Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C22H48N12O2 |
Molecular Weight | 512.6957 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
N[C@@H](CCCNC(N)=N)C(=O)NCCCN1CCN(CCCNC(=O)[C@@H](N)CCCNC(N)=N)CC1
InChI
InChIKey=HRDUUSCYRPOMSO-ROUUACIJSA-N
InChI=1S/C22H48N12O2/c23-17(5-1-7-31-21(25)26)19(35)29-9-3-11-33-13-15-34(16-14-33)12-4-10-30-20(36)18(24)6-2-8-32-22(27)28/h17-18H,1-16,23-24H2,(H,29,35)(H,30,36)(H4,25,26,31)(H4,27,28,32)/t17-,18-/m0/s1
Ciraparantag (PER-977, aripazine), developed by Perosphere Inc., is a small, synthetic, water-soluble, cationic molecule and can reverse the anticoagulation mediated by unfractionated heparin, low-molecular-weight heparin, factor Xa and factor IIa inhibitors, and fondaparinux. It has the potential to be a universal antidote, inhibiting nearly all anticoagulants except vitamin K antagonists and argatroban. In April 2015, ciraparantag received FDA fast-track designation as an investigational anticoagulant reversal agent. Phase I/II
trials are currently underway to evaluate the safety and efficacy
of PER977 in reversing anticoagulation of edoxaban,
LMWH, and UFH.2.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL244 Sources: http://adisinsight.springer.com/drugs/800037993 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Secondary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
634 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
10570 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
173 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3860 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
100 mg single, intravenous dose: 100 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
7755 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
200 mg single, intravenous dose: 200 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
861 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
25 mg single, intravenous dose: 25 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
861 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
50 mg single, intravenous dose: 50 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
151 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3800 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
15 mg single, intravenous dose: 15 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
0.32 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
0.24 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
100 mg single, intravenous dose: 100 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
0.33 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
200 mg single, intravenous dose: 200 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
0.19 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
25 mg single, intravenous dose: 25 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
0.24 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
50 mg single, intravenous dose: 50 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
100% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/33205809/ |
300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CIRAPARANTAG serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Sample Use Guides
Single intravenous doses of Ciraparantag (100–300 mg) that completelyreversed anticoagulation associated with a single doseof edoxaban (60 mg) in healthy volunteers within 10 minutesand maintained reversal over 24 hours with no rebound andno need for infusions or repeat administration.
Route of Administration:
Intravenous
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CHEMBL3544919
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71576543
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U2R67KV65Q
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10164
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300000034035
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C169854
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Ciraparantag
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DTXSID701045783
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BC-147
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1438492-26-2
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DB15199
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ACTIVE MOIETY