ATCvet code: QB03XA09
Pharmacodynamics
The veterinary medicinal product is a competitive and reversible inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH). The inhibition of HIF-PH induces a dose-dependent increase of endogenous erythropoietin (EPO) by stabilising HIF, resulting in increased erythropoiesis (red blood cell production).
In a clinical field trial, 75 cats were evaluated for effectiveness (40 received Varenzin and 35 received a control product), 68% of cats receiving Varenzin achieved treatment success after 28 days of treatment, compared to 17% in the placebo group, with a higher number of treatment successes observed in cats with earlier stages of CKD. Treatment success was defined as an increase of ≥4% points in haematocrit observed on Study Day 28 and/or an overall 25% increase in haematocrit from baseline (Study Day 0).
Pharmacokinetics
Pharmacokinetics were investigated in healthy adult cats. After an oral dose of 5 mg molidustat sodium per kg to cats, molidustat was rapidly absorbed reaching peak plasma concentrations within an hour. Bioavailability was high (approximately 80%). With a half-life of approx. 6 hours no relevant accumulation was observed after once daily dosing. A dose proportional increase of exposure (AUC) was observed within a dose range of 2.5 to 10 mg/kg.