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Lixivaptan
Systematic (IUPAC) name
N-[3-chloro-4-(5H-pyrrolo-[2,1-c][1,4]benzodiazepin-

10(11H)-ylcarbonyl)phenyl]-5-fluoro-2-methylbenzamide

Identifiers
CAS number 168079-32-1
ATC code none
PubChem 172997
Chemical data
Formula C 27H21ClFN3O2  
Mol. mass 473.926
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Lixivaptan (VPA-985) is a selective and orally active non-peptide vasopressin receptor antagonist selective for the V2 subtype.[1] It has been developed for the treatment of hyponatremia,[2] particularly in patients with conditions such as liver cirrhosis[3] or congestive heart failure[4] where hyponatremia can be a chronic symptom. As of 2008, it is still in clinical trials for these indications.[5]

References

  1. ^ Albright JD, Reich MF, Delos Santos EG, Dusza JP, Sum FW, Venkatesan AM, Coupet J, Chan PS, Ru X, Mazandarani H, Bailey T. 5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors. Journal of Medicinal Chemistry. 1998 Jul 2;41(14):2442-4. PMID 9651149
  2. ^ Wong F, Blei AT, Blendis LM, Thuluvath PJ. A vasopressin receptor antagonist (VPA-985) improves serum sodium concentration in patients with hyponatremia: a multicenter, randomized, placebo-controlled trial. Hepatology. 2003 Jan;37(1):182-91. PMID 12500203
  3. ^ Gerbes AL, Gülberg V, Ginès P, Decaux G, Gross P, Gandjini H, Djian J; VPA Study Group. Therapy of hyponatremia in cirrhosis with a vasopressin receptor antagonist: a randomized double-blind multicenter trial. Gastroenterology. 2003 Apr;124(4):933-9. PMID 12671890
  4. ^ Orlandi C, Zimmer CA, Gheorghiade M. Role of vasopressin antagonists in the management of acute decompensated heart failure. Current Heart Failure Reports. 2005 Sep;2(3):131-9. PMID 16138949
  5. ^ Farmakis D, Filippatos G, Kremastinos DT, Gheorghiade M. Vasopressin and vasopressin antagonists in heart failure and hyponatremia. Current Heart Failure Reports. 2008 Jun;5(2):91-6. PMID 18765079
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