Uncoupling of Cytochrome P450 2B6 and stimulation of reactive oxygen species production in pharmacogenomic alleles affected by interethnic variability
Biochim Biophys Acta Gen Subj. 2024 Mar 9:130595. doi: 10.1016/j.bbagen.2024.130595. Online ahead of print.ABSTRACTCytochrome P450 mediated substrate metabolism is generally characterized by the formation of reactive intermediates. In vitro and in vivo reaction uncoupling, results in the accumulation and dissociation of reactive intermediates, leading to increased ROS formation. The susceptibility towards uncoupling and altered metabolic activity is partly modulated by pharmacogenomic alleles resulting in amino acid substitutions. A large variability in the prevalence of these alleles has been demonstrated in CYP2B6, with ...
Source: Biochimica et Biophysica Acta - March 11, 2024 Category: Biochemistry Authors: Sabrina Yamoune Julian Peter M üller Immaculate Mbongo Langmia Catharina Scholl Julia Carolin Stingl Source Type: research

Uncoupling of Cytochrome P450 2B6 and stimulation of reactive oxygen species production in pharmacogenomic alleles affected by interethnic variability
Biochim Biophys Acta Gen Subj. 2024 Mar 9:130595. doi: 10.1016/j.bbagen.2024.130595. Online ahead of print.ABSTRACTCytochrome P450 mediated substrate metabolism is generally characterized by the formation of reactive intermediates. In vitro and in vivo reaction uncoupling, results in the accumulation and dissociation of reactive intermediates, leading to increased ROS formation. The susceptibility towards uncoupling and altered metabolic activity is partly modulated by pharmacogenomic alleles resulting in amino acid substitutions. A large variability in the prevalence of these alleles has been demonstrated in CYP2B6, with ...
Source: Biochimica et Biophysica Acta - March 11, 2024 Category: Biochemistry Authors: Sabrina Yamoune Julian Peter M üller Immaculate Mbongo Langmia Catharina Scholl Julia Carolin Stingl Source Type: research

Clinical Evaluation of the Effect of Encorafenib on Bupropion, Rosuvastatin, and Coproporphyrin I and Considerations for Statin Coadministration
CONCLUSION: The results from these clinical studies suggest that encorafenib does not cause clinically relevant CYP2B6 induction or inhibition but is an inhibitor of BCRP and may also inhibit OATP1B1/3 to a lesser extent. Based on these results, it may be necessary to consider switching statins or reducing statin dosage accordingly for coadministration with encorafenib.CLINICAL TRIAL REGISTRATION: ClinicalTrials.gov NCT03864042, registered 6 March 2019.PMID:38424308 | DOI:10.1007/s40262-024-01352-9 (Source: Clinical Breast Cancer)
Source: Clinical Breast Cancer - February 29, 2024 Category: Cancer & Oncology Authors: Joseph Piscitelli Micaela B Reddy Lance Wollenberg Laurence Del Frari Jason Gong Linda Wood Yizhong Zhang Kyle Matschke Jason H Williams Source Type: research

Clinical Evaluation of the Effect of Encorafenib on Bupropion, Rosuvastatin, and Coproporphyrin I and Considerations for Statin Coadministration
CONCLUSION: The results from these clinical studies suggest that encorafenib does not cause clinically relevant CYP2B6 induction or inhibition but is an inhibitor of BCRP and may also inhibit OATP1B1/3 to a lesser extent. Based on these results, it may be necessary to consider switching statins or reducing statin dosage accordingly for coadministration with encorafenib.CLINICAL TRIAL REGISTRATION: ClinicalTrials.gov NCT03864042, registered 6 March 2019.PMID:38424308 | DOI:10.1007/s40262-024-01352-9 (Source: Clinical Genitourinary Cancer)
Source: Clinical Genitourinary Cancer - February 29, 2024 Category: Cancer & Oncology Authors: Joseph Piscitelli Micaela B Reddy Lance Wollenberg Laurence Del Frari Jason Gong Linda Wood Yizhong Zhang Kyle Matschke Jason H Williams Source Type: research

Clinical Evaluation of the Effect of Encorafenib on Bupropion, Rosuvastatin, and Coproporphyrin I and Considerations for Statin Coadministration
CONCLUSION: The results from these clinical studies suggest that encorafenib does not cause clinically relevant CYP2B6 induction or inhibition but is an inhibitor of BCRP and may also inhibit OATP1B1/3 to a lesser extent. Based on these results, it may be necessary to consider switching statins or reducing statin dosage accordingly for coadministration with encorafenib.CLINICAL TRIAL REGISTRATION: ClinicalTrials.gov NCT03864042, registered 6 March 2019.PMID:38424308 | DOI:10.1007/s40262-024-01352-9 (Source: Clinical Colorectal Cancer)
Source: Clinical Colorectal Cancer - February 29, 2024 Category: Cancer & Oncology Authors: Joseph Piscitelli Micaela B Reddy Lance Wollenberg Laurence Del Frari Jason Gong Linda Wood Yizhong Zhang Kyle Matschke Jason H Williams Source Type: research

Clinical Evaluation of the Effect of Encorafenib on Bupropion, Rosuvastatin, and Coproporphyrin I and Considerations for Statin Coadministration
ConclusionThe results from these clinical studies suggest that encorafenib does not cause clinically relevant CYP2B6 induction or inhibition but is an inhibitor of BCRP and may also inhibit OATP1B1/3 to a lesser extent. Based on these results, it may be necessary to consider switching statins or reducing statin dosage accordingly for coadministration with encorafenib.Clinical Trial RegistrationClinicalTrials.gov NCT03864042, registered 6 March 2019. (Source: Clinical Pharmacokinetics)
Source: Clinical Pharmacokinetics - February 29, 2024 Category: Drugs & Pharmacology Source Type: research

Efficacy and Safety Of AXS-05 in Agitation Associated with Alzheimer's Disease: Results From ACCORD, a Phase 3, Double-Blind, Placebo-Controlled, Relapse Prevention Trial
Agitation is reported in up to 70% of individuals with Alzheimer's disease (AD) and is characterized by emotional distress, aggressive behaviors, disruptive irritability and disinhibition. Agitation is associated with increased caregiver burden, decreased functioning, accelerated cognitive decline, earlier nursing home placement, and increased mortality. AXS-05 (dextromethorphan-bupropion) is a novel, oral NMDA receptor antagonist and sigma-1 receptor agonist approved for the treatment of major depressive disorder and under evaluation for Alzheimer's disease-related agitation (ADA). (Source: The American Journal of Geriatric Psychiatry)
Source: The American Journal of Geriatric Psychiatry - February 18, 2024 Category: Geriatrics Authors: George Grossberg, Jeffrey Cummings, Candace Andersson, Caroline Streicher, Herriot Tabuteau Tags: Poster # NR11 Source Type: research

Pharmacological management of gambling disorder: an update of the literature
Expert Rev Neurother. 2024 Feb 15. doi: 10.1080/14737175.2024.2316833. Online ahead of print.ABSTRACTINTRODUCTION: Gambling disorder (GD) is a mental health condition characterized by persistent and problematic betting behavior. GD generates distress and impairment, and treatment options include psychological and pharmacological interventions.AREAS COVERED: This narrative review explores existing pharmacological treatments for GD. The following classes of medications were considered: opioid-receptor antagonists (e.g. naltrexone and nalmefene), serotonin reuptake inhibitors (e.g. fluvoxamine, paroxetine, sertraline, escital...
Source: Expert Review of Neurotherapeutics - February 15, 2024 Category: Neurology Authors: Gemma Mestre-Bach Marc N Potenza Source Type: research