KB3305

Identification

Generic Name
KB3305
DrugBank Accession Number
DB06349
Background

KB3305 is an investigational liver selective antagonist for the glucocorticoid receptor, developed by Karo Bio for the treatment of Type 2 Diabetes.

Type
Small Molecule
Groups
Investigational
Structure
Weight
Average: 850.194
Monoisotopic: 849.554353759
Chemical Formula
C54H75NO7
Synonyms
  • (4R)-4-((3S,5R,7R,8R,9S,10S,12S,13R,14S,17R)-7,12-DIHYDROXY-3-(2-(4-((8S,11R,13S,14S,17S)-17-HYDROXY-13-METHYL-3-OXO-17-PROP-1-YNYL-1,2,6,7,8,11,12,14,15,16-DECAHYDROCYCLOPENTA(A)PHENANTHREN-11-YL)-N-METHYL-ANILINO)ETHOXY)-10,13-DIMETHYL-2,3,4,5,6,7,8,9,
  • 3.BETA.,5.BETA.,7.ALPHA.,12.ALPHA.)-7,12-DIHYDROXY-3-(2-((4-((11.BETA.,17.BETA.)-17-HYDROXY-3-OXO-17-(1-PROPYN-1-YL)ESTRA-4,9-DIEN-11-YL)PHENYL)METHYLAMINO)ETHOXY)CHOLAN-24-OIC ACID
  • CHOLAN-24-OIC ACID, 7,12-DIHYDROXY-3-(2-((4-((11.BETA.,17.BETA.)-17-HYDROXY-3-OXO-17-(1-PROPYN-1-YL)ESTRA-4,9-DIEN-11-YL)PHENYL)METHYLAMINO)ETHOXY)-, (3.BETA.,5.BETA.,7.ALPHA.,12.ALPHA.)-
External IDs
  • A-348441

Pharmacology

Indication

Investigated for use/treatment in diabetes mellitus type 2.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

KB3305 is the first compound in a class of liver selective glucocorticoid antagonists. It inhibits the liver from increasing increase glucose production from the action of glucocorticoids, and may reduce the elevated hepatic glucose production in patients with type 2 diabetes, as well as risk factors including low density lipoprotein (LDL) cholesterols, triglycerides and free fatty acids in the plasma.

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

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.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
7Q26YN85LO
CAS number
639520-46-0
InChI Key
LEUWECPXLBIBOF-LXEVTIFISA-N
InChI
InChI=1S/C54H75NO7/c1-7-22-54(61)24-21-43-40-15-11-34-27-37(56)14-16-39(34)49(40)41(31-52(43,54)4)33-9-12-36(13-10-33)55(6)25-26-62-38-20-23-51(3)35(28-38)29-46(57)50-44-18-17-42(32(2)8-19-48(59)60)53(44,5)47(58)30-45(50)51/h9-10,12-13,27,32,35,38,40-47,50,57-58,61H,8,11,14-21,23-26,28-31H2,1-6H3,(H,59,60)/t32-,35+,38+,40+,41-,42-,43+,44+,45+,46-,47+,50+,51-,52-,53+,54-/m1/s1
IUPAC Name
SMILES
[H][C@@](C)(CCC(O)=O)[C@@]1([H])CC[C@@]2([H])[C@]3([H])[C@]([H])(O)C[C@]4([H])C[C@]([H])(CC[C@@]4(C)[C@@]3([H])C[C@]([H])(O)[C@@]12C)OCCN(C)C1=CC=C(C=C1)[C@@]1([H])C[C@]2(C)[C@@]([H])(CC[C@]2(O)C#CC)[C@]2([H])CCC3=CC(=O)CCC3=C12

References

General References
  1. Jacobson PB, von Geldern TW, Ohman L, Osterland M, Wang J, Zinker B, Wilcox D, Nguyen PT, Mika A, Fung S, Fey T, Goos-Nilsson A, Grynfarb M, Barkhem T, Marsh K, Beno DW, Nga-Nguyen B, Kym PR, Link JT, Tu N, Edgerton DS, Cherrington A, Efendic S, Lane BC, Opgenorth TJ: Hepatic glucocorticoid receptor antagonism is sufficient to reduce elevated hepatic glucose output and improve glucose control in animal models of type 2 diabetes. J Pharmacol Exp Ther. 2005 Jul;314(1):191-200. doi: 10.1124/jpet.104.081257. Epub 2005 Mar 22. [Article]
Not Available

Clinical Trials

Clinical Trials
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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
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Drug created at March 19, 2008 16:25 / Updated at October 07, 2024 17:36