Bisegliptin

Identification

Generic Name
Bisegliptin
DrugBank Accession Number
DB06127
Background

Bisegliptin is a compound for the treatment of type 2 diabetes. It is an orally active, dipeptidyl peptidase-IV (DPPIV) inhibitor which lowers blood glucose levels by blocking the degradation of the hormone GLP-1 thereby stimulating glucose-dependent insulin secretion and lowering blood glucose levels without hypoglycemic effects.

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 351.422
Monoisotopic: 351.195819872
Chemical Formula
C18H26FN3O3
Synonyms
  • Bisegliptin
External IDs
  • KRP-104

Pharmacology

Indication

Investigated for use/treatment in diabetes mellitus type 2.

Pharmacology
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Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Not Available

Mechanism of action

Bisegliptin is an orally active, dipeptidyl peptidase-IV (DPPIV) inhibitor which lowers blood glucose levels by blocking the degradation of the hormone GLP-1 thereby stimulating glucose-dependent insulin secretion and lowering blood glucose levels without hypoglycemic effects.

TargetActionsOrganism
UDipeptidyl peptidase 4Not AvailableHumans
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
Medicalerrors
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Toxicity

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
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Bisegliptin.
AcebutololThe therapeutic efficacy of Bisegliptin can be increased when used in combination with Acebutolol.
AcetazolamideThe therapeutic efficacy of Bisegliptin can be increased when used in combination with Acetazolamide.
AcetohexamideBisegliptin may increase the hypoglycemic activities of Acetohexamide.
Acetyl sulfisoxazoleThe therapeutic efficacy of Bisegliptin can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acidThe risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Bisegliptin.
AlbiglutideThe risk or severity of hypoglycemia can be increased when Bisegliptin is combined with Albiglutide.
AlclometasoneThe risk or severity of hyperglycemia can be increased when Alclometasone is combined with Bisegliptin.
AlogliptinThe risk or severity of angioedema can be increased when Bisegliptin is combined with Alogliptin.
AlteplaseThe risk or severity of angioedema can be increased when Alteplase is combined with Bisegliptin.
Interactions
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Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
9U5KQ79OK6
CAS number
862501-61-9
InChI Key
AKFNKZFJBFQFAA-DIOPXHOYSA-N
InChI
InChI=1S/C18H26FN3O3/c1-2-25-16(24)17-3-6-18(7-4-17,8-5-17)21-11-15(23)22-12-13(19)9-14(22)10-20/h13-14,21H,2-9,11-12H2,1H3/t13-,14-,17?,18?/m0/s1
IUPAC Name
ethyl 4-({2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl}amino)bicyclo[2.2.2]octane-1-carboxylate
SMILES
[H][C@@]1(F)CN(C(=O)CNC23CCC(CC2)(CC3)C(=O)OCC)[C@@]([H])(C1)C#N

References

General References
  1. Link [Link]
PubChem Substance
347910337
ChemSpider
9863621

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentType 2 Diabetes Mellitus2

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 Solubility0.294 mg/mLALOGPS
logP0.82ALOGPS
logP0.8ChemAxon
logS-3.1ALOGPS
pKa (Strongest Basic)9.46ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area82.43 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity88.4 m3·mol-1ChemAxon
Polarizability37.17 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Virus receptor activity
Specific Function
Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by bindi...
Gene Name
DPP4
Uniprot ID
P27487
Uniprot Name
Dipeptidyl peptidase 4
Molecular Weight
88277.935 Da

Drug created on November 18, 2007 18:30 / Updated on February 21, 2021 18:51