Ciraparantag (aripazine) is a drug under investigation as an
antidote
An antidote is a substance that can counteract a form of poisoning. The term ultimately derives from the Greek term φάρμακον ἀντίδοτον ''(pharmakon) antidoton'', "(medicine) given as a remedy". Antidotes for anticoagulants are s ...
for a number of
anticoagulant (anti-blood clotting) drugs, including
factor Xa inhibitors (
rivaroxaban,
apixaban
Apixaban, sold under the brand name Eliquis, is an anticoagulant medication used to treat and prevent blood clots and to prevent stroke in people with nonvalvular atrial fibrillation through directly inhibiting factor Xa. Specifically it i ...
and
edoxaban
Edoxaban, sold under the brand name Lixiana among others, is an anticoagulant medication and a direct factor Xa inhibitor. It is taken by mouth.
Compared with warfarin it has fewer drug interactions.
It was developed by Daiichi Sankyo an ...
),
dabigatran
Dabigatran, sold under the brand name Pradaxa among others, is an anticoagulant used to treat and prevent blood clots and to prevent stroke in people with atrial fibrillation. Specifically it is used to prevent blood clots following hip or kn ...
, and heparins (including
fondaparinux
Fondaparinux (trade name Arixtra) is an anticoagulant medication chemically related to low molecular weight heparins. It is marketed by GlaxoSmithKline. A generic version developed by Alchemia is marketed within the US by Dr. Reddy's Laboratorie ...
,
low molecular weight heparin
Low-molecular-weight heparin (LMWH) is a class of anticoagulant medications. They are used in the prevention of blood clots and treatment of venous thromboembolism (deep vein thrombosis and pulmonary embolism) and in the treatment of myocardial in ...
s (LMWH), and
unfractionated heparin).
Medical uses
Ciraparantag significantly reverses anticoagulation induced by a therapeutic dose of
edoxaban
Edoxaban, sold under the brand name Lixiana among others, is an anticoagulant medication and a direct factor Xa inhibitor. It is taken by mouth.
Compared with warfarin it has fewer drug interactions.
It was developed by Daiichi Sankyo an ...
within 10 minutes following injection.
This return to normal haemostasis persists over 24 hours following a single intravenous dose of the drug.
In addition to edoxaban, it also reverses the actions of LMWH and dabigatran.
Pharmacology
Mechanism of action
According to ''
in vitro
''In vitro'' (meaning in glass, or ''in the glass'') studies are performed with microorganisms, cells, or biological molecules outside their normal biological context. Colloquially called " test-tube experiments", these studies in biology ...
'' studies, the substance binds directly to anticoagulants via
hydrogen bonds and charge-charge interactions
from or to various parts of the molecule:
Chemistry
Ciraparantag consists of two
L-
arginine units connected with a
piperazine
Piperazine () is an organic compound that consists of a six-membered ring containing two nitrogen atoms at opposite positions in the ring. Piperazine exists as small alkaline deliquescent crystals with a saline taste.
The piperazines are a broad ...
containing linker chain.
See also
*
Andexanet alfa
Andexanet alfa, sold under the trade name Andexxa among others, is an antidote for the medications rivaroxaban and apixaban, when reversal of anticoagulation is needed due to uncontrolled bleeding. It has not been found to be useful for other fac ...
*
Idarucizumab
Idarucizumab, sold under the brand name Praxbind, is a monoclonal antibody used as a reversal agent for dabigatran.
Idarucizumab was developed by Boehringer Ingelheim. One study sponsored by the manufacturer found that idarucizumab effectively ...
*
Prothrombin complex concentrate
Prothrombin complex concentrate (PCC), also known as factor IX complex, is a medication made up of blood clotting factors II, IX, and X. Some versions also contain factor VII. It is used to treat and prevent bleeding in hemophilia B if pure ...
*
Vitamin K
Vitamin K refers to structurally similar, fat-soluble vitamers found in foods and marketed as dietary supplements. The human body requires vitamin K for post-synthesis modification of certain proteins that are required for blood coagulation ...
References
Amino acid derivatives
Antidotes
Guanidines
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