Rovatitan (rosuvastatin/valsartan) / Merck (MSD), LG Chem - LARVOL DELTA

Effectiveness and Safety of a Fixed-Dose Combination of Valsartan and Rosuvastatin (Rovatitan Tablet) in Patients with Concomitant Hypertension and Hyperlipidemia: An Observational Study. (PubMed, Drug Des Devel Ther) - "The study drug used for the treatment of concomitant hypertension and hyperlipidemia in a real-world setting was effective and was well tolerated. Therefore, the study drug is suggested as a good alternative to increase patient convenience and compliance, particularly in those taking multiple medications."

Journal • Observational data • Cardiovascular • Dyslipidemia • Hypertension

Physiologically-based pharmacokinetic model-based translation of OATP1B-mediated drug-drug interactions from coproporphyrin I to probe drugs. (PubMed, Clin Transl Sci) - "Here, we report physiologically-based pharmacokinetic (PBPK) model analysis for clinical DDI data generated in heathy subjects who received oral doses of cyclosporin A (CysA; 20 and 75 mg) as an OATP1B inhibitor, and the probe drugs (pitavastatin, rosuvastatin and valsartan)...Based on the accepted 498 parameter sets, the range of CL and K was narrowed, with coefficients of variation (CVs) of 9.3% and 11.1%, respectively, indicating that these parameters were practically identifiable. These results suggest that PBPK model analysis of CP-I is a promising translational approach to predict OATP1B-mediated DDIs in drug development."

Journal • PK/PD data

Effect of cyclosporin A and impact of dose staggering on OATP1B1/1B3 endogenous substrates and drug probes for assessing clinical drug interactions. (PubMed, Clin Pharmacol Ther) - "Ten healthy volunteers orally received OATP1B1/1B3 probe cocktail (2 mg pitavastatin, 5 mg rosuvastatin and 20 mg valsartan) and an oral dose of cyclosporin A (CysA, 20 mg and 75 mg) separated by a 1-h interval [20mg(-1h), and 75mg(-1h)]...Correlation between AUCR of pitavastatin, and C R or AUCR of CP-I were consistent between this study and our previous study using rifampicin as an OATP1B1/1B3 inhibitor. Non-linear regression analysis of AUCR of pitavastatin and CP-I against CysA C yielded K (109 ± 35 and 176±42 nM, respectively), similar to the K estimated by our physiologically based pharmacokinetic model analysis described previously (107 nM). The endogenous OATP1B1/1B3 biomarkers, particularly C R and AUCR of CP-I, corroborates OATP1B1/1B3 inhibition and yields valuable information that improve accurate DDI predictions in drug development, and enhance our understanding of interindividual variability in the magnitude of DDI."

Journal

To Evaluate Safety and Effectiveness of RovatitanTab. (clinicaltrials.gov) - P; N=1000; Not yet recruiting; Sponsor: LG Chem

Clinical • New trial • Dyslipidemia • Hypertension • Metabolic Disorders