Pub Date : 2024-09-19DOI: 10.1080/17425255.2024.2407616
Srinivas Kamath, Paul Joyce
Published in Expert Opinion on Drug Metabolism & Toxicology (Just accepted, 2024)
发表于《药物代谢与毒理学专家意见》（刚刚接受，2024 年）
{"title":"A critical need for ‘gut neutrality’: mitigating adverse drug-microbiome interactions","authors":"Srinivas Kamath, Paul Joyce","doi":"10.1080/17425255.2024.2407616","DOIUrl":"https://doi.org/10.1080/17425255.2024.2407616","url":null,"abstract":"Published in Expert Opinion on Drug Metabolism & Toxicology (Just accepted, 2024)","PeriodicalId":12250,"journal":{"name":"Expert Opinion on Drug Metabolism & Toxicology","volume":"1 1","pages":""},"PeriodicalIF":4.3,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142265451","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-09-13DOI: 10.1080/17425255.2024.2402493
Stefano Bellosta, Alberto Corsini
Statins are the primary therapeutic approach for treating hypercholesterolemia in hyperlipidemic high cardiovascular-risk patients, as stated by the recent European and American guidelines. However...
根据最近的欧美指南，他汀类药物是治疗高脂血症高心血管风险患者高胆固醇血症的主要治疗方法。然而...
{"title":"Drug interactions in cardiology: focus on statins and their combination with other lipid-lowering drugs","authors":"Stefano Bellosta, Alberto Corsini","doi":"10.1080/17425255.2024.2402493","DOIUrl":"https://doi.org/10.1080/17425255.2024.2402493","url":null,"abstract":"Statins are the primary therapeutic approach for treating hypercholesterolemia in hyperlipidemic high cardiovascular-risk patients, as stated by the recent European and American guidelines. However...","PeriodicalId":12250,"journal":{"name":"Expert Opinion on Drug Metabolism & Toxicology","volume":"9 1","pages":""},"PeriodicalIF":4.3,"publicationDate":"2024-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142180850","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-09-13DOI: 10.1080/17425255.2024.2401589
Lidiya Kukova, Kashif M. Munir, Ahmed Sayeed, Stephen N. Davis
GLP-1 receptor agonists provide multiple benefits for patients with type 2 diabetes. Nonetheless, there are also several significant adverse effects associated with these agents. A thorough underst...
{"title":"Assessing the therapeutic and toxicological profile of novel GLP-1 receptor agonists for type 2 diabetes","authors":"Lidiya Kukova, Kashif M. Munir, Ahmed Sayeed, Stephen N. Davis","doi":"10.1080/17425255.2024.2401589","DOIUrl":"https://doi.org/10.1080/17425255.2024.2401589","url":null,"abstract":"GLP-1 receptor agonists provide multiple benefits for patients with type 2 diabetes. Nonetheless, there are also several significant adverse effects associated with these agents. A thorough underst...","PeriodicalId":12250,"journal":{"name":"Expert Opinion on Drug Metabolism & Toxicology","volume":"32 1","pages":"1-14"},"PeriodicalIF":4.3,"publicationDate":"2024-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142265446","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-09-12DOI: 10.1080/17425255.2024.2402478
Hina Khan, Ammara Zamir, Imran Imran, Hamid Saeed, Faleh Alqahtani, Abdul Majeed, Majid Aziz, Muhammad Fawad Rasool
Glipizide is an oral antidiabetic drug widely used to treat non-insulin-dependent type II diabetes mellitus (NIDDM). This systematic review extensively examines all reported pharmacokinetic (PK) pa...
{"title":"Clinical pharmacokinetics of glipizide: a systematic review","authors":"Hina Khan, Ammara Zamir, Imran Imran, Hamid Saeed, Faleh Alqahtani, Abdul Majeed, Majid Aziz, Muhammad Fawad Rasool","doi":"10.1080/17425255.2024.2402478","DOIUrl":"https://doi.org/10.1080/17425255.2024.2402478","url":null,"abstract":"Glipizide is an oral antidiabetic drug widely used to treat non-insulin-dependent type II diabetes mellitus (NIDDM). This systematic review extensively examines all reported pharmacokinetic (PK) pa...","PeriodicalId":12250,"journal":{"name":"Expert Opinion on Drug Metabolism & Toxicology","volume":"2 1","pages":""},"PeriodicalIF":4.3,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142265514","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-09-11DOI: 10.1080/17425255.2024.2401600
Michael W Stewart
INTRODUCTIONThe modern treatment of chorioretinal vascular diseases follows the recent development and rapid adoption of drugs that inhibit vascular endothelial growth factor (VEGF). All anti-VEGF drugs are delivered intravitreally, with clinical behavior, including efficacy, durability, and safety, largely determined by their pharmacokinetic properties.AREAS COVEREDProperties of these new drugs include additional binding targets (placental growth factor (PlGF) and angiopoietin 2 (Ang 2)), binding affinity, potency, intravitreal half-life, and increased molar dose. A PubMed search for 'pharmacokinetics of anti-VEGF drugs' was performed from 2000 to 2023. Relevant studies were reviewed and referred to in the manuscript.EXPERT OPINIONEarly developers concentrated on improving efficacy, but since maximum efficacy with VEGF inhibition has been reached, development has pivoted to extending the duration of action. Durability strategies include inhibiting additional pathways (faricimab), increasing molar dose (abicipar, brolucizumab, faricimab, and aflibercept 8 mg), and prolonging the intravitreal half-life (abicipar and KSI-301). Recent phase 3 trials demonstrated modest improvements in durability, but failures that might be attributed to these strategies (conjugation and manufacturing processes) have occurred. Future drug development focuses on extending duration of action with implantable reservoirs (ranibizumab port delivery system), sustained release devices (tyrosine kinase inhibitors), and gene therapy.
{"title":"Intraocular drugs: pharmacokinetic strategies and the influence on efficacy and durability.","authors":"Michael W Stewart","doi":"10.1080/17425255.2024.2401600","DOIUrl":"https://doi.org/10.1080/17425255.2024.2401600","url":null,"abstract":"INTRODUCTIONThe modern treatment of chorioretinal vascular diseases follows the recent development and rapid adoption of drugs that inhibit vascular endothelial growth factor (VEGF). All anti-VEGF drugs are delivered intravitreally, with clinical behavior, including efficacy, durability, and safety, largely determined by their pharmacokinetic properties.AREAS COVEREDProperties of these new drugs include additional binding targets (placental growth factor (PlGF) and angiopoietin 2 (Ang 2)), binding affinity, potency, intravitreal half-life, and increased molar dose. A PubMed search for 'pharmacokinetics of anti-VEGF drugs' was performed from 2000 to 2023. Relevant studies were reviewed and referred to in the manuscript.EXPERT OPINIONEarly developers concentrated on improving efficacy, but since maximum efficacy with VEGF inhibition has been reached, development has pivoted to extending the duration of action. Durability strategies include inhibiting additional pathways (faricimab), increasing molar dose (abicipar, brolucizumab, faricimab, and aflibercept 8 mg), and prolonging the intravitreal half-life (abicipar and KSI-301). Recent phase 3 trials demonstrated modest improvements in durability, but failures that might be attributed to these strategies (conjugation and manufacturing processes) have occurred. Future drug development focuses on extending duration of action with implantable reservoirs (ranibizumab port delivery system), sustained release devices (tyrosine kinase inhibitors), and gene therapy.","PeriodicalId":12250,"journal":{"name":"Expert Opinion on Drug Metabolism & Toxicology","volume":"31 1","pages":"1-11"},"PeriodicalIF":4.3,"publicationDate":"2024-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142180851","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-09-11DOI: 10.1080/17425255.2024.2402496
Arianna Cella,Alessandro Marè,Gian Luigi Gigli,Marialuisa Zedde,Mariarosaria Valente,Giovanni Merlino
INTRODUCTIONAntithrombotic therapy is the mainstay of ischemic stroke prevention. Current drugs (antiplatelets and oral anticoagulants) lead to increased bleeding risks, and the rates of stroke recurrence, despite antithrombotic therapy, are still elevated. There is a need for novel antithrombotic therapies with superior effectiveness but without increased bleeding risk. Factor XIa inhibitors might cover this gap.AREAS COVEREDThis manuscript examines the pharmacokinetic and pharmacodynamic properties of asundexian and the current clinical evidence regarding its application in preventing ischemic stroke.EXPERT OPINIONAsundexian shows a very favoring pharmacokinetic profile. Despite asundexian being inferior to apixaban for cardioembolic ischemic stroke, it could be useful in patients with non-cardioembolic ischemic stroke. Although antiplatelet therapy is the recommended treatment to prevent non-cardioembolic ischemic stroke, adding an anticoagulant might have beneficial effects through the dual-pathway inhibition strategy. Due to the potential risk of hemorrhagic transformation, there is hesitation to administer anticoagulants early to patients who have recently had an ischemic stroke, especially if they are also on antiplatelet therapy. However, clinical trials on asundexian confirmed its safety for bleeding, even when used with antiplatelets. A phase 3 trial is currently investigating the efficacy of asundexian in preventing non-cardioembolic ischemic stroke.
{"title":"A pharmacokinetic and pharmacodynamic evaluation of asundexian: a novel factor XIa inhibitor for stroke prevention.","authors":"Arianna Cella,Alessandro Marè,Gian Luigi Gigli,Marialuisa Zedde,Mariarosaria Valente,Giovanni Merlino","doi":"10.1080/17425255.2024.2402496","DOIUrl":"https://doi.org/10.1080/17425255.2024.2402496","url":null,"abstract":"INTRODUCTIONAntithrombotic therapy is the mainstay of ischemic stroke prevention. Current drugs (antiplatelets and oral anticoagulants) lead to increased bleeding risks, and the rates of stroke recurrence, despite antithrombotic therapy, are still elevated. There is a need for novel antithrombotic therapies with superior effectiveness but without increased bleeding risk. Factor XIa inhibitors might cover this gap.AREAS COVEREDThis manuscript examines the pharmacokinetic and pharmacodynamic properties of asundexian and the current clinical evidence regarding its application in preventing ischemic stroke.EXPERT OPINIONAsundexian shows a very favoring pharmacokinetic profile. Despite asundexian being inferior to apixaban for cardioembolic ischemic stroke, it could be useful in patients with non-cardioembolic ischemic stroke. Although antiplatelet therapy is the recommended treatment to prevent non-cardioembolic ischemic stroke, adding an anticoagulant might have beneficial effects through the dual-pathway inhibition strategy. Due to the potential risk of hemorrhagic transformation, there is hesitation to administer anticoagulants early to patients who have recently had an ischemic stroke, especially if they are also on antiplatelet therapy. However, clinical trials on asundexian confirmed its safety for bleeding, even when used with antiplatelets. A phase 3 trial is currently investigating the efficacy of asundexian in preventing non-cardioembolic ischemic stroke.","PeriodicalId":12250,"journal":{"name":"Expert Opinion on Drug Metabolism & Toxicology","volume":"54 1","pages":""},"PeriodicalIF":4.3,"publicationDate":"2024-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142180870","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
INTRODUCTIONThe treatment of advanced cervical cancer is continuously developing. There is a critical need to explore new treatment options to improve cure rates and make treatment more affordable. Despite efforts in prevention, cervical cancer remains the fourth most common cancer worldwide in terms of both incidence and mortality.AREAS COVEREDThis article offers an updated and critical analysis of angiogenesis inhibitors used in the treatment of advanced cervical cancer. It should be noted that this is not a systematic review.EXPERT OPINIONBevacizumab is currently the primary antiangiogenic agent used alongside chemotherapy and has become the standard of care for advanced cervical cancer. However, there are still uncertainties regarding the molecular mechanisms and associations in cervical cancer that could help in optimizing the use of Bevacizumab. Factors such as cost, toxicity, and methodological issues in the GOG-240 trial must be considered.
{"title":"Pharmacokinetics and pharmacodynamics of angiogenesis inhibitors used to treat cervical cancer: current and future.","authors":"Aurora Gonzalez-Fierro,Guadalupe Domínguez-Gómez,Alma Chavez-Blanco,Alfonso Duenas-Gonzalez","doi":"10.1080/17425255.2024.2401586","DOIUrl":"https://doi.org/10.1080/17425255.2024.2401586","url":null,"abstract":"INTRODUCTIONThe treatment of advanced cervical cancer is continuously developing. There is a critical need to explore new treatment options to improve cure rates and make treatment more affordable. Despite efforts in prevention, cervical cancer remains the fourth most common cancer worldwide in terms of both incidence and mortality.AREAS COVEREDThis article offers an updated and critical analysis of angiogenesis inhibitors used in the treatment of advanced cervical cancer. It should be noted that this is not a systematic review.EXPERT OPINIONBevacizumab is currently the primary antiangiogenic agent used alongside chemotherapy and has become the standard of care for advanced cervical cancer. However, there are still uncertainties regarding the molecular mechanisms and associations in cervical cancer that could help in optimizing the use of Bevacizumab. Factors such as cost, toxicity, and methodological issues in the GOG-240 trial must be considered.","PeriodicalId":12250,"journal":{"name":"Expert Opinion on Drug Metabolism & Toxicology","volume":"21 1","pages":"1-9"},"PeriodicalIF":4.3,"publicationDate":"2024-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142180872","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-09-09DOI: 10.1080/17425255.2024.2401603
Mariela Nunez,Supratik Kar,Katherine A Rodriguez,Dariel Ondieki
INTRODUCTIONAlopecia Areata (AA), characterized by non-scarring hair loss due to the dysregulation of the JAK/STAT pathway, has long lacked effective treatment. In 2023, Ritlecitinib, a novel Janus kinase (JAK) 3 and tyrosine kinase family inhibitor, received its first approval from the US FDA to treat AA, followed by approvals in Japan, Europe, China, and the UK. This development aims to address the challenges faced by millions of individuals affected by this condition globally.AREAS COVEREDThis review offers an overview of Ritlecitinib's pharmacological properties, biological targets, and development strategies. It examines its mechanism of action, pharmacokinetics, pharmacodynamics, and clinical trial insights. Additionally, it covers the drug's chemical synthesis, contraindications, drug interactions, and potential adverse effects, with special attention to its use in adolescents, pregnant women, and the elderly.EXPERT OPINIONRitlecitinib represents a significant advancement in treating AA, offering a targeted approach with promising efficacy and a favorable safety profile. While long-term safety data and real-world effectiveness studies are needed, its oral administration and efficacy in both adults and adolescents position it as a potentially transformative therapy. Ongoing research should focus on optimizing treatment strategies, identifying predictive biomarkers, and assessing cost-effectiveness to fully realize Ritlecitinib's potential in improving outcomes.
{"title":"Unraveling Ritlecitinib: an in-depth analysis of JAK3 inhibitor for the treatment of alopecia areata.","authors":"Mariela Nunez,Supratik Kar,Katherine A Rodriguez,Dariel Ondieki","doi":"10.1080/17425255.2024.2401603","DOIUrl":"https://doi.org/10.1080/17425255.2024.2401603","url":null,"abstract":"INTRODUCTIONAlopecia Areata (AA), characterized by non-scarring hair loss due to the dysregulation of the JAK/STAT pathway, has long lacked effective treatment. In 2023, Ritlecitinib, a novel Janus kinase (JAK) 3 and tyrosine kinase family inhibitor, received its first approval from the US FDA to treat AA, followed by approvals in Japan, Europe, China, and the UK. This development aims to address the challenges faced by millions of individuals affected by this condition globally.AREAS COVEREDThis review offers an overview of Ritlecitinib's pharmacological properties, biological targets, and development strategies. It examines its mechanism of action, pharmacokinetics, pharmacodynamics, and clinical trial insights. Additionally, it covers the drug's chemical synthesis, contraindications, drug interactions, and potential adverse effects, with special attention to its use in adolescents, pregnant women, and the elderly.EXPERT OPINIONRitlecitinib represents a significant advancement in treating AA, offering a targeted approach with promising efficacy and a favorable safety profile. While long-term safety data and real-world effectiveness studies are needed, its oral administration and efficacy in both adults and adolescents position it as a potentially transformative therapy. Ongoing research should focus on optimizing treatment strategies, identifying predictive biomarkers, and assessing cost-effectiveness to fully realize Ritlecitinib's potential in improving outcomes.","PeriodicalId":12250,"journal":{"name":"Expert Opinion on Drug Metabolism & Toxicology","volume":"24 1","pages":"1-14"},"PeriodicalIF":4.3,"publicationDate":"2024-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142180874","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
INTRODUCTIONNicardipine is a type of calcium channel blocker that is commonly used in the treatment of angina pectoris, hypertension, and related cardiovascular disorders. This systematic review assesses the reported pharmacokinetic (PK) and associated pharmacodynamic (PD) parameters of nicardipine in humans.AREAS COVEREDAn exhaustive literature search using four internet databases was conducted up to 5 October 2023, which yielded 871 papers, of which 32 fulfilled the eligibility requirements by including human PK and related PD data. The area under the plasma concentration vs. time curve from zero to infinity (AUC0-∞) and maximum plasma concentration (Cmax) of nicardipine rise proportionately with increasing dosage. One study revealed that AUC0-∞ of nicardipine was increased by 5-fold in hepatic cirrhosis patients compared to the control subjects. Moreover, related PD data in renal-impaired hypertensive patients revealed that a notable reduction in blood pressure was associated with nicardipine administration.EXPERT OPINIONThis review covers comprehensive data on clinical PK, drug-drug interaction studies, effects of dosage form on ADME, and associated PD parameters of nicardipine using all relevant published studies. The present study will also aid in the development and evaluation of PK models for suggesting model-informed dosing regimens.PROSPERO NUMBERCRD42024533051.
{"title":"Clinical pharmacokinetics and pharmacodynamics of Nicardipine; a systematic review.","authors":"Ammara Ayub,Ammara Zamir,Imran Imran,Hamid Saeed,Abdul Majeed,Majid Aziz,Faleh Alqahtani,Muhammad Fawad Rasool","doi":"10.1080/17425255.2024.2402481","DOIUrl":"https://doi.org/10.1080/17425255.2024.2402481","url":null,"abstract":"INTRODUCTIONNicardipine is a type of calcium channel blocker that is commonly used in the treatment of angina pectoris, hypertension, and related cardiovascular disorders. This systematic review assesses the reported pharmacokinetic (PK) and associated pharmacodynamic (PD) parameters of nicardipine in humans.AREAS COVEREDAn exhaustive literature search using four internet databases was conducted up to 5 October 2023, which yielded 871 papers, of which 32 fulfilled the eligibility requirements by including human PK and related PD data. The area under the plasma concentration vs. time curve from zero to infinity (AUC0-∞) and maximum plasma concentration (Cmax) of nicardipine rise proportionately with increasing dosage. One study revealed that AUC0-∞ of nicardipine was increased by 5-fold in hepatic cirrhosis patients compared to the control subjects. Moreover, related PD data in renal-impaired hypertensive patients revealed that a notable reduction in blood pressure was associated with nicardipine administration.EXPERT OPINIONThis review covers comprehensive data on clinical PK, drug-drug interaction studies, effects of dosage form on ADME, and associated PD parameters of nicardipine using all relevant published studies. The present study will also aid in the development and evaluation of PK models for suggesting model-informed dosing regimens.PROSPERO NUMBERCRD42024533051.","PeriodicalId":12250,"journal":{"name":"Expert Opinion on Drug Metabolism & Toxicology","volume":"16 1","pages":""},"PeriodicalIF":4.3,"publicationDate":"2024-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142180873","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-09-09DOI: 10.1080/17425255.2024.2402931
Sophie Vieujean,Laurent Peyrin-Biroulet
INTRODUCTIONUlcerative colitis is a chronic inflammatory bowel disease, affecting the colorectal mucosae, with a relapsing-remitting course, characterized by the trafficking and gathering of lymphocytes in the inflammatory intestinal mucosa. Sphingosine-1-phosphate (S1P) receptor modulators preventing lymphocytes egress from lymphoid tissues to the active inflammation site is an alternative therapeutic option in this condition.AREA COVEREDWe carried out a comprehensive review of the literature available on Medline, Scopus and Embase regarding the pharmacokinetics of S1P receptor modulators. For each compound, we reviewed the mechanism of action, pharmacokinetic data and efficacy and safety data from phase 3 studies and real-life studies when available.EXPERT OPINIONS1P receptor modulators, including ozanimod and etrasimod (both currently on the market) as well as VTX002 (under development), are a new class of drugs for the treatment of moderate to severe ulcerative colitis, inducing and maintaining the remission. Due to its pharmacokinetic features, this class of drugs has certain advantages such as an oral administration, a short half-life, a high volume of distribution, and no immunogenicity. On the other hand, there are risks of cardiological and ophthalmological side-effects, as well as drug-drug interactions risk, that require special attention from the healthcare providers.
{"title":"Pharmacokinetics of S1P receptor modulators in the treatment of ulcerative colitis.","authors":"Sophie Vieujean,Laurent Peyrin-Biroulet","doi":"10.1080/17425255.2024.2402931","DOIUrl":"https://doi.org/10.1080/17425255.2024.2402931","url":null,"abstract":"INTRODUCTIONUlcerative colitis is a chronic inflammatory bowel disease, affecting the colorectal mucosae, with a relapsing-remitting course, characterized by the trafficking and gathering of lymphocytes in the inflammatory intestinal mucosa. Sphingosine-1-phosphate (S1P) receptor modulators preventing lymphocytes egress from lymphoid tissues to the active inflammation site is an alternative therapeutic option in this condition.AREA COVEREDWe carried out a comprehensive review of the literature available on Medline, Scopus and Embase regarding the pharmacokinetics of S1P receptor modulators. For each compound, we reviewed the mechanism of action, pharmacokinetic data and efficacy and safety data from phase 3 studies and real-life studies when available.EXPERT OPINIONS1P receptor modulators, including ozanimod and etrasimod (both currently on the market) as well as VTX002 (under development), are a new class of drugs for the treatment of moderate to severe ulcerative colitis, inducing and maintaining the remission. Due to its pharmacokinetic features, this class of drugs has certain advantages such as an oral administration, a short half-life, a high volume of distribution, and no immunogenicity. On the other hand, there are risks of cardiological and ophthalmological side-effects, as well as drug-drug interactions risk, that require special attention from the healthcare providers.","PeriodicalId":12250,"journal":{"name":"Expert Opinion on Drug Metabolism & Toxicology","volume":"21 1","pages":""},"PeriodicalIF":4.3,"publicationDate":"2024-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142180871","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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