Drug Metab Dispos 2021 Mar;49(3):287-288
Eur J Clin Pharmacol 2021 May 8. Epub 2021 May 8.
Department of Clinical Pharmacy, Faculty of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Purpose: There are limited data regarding the safety of direct oral anticoagulants (DOACs) during breastfeeding. The aim of the present study is to investigate the extent of excretion of DOACs into human milk according to the available clinical and experimental studies.Methods: On 16th January 2021, we systematically searched PubMed, Scopus, Embase, and Web of Science for all studies which investigated DOACs in breastfeeding without any time frame and language limitation. Read More
J Biomol Struct Dyn 2021 May 6:1-18. Epub 2021 May 6.
Department of Zoology, Molecular Endocrinology Lab, University of Lucknow, Lucknow, India.
The synthesized 1,5 diarylpenta-1,4-dien-3-one derivatives (compounds 1-6) as synthetic curcumin analogues were tested for their potential anticancer activity against human ovarian and lung adenocarcinoma cells. The absorption, distribution, metabolism, excretion, and toxicity (ADMET/pharmacokinetic) parameters of all the compounds were predicted by admetSAR software. The pharmacokinetics, pharmacodynamics and bioactivity scores properties based on Lipinski rule and Ghose filter, calculated with the help of Molinspiration and ChemDraw. Read More
Clin Pharmacol Drug Dev 2021 May 6. Epub 2021 May 6.
Mitsubishi Tanabe Pharma Corporation, Chuo-ku, Tokyo, Japan.
The neuroprotective agent edaravone is an intravenous treatment for amyotrophic lateral sclerosis. As intravenous administration burdens patients, orally administered treatments are needed. This phase 1, open-label, single-dose crossover study in 42 healthy adults evaluated bioequivalence of a 105-mg edaravone oral suspension and intravenous edaravone (60 mg/60 min). Read More
Drug Metab Dispos 2021 May 5. Epub 2021 May 5.
Novartis Institute for Biomedical Research, East Hanover, United States, United States.
Tropifexor (NVP-LJN452) is a highly potent, selective, non-steroidal, non-bile acid farnesoid X receptor (FXR) agonist for the treatment of nonalcoholic steatohepatitis (NASH). Its absorption, metabolism, and excretion were studied following a 1-mg oral dose of [C]tropifexor to four healthy male subjects. Mass balance was achieved with ~94% of the administered dose recovered in excreta through 312 hours collection period. Read More
Clin Pharmacol Drug Dev 2021 May 4. Epub 2021 May 4.
Protagonist Therapeutics, Inc, Newark, California, USA.
PN-943 is an orally stable, gastrointestinal-restricted peptide that binds specifically to α4ß7 integrin on leukocytes, blocking leukocyte trafficking to and activation in the gut, inhibiting colon inflammation and reducing signs and symptoms of active ulcerative colitis. Two pharmacokinetic/pharmacodynamic studies were conducted in healthy volunteers. Study 1 was a first-in-human study with 40 male subjects receiving PN-943, 100 to 1400 mg or placebo, as single doses and 57 male subjects receiving PN-943, 100 to 1000 mg or placebo, as multiple doses. Read More