Drug intelligence / Profile preview

cyclosporine + omeprazole

Development stage
Unknown
Lead developer
Sandoz
Modality
Small Molecules
Administration
Oral, Intravenous, Ophthalmic
01

Overview

Cyclosporine + omeprazole is a combination of two pharmaceutical agents used for different primary indications. Cyclosporine is an immunosuppressant that acts as a calcineurin inhibitor to suppress T-cell activation and cytokine production by binding to cyclophilin and inhibiting the phosphatase activity of calcineurin. This mechanism prevents the transcription of interleukin-2 and other cytokines critical for T-cell proliferation[4][6]. It is primarily indicated for preventing organ transplant rejection and treating certain autoimmune conditions. Omeprazole is a proton pump inhibitor (PPI) that irreversibly inhibits the H+/K+ ATPase enzyme in gastric parietal cells. This action blocks the final step in gastric acid secretion, leading to reduced stomach acidity[5][8]. Omeprazole is used mainly for gastroesophageal reflux disease (GERD), peptic ulcer disease, Helicobacter pylori eradication regimens, erosive esophagitis due to acid-mediated GERD, and other hypersecretory conditions. When coadministered, there may be pharmacokinetic interactions; omeprazole can alter blood concentrations of cyclosporine in some patients—both increased and decreased levels have been reported. The mechanism behind this interaction remains unclear but may involve effects on hepatic metabolism or absorption[1][2][3]. Clinical studies suggest that standard doses of omeprazole do not significantly affect cyclosporine levels in stable renal transplant patients; however, monitoring may be warranted due to case reports indicating variable effects[1][3].

Brand names
CequaProtonix
Other names
cyclosporineomeprazole
02

Targets

CN (Calcineurin)ATP4A (Potassium–transporting ATPase alpha chain 1)

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