PLN-74809
Identification
- Generic Name
- PLN-74809
- DrugBank Accession Number
- DB16515
- Background
PLN-74809 is a small-molecule that dually inhibits both αvβ6 and αvβ1 to treat both idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC)2. The compound was granted orphan drug designation by the US FDA in August 2018 for treatment of IPF, and Pliant Therapeutics recently raised $100 million in Series C financing to support further clinical development of this compound5. Phase 2a studies are currently evaluating PLN-74809 safety and efficacy for participants with IPF (NCT04396756)across 10 participating countries4, and for participants with PSC (NCT04480840). In addition, the compound is also currently in Phase 2a trials (NCT04565249) for the treatment of COVID-19 related acute respiratory distress syndrome6.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
- External IDs
- PLN-74809
Pharmacology
- Indication
Through dual inhibition of integrins αvβ6 and αvβ1, PLN-74809 reduces subsequent activation of TGF-β1, which is actively involved in the growth of fibrotic tissue in lung and bile ducts2. Further studies showed that PLN-74809 inhibited collagen gene expression in PSC and IPF patient tissue3.
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- Pharmacodynamics
Not Available
- Mechanism of action
Target Actions Organism UIntegrin alpha-V Not Available Humans UIntegrin beta-1 Not Available Humans UIntegrin beta-6 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
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- Not Available
- CAS number
- Not Available
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- External Links
- Not Available
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 2 Completed Treatment Idiopathic Pulmonary Fibrosis (IPF) 3 2 Completed Treatment Primary Sclerosing Cholangitis (PSC) 1 2 Recruiting Treatment Idiopathic Pulmonary Fibrosis (IPF) 1 2 Terminated Treatment Acute Respiratory Distress Syndrome (ARDS) / Coronavirus Disease 2019 (COVID‑19) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
- Not Available
- 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
- Voltage-gated calcium channel activity
- Specific Function
- The alpha-V (ITGAV) integrins are receptors for vitronectin, cytotactin, fibronectin, fibrinogen, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin and vWF...
- Gene Name
- ITGAV
- Uniprot ID
- P06756
- Uniprot Name
- Integrin alpha-V
- Molecular Weight
- 116036.855 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Virus receptor activity
- Specific Function
- Integrins alpha-1/beta-1, alpha-2/beta-1, alpha-10/beta-1 and alpha-11/beta-1 are receptors for collagen. Integrins alpha-1/beta-1 and alpha-2/beta-2 recognize the proline-hydroxylated sequence G-F...
- Gene Name
- ITGB1
- Uniprot ID
- P05556
- Uniprot Name
- Integrin beta-1
- Molecular Weight
- 88414.575 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Integrin alpha-V:beta-6 (ITGAV:ITGB6) is a receptor for fibronectin and cytotactin (PubMed:17545607, PubMed:17158881). It recognizes the sequence R-G-D in its ligands (PubMed:17545607, PubMed:17158881). Internalisation of integrin alpha-V/beta-6 via clathrin-mediated endocytosis promotes carcinoma cell invasion (PubMed:17545607, PubMed:17158881). ITGAV:ITGB6 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1 (PubMed:17158881). Integrin alpha-V:beta-6 (ITGAV:ITGB6) mediates R-G-D-dependent release of transforming growth factor beta-1 (TGF-beta-1) from regulatory Latency-associated peptide (LAP), thereby playing a key role in TGF-beta-1 activation (PubMed:15184403, PubMed:22278742, PubMed:28117447).
- Specific Function
- Integrin binding
- Gene Name
- ITGB6
- Uniprot ID
- P18564
- Uniprot Name
- Integrin beta-6
- Molecular Weight
- 85935.195 Da
Drug created at January 21, 2021 02:02 / Updated at December 17, 2022 02:23