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Patent Granted in US and EU, Core to Synaffix ADC Technology

The Netherlands, 03 November 2015 – Synaffix BV, today announced that a key patent has been granted in the US (US 8,859,629 B2) as well as in the EU (EP 2 563 753 B1), further strengthening its IP portfolio.  The patent covers “Fused cyclooctynes and their use in metal-free click reactions”, specifically BCN, a molecule that enables highly efficient conjugation to proteins bearing an azide.

BCN is ideally suited for reactions with proteins, given it comes with the highest combined solubility and reactivity of all the cyclooctynes available, in particular with regard to cyclooctynes with fused aromatic rings (DBCO/DIBO).  Further, conjugations with BCN are completely orthogonal and can occur rapidly in an aqueous environment and in the absence of a metal catalyst.  Previous versions of the click reaction required a copper catalyst, which led to protein oxidation or degradation in some cases.

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HydraSpace™ Polar Spacer

Forming an integral part of every toxSYN™ linker-payload, HydraSpace™ bears a negative charge at physiological pH and improves:

  1. Therapeutic efficacy
  2. Tolerability
  3. PK
  4. Manufacturability
Key publication about HydraSpace

GlycoConnect™ design easily matches payload potency with the most appropriate drug-antibody ratio (DAR).

Key publications about GlycoConnect™

toxSYN™ Linker-Payloads

Choose from the following linker-payloads, attach to your antibody under a technology evaluation and go straight into ADC product development following positive POC.
toxSYN™
Linker-Payload
Mode-of-Action Payload
(Active Catabolite)
1. SYNtecan E™*Topoisomerase 1 inhibitor Camptothecin-based
2. SYNeamicin D™*DNA
damaging agent
Calicheamicin-based
3. SYNeamicin G™*
4. SYN-PNU™*Nemorubicin-based
5. SYNstatin E™Microtubule
inhibitors
Auristatin-based
6. SYNstatin F™
7. SYNtansine™ Maytansine-based

* Patent protection filed by Synaffix, beyond the claims of GlycoConnect™ and HydraSpace™

** N-6-aminohexanoyl-maytansine (Ahx-maytansine)