Mechanism of Action†

Tolvaptan is a selective vasopressin V2-receptor antagonist1

  • Tolvaptan has an affinity for the V2-receptor that is 1.8 times that of native AVP1
    • Tolvaptan affinity for the V2-receptor is 29 times greater than for the V1a-receptor1
  • When taken orally, Tolvaptan inhibits the binding of vasopressin at the V2-receptor in the kidney1

Adapted from LUPIN-TOLVAPTAN Product Monograph1

Decreased binding of vasopressin to the V2-receptor lowers adenylate cyclase activity resulting in a decrease in intracellular cAMP concentrations1

AVP=arginine vasopressin; cAMP=adenosine 3′, 5′-cyclic monophosphate.
† Clinical significance is unknown.

Reference: 1. LUPIN-TOLVAPTAN DRAFT Product Monograph. Lupin Pharma Canada Ltd. January 28, 2025.