Long-Acting Strategies for Antibody Drugs: Structural Modification, Controlling Release, and Changing the Administration Route
AbstractBecause of their high specificity, high affinity, and targeting, antibody drugs have been widely used in the treatment of many diseases and have become the most favored new drugs for research in the world. However, some antibody drugs (such as small-molecule antibody fragments) have a short half-life and need to be administered frequently, and are often associated with injection-site reactions and local toxicities during use. Increasing attention has been paid to the development of antibody drugs that are long-acting and have fewer side effects. This paper reviews existing strategies to achieve long-acting antibody...
Source: European Journal of Drug Metabolism and Pharmacokinetics - April 18, 2024 Category: Drugs & Pharmacology Source Type: research

A Phase I Clinical Study Comparing the Pharmacokinetics, Safety, and Immunogenicity of GB221 Injection and Trastuzumab (Herceptin ®) in Healthy Chinese Adults
ConclusionGB221 demonstrated similar pharmacokinetics to trastuzumab and comparable safety and immunogenicity in healthy Chinese adults. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - April 2, 2024 Category: Drugs & Pharmacology Source Type: research

Assessment of the Effects of Abrocitinib on the Pharmacokinetics of Probe Substrates of Cytochrome P450 1A2, 2B6 and 2C19 Enzymes and Hormonal Oral Contraceptives in Healthy Individuals
ConclusionsBased on the study results, abrocitinib is a moderate inhibitor of CYP2C19. Caution should be exercised when using abrocitinib concomitantly with narrow therapeutic index medicines that are primarily metabolized by CYP2C19 enzyme. Abrocitinib is a mild inhibitor of CYP1A2; however, the impact is not clinically relevant, and no general dose adjustment is recommended for CYP1A2 substrates. Abrocitinib does not inhibit CYP3A or induce CYP1A2/2B6/2C19/3A and does not affect the pharmacokinetics of contraceptives.Clinical Trials RegistrationClinicalTrials.gov registration IDs: NCT03647670, NCT05067439, NCT03662516. (...
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 30, 2024 Category: Drugs & Pharmacology Source Type: research

A Phase I, Open-Label, Mass Balance Study of [14C]-Iberdomide in Healthy Subjects
ConclusionBiotransformation of iberdomide in humans included multiple oxidations of the morpholino moiety as well as glutarimide ring hydrolysis of parent and oxidized metabolites and a combination of these pathways. Iberdomide was the predominant component in human plasma, with metabolite M12 being the most prominent circulating metabolite. In excreta, similar iberdomide-derived radioactivity was found in urine and feces.Trial registration numberNCT03294603. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 23, 2024 Category: Drugs & Pharmacology Source Type: research

Correction: Population Pharmacokinetic Analysis of Vancomycin in Patients with Solid or Hematological Malignancy in Relation to the Quick Sequential Organ Failure Assessment Scores
(Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 18, 2024 Category: Drugs & Pharmacology Source Type: research

Kinetic Characterization of Estradiol Glucuronidation by Liver Microsomes and Expressed UGT Enzymes: The Effects of Organic Solvents
ConclusionOrganic solvents such as methanol, ethanol, and acetonitrile showed great potential in adjusting the glucuronidation of estradiol. DMSO is the most suitable solvent due to its minimal influence on estradiol glucuronidation. Researchers should be cautious in selecting appropriate solvents to get accurate results when assessing the metabolism of a new chemical entity. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 12, 2024 Category: Drugs & Pharmacology Source Type: research

Anti-calcitonin Gene-Related Peptide Monoclonal Antibodies in Migraine: Focus on Clinical Pharmacokinetics
AbstractThe calcitonin gene-related peptide transmission was the target for recent development of drugs that effectively prevent attacks of both episodic and chronic migraine. The aim of this narrative review was to offer deeper insight into pharmacokinetics of monoclonal antibodies approved for prevention of migraine attacks. For this narrative review, relevant literature was searched for in MEDLINE and Google Scholar databases, covering periods 1966 –2023 and 2006–2023, respectively. The ClinicalTrials.gov database was also searched for relevant clinical studies whose results had not been published previously in medi...
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 10, 2024 Category: Drugs & Pharmacology Source Type: research

Predicting Pharmacokinetics of Drugs Using Artificial Intelligence Tools: A Systematic Review
ConclusionOverall, artificial intelligence tools offer a robust, rapid, and precise means of predicting various pharmacokinetic parameters based on a dataset containing information of patients or drugs. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 8, 2024 Category: Drugs & Pharmacology Source Type: research

Anti-Calcitonin Gene-Related Peptide Monoclonal Antibodies in Migraine: Focus on Drug Interactions
AbstractCalcitonin gene-related peptide neurotransmission was the target for recent development of monoclonal antibodies that effectively prevent attacks of both episodic and chronic migraine. The aim of this narrative review was to offer deeper insight into drug-drug, drug-food and drug-disease interactions of monoclonal antibodies approved for prevention of migraine attacks. For this narrative review, relevant literature was searched for in MEDLINE and Google Scholar databases, covering the 1966 –2023 and 2006–2023 periods, respectively. The ClinicalTrials.gov database was also searched for relevant clinical studies ...
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 8, 2024 Category: Drugs & Pharmacology Source Type: research