KOS-2187
Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- KOS-2187
- DrugBank Accession Number
- DB05946
- Background
KOS-2187, a novel erythromycin-based motilin agonist, or motilide, as a clinical candidate for the treatment of gastrointestinal motility disorders such as gastroparesis and gastroesophageal reflux disease (GERD).
- Type
- Small Molecule
- Groups
- Investigational
- Structure
- Weight
- Average: 812.051
Monoisotopic: 811.508191415 - Chemical Formula
- C43H73NO13
- Synonyms
- (3R,4S,5S,6R,7R,9R,10S,11S,12R,13S,14R)-7,10,12,13-tetrahydroxy-4-(5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl)oxy-6-[3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-14-phenyl-oxacyclotetradecan-2-one
Pharmacology
- Indication
Investigated for use/treatment in gastroesophageal reflux disease (GERD) and gastrointestinal diseases and disorders (miscellaneous).
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- Pharmacodynamics
Not Available
- Mechanism of action
KOS-2187 is a potent, selective motilin receptor agonist that is chemically stable and orally bioavailable and lacks antibiotic activity. In preclinical studies, KOS-2187 showed an improved safety profile relative to erythromycin and accelerated gastric emptying, suggesting that it may provide symptom relief in several gastrointestinal diseases
Target Actions Organism UPromotilin Not Available 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- 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
- Not Available
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- Not Available
- CAS number
- Not Available
- InChI Key
- BCKWPVFDVOGCTM-UHFFFAOYSA-N
- InChI
- InChI=1S/C43H73NO13/c1-22(2)44(12)30-19-24(4)53-40(33(30)46)57-37-26(6)34(55-31-21-42(10,52-13)36(48)28(8)54-31)27(7)39(49)56-38(29-17-15-14-16-18-29)43(11,51)35(47)25(5)32(45)23(3)20-41(37,9)50/h14-18,22-28,30-38,40,45-48,50-51H,19-21H2,1-13H3
- IUPAC Name
- SMILES
- COC1(C)CC(OC2C(C)C(OC3OC(C)CC(C3O)N(C)C(C)C)C(C)(O)CC(C)C(O)C(C)C(O)C(C)(O)C(OC(=O)C2C)C2=CC=CC=C2)OC(C)C1O
References
- General References
- Not Available
- External Links
- ChemSpider
- 19672134
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
Property Value Source - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Plays an important role in the regulation of interdigestive gastrointestinal motility and indirectly causes rhythmic contraction of duodenal and colonic smooth muscle.
- Specific Function
- hormone activity
- Gene Name
- MLN
- Uniprot ID
- P12872
- Uniprot Name
- Promotilin
- Molecular Weight
- 12919.89 Da
Drug created at November 18, 2007 18:28 / Updated at July 23, 2024 18:02