Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H14Cl2FN3O |
Molecular Weight | 390.238 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H]1CC2=C(NC3=C2C=C(F)C(Cl)=C3)[C@@]4(N1)C(=O)NC5=C4C=C(Cl)C=C5
InChI
InChIKey=CKLPLPZSUQEDRT-WPCRTTGESA-N
InChI=1S/C19H14Cl2FN3O/c1-8-4-11-10-6-14(22)13(21)7-16(10)23-17(11)19(25-8)12-5-9(20)2-3-15(12)24-18(19)26/h2-3,5-8,23,25H,4H2,1H3,(H,24,26)/t8-,19+/m0/s1
Cipargamin is an experimental synthetic antimalarial molecule belonging to the spiroindolone class. It possesses both the potency (average IC50 of 550 pM against asexual blood-stage P. falciparum) and favorable pharmacokinetics (elimination half-life of ~24 hours in humans) needed for a single-dose cure, a feature that could help slow the onset of parasite resistance and that is not shared by existing, approved antimalarial drugs. KAE609 is also unique in its ability to block transmission to mosquitoes. Cipargamin is a parasite P-type ATPase4 inhibitor. Cipargamin in phase II clinical trials for the treatment of acute, uncomplicated malaria due to plasmodium falciparum monoinfection. Nausea was the most common reported adverse effect. The adverse events were generally mild and did not lead to any discontinuations of the drug.
Originator
Sources: http://adisinsight.springer.com/drugs/800035252
Curator's Comment: # Novartis
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
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161 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
991 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1170 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1770 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
468 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.91 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
14.1 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
19.8 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
29.4 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
6.42 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
21.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
28 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
23.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
26.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
22.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25114127 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
CIPARGAMIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT01524341
30 mg once a day for three days
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22508309
Cipargamin was found to inhibit the early and late development of Plasmodium falciparum gametocytes in vitro in a dose-dependent fashion over a range of 5 to 500 nM.
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FDA ORPHAN DRUG |
746820
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FDA ORPHAN DRUG |
595417
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Z7Q4FWA04P
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44469321
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100000163596
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DTXSID70152424
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9865
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1193314-23-6
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DB12306
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Cipargamin
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C169853
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ACTIVE MOIETY