Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C20H22F2N4O2S |
Molecular Weight | 420.476 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CON(C)C(=O)N1N=C(S[C@@]1(CCCN)C2=CC=CC=C2)C3=CC(F)=CC=C3F
InChI
InChIKey=LLXISKGBWFTGEI-FQEVSTJZSA-N
InChI=1S/C20H22F2N4O2S/c1-25(28-2)19(27)26-20(11-6-12-23,14-7-4-3-5-8-14)29-18(24-26)16-13-15(21)9-10-17(16)22/h3-5,7-10,13H,6,11-12,23H2,1-2H3/t20-/m0/s1
DescriptionCurator's Comment: Description was created based on several sources, including
http://adisinsight.springer.com/drugs/800026254
Curator's Comment: Description was created based on several sources, including
http://adisinsight.springer.com/drugs/800026254
Filanesib is a highly selective, targeted KSP inhibitor with a mechanism of action distinct from currently available myeloma therapies such as immunomodulatory drugs (IMiDs®) and proteasome inhibitors. Across multiple studies, filanesib has demonstrated activity in heavily pretreated multiple myeloma patients, with a consistent safety profile including no drug-induced peripheral neuropathy and limited non-hematologic toxicity. Adverse events are generally limited to transient, non-cumulative and predominantly asymptomatic myelosuppression (decreases in blood counts) when supportive measures are used. Alpha 1-acid glycoprotein (AAG), a plasma protein, is a potential patient selection marker for filanesib. AAG is undergoing further investigation in clinical trials and could represent the first patient selection marker for a myeloma therapy. Filanesib is in Phase II for Multiple myeloma treatment.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4581 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26396688 |
18.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27433944
intravenously either at a dose of 1.5 mg/m2 /day (schedule 1: days 1, 2, 15, and 16) or 3 mg/m2 /day (schedule 2: days 1 and 15).
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26396688
Filanesib inhibited His-tagged KSP motor domain assessed as inhibition of microtubule-stimulated KSP ATPase activity with IC50 18nM
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NCI_THESAURUS |
C67440
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FDA ORPHAN DRUG |
431114
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100000174864
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8A49OSO368
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DTXSID50237086
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C68937
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Filanesib
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CD-02
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44224257
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885060-09-3
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DB06040
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9771
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CHEMBL2347655
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ACTIVE MOIETY