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LTX-401

Lytix Biopharma AS

Drug Names(s): LTX401, LTX 401

Description: LTX-401 is a novel oncolytic ß-amino acid derivative with potential immunogenic properties.

Host defense peptides (HDPs) are naturally occurring peptides with important antimicrobial and immunomodulatory functions and are part of the innate immune system in virtually all species of animals. Several HDPs are reported to exhibit oncolytic properties, also termed oncolytic peptides, with an ability to cause the lysis of cancer cells. This ability has been confirmed by several synthetically designed peptides.

LTX-401 is a small amphipathic ß(2,2)-amino acid-derived antitumor molecule with an amphipathic conformation. Based on structure-activity-relationship (SAR) studies on short cationic peptides (<9 amino acid residues), it was discovered that the introduction of large lipophilic groups compensated for the peptide length. Additionally, by coupling two aromatic side-chains to the same carbon atom, the length could be further reduced to a minimum without losing cytotoxic activity.

These discoveries led to the production and synthesis of a panel of ß-peptidomimetics to help confirm the pharmacophore model of short cationic peptides, which dictates that such compounds should contain cationic-charged residues, in addition to bulky and lipophilic moieties for optimal activity. LTX-401 was chosen as the lead compound in this panel.


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