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lotiglipron   Click here for help

GtoPdb Ligand ID: 14092

Synonyms: example 10 [US10676465] [2] | PF-07081532 | PF07081532
Compound class: Synthetic organic
Comment: Lotiglipron (PF-07081532) is an oral, small-molecule glucagon-like peptide-1 receptor (GLP-1R) agonist [3]. It was developed for potential to treat type 2 diabetes and obesity.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
2D Structure
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2D Structure

An image of the ligand's 2D structure. For small molecules with SMILES these are drawn using the NCI/CADD Chemical Identifier Resolver. Click on the image to access the chemical structure search tool with the ligand pre-loaded in the structure editor. For other types of ligands, e.g. longer nucleotides and peptides, a manually drawn representation of the molecule may be provided.

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SMILES / InChI / InChIKey
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SMILES / InChI / InChIKey

SMILES (Simplified Molecular Input Line Entry Specification) A specification for unambiguously describing the structure of chemical molecules using short ASCII strings. Canonical SMILES specify a unique representation of the 2D structure without chiral or isotopic specifications. Isomeric SMILES include chiral specification and isotopes.

Standard InChI (IUPAC International Chemical Identifier) and InChIKey InChI is a non-proprietary, standard, textual identifier for chemical substances designed to facilitate linking of information and database searching. An InChIKey is a simplified version of a full InChI, designed for easier web searching.

Generated using the Chemistry Development Kit (CDK) (Willighagen EL et al. Journal of Cheminformatics vol. 9:33. 2017, doi:10.1186/s13321-017-0220-4; https://cdk.github.io/)

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Canonical SMILES C[C@]1(C2=CC=C(C=N2)Cl)OC3=C(C(=CC=C3)C4CCN(CC4)CC5=NC6=C(C=C(C=C6)C(=O)O)N5C[C@@H]7CCO7)O1
Isomeric SMILES C[C@@]1(OC2=CC=CC(=C2O1)C3CCN(CC3)CC4=NC5=C(N4C[C@@H]6CCO6)C=C(C=C5)C(=O)O)C7=NC=C(C=C7)Cl
InChI InChI=1S/C31H31ClN4O5/c1-31(27-8-6-21(32)16-33-27)40-26-4-2-3-23(29(26)41-31)19-9-12-35(13-10-19)18-28-34-24-7-5-20(30(37)38)15-25(24)36(28)17-22-11-14-39-22/h2-8,15-16,19,22H,9-14,17-18H2,1H3,(H,37,38)/t22-,31-/m0/s1
InChI Key SVPYZAJTWFQTSM-UGDMGKLASA-N

Generated using the Chemistry Development Kit (CDK) (Willighagen EL et al. Journal of Cheminformatics vol. 9:33. 2017, doi:10.1186/s13321-017-0220-4; https://cdk.github.io/)
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Summary of Clinical Use Click here for help
Development of lotiglipron (PF-07081532) was discontinued (in phase 2) in late 2023 following detection of elevated transaminase (indicative of liver injury) in trial participants [1].
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT05158244 Study of Multiple Oral Doses of PF-07081532 in Adult Participants With Type 2 Diabetes Mellitus Phase 1 Interventional Pfizer 3
NCT04305587 Multiple Escalating Oral Doses Study of PF-07081532 in Adult Participants With Type 2 Diabetes Mellitus Phase 1 Interventional Pfizer 3
NCT05579977 Trial to Learn About the Study Medicine (PF-07081532) and Rybelsus in People With Type 2 Diabetes and Separately PF-07081532 in People With Obesity Phase 2 Interventional Pfizer 1