REG1 is an anticoagulation system consisting of two drugs: pegnivacogin, a single-stranded 31-nucleotide aptamer that binds and inhibits Factor IXa, and anivamersen, a complementary sequence reversal 15-nucleotide control agent.[1][2] REG1 mechanism of action It involves inhibition of Factor IXa.[3]

REG1 is being developed for use in patients undergoing percutaneous coronary intervention and the treatment of acute coronary syndrome.[4] REG1 is associated with severe allergic reactions.[5] In the phase 2b RADAR trial,[6] 12 allergic-like reactions occurred shortly after administration of pegnivacogin in three patients with histories of allergy.

In one clinical trial, it was found that there was no evidence that REG1 reduced ischaemic events or bleeding compared with bivalirudin.[1]

References

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  1. ^ a b Lincoff, A. Michael; Mehran, Roxana; Povsic, Thomas J.; Zelenkofske, Steven L.; Huang, Zhen; Armstrong, Paul W.; Steg, P. Gabriel; Bode, Christoph; Cohen, Mauricio G.; Buller, Christopher; Laanmets, Peep (2016-01-23). "Effect of the REG1 anticoagulation system versus bivalirudin on outcomes after percutaneous coronary intervention (REGULATE-PCI): a randomised clinical trial". The Lancet. 387 (10016): 349–356. doi:10.1016/S0140-6736(15)00515-2. ISSN 0140-6736. PMID 26547100. S2CID 10905525.
  2. ^ Sinha, Gunjan (2013-12-01). "Regado's aptamer lines up against anticoagulants". Nature Biotechnology. 31 (12): 1060. doi:10.1038/nbt1213-1060. ISSN 1546-1696. S2CID 476227.
  3. ^ Becker RC, Chan MY (December 2009). "REG-1, a regimen comprising RB-006, a Factor IXa antagonist, and its oligonucleotide active control agent RB-007 for the potential treatment of arterial thrombosis". Curr. Opin. Mol. Ther. 11 (6): 707–15. PMID 20072947.
  4. ^ Vavalle, John Paul; Cohen, Mauricio G (2012). "The REG1 anticoagulation system: a novel actively controlled factor IX inhibitor using RNA aptamer technology for treatment of acute coronary syndrome". Future Cardiology. 8 (3): 371–382. doi:10.2217/fca.12.5. ISSN 1479-6678. PMC 3739693. PMID 22420328.
  5. ^ Lincoff, A. Michael; Mehran, Roxana; Povsic, Thomas J.; Zelenkofske, Steven L.; Huang, Zhen; Armstrong, Paul W.; Steg, P. Gabriel; Bode, Christoph; Cohen, Mauricio G.; Buller, Christopher; Laanmets, Peep (2016-01-23). "Effect of the REG1 anticoagulation system versus bivalirudin on outcomes after percutaneous coronary intervention (REGULATE-PCI): a randomised clinical trial". Lancet. 387 (10016): 349–356. doi:10.1016/S0140-6736(15)00515-2. ISSN 1474-547X. PMID 26547100. S2CID 10905525.
  6. ^ Povsic, Thomas J.; Vavalle, John P.; Aberle, Laura H.; Kasprzak, Jaroslaw D.; Cohen, Mauricio G.; Mehran, Roxana; Bode, Christoph; Buller, Christopher E.; Montalescot, Gilles; Cornel, Jan H.; Rynkiewicz, Andrzej (2012-08-02). "A Phase 2, randomized, partially blinded, active-controlled study assessing the efficacy and safety of variable anticoagulation reversal using the REG1 system in patients with acute coronary syndromes: results of the RADAR trial". European Heart Journal. 34 (31): 2481–2489. doi:10.1093/eurheartj/ehs232. ISSN 1522-9645. PMC 3895957. PMID 22859796.