Nerandomilast is a synthetic phosphodiesterase 4 (PDE4) inhibitor and pharmaceutical active pharmaceutical ingredient (API). It preferentially inhibits the PDE4B subtype, resulting in increased intracellular cyclic adenosine monophosphate (cAMP) and modulation of inflammatory and fibrotic signaling.
Nerandomilast was originally developed as BI 1015550 and is associated with the treatment of idiopathic pulmonary fibrosis (IPF) and progressive pulmonary fibrosis (PPF). It is an orally active small molecule and the pharmacologically active R-enantiomer.
Nerandomilast is a specialized PDE4 inhibitor API relevant to respiratory medicine, antifibrotic drug development, pharmaceutical formulation research and analytical testing.
The compound is particularly relevant to research involving pulmonary fibrosis, inflammatory signaling, PDE4B inhibition and lung fibroblast activity.
CAS Number: 1423719-30-5
Molecular Formula: C₂₀H₂₅ClN₆O₂S
Molecular Weight: 449.0 g/mol
Chemical Name: [1-[[(5R)-2-[4-(5-chloropyrimidin-2-yl)piperidin-1-yl]-5-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl]amino]cyclobutyl]methanol
Development Code: BI 1015550 / BI-1015550
Drug Class: Phosphodiesterase 4 Inhibitor
Therapeutic Class: Selective Immunosuppressant / Antifibrotic
Therapeutic Area: Respiratory Medicine / Pulmonology
Molecule Type: Synthetic Small Molecule
Stereochemistry: R-enantiomer
The CAS number, molecular formula and molecular weight are reported by PubChem and the IUPHAR/BPS Guide to Pharmacology.
Nerandomilast preferentially inhibits PDE4B, an enzyme responsible for hydrolysis of intracellular cAMP.
Its pharmacological mechanism includes:
Nerandomilast has been investigated particularly for its role in modifying inflammatory and fibrotic processes associated with interstitial lung disease.
Nerandomilast API is relevant to:
Nerandomilast is a PDE4B-preferential inhibitor developed for pulmonary fibrotic diseases.
Its antifibrotic activity is associated with modulation of intracellular cAMP and downstream inflammatory and profibrotic signaling pathways. It has been clinically developed for idiopathic pulmonary fibrosis and progressive pulmonary fibrosis.
Nerandomilast preferentially inhibits PDE4B compared with other PDE4 isoforms.
PDE4 enzymes regulate intracellular cAMP by hydrolyzing it. Inhibition of PDE4B increases cAMP signaling and can influence inflammatory cytokines and profibrotic growth-factor pathways.
Nerandomilast is a synthetic organic small molecule with molecular formula C₂₀H₂₅ClN₆O₂S and molecular weight 449.0 g/mol.
PubChem reports an XLogP3-AA value of approximately 1.3, topological polar surface area of 123 Ų, and one stereogenic center corresponding to the R-enantiomer.
Note: A standardized pharmacopoeial description of appearance, melting point and solubility was not identified from an authoritative public monograph. Therefore, these properties should not be presented as official API release specifications without your validated product specification.
A controlled Nerandomilast API manufacturing process may involve:
Typical Nerandomilast API testing may include:
Because Nerandomilast contains a defined stereogenic center and the R-enantiomer is the active form, chiral purity is an important quality attribute.
Store Nerandomilast API in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive moisture, heat and direct light.
Final commercial storage conditions should be based on validated stability data and the applicable API specification.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |