PrJINARC®: A selective vasopressin V2-receptor antagonist with 2 modes of action (in vitro data)1,2†
Transcript
JINARC, tolvaptan mechanism of action.
JINARC is the first treatment indicated to slow the progression of kidney enlargement and expanded to also to slow kidney function decline in patients with autosomal dominant polycystic kidney disease (ADPKD). JINARC a selective vasopressin V2-receptor antagonist, inhibits the binding of vasopressin at the V2-receptor in renal tubular epithelial cells.
Decreased binding of vasopressin lowers adenylate cyclase activity. Which results in decreased intracellular cyclic AMP concentrations. In vitro analysis showed that, by reducing cyclic AMP levels in these cells, the rate of cell proliferation and fluid secretion into the cystic lumen was reduced. Which in turn decreased the rate of AVP-stimulated cyst growth.
JINARC has 1.8x higher affinity to the V2-receptor than native arginine vasopressin
† Clinical significance unknown.