PMID- 30230694
OWN - NLM
STAT- MEDLINE
DCOM- 20200728
LR  - 20201125
IS  - 2160-7648 (Electronic)
IS  - 2160-763X (Print)
IS  - 2160-763X (Linking)
VI  - 8
IP  - 4
DP  - 2019 May
TI  - Effect of a High-Fat Meal on the Pharmacokinetics of the HIV Integrase Inhibitor 
      Cabotegravir.
PG  - 443-448
LID - 10.1002/cpdd.620 [doi]
AB  - Cabotegravir is an integrase inhibitor in clinical development for the treatment 
      and prevention of HIV infection using oral tablets for short-term, lead-in use 
      before subsequent administration of a long-acting injectable formulation. This 
      phase 1, single-center, randomized, 2 x 2 crossover study evaluated the effect of 
      a high-fat meal on the pharmacokinetics (PK) of oral cabotegravir. Healthy adults 
      received oral cabotegravir 30 mg as a single dose on 2 separate occasions, either 
      after fasting or following a high-fat meal ( approximately 53% fat,  approximately 870 kcal). Safety 
      evaluations and serial PK samples were collected, and a mixed-effects model was 
      used to determine within-participant treatment comparison of noncompartmental PK 
      parameters. Twenty-four patients were enrolled and had a mean body mass index of 
      25.6 kg/m(2) ; 67% were male. Compared with the fasting state, coadministration 
      of cabotegravir with a high-fat meal increased plasma cabotegravir area under the 
      concentration-time curve and maximal drug concentration, each by 14%. The slight 
      14% to 17% increase in exposure associated with a high-fat, high-calorie meal was 
      not considered clinically significant. No grade 3/4 adverse events (AEs), 
      drug-related AEs, or AEs leading to discontinuation were reported.
CI  - (c) 2018, The Authors. Clinical Pharmacology in Drug Development published by Wiley 
      Periodicals, Inc. on behalf of The American College of Clinical Pharmacology.
FAU - Patel, Parul
AU  - Patel P
AD  - ViiV Healthcare, Research Triangle Park, NC, USA.
FAU - Ford, Susan L
AU  - Ford SL
AD  - GlaxoSmithKline, Research Triangle Park, NC, USA.
FAU - Lou, Yu
AU  - Lou Y
AD  - PAREXEL International, Durham, NC, USA.
FAU - Bakshi, Kalpana
AU  - Bakshi K
AD  - GlaxoSmithKline, Upper Providence, PA, USA.
FAU - Tenorio, Allan R
AU  - Tenorio AR
AD  - ViiV Healthcare, Research Triangle Park, NC, USA.
FAU - Zhang, Zhiping
AU  - Zhang Z
AD  - PAREXEL International, Durham, NC, USA.
FAU - Pan, Rennan
AU  - Pan R
AD  - GlaxoSmithKline, Upper Providence, PA, USA.
FAU - Spreen, William
AU  - Spreen W
AD  - ViiV Healthcare, Research Triangle Park, NC, USA.
LA  - eng
SI  - ClinicalTrials.gov/NCT02799264
PT  - Clinical Trial, Phase I
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
DEP - 20180919
PL  - United States
TA  - Clin Pharmacol Drug Dev
JT  - Clinical pharmacology in drug development
JID - 101572899
RN  - 0 (HIV Integrase Inhibitors)
RN  - 0 (Pyridones)
RN  - 0 (Tablets)
RN  - HMH0132Z1Q (cabotegravir)
SB  - IM
MH  - Administration, Oral
MH  - Adolescent
MH  - Adult
MH  - Area Under Curve
MH  - Body Mass Index
MH  - Child
MH  - Cross-Over Studies
MH  - Diet, High-Fat/*adverse effects
MH  - Fasting/*blood
MH  - Female
MH  - HIV Integrase Inhibitors/administration & dosage/*pharmacokinetics
MH  - Healthy Volunteers
MH  - Humans
MH  - Male
MH  - Meals
MH  - Middle Aged
MH  - Models, Theoretical
MH  - Pyridones/administration & dosage/*pharmacokinetics
MH  - Tablets
MH  - Young Adult
PMC - PMC6585996
OTO - NOTNLM
OT  - absorption
OT  - food
OT  - high-fat
OT  - integrase inhibitor
OT  - pharmacokinetics
EDAT- 2018/09/20 06:00
MHDA- 2020/07/29 06:00
PMCR- 2019/06/20
CRDT- 2018/09/20 06:00
PHST- 2018/02/23 00:00 [received]
PHST- 2018/08/16 00:00 [accepted]
PHST- 2018/09/20 06:00 [pubmed]
PHST- 2020/07/29 06:00 [medline]
PHST- 2018/09/20 06:00 [entrez]
PHST- 2019/06/20 00:00 [pmc-release]
AID - CPDD620 [pii]
AID - 10.1002/cpdd.620 [doi]
PST - ppublish
SO  - Clin Pharmacol Drug Dev. 2019 May;8(4):443-448. doi: 10.1002/cpdd.620. Epub 2018 
      Sep 19.