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Bioequivalence Study of Two Formulations of Mifepristone Tablets in Healthy Chinese Subjects Under Fasting Conditions
In conclusion, the test and reference mifepristone were bioequivalent and well tolerated under fasting conditions. (Source: Clinical Pharmacology in Drug Development)
Source: Clinical Pharmacology in Drug Development - May 6, 2023 Category: Drugs & Pharmacology Authors: Mupeng Li, Xinchu Yi, Lianlian Fan, Luoxi Yang, Shan Xie, Jianzhong Shentu Tags: Original Article Source Type: research

A Phase 1, Open ‐Label, Fixed‐Sequence, Drug–Drug Interaction Study of Zanubrutinib with Rifabutin in Healthy Volunteers
AbstractZanubrutinib is a second-generation Bruton tyrosine kinase inhibitor that is primarily metabolized by CYP3A enzymes. Previous drug –drug interaction (DDI) studies have demonstrated that co-administration of zanubrutinib with rifampin, a strong CYP3A inducer, reduces zanubrutinib plasma concentrations, potentially impacting activity. The impact of the co-administration of zanubrutinib with less potent CYP3A inducers is unclear . This phase 1, open-label, fixed-sequence DDI study evaluated the pharmacokinetics, safety, and tolerability of zanubrutinib when co-administered with steady-state rifabutin, a known CYP3A ...
Source: Clinical Pharmacology in Drug Development - May 5, 2023 Category: Drugs & Pharmacology Authors: Bilal Tariq, Stephanie Conto, Aileen Cohen, Srikumar Sahasranaman, Ying C. Ou Tags: Original Article Source Type: research

Comparative Pharmacokinetics and Safety Studies of Dexibuprofen Injection and a Branded Product Ibuprofen Injection in Healthy Chinese Volunteers
AbstractIbuprofen, a nonsteroidal anti-inflammatory drug, is considered a safe and effective analgesic for treating different types of pain and joint disorders. Dexibuprofen, S-(+)-ibuprofen, is the single pharmacologically active enantiomer of ibuprofen. It is more potent than the racemic formulation of ibuprofen in terms of analgesic and anti-inflammatory properties and causes less acute gastric damage. For the first time, in the present single-dose, randomized, open-label, 2-period crossover study, the safety and pharmacokinetic (PK) characteristics of a single-dose dexibuprofen injection (0.2  g) were evaluated in hea...
Source: Clinical Pharmacology in Drug Development - May 5, 2023 Category: Drugs & Pharmacology Authors: Wenyan Hua, Wenjia Zhou, Mei Su, Quanying Zhang, Shunlin Zong, Meng Wang Tags: Original Article Source Type: research

Evaluation of the Cytochrome P450 3A and P ‐glycoprotein Drug‐Drug Interaction Potential of Futibatinib
AbstractFutibatinib, a selective, irreversible fibroblast growth factor receptor 1 –4 inhibitor, is being investigated for tumors harboringFGFR aberrations and was recently approved for the treatment ofFGFR2 fusion/rearrangement-positive intrahepatic cholangiocarcinoma. In vitro studies identified cytochrome P450 (CYP) 3A as the major CYP isoform in futibatinib metabolism and indicated that futibatinib is likely a P-glycoprotein (P-gp) substrate and inhibitor. Futibatinib also showed time-dependent inhibition of CYP3A in vitro. Phase I studies investigated the drug-drug interactions of futibatinib with itraconazole (a du...
Source: Clinical Pharmacology in Drug Development - May 4, 2023 Category: Drugs & Pharmacology Authors: Ikuo Yamamiya, Allen Hunt, Toru Takenaka, Daryl Sonnichsen, Mark Mina, Yaohua He, Karim A. Benhadji, Ling Gao Tags: Original Article Source Type: research

Pharmacokinetics and Bioequivalence of 2 Nifedipine Controlled ‐Release Tablets: A Randomized, Single‐Dose, 2‐Period Crossover Study in Healthy Chinese Volunteers Under Fasting and Fed Conditions
AbstractThe aim of this study was to evaluate the bioequivalence of generic nifedipine controlled-release tablet compared to branded product under fasting and fed conditions. A randomized, single-dose, 2-period, crossover study with a 7-day washout period was performed in 84 healthy Chinese volunteers (fasting cohort, n  = 42; fed cohort, n = 42). In each study period, volunteers were assigned to receive a single oral dose of the generic or reference product (30 mg). Blood samples were collected before dosing and up to 72 hours after administration. The plasma concentration of nifedipine was determined by a v alidate...
Source: Clinical Pharmacology in Drug Development - May 3, 2023 Category: Drugs & Pharmacology Authors: Liang Xin, Qing Chen, Dandan Chen, Yijhen Li, Yiqun Li, Qingqing Wu, Yang Zou, Wei Wang, Jingying Jia, Chen Yu, Yanmei Liu Tags: Original Article Source Type: research

Pharmacokinetic Drug ‐Drug Interaction With Coadministration of Cannabidiol and Everolimus in a Phase 1 Healthy Volunteer Trial
AbstractWhen highly purified cannabidiol (CBD; Epidiolex) and the mammalian target of rapamycin inhibitor everolimus are used concomitantly in the treatment of tuberous sclerosis complex, there is evidence of a pharmacokinetic (PK) interaction, leading to increased everolimus systemic exposure. We evaluated the effect of steady-state CBD exposure following multiple clinically relevant CBD doses on everolimus PK in healthy adult participants in a single-center, fixed-sequence, open-label, phase 1 study. All participants received oral everolimus 5  mg on day 1, followed by a 7-day washout. On days 9–17, participants recei...
Source: Clinical Pharmacology in Drug Development - May 3, 2023 Category: Drugs & Pharmacology Authors: Louise Wray, Joris Berwaerts, David Critchley, Kerry Hyland, Cuiping Chen, Ching Thai, Bola Tayo Tags: Original Article Source Type: research

Disposition and Mass Balance of Etrasimod in Healthy Subjects and In Vitro Determination of the Enzymes Responsible for Its Oxidative Metabolism
AbstractEtrasimod (APD334) is an investigational, once-daily, oral, selective sphingosine 1-phosphate receptor 1,4,5 modulator (S1P1,4,5) in development for treatment of various immune-mediated inflammatory disorders. The disposition and mass balance of a single 2-mg [14C]etrasimod dose were evaluated in 8 healthy males. An in vitro study was also conducted to identify etrasimod's oxidative metabolizing enzymes. Peak concentrations of etrasimod and total radioactivity in plasma and whole blood were typically reached 4 –7 hours postdose. Etrasimod constituted 49.3% of total radioactivity plasma exposure, with multiple mi...
Source: Clinical Pharmacology in Drug Development - May 3, 2023 Category: Drugs & Pharmacology Authors: Caroline A. Lee, D. Alexander Oh, Yong Tang, Ping Yi, Mohammad Bashir, Stephen English, Marie Croft, Anthony Blackburn, Steve Bloom, Kye Gilder, John S. Grundy Tags: Original Article Source Type: research