北京若生智能科技有限公司
Drug Database
DI

diltiazem (Cardizem SR / Corolater)

✓ Approved

Bausch Health Companies Inc. · CACNA1C · 小分子

什么是 diltiazem？

diltiazem 是一种小分子，由Bausch Health Companies Inc.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Cardizem SR, Corolater
公司Bausch Health Companies Inc.
药物类别小分子
分子靶点CACNA1C
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Bausch Health Companies Inc.

作用机制

分子靶点

diltiazem 作用于 1 个分子靶点：

CACNA1Ccalcium voltage-gated channel subunit alpha1 C (CACNL1A1, CACNA1C-IT2)
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

diltiazem 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
Vascular disordersHypertension✓ Approved
Cardiac disordersAngina pectoris✓ Approved

相关研究文献

PubMedHepatology (Baltimore, Md.)2026-10-26

Phase 1b study of miricorilant in patients with presumed metabolic dysfunction-associated steatohepatitis (MASH).

Alkhouri Naim N, Rudraraju Madhavi M, Leibowitz Mark M, Jenders Robert A RA et al.

Miricorilant, an oral nonsteroidal selective glucocorticoid receptor modulator, is being investigated as a therapy that modulates hepatic cortisol activity in patients with metabolic dysfunction-associated steatohepatitis (MASH). This phase 1b study evaluated miricorilant's efficacy and safety. Seventy patients with presumed MASH received oral miricorilant daily (30-150 mg) or intermittent (100-200 mg once, twice, or thrice weekly) dosing regimens for 12 or 24 weeks. Across dosing regimens, reductions in relative liver fat content (LFC) ranged from 10.1% to 76.6%. Improvements in MASH liver function markers and the enhanced liver fibrosis (ELF) score were observed across regimens. Treatment-emergent adverse events (TEAE) leading to drug interruption/discontinuation occurred in 12.9% of patients (n=9) each; most were due to aminotransferase elevations during an excessively rapid drop in LFC (up to 70.2% at week 6) and in patients receiving daily dosing. Intermittent dosing enabled more patients to complete 12 weeks of treatment without discontinuation due to TEAEs. Intermittent dosing with miricorilant 100 mg twice weekly had the best benefit-risk profile; this cohort demonstrated a mean LFC reduction of 28.2% at week 12, with a corresponding decline in liver enzymes (ALT, -3.8 U/L; AST, -6.0 U/L). Patients in this cohort also had numerical improvement in lipid profiles, glycemic markers, and fibrosis biomarkers. Intermittent miricorilant dosing of 100 mg twice weekly achieved meaningful reductions in LFC and improved liver health markers with a favorable safety profile. This regimen is being evaluated in the phase 2b MONARCH study (NCT06108219).

PMID 42929711
阅读全文 →
PubMedJournal of clinical pharmacology2026-10-26

Pharmacokinetics and Safety of Deuremidevir Hydrobromide (JT001) in Subjects with Mild and Moderate Renal Impairment: An Open-Label, Parallel-Group Phase I Study.

Lu Tong T, Tan Xi X, Kuang Shijuan S, Meng Qin Q et al.

JT001 (deuremidevir hydrobromide, VV116) is an oral antiviral prodrug that is rapidly converted in vivo to its active metabolite, 116-N1. Since 116-N1 is mainly cleared by the kidneys, renal impairment may increase its systemic exposure. This study evaluated the pharmacokinetics of 116-N1 following a single 0.3-g oral dose of JT001 in participants with mild or moderate renal impairment and matched healthy controls. Absorption was generally similar across groups, with comparable time to peak concentration. However, declining renal function increased exposure to 116-N1 and slowed its elimination. Terminal half-life increased from 5.31 to 8.13 and 11.2 h in mild and moderate impairment. Apparent oral clearance decreased from 34.3 L/h in healthy participants to 21.4 and 13.8 L/h in patients with mild and moderate renal impairment, respectively. Twenty-four participants (eight per renal function group) were enrolled. Geometric mean AUC0-t increased by 63% in participants with mild renal impairment (geometric mean ratio [GMR] 163.31%, 90% CI 135.99%-196.12%) and by 157% in those with moderate renal impairment (GMR 257.42%, 90% CI 214.35%-309.13%), whereas Cmax remained comparable between groups. JT001 was generally well tolerated, with no serious or grade ≥3 treatment-related adverse events. To further assess clinical relevance of these findings, the renal impairment data were incorporated into an updated population pharmacokinetic model. Simulations suggested that the approved regimen was suitable for patients with mild renal impairment, whereas a reduced regimen of 300 mg twice daily on Day 1 followed by 200 mg twice daily on Days 2-5 was recommended for patients with moderate renal impairment.

PMID 42928460
阅读全文 →
PubMedThe New England journal of medicine2026-10-26

Divarasib as Compared with Sotorasib or Adagrasib in KRAS G12C-Mutated NSCLC.

Skoulidis Ferdinandos F, Ahn Myung-Ju MJ, Gadgeel Shirish S, Popat Sanjay S et al.

Divarasib, a next-generation, oral KRAS G12C inhibitor, is more potent and selective in vitro than the first-generation KRAS G12C inhibitors sotorasib and adagrasib. In this phase 3, international, open-label trial, patients with previously treated KRAS G12C-mutated advanced or metastatic non-small-cell lung cancer (NSCLC) were randomly assigned to receive divarasib orally at a dose of 400 mg once daily or control treatment (sotorasib orally at a dose of 960 mg once daily or adagrasib orally at a dose of 600 mg twice daily) until the occurrence of disease progression, unacceptable adverse events, loss of clinical benefit, withdrawal of consent, death, or trial termination. The primary end point was progression-free survival as assessed by blinded independent central review. Secondary end points included overall survival, confirmed overall response, duration of response, patient-reported outcomes, and safety. A total of 338 patients received divarasib (167 patients) or control treatment (171 patients; 156 received sotorasib and 15 received adagrasib). The median follow-up was 14.3 months. The median progression-free survival was 9.8 months with divarasib and 5.7 months with control treatment (hazard ratio for disease progression or death, 0.58; 95% confidence interval [CI], 0.44 to 0.76; P<0.001). The median overall survival was 17.7 months with divarasib and 12.0 months with control treatment (hazard ratio for death, 0.56; 95% CI, 0.41 to 0.78; P<0.001). Of the 328 patients who could be evaluated for response, a confirmed response occurred in 58.4% in the divarasib group and in 32.3% in the control group. The median duration of response was 11.9 months with divarasib and 6.9 months with control treatment. Fewer grade 3 or 4 treatment-related adverse events were noted with divarasib (24.6%) than with control treatment (34.5%). Among patients with previously treated KRAS G12C-mutated advanced or metastatic NSCLC, divarasib led to significantly longer progression-free and overall survival than control treatment. (Supported by F. Hoffmann-La Roche; Krascendo 1 ClinicalTrials.gov number, NCT06497556.).

PMID 42929675
阅读全文 →
PubMedThe New England journal of medicine2026-10-26

Osimertinib-Savolitinib in Advanced NSCLC after Progression during EGFR-TKI Therapy.

Lu Shun S, Girard Nicolas N, Yang James Chih-Hsin JC, Shepherd Frances A FA et al.

Savolitinib is an oral, potent, highly selective MET-tyrosine kinase inhibitor (TKI). Combination therapy with savolitinib and osimertinib, an epidermal growth factor receptor (EGFR)-TKI, has shown activity in patients with EGFR-mutated, advanced non-small-cell lung cancer (NSCLC) with MET overexpression, MET amplification, or both, after progression during EGFR-TKI therapy. In this international, phase 3, open-label trial, we randomly assigned, in a 1:1 ratio, patients with EGFR-mutated, locally advanced or metastatic NSCLC with MET overexpression (staining intensity of 3+ for MET in ≥90% of tumor cells on immunohistochemical analysis), MET amplification (≥10 gene copies on fluorescence in situ hybridization), or both whose disease had progressed during osimertinib therapy to receive osimertinib (at a dose of 80 mg once daily) plus savolitinib (300 mg twice daily) or intravenous platinum-pemetrexed. The primary end point was progression-free survival, as assessed by blinded independent central review. Secondary end points included overall survival and safety. Of the 1746 patients screened, 338 were randomly assigned to receive osimertinib-savolitinib (171 patients) or platinum-pemetrexed (167 patients). Osimertinib-savolitinib led to significantly longer progression-free survival than platinum-pemetrexed (hazard ratio for disease progression or death, 0.55; 95% confidence interval [CI], 0.42 to 0.72; P<0.001), as well as significantly longer overall survival (hazard ratio for death, 0.68; 95% CI, 0.50 to 0.91; P = 0.01; final analysis). The Kaplan-Meier estimate of 12-month progression-free survival was 36% in the osimertinib-savolitinib group and 10% in the platinum-pemetrexed group, and the estimate of 12-month overall survival was 70% and 53%, respectively. The most frequently reported adverse events that occurred during treatment in the osimertinib-savolitinib group were peripheral edema (in 49% of the patients), anemia (in 26%), and diarrhea (in 26%). Grade 3 or higher adverse events during treatment were reported in 64% of the patients in the osimertinib-savolitinib group and in 63% of those in the platinum-pemetrexed group. Osimertinib-savolitinib led to significantly longer progression-free and overall survival than platinum-pemetrexed among patients with EGFR-mutated, locally advanced or metastatic NSCLC with MET overexpression, MET amplification, or both that had progressed during osimertinib therapy (Funded by AstraZeneca; SAFFRON ClinicalTrials.gov number, NCT05261399.).

PMID 42929693
阅读全文 →
PubMedDentistry journal2026-10-26

Changes in Oral Health Knowledge, Beliefs, and Self-Reported Practices Among Preschool Teachers Between 3 and 12 Months After School-Based Education.

Koc Gunes G, Baygin Ozgul O

Background/Objectives: Preschool teachers can reinforce oral health practices, but the persistence of educational messages requires evaluation. This study assessed changes in oral health knowledge, beliefs, and self-reported practices between 3 and 12 months after school-based education. Methods: Education reached 240 teachers in 63 schools in Trabzon, Turkey. Questionnaires were completed by 222 teachers at 3 months and 152 at 12 months. Paired analyses included the 152 teachers assessed at both follow-ups. Responses were compared using McNemar tests. No matched pre-education assessment or concurrent control group was available. Results: The paired cohort represented 63.3% of trained teachers. Endorsement of fluoride-containing products for caries prevention decreased from 63.8% to 40.1%, recognition of enamel strengthening from 82.9% to 66.4%, and identification of first-tooth eruption as the time to begin cleaning from 92.8% to 75.7% (all p < 0.001). Recognition that avulsed primary teeth should not be replanted decreased from 83.6% to 70.4% (p < 0.001), whereas endorsement of immediate permanent-tooth replantation changed little (91.4% versus 89.5%; p = 0.508). Twice-daily brushing decreased from 82.9% to 73.0% (p = 0.001). Tests were exploratory and unadjusted for multiple comparisons. Conclusions: Between 3 and 12 months, several preventive messages were less frequently endorsed, and some self-reported practices changed. These findings identify topics for updated content and refresher education concerning fluoride, early oral care, primary-tooth avulsion, and routine preventive dental visits. The observations do not establish initial educational effectiveness or clinical benefit in children.

PMID 42930428
阅读全文 →
PubMedArchives of animal nutrition2026-10-26

Amino acid digestibility of whole yeast and autolysed yeast derived from sugarcane ethanol production and effects on excreta bacterial populations in caecectomised laying hens.

Kaewtapee Chanwit C, Thongthung Hathaipat H, Petchpoung Krittaya K, Chungopast Sirinapa S

Yeast biomass represents a renewable source of single-cell protein that can be used as an alternative feed ingredient in laying hen diets. The objective of this study was to determine the amino acid (AA) digestibility and excreta bacterial populations of whole yeast and autolysed yeast in caecectomised laying hens. Six caecectomised laying hens were housed individually in metabolism cages and fed either a basal diet or one of two diets, containing either whole yeast or autolysed yeast. The diets and hens were applied in a duplicate 3 × 3 Latin square design. In each period, the laying hens were fed their respective diet for 8 d and excreta samples were collected quantitatively twice daily during days 5-8. On day 9, a sterile plastic bag was attached to the cloaca of each hen to collect excreta for microbiota analysis. The crude protein (CP) contents were 342 and 334 g/kg dry matter (DM) in the whole yeast and autolysed yeast, respectively. The contents of neutral detergent fibre and acid detergent fibre were higher in the whole yeast (158 and 21 g/kg DM, respectively) than in the autolysed yeast (65 and 1 g/kg DM, respectively). Both in vitro protein digestibility and AA digestibility in the caecectomised laying hens were higher (p < 0.05) in the autolysed yeast than in the whole yeast. However, there were no differences (p > 0.05) in the gene copy numbers of bacteria among the experimental diets. This suggests that yeast products derived from sugarcane ethanol production could be considered alternative protein sources. Accurate information on the AA digestibility of yeast products is important for estimating their contribution to digestible AA supply and for their appropriate inclusion in laying hen diets.

PMID 42928071
阅读全文 →

注册免费账户还可查看另外 9996 篇文献

免费注册查看全部文献 →

了解更多diltiazem