Innovative Platform - ‘OptiLinked’ FDCs

Solid tumours require therapies that can penetrate tumours rapidly and completely, whilst clearing from normal tissues quickly. With its revolutionary OptiLink^TM technology platform, Antikor has adopted an altogether more novel approach for ADCs using much smaller antibody fragments (single-chain scFvs) that are relatively easy to discover and can be selected with a high number of surface lysine residues for multiple drug-molecule conjugation via their -NH2 side-chains. Quite counter-intuitively, this provides far higher payloads loadings on a small fragment than have so far been achieved with whole MAbs, without running the risk of product manufacturing or stability problems.

References

1. Deonarain MP, Yahioglu G. Current strategies for the discovery and bioconjugation of smaller, targetable drug conjugates tailored for solid tumor therapy. Expert Opin Drug Discov. 2021 Jun;16(6):613-624. doi: 10.1080/17460441.2021.1858050. Epub 2021 Jan 11. PMID: 33275475.

2. Deonarain MP, Xue Q. Tackling solid tumour therapy with small-format drug conjugates. Antib Ther. 2020 Nov 25;3(4):237-245. doi: 10.1093/abt/tbaa024. PMID: 33928231; PMCID: PMC7990258.

3. Anti-HER2, high-DAR Antibody Fragment Drug Conjugates (FDC) with a Glucuronide-based MMAE linker-payload demonstrates superior efficacy over IgG-based ADCs. Manuscript in preparation for 2024

OptiLinked-FDC platform advantages:-

Maximisation of drug potency by facilitating higher drug-loading ratios for targeted delivery of many active drug molecules per receptor and cell
Small format to enable fast and even tumour penetration ensuring more rapid efficacy
Small format and lack of Fc to facilitate fast clearance from normal tissues, reduced vasculature exposure and dose-limiting haematological toxicities
Prevention of unwanted molecular interactions that inhibit drug activity
Applicable to most antibody fragment formats, improving their versatility for a 3rd party
Ability to reverse engineer whole MAb and ADCs to make next-generation FDC versions
Improved drug-conjugate manufacturing, cost-of-goods, solubility and formulation
Preserved scFv stability and binding functions
Improved pharmacokinetics/dynamics over whole MAbs