北京若生智能科技有限公司
Drug Database
PI

pitavastatin + valsartan (Livalsartan / Livasartan)

✓ Approved

JW Pharmaceutical · AGTR1 · 小分子

什么是 pitavastatin + valsartan？

pitavastatin + valsartan 是一种小分子，由JW Pharmaceutical研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Livalsartan, Livasartan
公司JW Pharmaceutical
药物类别小分子
分子靶点AGTR1, HMGCR
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, JW Pharmaceutical

作用机制

分子靶点

pitavastatin + valsartan 作用于 2 个分子靶点：

AGTR1angiotensin II receptor type 1 (HAT1R, AT1)
HMGCR3-hydroxy-3-methylglutaryl-CoA reductase (LDLCQ3, LGMDR28)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

pitavastatin + valsartan 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Metabolism and nutrition disordersHypercholesterolaemia✓ Approved
Vascular disordersHypertension✓ Approved

相关研究文献

PubMedInternational journal of legal medicine2026-09-10

Differentiating therapeutic use and potential impairment in the forensic interpretation of valsartan concentrations in road traffic offenders.

Dziadosz Marek M, Marquenie Lisa L, Rosenberger Wolfgang W, Klintschar Michael M et al.

Based on the presented case, general challenges in the interpretation of cardiovascular drug concentrations in the context of active participation in road traffic are discussed. Particular emphasis is placed on the assessment of valsartan concentrations, for which no clearly defined threshold between therapeutic and toxic ranges has been established. The case of a 59‑year‑old male who experienced a medical incident while driving enabled the identification of a valsartan concentration of 12.7 µg/mL, which was well above the expected range. Potential interactions with concomitantly administered medications are also considered.

PMID 42717101
阅读全文 →
PubMedDrug metabolism and pharmacokinetics2026-09-07

Physiologically-based pharmacokinetic modeling of coproporphyrin I, an endogenous OATP1B substrate, in cynomolgus monkeys: Bridging the inhibitory effect of rifampicin to humans.

Yoshikado Takashi T, Tomoda Yukana Y, Kasai Kouki K, Toda Reiki R et al.

Coproporphyrin I (CP-I), an endogenous substrate of OATP1B, is gaining attention as a biomarker for predicting drug-drug interactions (DDIs) mediated by hepatic organic anion transporting polypeptide 1B (OATP1B). Its application for bridging preclinical and clinical DDI predictions has been widely studied in cynomolgus monkeys. This study aimed to construct a physiologically based pharmacokinetic (PBPK) model of CP-I in monkeys based on our human CP-I model. First, reported DDIs involving an OATP1B substrate pitavastatin and an OATP1B inhibitor rifampicin at several doses were simultaneously analyzed using PBPK coupled with a cluster Gauss-Newton method (CGNM), estimating the in vivo inhibition constant (Ki,u,OATP1B,PTV) in the cynomolgus monkeys. Considering substrate-dependent difference in Ki,u,OATP1B (CP-I vs. pitavastatin) examined in plated monkey hepatocytes, the in vivo Ki was converted to that for CP-I (Ki,u,OATP1B,CP-I). A middle-out approach enabled simultaneous fitting using plasma CP-I and rifampicin. The synthesis rate and hepatic overall intrinsic clearance of CP-I were found to be identifiable by the CGNM. Both parameters were several-fold higher in monkeys than in humans, suggesting the difference in the DDI sensitivity. In conclusion, this study demonstrates that the integrated PBPK-CGNM approach enables quantitative assessment of OATP1B-mediated DDIs in preclinical species while accounting for interspecies differences.

PMID 42704965
阅读全文 →
PubMedHypertension research : official journal of the Japanese Society of Hypertension2026-09-04

Effect of sacubitril/valsartan on serum uric acid and blood pressure in patients with hypertension and asymptomatic hyperuricemia: A randomized clinical trial.

Wu Meng-Bo MB, Yang Jiao J, Ding Cong-Cong CC, Xiong Hong-Liang HL et al.

Hyperuricemia commonly coexists with hypertension and is associated with increased renal and cardiovascular risk, yet few antihypertensive agents lower serum uric acid. This study compared the urate-lowering effects of sacubitril/valsartan versus valsartan in adults with primary hypertension and asymptomatic hyperuricemia. This single-center, prospective, randomized, open-label clinical trial enrolled adults with mild-to-moderate primary hypertension and fasting serum uric acid ≥ 420 μmol/L from September 2021 to December 2024, with 12 weeks of follow-up. Participants were randomized 1:1 to sacubitril/valsartan 200 mg once daily or valsartan 160 mg once daily. A standardized stepwise add-on protocol with amlodipine was used to achieve blood pressure control. The primary outcome was the change in fasting serum uric acid from baseline to week 12. In the primary intention-to-treat analysis using multiple imputation, treatment-effect estimates were pooled across imputed datasets using Rubin's rules. In the fully adjusted model, sacubitril/valsartan was associated with a greater reduction in serum uric acid at week 12 than valsartan (β = 30.13 μmol/L; 95% CI, 4.33-55.92; P = 0.022). Similar findings were observed in the per-protocol analysis. Blood pressure control at week 12 was comparable between treatment groups, although more participants assigned to valsartan required escalation to amlodipine 10 mg than those assigned to sacubitril/valsartan (17/75 [22.67%] vs. 4/75 [5.33%]; P = 0.008). In adults with primary hypertension and asymptomatic hyperuricemia, sacubitril/valsartan was associated with greater serum uric acid reduction than valsartan over 12 weeks while achieving comparable blood pressure control. These findings suggest that sacubitril/valsartan may have a favorable uric acid profile among hypertensive patients with asymptomatic hyperuricemia. Trial Registration Chinese Clinical Trial Registry: ChiCTR2100050320 ( https://www.chictr.org.cn ). Date of Registration: September 1, 2021.

PMID 42693259
阅读全文 →
PubMedOrganic letters2026-09-04

Enantiodivergent C3-Selective Reduction of Arylvinyl-Substituted 3,5-Dicarbonyl Esters Enabled by Engineered Ketoreductases.

Wu Xiaoqiu X, Zhang Mingyu M, Yao Mingyang M, Liu Ning N et al.

Chiral arylvinyl-substituted 3-hydroxy-5-oxo esters are valuable motifs in pharmaceuticals, yet their enantiocontrolled synthesis remains challenging. Herein, we report a biocatalytic system using ketoreductases (KREDs) for the highly C3-selective reduction of arylvinyl-substituted 3,5-dicarbonyl esters. Through semirational protein engineering, RasADH-E189D afforded the representative (S)-products in 89-99% conversion and 93-99% ee. Complementary (R)-products were obtained using KmCR2 and several other variants with up to 97% conversion and >99% ee, including a key intermediate for the synthesis of pitavastatin. Preparative-scale reactions (greater than 100 mg) further demonstrated the practicality of this platform. Protein-ligand docking among the substrate, cofactor, and KREDs provided mechanistic insights for great stereoselectivity.

PMID 42695844
阅读全文 →
PubMedScientific reports2026-09-03

Correction: Sacubitril/valsartan attenuates renal injury caused by cecal ligation and puncture via TLR4/NFκB/NLRP3 inhibition and reduced oxidative stress and apoptosis in rats.

Mohyeldin Reham H RH, Abdelnaser Mahmoud M, Rofaeil Remon Roshdy RR, Attya Mina Ezzat ME et al.

PMID 42686953
阅读全文 →
PubMedInternational journal of clinical pharmacology and therapeutics2026-09-03

Pharmacotherapy of heart failure: Impact of the 2021 guideline update on guideline-directed medical therapy assessed using a Japanese employee health insurance claims database.

Uno Takaya T, Hosomi Kouichi K, Yokoyama Satoshi S

To investigate the impact of the 2021 guideline update on guideline-directed medical therapy (GDMT) utilization in patients with heart failure (HF). The 2021 update of the Japanese guidelines for HF management followed the introduction of sacubitril/valsartan and dapagliflozin into clinical practice. However, the impact of this guideline update on drug utilization patterns remains unclear. Patient data were obtained from the Japanese employee health insurance claims database (JMDC). The simple GDMT score was determined based on the combination and dose of four key pharmacological classes: β-blockers, renin-angiotensin system inhibitors, mineralocorticoid receptor antagonists, and sodium-glucose cotransporter 2 inhibitors. Because a simple GDMT score of ≥ 5 has been associated with improved prognosis in patients with HF, patients with scores ≥ 5 were classified into the high-score group for analysis. Following the guideline update, the proportion of patients in the high-score group increased from 6.97% (n = 4,013) to 9.33% (n = 6,363), standardized difference 0.09. The mean simple GDMT score also showed a small but statistically significant increase (5.72 ± 0.79 vs. 6.00 ± 1.09) with standardized difference 0.28. This upward trend was particularly marked for the prescription rates of sacubitril/valsartan and dapagliflozin (sacubitril/valsartan: 1.40% before the update vs. 22.57% after the update; standardized difference, 0.69; dapagliflozin: 12.41% before the update vs. 26.64% after the update; standardized difference, 0.36). The 2021 guideline update was associated with increased use of sacubitril/valsartan and dapagliflozin, resulting in greater overall GDMT intensity. However, these findings are limited to data from 2021, and further long-term studies are needed to evaluate trends in GDMT utilization.

PMID 42687846
阅读全文 →

注册免费账户还可查看另外 7397 篇文献

免费注册查看全部文献 →

了解更多pitavastatin + valsartan