This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Name
ONT-093
Accession Number
DB14069
Description

ONT-093 is an orally bioavailable inhibitor of P-glycoprotein (P-gp). In pre-clinical studies, ONT-093 could inhibit P-gp and reverse multidrug resistance at nM concentrations with no effect on paclitaxel pharmacokinetics.

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 494.683
Monoisotopic: 494.30456186
Chemical Formula
C32H38N4O
Synonyms
Not Available
External IDs
  • OC 144-093
  • ONT 093
  • ONT-093
  • ONT093

Pharmacology

Indication
Not Available
Contraindications & Blackbox Warnings
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Pharmacodynamics
Not Available
Mechanism of action
TargetActionsOrganism
AP-glycoprotein 1
inhibitor
Humans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half-life
Not Available
Clearance
Not Available
Adverse Effects
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Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AfatinibThe serum concentration of Afatinib can be increased when it is combined with ONT-093.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with ONT-093.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with ONT-093.
AvatrombopagThe serum concentration of Avatrombopag can be increased when it is combined with ONT-093.
BaricitinibThe serum concentration of Baricitinib can be increased when it is combined with ONT-093.
BelinostatThe serum concentration of Belinostat can be increased when it is combined with ONT-093.
BendamustineThe serum concentration of Bendamustine can be increased when it is combined with ONT-093.
BetrixabanThe serum concentration of Betrixaban can be increased when it is combined with ONT-093.
BinimetinibThe serum concentration of Binimetinib can be increased when it is combined with ONT-093.
BisoprololThe serum concentration of Bisoprolol can be increased when it is combined with ONT-093.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

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  • Action
    Action

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Food Interactions
Not Available

Products

Categories

Drug Categories
Classification
Not classified

Chemical Identifiers

UNII
Not Available
CAS number
216227-54-2
InChI Key
RSJCLODJSVZNQA-BQYQJAHWSA-N
InChI
InChI=1S/C32H38N4O/c1-6-37-21-7-8-24-9-11-27(12-10-24)32-35-30(25-13-17-28(18-14-25)33-22(2)3)31(36-32)26-15-19-29(20-16-26)34-23(4)5/h7-20,22-23,33-34H,6,21H2,1-5H3,(H,35,36)/b8-7+
IUPAC Name
4-(2-{4-[(1E)-3-ethoxyprop-1-en-1-yl]phenyl}-4-{4-[(propan-2-yl)amino]phenyl}-1H-imidazol-5-yl)-N-(propan-2-yl)aniline
SMILES
[H]\C(COCC)=C(\[H])C1=CC=C(C=C1)C1=NC(=C(N1)C1=CC=C(NC(C)C)C=C1)C1=CC=C(NC(C)C)C=C1

References

General References
  1. Chi KN, Chia SK, Dixon R, Newman MJ, Wacher VJ, Sikic B, Gelmon KA: A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer. Invest New Drugs. 2005 Aug;23(4):311-5. doi: 10.1007/s10637-005-1439-x. [PubMed:16012790]
ChemSpider
4953358
ChEMBL
CHEMBL313113

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000423 mg/mLALOGPS
logP7.21ALOGPS
logP6.81ChemAxon
logS-6.1ALOGPS
pKa (Strongest Acidic)12.39ChemAxon
pKa (Strongest Basic)5.26ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area61.97 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity169.25 m3·mol-1ChemAxon
Polarizability61.43 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Chi KN, Chia SK, Dixon R, Newman MJ, Wacher VJ, Sikic B, Gelmon KA: A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer. Invest New Drugs. 2005 Aug;23(4):311-5. doi: 10.1007/s10637-005-1439-x. [PubMed:16012790]
  2. Newman MJ, Rodarte JC, Benbatoul KD, Romano SJ, Zhang C, Krane S, Moran EJ, Uyeda RT, Dixon R, Guns ES, Mayer LD: Discovery and characterization of OC144-093, a novel inhibitor of P-glycoprotein-mediated multidrug resistance. Cancer Res. 2000 Jun 1;60(11):2964-72. [PubMed:10850444]
  3. Hodges LM, Markova SM, Chinn LW, Gow JM, Kroetz DL, Klein TE, Altman RB: Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenet Genomics. 2011 Mar;21(3):152-61. doi: 10.1097/FPC.0b013e3283385a1c. [PubMed:20216335]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Hodges LM, Markova SM, Chinn LW, Gow JM, Kroetz DL, Klein TE, Altman RB: Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenet Genomics. 2011 Mar;21(3):152-61. doi: 10.1097/FPC.0b013e3283385a1c. [PubMed:20216335]
  2. Chi KN, Chia SK, Dixon R, Newman MJ, Wacher VJ, Sikic B, Gelmon KA: A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer. Invest New Drugs. 2005 Aug;23(4):311-5. doi: 10.1007/s10637-005-1439-x. [PubMed:16012790]

Drug created on June 14, 2018 16:38 / Updated on June 12, 2020 10:53

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