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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
Structure of FILANESIB

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

HIDE SMILES / InChI

Description

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 TargetPharmacologyConditionPotency
18.0 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
72 ng/mL
2.5 mg/m² single, intravenous
FILANESIB plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
1570 ng × h/mL
2.5 mg/m² single, intravenous
FILANESIB plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
66 h
2.5 mg/m² single, intravenous
FILANESIB plasma
Homo sapiens

Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as perpetrator​

PubMed

Sample Use Guides

In Vivo Use Guide
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
Filanesib inhibited His-tagged KSP motor domain assessed as inhibition of microtubule-stimulated KSP ATPase activity with IC50 18nM