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Clinical Trials Cardiovascular & Renal

Lixivaptan

also known as: Jinarc Alternative, VPA-985

An oral aquaretic — a selective V2 receptor antagonist that promotes free water excretion without sodium loss, relevant to vasopressin/ADH peptide pharmacology.

A non-peptide oral antagonist of the vasopressin V2 receptor in renal collecting ducts, producing electrolyte-free water diuresis (aquaresis) for hyponatremia management.

Mechanism of action

Selectively blocks the vasopressin V2 receptor on principal cells of the renal collecting duct, preventing aquaporin-2 insertion into the apical membrane. This blocks ADH-mediated water reabsorption, promoting excretion of free water (aquaresis) without affecting sodium, potassium, or other electrolytes. In ADPKD, V2 receptor blockade also reduces cAMP-driven cyst growth.

Primary uses

  • Autosomal dominant polycystic kidney disease (investigational)
  • Hyponatremia (SIADH)
  • Vasopressin physiology reference

Typical dosing

25–100 mg twice daily (oral)

Investigational dosing. Tolvaptan (approved V2 antagonist) dosed at 15–60 mg/day for comparison.

Regulatory status

Not yet FDA-approved. In clinical trials for autosomal dominant polycystic kidney disease (ADPKD). Tolvaptan (Jynarque/Samsca, related V2 antagonist) is FDA-approved for ADPKD and hyponatremia.

References

  1. [clinical-trial] ClinicalTrials.gov NCT04064346 (ALERT, lixivaptan in ADPKD).

Related peptides

Vasopressin

Vasostrict — the endogenous antidiuretic hormone as an ICU vasopressor. FDA-approved April 2014 for adults with vasodilatory shock (post-cardiotomy, sepsis) who remain hypotensive despite fluids and catecholamines. Works through V1a receptors on vascular smooth muscle — a receptor axis pharmacologically distinct from catecholamine receptors, preserving its vasopressor effect when adrenergic receptors are desensitised.

Desmopressin

DDAVP — the classic V2-selective vasopressin analog. FDA-approved February 1978 for central diabetes insipidus; decades of label expansion added primary nocturnal enuresis, nocturia (Noctiva / Nocdurna), and hemostatic use in mild hemophilia A and type 1 von Willebrand disease. WHO Essential Medicines List.

Terlipressin

Terlivaz — the first and only FDA-approved drug for hepatorenal syndrome (HRS). FDA-approved September 2022 (Mallinckrodt) for adults with HRS with rapid reduction in kidney function, after a multi-decade regulatory history including four prior Complete Response Letters and the successful CONFIRM Phase 3 trial (NEJM 2021).

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Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.