Expert opinion on drug metabolism & toxicology最新文献_第8页

The influence of pharmacodynamics and pharmacokinetics on the antimigraine efficacy and safety of novel anti-CGRPergic pharmacotherapies: a narrative review. 药效学和药代动力学对新型抗 CGRP 能药物疗法的抗偏头痛疗效和安全性的影响：叙述性综述。

Expert opinion on drug metabolism & toxicology Pub Date : 2025-01-01 Epub Date: 2024-09-30 DOI: 10.1080/17425255.2024.2409253

Abimael González-Hernández, Carlos M Villalón

{"title":"The influence of pharmacodynamics and pharmacokinetics on the antimigraine efficacy and safety of novel anti-CGRPergic pharmacotherapies: a narrative review.","authors":"Abimael González-Hernández, Carlos M Villalón","doi":"10.1080/17425255.2024.2409253","DOIUrl":"10.1080/17425255.2024.2409253","url":null,"abstract":"Introduction: Migraine is a complex disorder, and its etiology is not yet fully understood. In the last 40 years, calcitonin gene-related peptide (CGRP) has been central to the understanding of migraine pathophysiology, leading to the development of new molecules targeting the CGRPergic system. These new molecules, such as gepants and monoclonal antibodies, are effective, well-tolerated, and safe, and are approved for clinical use.Areas covered: By searching multiple electronic scientific databases, this narrative review examined: (i) the role of CGRP in migraine; and (ii) the current knowledge on the effects of CGRPergic antimigraine pharmacotherapies, including a brief analysis of their pharmacodynamic and pharmacokinetic characteristics.Expert opinion: Current anti-CGRPergic medications, although effective, have limitations, such as side effects and lack of antimigraine efficacy in some patients. The existence of patients with medication-resistant migraine may be due to the: (i) complex migraine pathophysiology, in which several systems appear to be deregulated before, during, and after a migraine attack; and (ii) pharmacodynamic and pharmacokinetic properties of antimigraine medications. As envisioned here, although seminal studies support the notion that CGRP plays a key role in migraine headache, the dysfunction of CGRPergic transmission does not seem to be relevant in all cases.","PeriodicalId":94005,"journal":{"name":"Expert opinion on drug metabolism & toxicology","volume":" ","pages":"41-52"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142335162","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Pharmacokinetic evaluation of fezolinetant for the treatment of vasomotor symptoms caused by menopause. 用于治疗更年期引起的血管运动症状的非索内酯的药代动力学评估。

Expert opinion on drug metabolism & toxicology Pub Date : 2025-01-01 Epub Date: 2024-10-16 DOI: 10.1080/17425255.2024.2416046

Laura Cucinella, Sara Tedeschi, Stefano Memoli, Chiara Cassani, Ellis Martini, Rossella E Nappi

{"title":"Pharmacokinetic evaluation of fezolinetant for the treatment of vasomotor symptoms caused by menopause.","authors":"Laura Cucinella, Sara Tedeschi, Stefano Memoli, Chiara Cassani, Ellis Martini, Rossella E Nappi","doi":"10.1080/17425255.2024.2416046","DOIUrl":"10.1080/17425255.2024.2416046","url":null,"abstract":"Introduction: Vasomotor symptoms (VMS) affect the majority of menopausal women, with possible negative impact on several domains of quality of life (QoL). Although menopausal hormone therapy (MHT) represents an effective treatment, the risk-benefit profile is not favorable for every woman. Non-hormonal options are limited in number and efficacy.Areas covered: Fezolinetant is a novel oral non-hormonal drug recently approved for the treatment of moderate-severe VMS. It acts as an antagonist of neurokinin 3 receptor (NK3R), the main target of neurokinin B (a tachykinin over-expressed by kisspeptin/neurokinin B/dynorphin [KNDy] neurons after menopausal hypoestrogenism), involved in the modulation of the thermoregulatory hypothalamic center. Here, we report pharmacodynamics and pharmacokinetic properties of fezolinetant as well as its efficacy and safety data from available clinical trials.Expert opinion: Fezolinetant has shown efficacy in reducing the frequency and severity of VMS with a positive impact on sleep- and health-related QoL and acceptable safety and tolerability profile. Given the limited availability of effective non-hormonal options for VMS, fezolinetant could potentially represent a game-changer for care of menopausal women, especially when relative or absolute contraindications to MHT use are present. Further studies to gain more information about the safety profile and potential extra-VMS benefits or disadvantages are warranted in real-life clinical practice.","PeriodicalId":94005,"journal":{"name":"Expert opinion on drug metabolism & toxicology","volume":" ","pages":"105-113"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142402466","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Impact of pediatric continuous renal replacement therapy parameters on meropenem, piperacillin, and tazobactam pharmacokinetics: an in vitro model. 儿童连续肾替代治疗参数对美罗培南、哌拉西林和他唑巴坦药代动力学的影响：体外模型

Expert opinion on drug metabolism & toxicology Pub Date : 2024-12-22 DOI: 10.1080/17425255.2024.2443754

Michael Thy, Floura Kecili, Saik Urien, Naim Bouazza, Frantz Foissac, Léo Froelicher Bournaud, Steeve Rouillon, Sihem Benaboud, Fabrice Lesage, Jean-Marc Tréluyer, Gabrielle Lui, Mehdi Oualha

{"title":"Impact of pediatric continuous renal replacement therapy parameters on meropenem, piperacillin, and tazobactam pharmacokinetics: an in vitro model.","authors":"Michael Thy, Floura Kecili, Saik Urien, Naim Bouazza, Frantz Foissac, Léo Froelicher Bournaud, Steeve Rouillon, Sihem Benaboud, Fabrice Lesage, Jean-Marc Tréluyer, Gabrielle Lui, Mehdi Oualha","doi":"10.1080/17425255.2024.2443754","DOIUrl":"10.1080/17425255.2024.2443754","url":null,"abstract":"Background: Limited data exist on how continuous renal replacement therapy (CRRT) affects antimicrobial dosing in pediatric patients. This study examined the impact of pediatric CRRT parameters on the pharmacokinetics (PK) of meropenem, piperacillin, and tazobactam using an in vitro CRRT model.Research design and methods: An in vitro CRRT model with a pediatric ST60 circuit was used to assess antimicrobial clearance during continuous veno-venous hemodialysis (CVVHD) or hemofiltration (CVVH). Antimicrobials were administered intermittently or continuously, with samples taken pre- and post-filter, and from the effluent. The model tested two conditions: 1) off treatment (0 mL/kg/h), and 2) an elimination phase, with CRRT flow rates ranging from 40 to 400 mL/kg/h.Results: Clearance of meropenem, piperacillin, and tazobactam increased significantly with higher dialyzate/ultrafiltration flow rates (p < 0.001). Median clearance rates differed significantly by CRRT flow rates and modality (p < 0.001). Under CVVHD, the saturation coefficient (Sa) decreased with increasing dialyzate flow rates, while under CVVH, the sieving coefficient (Sc) remained stable regardless of ultrafiltration rates.Conclusions: The clearance of low protein-binding, low molecular weight antimicrobials increases with higher CRRT effluent flow rates, with modality-specific differences in clearance dynamics.","PeriodicalId":94005,"journal":{"name":"Expert opinion on drug metabolism & toxicology","volume":" ","pages":"1-9"},"PeriodicalIF":0.0,"publicationDate":"2024-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142848742","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

The oral GnRH antagonists, a new class of drugs in gynecology: from pharmacokinetics to possible clinical applications. 口服 GnRH 拮抗剂--妇科领域的一类新药：从药物动力学到可能的临床应用。

Expert opinion on drug metabolism & toxicology Pub Date : 2024-12-17 DOI: 10.1080/17425255.2024.2441981

Marta Barretta, Michele Vignali, Antonio La Marca, Giovanni Grandi

{"title":"The oral GnRH antagonists, a new class of drugs in gynecology: from pharmacokinetics to possible clinical applications.","authors":"Marta Barretta, Michele Vignali, Antonio La Marca, Giovanni Grandi","doi":"10.1080/17425255.2024.2441981","DOIUrl":"10.1080/17425255.2024.2441981","url":null,"abstract":"Introduction: In ovarian steroid-dependent diseases such as uterine fibroids, endometriosis and adenomyosis, oral GnRH antagonists have emerged as new therapeutic alternatives. These oral GnRH antagonists offer key advantages, including oral administration, dose-dependent estrogen suppression and rapid reversibility.Areas covered: This review examines the pharmacological, clinical and therapeutic profiles of the latest non-peptide oral GnRH antagonists, through an analysis of clinical evidence and randomized clinical trials, to provide a comprehensive and up-to-date overview of their clinical applications and potential benefits.Expert opinion: The clinical trials examined demonstrated significant efficacy in reducing heavy menstrual bleeding in women with fibroids and pelvic pain in women with endometriosis, with more than 70% of patients achieving primary endpoints. The use of add-back therapy minimized bone mass density loss, ensuring long-term safety. Adverse events were dose-dependent but generally well tolerated. In our opinion, the strength of oral GnRH antagonists lies in their pharmacological properties. Oral administration increases convenience, allows adjustable dosing and ensures a dose-dependent effect. These drugs provide an immediate antagonistic effect without the flare-up phenomenon. Furthermore, they are expected to act on ectopic endometrial and smooth muscle cell receptors, potentially providing additional anti-proliferative effects. However, further research is needed: long term clinical trials must compare them with existing treatments.","PeriodicalId":94005,"journal":{"name":"Expert opinion on drug metabolism & toxicology","volume":" ","pages":"1-13"},"PeriodicalIF":0.0,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142819641","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Pharmacokinetic studies in dialysis-dependent patients: limited data availability. 透析依赖型患者的药代动力学研究：可用数据有限。

Expert opinion on drug metabolism & toxicology Pub Date : 2024-12-15 DOI: 10.1080/17425255.2024.2441141

George R Bailie, Nancy A Mason

引用次数: 0

Immune-mediated liver injury caused by immune checkpoint inhibitors exhibits distinct clinical features that differ from autoimmune hepatitis. 免疫检查点抑制剂引起的免疫介导肝损伤表现出不同于自身免疫性肝炎的独特临床特征。

Expert opinion on drug metabolism & toxicology Pub Date : 2024-12-12 DOI: 10.1080/17425255.2024.2434642

Yan Wang, Yu Su, Tiantian Guo, Mengyu Zhao, Liwei Liu, Wei Chen, Xinyan Zhao

{"title":"Immune-mediated liver injury caused by immune checkpoint inhibitors exhibits distinct clinical features that differ from autoimmune hepatitis.","authors":"Yan Wang, Yu Su, Tiantian Guo, Mengyu Zhao, Liwei Liu, Wei Chen, Xinyan Zhao","doi":"10.1080/17425255.2024.2434642","DOIUrl":"https://doi.org/10.1080/17425255.2024.2434642","url":null,"abstract":"Background: Immune-mediated liver injury caused by immune checkpoint inhibitors (ILICI) and autoimmune hepatitis (AIH) are both related to the distorted immune system. However, ILICI differs from AIH in several distinct ways. We aimed to study the differences between ILICI and AIH.Research design and methods: This is a retrospective study collecting clinical data of ILICI (2016.1-2024.2) and AIH (2002.1-2023.6) patients. Demographic, clinicopathological, radiological characteristics, treatment and outcomes were analyzed.Results: A total of 71 ILICI and 158 AIH cases were included. ILICI group had older patients and fewer females (age: 66 vs. 56 years, gender: 28.2% vs. 85.4%, p < 0.001). They had lower ALT, AST, TBil, IgG levels, and lower titers of ANA. Some ILICI patients exhibited bile duct edema and dilation, while AIH patients typically had liver fibrosis in CT/MRI. Histologically, ILICI showed bile duct injury, inflammatory cells infiltration with fewer plasma cells. Glucocorticoid treatment was less common, but ALT level recovery was faster in ILICI patients (41 vs. 140 days, p < 0.001).Conclusions: ILICI generally affects older patients without a female predilection and is linked to milder, acute liver injury. High ANA titers, elevated IgG, and prominent plasma cell infiltration were less common. Liver function normalizes more quickly in ILICI.","PeriodicalId":94005,"journal":{"name":"Expert opinion on drug metabolism & toxicology","volume":" ","pages":"1-9"},"PeriodicalIF":0.0,"publicationDate":"2024-12-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142815359","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Methadone metabolism and cytochrome P450 polymorphisms: a systematic review and meta-analysis. 美沙酮代谢与细胞色素 P450 多态性：系统回顾与荟萃分析。

Expert opinion on drug metabolism & toxicology Pub Date : 2024-11-28 DOI: 10.1080/17425255.2024.2432664

Seenae Eum, Nicholas P Vernacchia, Nia Doughty, Sahar Mehrzad, Andrew H Talal, Fatemeh Chalabianloo, Evan D Kharasch

{"title":"Methadone metabolism and cytochrome P450 polymorphisms: a systematic review and meta-analysis.","authors":"Seenae Eum, Nicholas P Vernacchia, Nia Doughty, Sahar Mehrzad, Andrew H Talal, Fatemeh Chalabianloo, Evan D Kharasch","doi":"10.1080/17425255.2024.2432664","DOIUrl":"https://doi.org/10.1080/17425255.2024.2432664","url":null,"abstract":"Introduction: Confusion regarding methadone metabolism exists, hampering optimal clinical use. A systematic review was conducted to assess the impacts of cytochrome P450 (CYP) genetic polymorphisms on methadone outcomes.Methods: MEDLINE, EMBASE, Web of Science, PsycINFO, and CENTRAL were searched to identify studies reporting methadone dose-adjusted plasma concentrations, clearance, maintenance dose, or treatment response in relation to CYP polymorphisms in humans. ROBINS-I was used to evaluate risk of bias in included studies. Each outcome was synthesized for each CYP using the ratio of means or odds ratio as the effect size measure.Results: Ten, two, fourteen, and five studies were included in the meta-analyses of the concentration, clearance, dose, and treatment response, respectively. The CYP2B6 c.516 G>T variant was robustly associated with (S)-methadone concentrations (GT+TTvs.GG: ratio of means (RoM) 1.40, p < 0.01) and clearance (GT+TTvs.GG: RoM 0.65, p < 0.01) but less with (R)- or (R,S)-methadone. The CYP2B6 variant also affected methadone dose for opioid use disorder (GT+TTvs.GG: RoM 0.93, p = 0.04). CYP2C19, CYP2C9, CYP2D6, and CYP3A5 polymorphisms did not influence any of the assessed outcomes.Conclusions: CYP2B6 genetics had statistically significant impacts on (S)-methadone and less so on (R)-methadone exposure and clearance and was statistically significantly but not clinically meaningfully associated with dose requirements.","PeriodicalId":94005,"journal":{"name":"Expert opinion on drug metabolism & toxicology","volume":" ","pages":"1-16"},"PeriodicalIF":0.0,"publicationDate":"2024-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142741795","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A novel in vivo approach to monitoring Cyp3a induction and inhibition by bioluminescent urinalysis. 生物发光尿液分析监测Cyp3a诱导和抑制的一种新的体内方法。

Expert opinion on drug metabolism & toxicology Pub Date : 2024-11-28 DOI: 10.1080/17425255.2024.2434645

James J Cali, Dongping Ma, Katarina Bohm, Dieter H Klaubert

{"title":"A novel in vivo approach to monitoring Cyp3a induction and inhibition by bioluminescent urinalysis.","authors":"James J Cali, Dongping Ma, Katarina Bohm, Dieter H Klaubert","doi":"10.1080/17425255.2024.2434645","DOIUrl":"https://doi.org/10.1080/17425255.2024.2434645","url":null,"abstract":"Background: Adverse drug-drug interactions (DDI) may occur when one drug accelerates or slows a second drug's metabolism by, respectively, inducing or inhibiting a cytochrome P450 (CYP) that metabolizes that second drug. We developed an in vivo method employing urinalysis to complement in vitro CYP induction and inhibition measurements widely used to predict DDIs.Research design and methods: Focusing on Cyp3a enzymes, the major mammalian drug metabolizers, we applied luciferin-IPA, a selective Cyp3a probe substrate to mice after Cyp3a inducers and inhibitor treatments. Cyp3a converts the probe to a metabolite that is eliminated in urine and drives light output when mixed with a luciferase reaction mixture. We hypothesized that urine from an initial renal elimination phase would, respectively, drive elevated or reduced light output as a reflection of Cyp3a induction or inhibition.Results: Luciferase mixed with urine from Cyp3a-induced mice showed enhanced signals, while a Cyp3a inhibitor diminished induced and basal signals versus vehicle.Conclusions: A Cyp3a-selective luminogenic probe substrate enables rapid urinalysis-based testing for detecting Cyp3a induction and inhibition and predicting Cyp3a-dependent DDIs. The study serves as a proof of concept for using caged luciferins for in vivo enzyme activity tests with a readily accessible sample type.","PeriodicalId":94005,"journal":{"name":"Expert opinion on drug metabolism & toxicology","volume":" ","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2024-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142752530","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A three-arm clinical study to compare pharmacokinetic and pharmacodynamic similarity of the denosumab biosimilar LY06006 with reference denosumab in healthy male subjects. 一项三臂临床研究，比较健康男性受试者体内地诺单抗生物仿制药 LY06006 与参考药物地诺单抗的药代动力学和药效学相似性。

Expert opinion on drug metabolism & toxicology Pub Date : 2024-11-24 DOI: 10.1080/17425255.2024.2432673

Rainard Fuhr, Xuejiao Sun, Xi Wang, Ying Dong, Joe Tai, Ming Zhou, Changlin Dou

{"title":"A three-arm clinical study to compare pharmacokinetic and pharmacodynamic similarity of the denosumab biosimilar LY06006 with reference denosumab in healthy male subjects.","authors":"Rainard Fuhr, Xuejiao Sun, Xi Wang, Ying Dong, Joe Tai, Ming Zhou, Changlin Dou","doi":"10.1080/17425255.2024.2432673","DOIUrl":"10.1080/17425255.2024.2432673","url":null,"abstract":"Background: This study aimed to evaluate the pharmacokinetic (PK), pharmacodynamic (PD) similarity, comparable safety, and immunogenicity between LY06006, European Union-sourced denosumab (EU-DEN), and United States-sourced denosumab (US-DEN).Research design and methods: In this double-blind, parallel-group, and single-dose study, 300 healthy male subjects were randomized 1:1:1 to receive a 60 mg dose of either LY06006, EU-DEN, or US-DEN subcutaneously. This study lasted for 253 days. Primary PK endpoints included maximum serum concentration (Cmax), area under the concentration-time curve (AUC) from time zero to last quantifiable concentration (AUC0-t), and AUC from time zero to infinity (AUC0-inf). Pharmacokinetic equivalence was concluded if the two-sided 90% confidence interval (CI) for the geometric least squares mean ratio (GLSMR) of primary endpoints were within 80%-125%. Other PK parameters, PD parameters, safety, and immunogenicity assessments were also conducted during the study.Results: The 90% CIs for ratios of GLSMR were within the predefined equivalence margin for AUC0-inf (89.0%-111.1%), AUC0-t (89.7%-111.3%), and Cmax (92.3%-106.7%). The PD parameters, safety, and immunogenicity of LY06006 were also comparable to US-DEN and EU-DEN.Conclusion: LY06006 was highly similar to US-DEN and EU-DEN in terms of PK, PD, safety and immunogenicity in healthy male subjects.Clinical trial registration: www.clinicaltrials.gov identifier is NCT06095427.","PeriodicalId":94005,"journal":{"name":"Expert opinion on drug metabolism & toxicology","volume":" ","pages":"1-9"},"PeriodicalIF":0.0,"publicationDate":"2024-11-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142712290","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Pharmacokinetic evaluation of bictegravir + emtricitabine + tenofovir alafenamide in HIV treatment. 比特拉韦+恩曲他滨+替诺福韦-阿拉非那胺在艾滋病治疗中的药代动力学评估。

Expert opinion on drug metabolism & toxicology Pub Date : 2024-11-13 DOI: 10.1080/17425255.2024.2428820

Elena Bruzzesi, Camilla Muccini, Antonella Castagna

{"title":"Pharmacokinetic evaluation of bictegravir + emtricitabine + tenofovir alafenamide in HIV treatment.","authors":"Elena Bruzzesi, Camilla Muccini, Antonella Castagna","doi":"10.1080/17425255.2024.2428820","DOIUrl":"https://doi.org/10.1080/17425255.2024.2428820","url":null,"abstract":"Introduction: The combination of bictegravir, emtricitabine, and tenofovir alafenamide (BIC/FTC/TAF) represents a valid option of antiretroviral therapy (ART) as first line regimen both in ART-naïve and -experienced people with HIV (PWH). This review evaluates the pharmacokinetic profiles of these drugs and their clinical implications.Areas covered: This article discusses the pharmacokinetics and pharmacodynamics of BIC/FTC/TAF. It covers their efficacy, safety, tolerability, and potential drug-drug interactions. It also examines the benefits of this combination therapy, including improved adherence due to once-daily dosing and reduced toxicity compared to previous therapies. The review includes data from phase III trials and real-world studies, with a focus on treatment outcomes in diverse populations.Expert opinion: BIC/FTC/TAF's high genetic barrier to resistance and independence from boosting agents represent strengths from the pharmacokinetic perspective. The combination's once-daily, single-tablet regimen ensures consistent therapeutic drug levels and makes this regimen a viable treatment choice even for those with suboptimal adherence. With clinical trial data demonstrating efficacy and safety, as well as ease of use, BIC/FTC/TAF plays a central role in international guidelines. As the HIV treatment landscape continues to evolve, this regimen will remain a cornerstone of oral ART and may serve as a model for future therapies.","PeriodicalId":94005,"journal":{"name":"Expert opinion on drug metabolism & toxicology","volume":" ","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2024-11-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142635044","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0