2014
DOI: 10.2337/dc14-1038
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Efficacy and Safety of Oral Methazolamide in Patients With Type 2 Diabetes: A 24-Week, Placebo-Controlled, Double-Blind Study

Abstract: OBJECTIVETo evaluate the safety and efficacy of methazolamide as a potential therapy for type 2 diabetes. RESEARCH DESIGN AND METHODSThis double-blind, placebo-controlled study randomized 76 patients to oral methazolamide (40 mg b.i.d.) or placebo for 24 weeks. The primary efficacy end point for methazolamide treatment was a placebo-corrected reduction in HbA 1c from baseline after 24 weeks (DHbA 1c ). RESULTSMean 6 SD baseline HbA 1c was 7.1 6 0.7% (54 6 5 mmol/mol; n 5 37) and 7.4 6 0.6% (57 6 5 mmol/mol; n … Show more

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Cited by 14 publications
(12 citation statements)
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“…MTZ could have an effect on organs such as the liver to regulate blood parameters. MTZ is a hepatic insulin sensitizer that lowers blood glucose to treat type 2 diabetes (Konstantopoulos et al, 2012; Simpson et al, 2014). Therefore, the effects of MTZ on blood parameters and plaque histopathology may be independent of the effects of MTZ on plaque calcification.…”
Section: Discussionmentioning
confidence: 99%
“…MTZ could have an effect on organs such as the liver to regulate blood parameters. MTZ is a hepatic insulin sensitizer that lowers blood glucose to treat type 2 diabetes (Konstantopoulos et al, 2012; Simpson et al, 2014). Therefore, the effects of MTZ on blood parameters and plaque histopathology may be independent of the effects of MTZ on plaque calcification.…”
Section: Discussionmentioning
confidence: 99%
“…Out of the identified compounds, one, the carbonic anhydrase inhibitor methazolamide (MTZ), was then further investigated. MTZ exhibited glucoselowering effects and enhanced glucose tolerance in animal models of T2D (Konstantopoulos et al 2012) and successfully improved glycaemic control in T2D patients in a Phase 2 clinical trial (Simpson et al 2014) indicating that this agent is a promising new agent to improve insulin sensitivity in T2D. Although this drug discovery endeavour was successful, the complex and multi-tissue nature of T2D means that targeting insulin resistance alone will not combat all the problems that occur in this disease.…”
Section: Ges In T2d Drug Discoverymentioning
confidence: 99%
“…In fact, by screening available libraries of off-patent, FDA-approved drugs, the timeline from drug discovery to clinical use can be significantly truncated. This approach has been used previously to fast-track an insulin-sensitising drug from GES generation to a successful Phase 2 clinical trial in just three years (Konstantopoulos et al 2011, Simpson et al 2014 (discussed in detail in the following section).…”
Section: Ges For Drug Discoverymentioning
confidence: 99%
“…Furthermore, MTZ was shown to exhibit a hypoglycemic effect in streptozotocin (STZ)-induced DM rats and diabetic db/db mice; it also improves glucose tolerance in diet-induced insulin-resistant obese mice 16 . MTZ was shown to reduce HbA1c levels in diabetic db/db mice (16 ± 5% [151 ± 31 mmol/mol]) 16 and patients with T2DM (-0.39% [95% CI -0.82, 0.04]; -4.3 mmol/mol [-9.0, 0.4]) 17 . To the best of our knowledge, no studies have investigated the role of MTZ in the treatment of DCM.…”
Section: Introductionmentioning
confidence: 99%