Tubulis GmbH  

TUB-040 is built with ethynylphosphonamidate conjugation chemistry, demonstrates high and long-lasting anti-tumor efficacy via Topoisomerase-I inhibition and excellent tolerability predictive of a wide therapeutic window in humans per preclinical proof-of-concept data for TUB-040.

The ADC candidate is directed against Napi2b, an antigen highly overexpressed in ovarian cancer and lung adenocarcinoma. Its IgG1 antibody targeting Napi2b is connected to its payload, the Topoisomerase I inhibitor Exatecan through a cleavable linker system. The company’s P5 conjugation technology was used to build TUB-040 with a homogenous DAR of 8. TUB-040 induces DNA damage and cell death, without causing unspecific uptake and cytotoxicity in healthy, target-negative cells. Moreover, Pharmacokinetic analysis showed that TUB-040 is highly stable, thus efficiently delivering its payload to the tumor while reducing offsite toxicities.

Tubulis expects to start its first Phase 1/2a clinical trial in 2024.... More Info Less Info

TUB-030 is a novel ADC built with ethynylphosphonamidate conjugation chemistry and shows long-lasting anti-tumor activity via Topoisomerase-I inhibition with an optimized therapeutic index, enabling 5T4 for targeted cancer therapy.

TUB-030 is an ADC that targets the oncofetal 5T4 antigen. 5T4 is a tumor-associated protein that is overexpressed in various types of cancers, including bladder, lung, breast, stomach, esophagus, head and neck, colon, and ovarian cancer. Tubulis’ ADC candidate differs from previous ADCs targeting 5T4 by implementing several layers of differentiation in terms of antibody, payload and conjugation technology. It combines the company’s proprietary P5 conjugation technology with its Tubutecan topoisomerase-I payload platform, resulting in a homogenous DAR (drug-antibody-ratio) of 8. TUB-030 has shown strong cytotoxicity towards cancer cells from different tumor indications with a broad range of 5T4 expression levels. Preclinical pharmacokinetic analysis further demonstrated the highly stable profile of TUB-030, enabling the efficient delivery of the payload to the tumor.... More Info Less Info