Delparantag  (Synonyms: PMX-60056)

Delparantag (PMX-60056) is a salicylamide derivative and an effective unfractionated heparin (UFH) and low molecular weight heparin (LMWH) reversing agent. Delparantag shows ability to neutralize the anticoagulation and bleeding effects of UFH and LMWH^[1][2].

Delparantag is designed to restore coagulation by specifically binding to the pentasaccharide and disrupting UFH and LMWH interaction with antithrombin^[1].
In heparinized plasma, Delparantag (PMX-60056) is more potent on a gravimetric basis than protamine at neutralizing both anti-Xa and anti-IIa activities. Delparantag is able to completely neutralize heparin at an approximate 2:1 gravimetric ratio. The amount of residual anti-IIa and anti-Xa activity was significantly less with Delparantag at a concentration of 50 mg/mL. In plasma anticoagulated with enoxaparin, Delparantag produces a concentration-dependent neutralization of anti-Xa activity. The amount of anti-Xa activity remaining after supplementation of the neutralizing agent is significantly less with Delparantag at concentrations above 25 mg/mL^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Delparantag (PMX-60056; 0.5 mg/kg, 1.0 mg/kg, or 2.0 mg/kg; intravenous injection; once; male Sprague-Dawley rats) treatment neutralizes the antithrombotic, anticoagulant, and bleeding effects of heparins as effectively as protamine sulfate and may be slightly more efficacious against LMWHs^[2].
Plasma half-life elimination of Delparantag is between 3 and 5 min^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1126.31

C₅₆H₇₉N₁₃O₁₂

872454-31-4

K-{Oaa}-K-{Oaa}-K-{Oaa}-K

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Mahan CE. A 1-year drug utilization evaluation of protamine in hospitalized patients to identify possible future roles of heparin and low molecular weight heparin reversal agents. J Thromb Thrombolysis. 2014 Apr;37(3):271-8.  [Content Brief]

  [2]. Kuziej J, et al. In vivo neutralization of unfractionated heparin and low-molecular-weight heparin by a novel salicylamide derivative. Clin Appl Thromb Hemost. 2010 Aug;16(4):377-86.  [Content Brief]