Clinical Pharmacology in Drug Development Clinical Pharmacology in Drug Development RSS feedThis is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

Comparison of Two Manufacturing Processes of Daprodustat for Bioequivalence and Dissolution in Healthy Volunteers: A Randomized Crossover Study
AbstractDaprodustat, an orally bioavailable hypoxia-inducible factor –prolyl hydroxylase enzyme inhibitor, has recently completed phase 3 clinical development for treating anemia of chronic kidney disease. Part A of this 2-part, randomized, double-blind, single-dose, cross-over study (NCT04640311) compared pharmacokinetic properties of a single oral dose of daprodu stat 4 mg tablets manufactured via twin-screw wet granulation (process 1) to 2 sets of 4 mg tablets manufactured via high-shear wet granulation (process 2), to assess the impact of different dissolution profiles on pharmacokinetics. Part B assessed the bioequi...
Source: Clinical Pharmacology in Drug Development - May 2, 2023 Category: Drugs & Pharmacology Authors: Bonnie Shaddinger, Kelly M. Mahar, Mike Sprys, Susan M. Andrews, Sayantan Chattoraj, Rubeen Israni, Alex Cobitz Tags: Original Article Source Type: research

Issue Information
(Source: Clinical Pharmacology in Drug Development)
Source: Clinical Pharmacology in Drug Development - May 1, 2023 Category: Drugs & Pharmacology Tags: Issue Information Source Type: research

A Phase 1 First ‐in‐Human Pharmacokinetic and Pharmacodynamic Study of JNJ‐64264681, a Covalent Inhibitor of Bruton's Tyrosine Kinase
AbstractJNJ-64264681 is an irreversible covalent inhibitor of Bruton's tyrosine kinase. This phase 1, first-in-human, 2-part (single-ascending dose [SAD]; multiple-ascending dose [MAD]) study evaluated the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD; Bruton's tyrosine kinase occupancy [BTKO]) of JNJ-64264681 oral solution in healthy participants. For SAD (N = 78), 6 increasing doses of JNJ-64264681 (4 –400 mg) or placebo were evaluated in fasted males. The effects of sex, food, and a capsule formulation were evaluated in separate cohorts. For MAD (N = 27), sequential cohorts of male and female ...
Source: Clinical Pharmacology in Drug Development - May 1, 2023 Category: Drugs & Pharmacology Authors: Jocelyn H. Leu, Xin Miao, Kevin Shalayda, Kevin J. Coe, Ariane Kahnt, Bonnie Wu, Megan Schnarr, Carol Franks, James Devlin, Tong ‐Yuan Yang, James A. Palmer, Mai Zhang, Honghui Zhou, Wim Van Damme, Sophie Smets, Zuleima Aguilar, Sandra R Tags: Original Article Source Type: research

Exposure ‐Response Analysis to Assess the Concentration‐QTc Relationship of Iberdomide
AbstractIberdomide is an orally available cereblon-modulating agent being developed for the treatment of hematologic malignancies and autoimmune-mediated diseases. To assess the potential concentration-QTc relationship in humans and to ascertain or exclude a potential QT effect by iberdomide, a plasma concentration and ΔQTcF (change from baseline of corrected QT interval using the Fridericia formula) model of iberdomide was developed. Iberdomide concentration and paired high-quality, intensive electrocardiogram signal from a single-ascending-dose study in healthy subjects (N = 56) were included in the analysis. The prim...
Source: Clinical Pharmacology in Drug Development - April 21, 2023 Category: Drugs & Pharmacology Authors: Yiming Cheng, Allison Gaudy, Liangang Liu, Ying Ye, Michael Thomas, Yongjun Xue, Simon Zhou, Yan Li Tags: Original Article Source Type: research

Rimegepant 75  mg in Subjects With Hepatic Impairment: Results of a Phase 1, Open‐Label, Single‐Dose, Parallel‐Group Study
AbstractRimegepant is a small-molecule calcitonin gene –related peptide receptor antagonist (gepant) with demonstrated efficacy and safety in the acute and preventive treatment of migraine. Here, we report the pharmacokinetics and safety of a single 75-mg oral dose of rimegepant in subjects with severe, moderate, or mild hepatic impairment and matched healthy subjects from an open-label, single-dose, 4-group phase 1 study. Thirty-six subjects aged 41-71 years were enrolled, including 6 each with severe, moderate, or mild hepatic impairment and 18 healthy subjects. All subjects completed the study. A<20% increase in to...
Source: Clinical Pharmacology in Drug Development - April 19, 2023 Category: Drugs & Pharmacology Authors: Rajinder Bhardwaj, Andrea Ivans, Joseph Stringfellow, Beth Morris, Vladimir Coric, Robert Croop, Richard Bertz Tags: Original Article Source Type: research

Pharmacokinetics and Bioequivalence of Fluconazole Capsules Manufactured in France and China in Healthy Chinese Participants: Open ‐Label, Randomized, Single‐Dose, 2‐Way, Crossover Bioequivalence Study Under Fasted and Fed Conditions
AbstractThis was an open-label, randomized study in healthy Chinese participants to assess the bioequivalence of 2 fluconazole 150-mg capsules under fasted and fed conditions. The study consisted of 2 treatment periods, separated by a 14-day washout period. Thirty-six participants were enrolled, with 18 participants each in the fasted and fed groups. In each treatment period, participants received a single oral dose of the test or reference fluconazole 150-mg capsule. After washout, participants received the alternate treatment. Blood samples for pharmacokinetic analysis were collected from 1 hour before dosing to 72 hours...
Source: Clinical Pharmacology in Drug Development - April 13, 2023 Category: Drugs & Pharmacology Authors: Naihan Chen, Qing He, Ying Ma, Shixue Liu, Hua Wei, Ao Peng Tags: Original Article Source Type: research

Pharmacokinetics and Safety Evaluation of Maribavir in Healthy Japanese and Matched White Participants: A Phase I, Open ‐Label Study
This study demonstrated higher maribavir systemic exposure in Japanese than White participants and similar s afety outcomes. This difference in exposure is not considered clinically important and its significance remains to be determined. (Source: Clinical Pharmacology in Drug Development)
Source: Clinical Pharmacology in Drug Development - April 10, 2023 Category: Drugs & Pharmacology Authors: Ivy Song, Ben Suttle, Jingyang Wu, Katarina Ilic Tags: Original Article Source Type: research

Bioequivalence Study of Ezetimibe Tablets After a Single Oral Dose of 10  mg in Healthy Japanese Subjects Under Fasting Conditions
This study compared the pharmacokinetic and safety profiles between a new generic and a branded reference product of 10-mg ezetimibe (EZE) tablets in 24 healthy Japanese male volunteers under fasting conditions, obtaining sufficient evidence for the marketing approval of the new generic product. The bioequivalence study was conducted with an open-label, 2 × 2, single-dose, crossover design in which the test and reference products were administered to volunteers after fasting for ≥10 hours. Blood samples were collected 24 times before to 72 hours after the administration of the investigational drug. We evaluated the pe...
Source: Clinical Pharmacology in Drug Development - April 6, 2023 Category: Drugs & Pharmacology Authors: Shigenori Wada, Yoshiyuki Sasagane, Seiya Kagatani, Hiroaki Nakagami Tags: Original Article Source Type: research