Landiolol: A Comprehensive Monograph on an Ultra-Short-Acting, Highly Cardioselective β1-Adrenergic Antagonist

I. Foundational and Chemical Profile

1.1 Identification and Nomenclature

Landiolol is a small molecule drug classified as a cardioselective beta-adrenergic antagonist.[1] It is identified within major drug databases by its DrugBank Accession Number, DB12212, and its Chemical Abstracts Service (CAS) Registry Number, 133242-30-5.[1] The hydrochloride salt form, which is commonly used in clinical formulations, is identified by CAS Number 144481-98-1.[3]

The compound is known by a variety of chemical names and synonyms across scientific literature and regulatory documents. Its International Union of Pure and Applied Chemistry (IUPAC) name ismethyl 3-(4-{(2S)-2-hydroxy-3-[{2-[(morpholin-4-ylcarbonyl)amino]ethyl}amino]propoxy}phenyl)propanoate.[1]

Common synonyms for Landiolol include:

• ONO-1101 [2]
• LDLL600 [3]
• (-)-2,2-dimethyl-1,3-dioxolan-4S-ylmethyl 3-[3-[2-(morpholinocarbonylamino)ethylamino]-2S-hydroxypropoxy]phenyl]propionate [1]
• methyl 3-(4-{(2S)-2-hydroxy-3-[{2-[(morpholin-4-ylcarbonyl)amino]ethyl}amino]propoxy}phenyl)propanoate [1]

This precise chemical identification is fundamental to ensuring the accurate attribution of all subsequent pharmacological, pharmacokinetic, and clinical data to the correct molecular entity, preventing ambiguity in research and clinical practice.

1.2 Molecular Structure and Physicochemical Properties

Landiolol's distinct therapeutic profile is a direct consequence of its specific molecular structure and resulting physicochemical properties. Its chemical formula is C25​H39​N3​O8​, corresponding to an average molecular weight of approximately 509.6 g/mol and a precise monoisotopic mass of 509.273715228 Da.[1]