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19 News |  |
- | idarubicin hydrochloride / Generic mfg.
Preclinical, Journal: In vitro evaluation of the reductive carbonyl idarubicin metabolism to evaluate inhibitors of the formation of cardiotoxic idarubicinol via carbonyl and aldo-keto reductases. (Pubmed Central) - Jan 4, 2024
Over-expression of AKR1C3 verified the importance of AKR1C3 for idarubicinol formation and showed that ranirestat is also a potent inhibitor of this enzyme. Taken together, our study underlines the importance of AKR1C3 and CBR1 for the reduction of idarubicin and identifies potent inhibitors of metabolic formation of the cardiotoxic idarubicinol, which should now be tested in vivo to evaluate whether such combinations can increase the cardiac safety of idarubicin therapies while preserving its efficacy.
- | ranirestat (AS-3201) / Sumitomo Pharma, Eisai, chlorogenic acid / Jiuzhang Biotech
Journal: Cheminformatics identification of modulators of key carbohydrate-metabolizing enzymes from C. cujete for type-2 diabetes mellitus intervention. (Pubmed Central) - Nov 16, 2023
Taken together, our study underlines the importance of AKR1C3 and CBR1 for the reduction of idarubicin and identifies potent inhibitors of metabolic formation of the cardiotoxic idarubicinol, which should now be tested in vivo to evaluate whether such combinations can increase the cardiac safety of idarubicin therapies while preserving its efficacy. The MD simulation results revealed compounds such as benzoic acid (-48.414
- || ranirestat (AS-3201) / Sumitomo Dainippon, Eisai
Retrospective data, Review, Journal: Ranirestat Improves Electrophysiologic but not Clinical Measures of Diabetic Polyneuropathy: A Meta-Analysis. (Pubmed Central) - Jan 10, 2023
Treatment-emergent adverse events [risk ratio (RR) 0.85 (95%CI: 0.63-1.14); P = 0.28; I = 0%] and severe adverse events [RR 1.35 (95%CI: 0.86-2.11); P = 0.20; I = 0%] were comparable across study groups. In people with established DPN with long-standing diabetes, ranirestat is safe and effective in improving electrophysiologic but not clinical DPN.
- || ranirestat (AS-3201) / Sumitomo Dainippon, Eisai
Clinical, PK/PD data, Journal: Pharmacokinetics and Safety of Ranirestat in Patients With Hepatic Impairment. (Pubmed Central) - Aug 1, 2021
All adverse events were mild in severity. Based on these findings, no dose adjustment will be required for ranirestat in patients with mild or moderate hepatic impairment.
- | ranirestat (AS-3201) / Sumitomo Dainippon, Eisai
Journal: Glucose induces metabolic reprogramming in neutrophils during type 2 diabetes to form constitutive extracellular traps and decreased responsiveness to lipopolysaccharides. (Pubmed Central) - Jan 21, 2021
Interestingly, supplementation of NADPH and pharmacological inhibitor of aldose reductase, ranierstat, restored NETs formation in presence of LPS. Our study provides novel insights on the metabolic reprogramming of neutrophils, which may lead to susceptibility of T2D subjects to infections.
- | ranirestat (AS-3201) / Sumitomo Dainippon, Eisai
Preclinical, Journal: Ranirestat Improved Nerve Conduction Velocities, Sensory Perception, and Intraepidermal Nerve Fiber Density in Rats with Overt Diabetic Polyneuropathy. (Pubmed Central) - Jun 11, 2020
Ranirestat improved the peripheral nervous dysfunctions in rats with advanced diabetic polyneuropathy. Ranirestat could have potential for regeneration in the peripheral nervous system of diabetic rats.
- | ranirestat (AS-3201) / Sumitomo Dainippon, Eisai
Preclinical, Journal: A novel method of producing the key intermediate ASI-2 of ranirestat using a porcine liver esterase (PLE) substitute enzyme. (Pubmed Central) - Jul 17, 2019
A novel esterase EstBT that produces Z-MME-AE was purified from Bacillus thuringiensis NBRC13866 and was stably produced in Escherichia coli JM109 cells. Using EstBT rather than porcine liver esterase (PLE), ASI-2 was synthesized with a 17% higher total yield by a novel method, suggesting that the esterase EstBT is a PLE substitute enzyme and therefore, may be of interest for future industrial applications.
- | ranirestat (AS-3201) / Sumitomo Dainippon, Eisai
Clinical, Journal: Aldose reductase inhibitor ranirestat significantly improves nerve conduction velocity in diabetic polyneuropathy: a randomized double-blind placebo-controlled study in Japan. (Pubmed Central) - Jul 11, 2019
Ranirestat (40 mg/day) was well tolerated and improved nerve conduction velocity. Regarding symptoms and signs, no detectable benefits over the placebo were observed in the ranirestat group during the 52 weeks of treatment.
- | ranirestat (AS-3201) / Sumitomo Pharma, Eisai
Trial completion: Safety and Efficacy of AS-3201 in the Treatment of Diabetic Sensorimotor Polyneuropathy (clinicaltrials.gov) - Feb 22, 2014
P3, N=500, Completed, Sponsor: Dainippon Sumitomo Pharma
Regarding symptoms and signs, no detectable benefits over the placebo were observed in the ranirestat group during the 52 weeks of treatment. No longer recruiting --> Completed
- ||||||| ranirestat (AS-3201) / Sumitomo Pharma, Eisai
Trial completion: Evaluating the Efficacy and Safety of Oral Ranirestat (40 and 80 mg) in Mild to Moderate Diabetic Sensorimotor Polyneuropathy (clinicaltrials.gov) - Feb 6, 2013
P2/3, N=800, Completed, Sponsor: Eisai Inc.
No longer recruiting --> Completed Active, not recruiting --> Completed