Exatecan: From a Potent Monotherapy Candidate to a Premier Antibody-Drug Conjugate Payload

Section 1: Molecular Profile and Physicochemical Characteristics

1.1 Identification and Nomenclature

Exatecan is an investigational small molecule drug recognized for its potent antineoplastic properties.[1] As a key entity in oncology research, it is cataloged across major chemical and pharmacological databases under a variety of identifiers, which are essential for accurate cross-referencing of scientific literature and clinical data. The primary generic name for the compound is Exatecan.[1]

In the context of its development and clinical evaluation, Exatecan is most frequently referred to by its research and development code, DX-8951.[2] The vast majority of clinical studies have utilized its mesylate salt form, designated

DX-8951f, to improve its physicochemical properties for intravenous administration.[1] Other synonyms and codes that appear in various databases include DX 8951, CS-147, and the code name DX-8951f for the mesylate hydrate form.[9]

The definitive chemical identifier for the free base form of the molecule is its Chemical Abstracts Service (CAS) Number, 171335-80-1.[1] This number uniquely identifies the specific chemical substance, distinct from its various salts and formulations. To provide a consolidated reference, the key identifiers for Exatecan are summarized in Table 1.

Table 1: Key Identifiers for Exatecan

1.2 Chemical Structure, Class, and Stereochemistry