CYP1A2 (Cytochrome P450, family 1, subfamily A, polypeptide 2)

Limitations include elements of study design, study populations, and confounders. There is evidence to suggest possible increased cancer risks for frequent, long-term hair dye use in specific populations.

<b></b> Phenazines isolated from <i>Streptomyces murinus </i>ZMA01 exhibit promising antimicrobial and anticancer activities with favorable ADMET profiles. These findings underscore their therapeutic potential and warrant further <i>in vivo</i> studies and targeted delivery optimization for treating microbial infections and cancers.

This study established and validated a pro-gnostic model for breast cancer based on lipid metabolism-related genes. It revealed that low ALDH2 expression is closely associated with poor prognosis and immunosuppression, suggesting its potential as a prognostic biomarker and therapeutic target in breast cancer.

The findings indicate that major P450 differ in the magnitude of their hydroxyeicosatetraenoic acid and epoxyeicosatrienoic acid formation rates, which is a significant for studying diseases that is known to be influenced by alterations in these pathways. Altered enantioselectivity could have implications in diseases such as hypertension, cancer, inflammation, and cardiovascular disorders.

Resveratrol showed a mixed type of inhibition of recombinant human protein and a competitive inhibition of rat liver microsomal CYP1A. We can conclude that resveratrol is an in vitro inhibitor of CYP1A2, but it increases the benzo&lsqb;a]pyrene CYP induction effect in vivo.

Additionally, 16S rRNA sequencing revealed that TCDCA mitigated AFB1-induced gut microbiota dysbiosis by increasing the abundance of Akkermansia and decreasing harmful genera such as Megamonas. Collectively, TCDCA mitigates AFB1-induced growth suppression and hepatotoxicity through mechanisms involving metabolic regulation, antioxidation, inhibition of pyroptosis and inflammation, reinforcement of intestinal barrier function, and modulation of gut microbiota.

A clinical drug-drug interaction (DDI) study was designed to evaluate the effect of single and multiple oral doses of encorafenib on the single oral dose pharmacokinetics (PK) of the cytochrome P450 (CYP) enzyme probe substrates, losartan (CYP2C9), midazolam (CYP3A4), caffeine (CYP1A2), omeprazole (CYP2C19), and dextromethorphan (CYP2D6) administered as a cocktail (Inje). Based on these results regarding co-administration with encorafenib, sensitive substrates of CYP3A should be avoided or dose adjusted based on the recommendations of their approved product labeling. This information has been included in the updated prescribing information for encorafenib.

In silico analysis revealed that Cas III-ia possesses potential oral bioavailability, high gastrointestinal absorption, the capacity to penetrate the blood-brain barrier, and is a potential target of glycoproteins, but not a substrate of CYP1A2, CYP2C19, CYP2C9, CYP2D6, and CYP3A4. Our findings strongly suggest that Cas III-ia holds excellent promise as a potential compound for treating human malignant glioma.

Additional studies evaluated the impact of strong CYP3A4 perpetrators and imatinib on a single 40 mg dose of asciminib. This PBPK model was applied in lieu of clinical pharmacology studies to support the new drug application of Scemblix® and to bridge data from 40 mg BID to the 80 mg QD and 200 mg BID dose regimens. The PBPK predictions informed the drug product label and are estimated to have replaced at least 10 clinical studies.

Skimmianin, glycyrrhetic acid Me ester, and apigenin were found to inhibit some members of the cytochrome family, like CYP1A2, CYP2D6, CYP3A4, CYP2C19, and CYP2C9, indicating their anti-drug-resistant properties. These findings suggest that DEAE may serve as a promising natural therapeutic as an antioxidant and also as an anticancer and anti-metastasis candidate against lung cancer.

These findings indicate that interactions based on metabolism might occur when tea polyphenols are combined with medications. This study provides evidence that tea polyphenols significantly affect CYP450 enzyme expression, offering insights into the potential interactions between tea consumption and drug metabolism.

Recent reports have indicated that the minor allele of the nuclear transcription factor I/B (NFIB), rs28379954 T>C, affects the metabolism of risperidone and clozapine, which are mediated by CYP2D6 and CYP1A2, respectively. First, we reanalyzed the association between rs28379954 T>C and CYP2D6 activity in three independent cohorts exposed to CYP2D6 substrates (propafenone, tamoxifen, and sparteine) which revealed no association...We identified significant downregulation of several metabolic pathways related to hepatic functionality, PPAR signaling, and drug metabolism for NFIB, NFIC, and NFIX, whereas pathways associated with cancer biology were significantly induced. In summary our findings provide further insight into hepatic CYP regulation via the NFI network with implications for the understanding of interindividual variability of drug metabolism.