Effects of breviscapine and C3435T MDR1 gene polymorphism on the pharmacokinetics of fexofenadine, a P-glycoprotein substrate, in healthy volunteers was written by Zhao, Yingying;Miao, Zhimin;Jiang, Mingzhao;Zhou, Xuan;Lai, Yong. And the article was included in Xenobiotica in 2021.COA of Formula: C32H39NO4 The following contents are mentioned in the article:
Breviscapine (BRE) is usually used for long-term use in patients with cardiovascular diseases such as coronary heart disease, angina pectoris, and cerebral thrombosis. It is possible to combine it with P-glycoprotein (P-gp) substrates in clinic. At present, little is known about whether the simultaneous use of BRE affects the disposal of P-gp substrates. The aim of this study was to evaluate the effect of BRE on the pharmacokinetics of fexofenadine (FEX), a P-gp probe substrate and its associations with the MDR1 C3435T genetic polymorphism in healthy volunteers. In this randomised, open-label, placebo-controlled, two-phase crossover clin. study, drug interactions were evaluated in healthy volunteers. FEX was used as a phenotypic probe for P-gp. In each phase, 18 volunteers were given daily doses of 120 mg (40 mg, three times a day) of BRE tablet or a placebo for 14 days. On day 15, a single oral dose of 120 mg FEX hydrochloride was given orally. Blood samples were collected at predefined time intervals, and plasma levels of FEX were determined by ultra-high performance liquid chromatog.-tandem mass spectrometry (UHPLC-MS/MS). The pharmacokinetic parameters were calculated by non-compartmental method, and bioequivalence was evaluated. Results showed that BRE pretreatment did not significantly affect the pharmacokinetics of FEX. The peak maximum plasma concentration (Cmax) and the area under the plasma concentration-time curve from zero to infinity (AUCinf) mean value of FEX with BRE and placebo-treated groups were 699 ng/mL vs. 710 ng/mL and 2972.5 ng·h/mL vs. 3460.5 ng·h/mL, resp. The geometric mean ratios (90% confidence intervals) for FEX Cmax and AUCinf were within the pre-specified range of 0.8-1.25, indicating that FEX in the two pretreatment phases were bioequivalent. Pharmacokinetic parameters of FEX showed no statistically significant difference between MDR1 C3435T CC, CT and TT genotype, revealing that BRE and MDR1 C3435T gene polymorphisms did not affect the pharmacokinetics of FEX in healthy volunteers. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0COA of Formula: C32H39NO4).
2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.COA of Formula: C32H39NO4
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem