Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H23F2N5O |
| Molecular Weight | 411.4477 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1(C)N(CCN2C(NC3=CC=C(F)C=C3)=C(N=C12)C4=CC=C(F)C=C4)C(=O)CN
InChI
InChIKey=BUPRVECGWBHCQV-UHFFFAOYSA-N
InChI=1S/C22H23F2N5O/c1-22(2)21-27-19(14-3-5-15(23)6-4-14)20(26-17-9-7-16(24)8-10-17)28(21)11-12-29(22)18(30)13-25/h3-10,26H,11-13,25H2,1-2H3
| Molecular Formula | C22H23F2N5O |
| Molecular Weight | 411.4477 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
GNF-156 (ganaplacide or KAF-156) is an antimalarial agent that is part of the imidazolopiperazine family. It exerts activity against pre-erythrocytic liver stages, asexual and sexual blood stages. An improvement compared to existing antimalarial drug combinations is that this compound shows promising single-dose antimalarial activity, and no serious safety and tolerability concerns in humans are known so far. Phase II clinical trials have been completed for GNF-156. Its potential is also being investigated in combination with lumefantrine (an aryl-amino alcohol) in LUM-KAF156.
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:43:33 UTC 2023
by
admin
on
Sat Dec 16 11:43:33 UTC 2023
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| Record UNII |
85VMN9JU7A
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| Record Status |
Validated (UNII)
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FDA ORPHAN DRUG |
895622
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DTXSID701105307
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Ganaplacide
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85VMN9JU7A
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49856296
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C175070
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10761
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1261113-96-5
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100000178050
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ACTIVE MOIETY |
Consistent with the previously reported activity profile of this series, the clinical candidate KAF156 shows blood schizonticidal activity with 50% inhibitory concentrations of 6 to 17.4 nM against P. falciparum drug-sensitive and drug-resistant strains, as well as potent therapeutic activity in a mouse models of malaria with 50, 90, and 99% effective doses of 0.6, 0.9, and 1.4 mg/kg, respectively. When administered prophylactically in a sporozoite challenge mouse model, KAF156 is completely protective as a single oral dose of 10 mg/kg. Finally, KAF156 displays potent Plasmodium transmission blocking activities both in vitro and in vivo. Collectively, our data suggest that KAF156, currently under evaluation in clinical trials, has the potential to treat, prevent, and block the transmission of malaria.
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