Clinical Pharmacology in Drug Development This 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.

Pharmacokinetic and Bioequivalence Evaluation of Single ‐Tablet and Separate‐Tablet Regimens for Ainuovirine, Lamivudine, and Tenofovir Disoproxil Fumarate in Chinese Healthy Subjects
AbstractThis was a single-dose, randomized, open-label, 2-period crossover study to evaluate the bioequivalence of the ACC008 (test formulation [T]) versus coadministered ainuovirine (ANV) 150  mg, lamivudine (3TC) 300 mg, and tenofovir disoproxil fumarate 300 mg (reference formulation [R]) in the fasted state among the Chinese healthy adults. Eligible subjects were randomized into 2 cohorts to received treatment in 1 of 2 sequences (T → R, R → T). PK samples were collected fro m 1 hour before dosing to 144 hours after dosing in each period. The concentrations of ANV, 3TC, and tenofovir in plasma were determin...
Source: Clinical Pharmacology in Drug Development - July 20, 2023 Category: Drugs & Pharmacology Authors: Lei Huang, Jing Lei, Yuanxun Yang, Tingting Ma, Hui Lin, Bei Cao, Juan Li Tags: Original Article Source Type: research

Pharmacokinetics of the Akt Serine/Threonine Protein Kinase Inhibitor, Capivasertib, Administered to Healthy Volunteers in the Presence and Absence of the CYP3A4 Inhibitor Itraconazole
AbstractCapivasertib is a potent, selective inhibitor of all 3 Akt isoforms (Akt1/2/3), and it is currently being tested in Phase III trials for the treatment of prostate and breast cancer. To investigate the effect of a cytochrome P450 3A4 (CYP3A4) inhibitor on the pharmacokinetics of capivasertib, a Phase I drug –drug interaction study of capivasertib and itraconazole was conducted in 11 healthy volunteers (median age, 54 years). The 8-day study had 3 stages: Participants received a single dose of capivasertib 80 mg in Stage 1, 4 doses of itraconazole 200 mg over 3 days in Stage 2, and a final dose of capivasertib ...
Source: Clinical Pharmacology in Drug Development - July 15, 2023 Category: Drugs & Pharmacology Authors: Claire Miller, Roberto Sommavilla, Simon T. Barry, Cath Eberlein, Thomas Morris, Ian Wadsworth, Marie Cullberg Tags: Original Article Source Type: research

Pharmacokinetics, Safety, and Tolerability of Vonoprazan ‐ or Esomeprazole‐Based Bismuth‐Containing Quadruple Therapy: A Phase 1, Double‐Blind, Parallel‐Group Study in Adults with Helicobacter pylori Infection in China
In conclusion, vonoprazan had no significant effect on plasma bismuth exposure compared with esomeprazole. (Source: Clinical Pharmacology in Drug Development)
Source: Clinical Pharmacology in Drug Development - July 14, 2023 Category: Drugs & Pharmacology Authors: Jia Miao, Chao Hu, Jie Tang, Wenyan Wang, Ying Wang, Ruoting Men, Li Yang, Liqun Gu, Naoki Yoshida, Richard Czerniak Tags: Original Article Source Type: research

Current Status of Weekly Insulin Analogs and Their Pharmacokinetic/Pharmacodynamic Evaluation by the Euglycemic Clamp Technique
AbstractDiabetes mellitus represents a significant global health threat characterized by hyperglycemia caused by inadequate insulin secretion and/or insulin resistance. Exogenous insulin supplements had been recognized as a crucial treatment for achieving successful glycemic control in patients with Type 1 and most patients with Type 2 diabetes. Over the past century, substantial progress has been made in the development of novel insulin formulations, including the super-fast-acting and long-acting basal insulin analogs, of which the latter is indispensable for the management of nocturnal fasting and intraprandial blood gl...
Source: Clinical Pharmacology in Drug Development - July 13, 2023 Category: Drugs & Pharmacology Authors: Na An, Xuhong Wang, Anshun He, Wei Chen Tags: Review Source Type: research

Comparative Bioavailability of Two Daily Subcutaneous Doses Versus a Single Dose of Intramuscular and Vaginal Progesterone Formulations in Healthy Postmenopausal Females
AbstractProgesterone is a naturally occurring endocrine hormone. It is used for luteal phase support to improve success rates in assisted reproduction. This was a single-center, comparative bioavailability, open-label, randomized, 3-period, 6-sequence, crossover study to compare the rate and extent of absorption of subcutaneous (SC) progesterone 25 mg twice daily, versus vaginal (Vag) gel once daily (90 mg progesterone) and 50 mg of intramuscular (IM) progesterone injection once daily in healthy postmenopausal females. Eighteen healthy, postmenopausal, female nonsmokers aged 55 –65 years were dosed. Data from 17 subjects...
Source: Clinical Pharmacology in Drug Development - July 13, 2023 Category: Drugs & Pharmacology Authors: Mario Tanguay, Barbara Cometti, Sylvie Boudreault Tags: Original Article Source Type: research

Pharmacokinetic Similarity of ABP 654, an Ustekinumab Biosimilar Candidate: Results from a Randomized, Double ‐blind Study in Healthy Subjects
AbstractABP 654 is a proposed biosimilar to ustekinumab reference product (RP) which works through antagonism of interleukin-12 and interleukin-23. Ustekinumab RP is used for the treatment of chronic inflammatory conditions, including some forms of plaque psoriasis, psoriatic arthritis, Crohn's disease, and ulcerative colitis. A randomized, double-blinded, single-dose, 3-arm, parallel-group study was conducted to assess the pharmacokinetic (PK) similarity of ABP 654 with ustekinumab RP sourced from the United States (US) and the European Union (EU); the PK similarity of ustekinumab US versus ustekinumab EU; and the compara...
Source: Clinical Pharmacology in Drug Development - July 8, 2023 Category: Drugs & Pharmacology Authors: Vincent Chow, Daniel T. Mytych, Shyamal Das, Janet Franklin Tags: Original Article Source Type: research

Bioequivalence of Two 6 ‐Mercaptopurine Tablet Formulations in Healthy Fasting Chinese Volunteers
AbstractThe supply of branded 6-mercaptopurine (6-MP) is limited in China, necessitating the local production and clinical evaluation of generic alternatives. We evaluated the in vivo bioequivalence (BE) of a new generic mercaptopurine tablet (50  mg) formulation by comparing peak plasma concentration and area under the concentration–time curve (AUC) with a branded 6-MP formulation as the reference in 36 healthy fasting Chinese adults. The in vivo BE was evaluated by the average BE test. The safety parameters of the test and reference for mulations were also evaluated. The geometric mean ratios for AUC over the dosing i...
Source: Clinical Pharmacology in Drug Development - July 6, 2023 Category: Drugs & Pharmacology Authors: Yaping Deng, Guohua Wang, Guojun Jiang, Dandan Song, Xian Xu, Dandan Zhao, Guojun Tan, Zijun Tan, Jian Chen Tags: Original Article Source Type: research

Evaluation of Drug –Drug Interaction Potential of Enarodustat (JTZ‐951) Using a Cytochrome P450 Probe Cocktail
AbstractThe drug interaction potential of enarodustat (doses: 25, 50  mg) on the activity of cytochrome P450 (CYP) 1A2, 2C9, 2C19, 2D6, and 3A4 was evaluated after once-daily administration for 15 days in a phase 1 multiple-ascending-dose study in healthy subjects. Probe substrates specific for the enzymes, i.e., caffeine (CYP1A2), tolbutamide (CYP2C9), omeprazole (CYP2C19), dextromethorphan (CYP2D6), and midazolam (CYP3A4), were administered orally as a cocktail with (day 15) and without (day −3) enarodustat. Drug interaction was based on geometric mean maximum plasma concentration (Cmax) and area under the plasma co...
Source: Clinical Pharmacology in Drug Development - July 5, 2023 Category: Drugs & Pharmacology Authors: Sudhakar M. Pai, Hiroyuki Yamada, Hiroyuki Murata Tags: Original Article Source Type: research