| Description |
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].
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| Related Catalog |
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| In Vitro |
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].
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| In Vivo |
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]. Animal Model: Male Sprague-Dawley rats (250-275 g) injected with UFH or LMWH (2.0 mg/kg)[2] Dosage: 0.5 mg/kg, 1.0 mg/kg, or 2.0 mg/kg Administration: Intravenous injection; once Result: Neutralizes the antithrombotic, anticoagulant, and bleeding effects of heparins as effectively as protamine sulfate and may be slightly more efficacious against LMWHs.
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| References |
[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. [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.
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