Drug intelligence / Profile preview

safinamide + rosuvastatin

Development stage
Unknown
Lead developer
Zambon
Modality
Small Molecules
Administration
Oral
01

Overview

This combination refers to the concomitant use of **safinamide** and **rosuvastatin** as independent drugs, not as a branded fixed-dose combination formulation. Safinamide is a selective, reversible **monoamine oxidase B (MAO-B) inhibitor** primarily used as adjunctive therapy for Parkinson's disease, particularly for managing motor fluctuations in patients already receiving levodopa/carbidopa. Its mechanisms include inhibition of MAO-B, blockade of sodium and calcium channels, and inhibition of glutamate release, leading to increased brain dopamine levels and reduced glutamatergic excitotoxicity. Rosuvastatin is a **hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor (statin)**, used to lower cholesterol levels and reduce cardiovascular risk. There is no evidence of a marketed co-formulation tablet/capsule of safinamide plus rosuvastatin; however, their co-administration is possible and described due to potential pharmacokinetic interactions. Safinamide can **transiently inhibit the Breast Cancer Resistance Protein (BCRP)** in vitro, and drug-drug interaction studies in humans show a weak interaction with rosuvastatin (area under the curve [AUC] increase between 1.25 and 2.0 fold), but not considered clinically significant for most patients. Monitoring is still recommended when used together[1][4]. Primary indications: safinamide is for **Parkinson's disease** (as an adjunct), and rosuvastatin is for **hypercholesterolemia** and cardiovascular risk reduction.

02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)NaV (Voltage-gated sodium channels)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)ABCG2 (Breast cancer resistance protein)MAOB (Monoamine oxidase B)CaV (Voltage-gated calcium channel protein complex)

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