents, cabotegravir (GSK1265744LA, CAB LA) and rilpivirine (TMC278LA, RPV LA), for use as chemoprophylaxis for HIV prevention...
January 2016: Current Opinion in HIV and AIDS
https://www.readbyqxmd.com/read/26340566/drug-interaction-profile-of-the-hiv-integrase-inhibitor-cabotegravir-assessment-from-in-vitro-studies-and-a-clinical-investigation-with-midazolam
#7
Melinda J Reese, Gary D Bowers, Joan E Humphreys, Elizabeth P Gould, Susan L Ford, Lindsey O Webster, Joseph W Polli
1. Cabotegravir (CAB; GSK1265744) is a potent HIV integrase inhibitor in clinical development as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. 2. This work investigated if CAB was a substrate for efflux transporters, the potential for CAB to interact with drug-metabolizing enzymes and transporters to cause clinical drug interactions, and the effect of CAB on the pharmacokinetics of midazolam, a CYP3A4 probe substrate, in humans. 3. CAB is a substrate for Pgp and BCRP; however, its high intrinsic membrane permeability limits the impact of these transporters on its intestinal absorption...
2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/26201299/cabotegravir-plus-rilpivirine-once-a-day-after-induction-with-cabotegravir-plus-nucleoside-reverse-transcriptase-inhibitors-in-antiretroviral-naive-adults-with-hiv-1-infection-latte-a-randomised-phase-2b-dose-ranging-trial
#8
RANDOMIZED CONTROLLED TRIAL
David A Margolis, Cynthia C Brinson, Graham H R Smith, Jerome de Vente, Debbie P Hagins, Joseph J Eron, Sandy K Griffith, Marty H St Clair, Marita C Stevens, Peter E Williams, Susan L Ford, Britt S Stancil, Melinda M Bomar, Krischan J Hudson, Kimberly Y Smith, William R Spreen
BACKGROUND: In phase 1 trials, the HIV-1 integrase strand transfer inhibitor cabotegravir (GSK1265744) was well tolerated, both alone, and in combination with the non-nucleoside reverse transcriptase inhibitor rilpivirine. We assessed cabotegravir plus rilpivirine, as a two-drug oral antiretroviral regimen, for the maintenance of viral suppression in antiretroviral-naive HIV-1-infected individuals. METHODS: In the phase 2b Long-Acting antireTroviral Treatment Enabling (LATTE) trial, a multicentre study done in Canada and the USA, antiretroviral-naive HIV-1-infected adults (aged ≥18 years) were randomly allocated in a 1:1:1:1 ratio to oral cabotegravir 10 mg once a day, 30 mg once a day, 60 mg once a day, or oral efavirenz 600 mg once a day with dual nucleoside reverse transcriptase inhibitors (NRTIs) for 24 weeks of induction...
October 2015: Lancet Infectious Diseases
https://www.readbyqxmd.com/read/26134155/disposition-and-metabolism-of-cabotegravir-a-comparison-of-biotransformation-and-excretion-between-different-species-and-routes-of-administration-in-humans
#9
Gary David Bowers, Amanda Culp, Melinda J Reese, Glenn Tabolt, Lee Moss, Stephen Piscitelli, Phuong Huynh, David Wagner, Susan L Ford, Elizabeth P Gould, Rennan Pan, Yu Lou, David A Margolis, William R Spreen
1.  Cabotegravir [(3S,11aR)-N-[(2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide] is an HIV-1 integrase inhibitor under development as a tablet for both oral lead-in therapy and long-acting (LA) injectable for intramuscular dosing. 2. Metabolism, pharmacokinetics and excretion were investigated in healthy human subjects who received either a single oral dose (28.2 mg) of [(14)C]cabotegravir in a mass balance study, or LA formulations of unlabeled cabotegravir (200-800 mg), intramuscularly or subcutaneously, in a separate study...
2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/26049951/cabotegravir-long-acting-for-hiv-1-prevention
#10
REVIEW
Chasity D Andrews, Walid Heneine
PURPOSE OF REVIEW: Preexposure prophylaxis (PrEP) with daily Truvada has demonstrated clinical efficacy against HIV-1 acquisition that correlates with high adherence. Long-acting antiretroviral drugs offer an alternative to daily regimens and may improve PrEP adherence. This review summarizes the preclinical nonhuman primate studies for evaluating the efficacy of cabotegravir long-acting as PrEP and the ongoing phase 2a studies assessing safety, tolerability, and acceptability of cabotegravir long-acting...
July 2015: Current Opinion in HIV and AIDS
https://www.readbyqxmd.com/read/26049949/long-acting-antiviral-agents-for-hiv-treatment
#11
REVIEW
David A Margolis, Marta Boffito
PURPOSE OF REVIEW: Long-acting antiretroviral (ARV) agents are currently under development for the treatment of chronic HIV infection. This review focuses on data recently produced on injectable ARVs for patients living with HIV/AIDS and on the patients' perspectives on the use of these agents. RECENT FINDINGS: Crystalline nanoparticle formulations of the nonnucleoside reverse transcriptase inhibitor rilpivirine (TMC278) and of the HIV-1 integrase strand transfer inhibitor cabotegravir (GSK1265744) have progressed into phase II clinical trials as injectable maintenance therapy for patients living with HIV/AIDS with an undetectable viral load...
July 2015: Current Opinion in HIV and AIDS
https://www.readbyqxmd.com/read/26049948/formulation-and-pharmacology-of-long-acting-cabotegravir
#12
REVIEW
Christine Trezza, Susan L Ford, William Spreen, Rennan Pan, Stephen Piscitelli
PURPOSE OF REVIEW: Long-acting cabotegravir may provide a novel therapeutic option for both the treatment and prevention of HIV-1 infection that does not necessitate adherence to a daily regimen. The present review will highlight the unique formulation properties and pharmacologic attributes of long-acting cabotegravir nanosuspension. RECENT FINDINGS: Cabotegravir is a potent integrase strand transfer inhibitor that has been formulated as an oral tablet for daily administration and as a long-acting injectable nanosuspension...
July 2015: Current Opinion in HIV and AIDS
https://www.readbyqxmd.com/read/26049947/formulation-and-pharmacology-of-long-acting-rilpivirine
#13
REVIEW
Peter E Williams, Herta M Crauwels, Esther D Basstanie
PURPOSE OF REVIEW: Rilpivirine (RPV), a nonnucleoside reverse transcriptase inhibitor, is a potent antiretroviral (ARV) effective for HIV treatment at 25 mg daily oral dose. Its physio-chemical and pharmacological properties enable formulation of RPV as a long-acting injectable nanosuspension. This review summarizes these properties supporting the potential of intermittent parenteral administration of rilpivirine long acting (RPV LA) in both treatment and prevention of HIV-1 infection...
July 2015: Current Opinion in HIV and AIDS
https://www.readbyqxmd.com/read/25394037/hiv-treatment-2020-what-will-it-look-like
#14
Roy Gulick
Currently there are 28 approved antiretroviral drugs in six mechanistic classes, and recommended first-line regimens are highly potent, well tolerated, and as convenient as one pill, once-a-day. How will HIV treatment change by 2020? Over the next few years, we are likely to see potent 2-drug regimens tested head-to-head with standard three-drug regimens, and some of these will likely become standard-of-care. Newer agents with novel drug resistance profiles (e.g. doravirine, an NNRTI) or new mechanisms of action (e...
2014: Journal of the International AIDS Society
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