Tubulis has developed a suite of complementary technology platforms for the discovery and development of a new generation of versatile and customizable antibody-drug conjugates (ADCs). At the heart of our proprietary platforms are completely new conjugation technologies, that allow us to overcome the main limitations of ADC technologies to date:
- target-independent toxicities, such as premature payload loss and unspecific cell uptake DAR8 conjugation
- restricted ADC design space to match target biology with appropriate payload class and the right drug-to-antibody ratio
Depending on the indication and the needs for both the chemical component and the antibody, we can leverage the right platform to create uniquely matched ADCs with superior biophysical properties that enable us to provide drug candidates that can make a difference in a variety of cancer indications and beyond.
The new generation of ADCs
P5 conjugation platform
Homogeneous, stable high-DAR ADCs
Our P5 conjugation technology allows to rapidly generate ultra- stable ADCs with unprecedented linker stability and chemical flexibility, providing us with the opportunity to develop truly differentiated ADCs.
- Homogenous DAR8 conjugation
- Chemical flexibility and broad ADC design possibilities
- Novel cysteine-selective chemistry
- Unique stability and selectivity
Both conjugation technology platforms are covered through our extensive IP portfolio.
Tubutecan – topo-I payload platform
Improving patient benefit by increasing the therapeutic window
Our proprietary linker-payload platform offers optimized on- target delivery of potent topoisomerase-I inhibitors combined with active reduction of unwanted target-independent toxicities. For the first time, we achieve stable and high payload attachment (DAR8) without compromising on the biophysical properties of the whole ADC molecule.
Approved Topo-I ADC using maleimide-based conjugation loses over 60 % of its payload over time resulting in an average drug- to-antibody ratio of only 3 after three days. Tubulis’ ADC using the proprietary P5 conjugation technology remains stable over seven days in serum.
The unique profile of Tubutecan based ADCs translates to long lasting in-vivo potency where a single dose treatment of 1 mg/kg results in significant benefit and complete remission in all animals over a period of 90 days.
The Tub-tag® platform
Remodeling the ADC microenvironment
The Tub-tag® conjugation platform was inspired by microtubule biology and adds a significant amount of stability to the ADC product candidates by modulating the antibody to provide a highly beneficial microenvironment for the payload. Moreover, the human-derived nature of the Tub-tag® lowers the risk of the ADC causing unwanted immune reactions.
- Homogenous DAR2 or DAR4 conjugation
- Defined drug loads with high DAR flexibility
- Tub-tag® provides highly beneficial microenvironment for site-specific payload conjugation
