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Issue Information
(Source: Clinical Pharmacology in Drug Development)
Source: Clinical Pharmacology in Drug Development - April 24, 2024 Category: Drugs & Pharmacology Tags: Issue Information Source Type: research

Comparative Pharmacokinetics and Safety Assessment of 1st ‐ and 2nd‐Generation Zinpentraxin Alfa Drug Products in Healthy Volunteers: A Randomized Crossover Study
AbstractZinpentraxin alfa is a recombinant form of the human pentraxin-2 that was studied in idiopathic pulmonary fibrosis (IPF). To improve the purity and yield of the drug material, a 2nd-generation drug product was developed. To characterize  and compare the pharmacokinetic (PK) properties of the 1st- and 2nd-generation zinpentraxin alfa, PK studies were conducted in healthy volunteers (HVs). In a phase 1 randomized, double-blind, 2-sequence crossover, sequential 2-stage study (ISRCTN59409907), single intravenous (IV) doses of 1st- and 2nd-generation zinpentraxin alfa at 10 mg/kg were studied with a blinded interim an...
Source: Clinical Pharmacology in Drug Development - April 23, 2024 Category: Drugs & Pharmacology Authors: Tu H. Mai, Rajbharan Yadav, Audrey Arjomandi, Christine Jung, Monika M. Meier, Francis Donaldson, Rui Zhao, Han ‐Ting Ding, Joy C. Hsu, Nikhil Kamath, Lin Pan Tags: Original Article Source Type: research

Safety, Tolerability, and Pharmacokinetics of Anaprazole, a Novel Proton Pump Inhibitor, in Healthy Chinese Subjects
In conclusion, anaprazole sodium enteric-coated tablets were found to be sa fe and well tolerated in healthy Chinese individuals. Anaprazole is absorbed and metabolized consistently in the human body without any accumulation. (Source: Clinical Pharmacology in Drug Development)
Source: Clinical Pharmacology in Drug Development - April 18, 2024 Category: Drugs & Pharmacology Authors: Fangfang Wang, Xiaoye Niu, Fei Liu, Xifeng Ma, Fang Cheng, Haiyan Xu, Li Wang, Yanjun Xu, Haiyan Li Tags: Original Article Source Type: research

Effects of Quinidine or Rifampin Co ‐administration on the Single‐Dose Pharmacokinetics and Safety of Rilzabrutinib (PRN1008) in Healthy Participants
AbstractThis open-label, phase 1 study was conducted with healthy adult participants to evaluate the potential drug-drug interaction between rilzabrutinib and quinidine (an inhibitor of P-glycoprotein [P-gp] and CYP2D6) or rifampin (an inducer of CYP3A and P-gp). Plasma concentrations of rilzabrutinib were measured after a single oral dose of rilzabrutinib 400  mg administered on day 1 and again, following a wash-out period, after co-administration of rilzabrutinib and quinidine or rifampin. Specifically, quinidine was given at a dose of 300 mg every 8 hours for 5 days from day 7 to day 11 (N = 16) while rifampin was gi...
Source: Clinical Pharmacology in Drug Development - April 17, 2024 Category: Drugs & Pharmacology Authors: Christian Rask ‐Madsen, Suresh Katragadda, Mengyao Li, Sibel Ucpinar, Leslie Chinn, Puneet Arora, Patrick Smith Tags: Original Article Source Type: research

Population Pharmacokinetics and Dosing Simulations for Aripiprazole 2 ‐Month Ready‐to‐Use Long‐Acting Injectable in Adult Patients With Schizophrenia or Bipolar I Disorder
AbstractA ready-to-use (RTU) long-acting injectable (LAI) formulation of aripiprazole monohydrate for administration once every 2 months, available in 960 mg (Ari 2MRTU 960) or 720 mg doses, has been developed for the treatment of schizophrenia or bipolar I disorder. A previously developed and validated population pharmacokinetic model for characterizing aripiprazole plasma concentrations following administration of oral aripiprazole or aripiprazole once-monthly (AOM) intramuscular injection was expanded to include the RTU LAI formulation of aripiprazole (Ari RTU LAI). Overall, 8899  aripiprazole pharmacokinetic samples f...
Source: Clinical Pharmacology in Drug Development - April 12, 2024 Category: Drugs & Pharmacology Authors: Yanlin Wang, Matthew Harlin, Frank Larsen, Xiaofeng Wang, Wansu Park, Benjamin Rich, Jogarao V. Gobburu, Arash Raoufinia Tags: Original Article Source Type: research

Bioequivalence of Elagolix/Estradiol/Norethindrone Acetate Fixed ‐Dose Combination Product: Phase 1 Results in Healthy Pre‐ and Postmenopausal Women
AbstractFixed-dose combination (FDC) therapies can enhance patient convenience and adherence to prescribed treatment regimens. Elagolix is a novel oral gonadotropin-releasing hormone receptor antagonist approved for management of moderate to severe pain associated with endometriosis and heavy menstrual bleeding associated with uterine fibroids. Hormonal add-back therapy can attenuate the reversible hypoestrogenic effects of elagolix. An FDC formulation containing elagolix/estradiol (E2)/norethindrone acetate (NETA) 300/1/0.5  mg as the morning dose and an elagolix 300 mg capsule as the evening dose, were evaluated in 2 b...
Source: Clinical Pharmacology in Drug Development - April 10, 2024 Category: Drugs & Pharmacology Authors: Mong ‐Jen Chen, Patrick Marroum, Yi‐Lin Chiu, Melina Neenan, Nael M. Mostafa, Mohamad Shebley Tags: Original Article Source Type: research

A Population Pharmacokinetic Assessment of the Effect of Food on Selumetinib in Patients with Neurofibromatosis Type 1 ‐Related Plexiform Neurofibromas and Healthy Volunteers
AbstractSelumetinib is clinically used for pediatric patients with neurofibromatosis type 1 and symptomatic, inoperable plexiform neurofibromas. Until recently, selumetinib had to be taken twice daily, after 2 hours of fasting and followed by 1 hour of fasting, which could be inconvenient. This population analysis evaluated the effect of low- and high-fat meals on the pharmacokinetic (PK) parameters of selumetinib and its active metabolite N-desmethyl selumetinib. The dataset comprised 511 subjects from 15 clinical trials who received ≥1 dose of selumetinib and provided ≥1 measurable postdose concentration of selumetin...
Source: Clinical Pharmacology in Drug Development - April 9, 2024 Category: Drugs & Pharmacology Authors: Peiying Zuo, Million Arefayene, Wei ‐Jian Pan, Tomoko Freshwater, Jonathan Monteleone Tags: Original Article Source Type: research

Pharmacokinetics of Nitazoxanide Dry Suspensions After Single Oral Doses in Healthy Subjects: Food Effects Evaluation and Bioequivalence Study
AbstractNitazoxanide (NTZ) is an effective antiparasitic drug with potent antiviral and antimicrobial activity. This randomized, open-label, 2-sequence, 2-period crossover trial was designed to evaluate the bioequivalence (BE) of the NTZ dry suspension in healthy subjects and investigated the effect of food intake on the pharmacokinetic (PK) properties of tizoxanide (an active metabolite of NTZ, TIZ). Sixty healthy Chinese subjects were enrolled and received a single dose of 500  mg/25 mL of preparations on days 1 and 4 under overnight fasting or fed conditions, respectively. The plasma concentration of TIZ was determine...
Source: Clinical Pharmacology in Drug Development - April 5, 2024 Category: Drugs & Pharmacology Authors: Chenning Zhang, Rui Liang, Dejie Liu, Xianghua Wang, Shuhua Yang, Qingwen Hu, Qing Wen, Hengli Zhao Tags: Original Article Source Type: research

Issue Information
(Source: Clinical Pharmacology in Drug Development)
Source: Clinical Pharmacology in Drug Development - April 4, 2024 Category: Drugs & Pharmacology Tags: Issue Information Source Type: research

A Randomized, Single ‐Dose, Parallel‐Controlled Phase 1 Clinical Comparison of an Omalizumab Biosimilar Candidate with Reference Omalizumab in Healthy Chinese Male Volunteers
This study evaluated the bioequivalence of omalizumab, a humanized monoclonal antibody against immunoglobulin-E (IgE), with one of its biosimilar candidates. The study was designed as a randomized, double-blind, parallel-controlled trial. A total of subjects who met the inclusion criteria and did not meet the exclusion criteria were dynamically randomly assigned to receive the test drug or the reference drug with a single subcutaneous injection of 150  mg by the minimization method. The test group and the reference group had similar demographic characteristics and baseline characteristics of total IgE. The 90% confidence ...
Source: Clinical Pharmacology in Drug Development - April 4, 2024 Category: Drugs & Pharmacology Authors: Jie Cheng, Chenguang Wang, Jin Xu, Chunyang Zhao, Rong Song, Yijun Wang, Yang Zou, Xunmin Zhang, Yong Shan, Jian Zhou, Jing ‐Ying Jia Tags: Original Article Source Type: research

Evaluation of Bioequivalence for Avapritinib Tablets in Chinese Participants Under Fasting Conditions Using a Reference ‐Scaled Average Bioequivalence Method
This study aimed to assess the bioequivalence of 2 avapritinib tablets formulations. A randomized, open-label, single-center trial was conducted on fasting, healthy Chinese participants. The study utilized a partial replicated design with 3 sequences and 3 periods. Participants were assigned to 1 of 3 sequences, with each sequence receiving the reference formulation twice and the test formulation once. Plasma samples were collected and analyzed to determine pharmacokinetic parameters. The bioequivalence of the 2 avapritinib formulations was assessed using reference-scaled average bioequivalence for the maximum plasma conce...
Source: Clinical Pharmacology in Drug Development - March 25, 2024 Category: Drugs & Pharmacology Authors: Zenglian Yue, Yin Wang, Zeng Li, Tao Jin, Yucheng Sheng Tags: Original Article Source Type: research

A Phase 1, Randomized, Double ‐Blind, Placebo‐Controlled, Single Ascending Dose Study to Evaluate the Pharmacokinetics, Immunogenicity, Safety, and Tolerability After Subcutaneous Administration of Tozorakimab in Healthy Chinese Participants
AbstractTozorakimab is a high-affinity human immunoglobulin G1 monoclonal antibody that neutralizes interleukin (IL)-33, an IL-1 family cytokine. This phase 1, single-center, randomized, double-blind, placebo-controlled, single ascending dose study (NCT05070312) evaluated tozorakimab in a healthy Chinese population. Outcomes included the characterization of the pharmacokinetic (PK) profile and immunogenicity of tozorakimab. Safety outcomes included treatment-emergent adverse events (TEAEs) and clinical laboratory, electrocardiogram, and vital sign parameters. Healthy, non-smoking, male, and female Chinese participants aged...
Source: Clinical Pharmacology in Drug Development - March 25, 2024 Category: Drugs & Pharmacology Authors: Yunfei Li, Hua Zhang, Hitesh Pandya, Liyan Miao, Fred Reid, Eulalia Jimenez, Muhammad Waqas Sadiq, Rachel Moate, Alejhandra Lei, Xiao ‐Hong Zhou, Chris Kell, Junjie Ding, Guanlin Zhang, Lina Zhao, Xiaoyun Ge Tags: Original Article Source Type: research

Clinical Pharmacology of GP40321 (Insulin Glulisine Biosimilar): Pharmacokinetic and Pharmacodynamic Comparability in a Hyperinsulinemic ‐Euglycemic Clamp Procedure
AbstractThe aim of the study was to compare the pharmacokinetics (PK) and pharmacodynamics (PD) of T-glu (GP40321, test drug), and reference insulin glulisine in a hyperinsulinemic-euglycemic clamp procedure. During this study, 34 healthy male volunteers underwent the hyperinsulinemic-euglycemic clamp procedure following subcutaneous 0.3  U/kg injection of T-glu or reference insulin glulisine in a randomized, double-blind, crossover study. Plasma glucose levels were monitored every 5 minutes for 8 hours. Glucose infusion rate adjustment was based on the blood glucose measurements. Evaluation of PD was performed using th...
Source: Clinical Pharmacology in Drug Development - March 22, 2024 Category: Drugs & Pharmacology Authors: Ekaterina Koksharova, Roman Drai, Sergei Noskov, Artem Dorotenko, Ekaterina Protsenko, Kseniia Radaeva, Anna Arefeva, Maria Gefen, Gagik Galstyan, Igor Makarenko Tags: Original Article Source Type: research

Comparative Bioequivalence and Food Effect of Two Formulations of 30 ‐mg Nifedipine Controlled‐Release Tablets in Healthy Chinese Adults
The objective of this trial was to assess the bioequivalence of a 30-mg nifedipine controlled-release tablet and a reference drug in a cohort of healthy Chinese individuals. Two independent open-label, randomized, single-dose, crossover studies were conducted, 1 under fasting conditions (N = 44, with 1 participant dropping out midway) and the other under fed conditions (N = 44, with 4 participants dropping out midway). Plasma concentrations of nifedipine were determined using liquid chromatography-mass spectrometry, and pharmacokinetic (PK) parameters were calculated using noncompartmental analysis with Phoenix WinNonlin 8...
Source: Clinical Pharmacology in Drug Development - March 14, 2024 Category: Drugs & Pharmacology Authors: Huizi Zhang, Siyang Wang, Hongxia Wang, Tingting Zhi, Jian Ren, Yanhui Wang, Zhiqing Yao, Pan Zhang, Naobei Ye, Ruiqin Zhang Tags: Original Article Source Type: research

Safety, Tolerability, and Pharmacokinetics of Single ‐ and Multiple‐Ascending Doses of Sunobinop in Healthy Participants
AbstractSunobinop is an investigational, potent, selective partial agonist at the nociceptin/orphanin FQ peptide receptor in vitro. Three phase 1 studies were conducted to evaluate the safety, tolerability, and pharmacokinetics (PK) of escalating single- and multiple-dose administration of sunobinop in healthy participants. Study 1 was a randomized, double-blind, placebo-controlled, single-ascending dose study. Study 2 was a randomized, double-blind, placebo-controlled, multiple-ascending dose study. Study 3 was a randomized, open-label, single-dose, 4-way crossover study of oral and sublingual sunobinop comparing morning ...
Source: Clinical Pharmacology in Drug Development - March 13, 2024 Category: Drugs & Pharmacology Authors: Alessandra Cipriano, Ram P. Kapil, Mingyan Zhou, Manjunath S. Shet, Garth T. Whiteside, Sandra K. Willsie, Stephen C. Harris Tags: Original Article Source Type: research