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Drug intelligence / Profile preview
glyceryl trinitrate
- Development stage
- Unknown
- Lead developer
- Key Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Transdermal
01
Overview
The GTN patch (glyceryl trinitrate patch) is a transdermal formulation of glyceryl trinitrate (nitroglycerin), a well-established organic nitrate vasodilator. It is primarily indicated for the prevention of angina pectoris caused by coronary artery disease. Upon application, glyceryl trinitrate is absorbed through the skin and undergoes enzymatic bioactivation, primarily by mitochondrial aldehyde dehydrogenase (ALDH2), to release nitric oxide (NO) or a related active vasodilator species. Nitric oxide then activates soluble guanylyl cyclase (sGC), leading to increased levels of cyclic guanosine monophosphate (cGMP) and subsequent relaxation of vascular smooth muscle cells. This results in vasodilation, predominantly venodilation, which reduces cardiac preload and myocardial oxygen demand. In addition to its approved cardiovascular uses, the GTN patch has been investigated for off-label indications, including the promotion of arteriovenous fistula maturation in patients with end-stage renal failure, and the treatment of various tendinopathies.
- Brand names
- DeponitMinitranNitro-DiscNitro-DurNitrodermTransiderm-Nitro
- Other names
- glyceryl trinitrate patchGTN patchnitroglycerin patchnitroglycerin transdermaltransdermal nitroglycerin
02
Targets
ALDH2 (Mitochondrial Aldehyde Dehydrogenase)
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