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Cicletanine + magnesium
- Development stage
- Phase 2
- Lead developer
- Gilead Sciences
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Cicletanine + magnesium is a combination of two agents with distinct pharmacological actions. Cicletanine is a furopyridine derivative and thiazide-like diuretic approved in France for the treatment of hypertension. It acts by inhibiting protein kinase C (PKC), reversing vasoconstriction through inhibition of PKC-mediated Na/K-ATPase phosphorylation, and may also stimulate vascular nitric oxide synthesis while inhibiting superoxide production. Magnesium (as magnesium citrate) is an osmotic laxative and mineral supplement that increases fluid in the colon via high osmolality and may stimulate peristalsis through cholecystokinin release. The combination could theoretically be used to address both hypertension (via cicletanine) and hypomagnesemia or constipation (via magnesium), but there are no widely recognized fixed-dose pharmaceutical products combining these two agents[1][2][4][5][6].
- Other names
- cycletanidecicletaninacicletanine hydrochloridemagnesium citrate
02
Targets
PKC (Protein kinase C family)
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