Tubulis GmbH  

Tubulis’ lead antibody-drug conjugate (ADC) candidate TUB-040 is directed against NaPi2b, an antigen highly overexpressed in ovarian cancer and lung adenocarcinoma.

It consists of an IgG1 antibody targeting NaPi2b connected to the topoisomerase I inhibitor Exatecan through a cleavable linker system based on the company’s proprietary P5 conjugation technology with a homogeneous drug-to-antibody-ratio (DAR) of 8. P5 conjugation is a novel chemistry for cysteine-selective conjugation that enables ADC generation with unprecedented linker stability and superior biophysical properties.

Preclinical pharmacokinetic analysis showed that TUB-040 efficiently delivers its payload to the tumor while reducing off-site toxicities. The candidate demonstrated effective and durable responses as well as an excellent safety profile in a range of preclinical solid tumor models.

TUB-040 is currently being investigated in a multicenter Phase I/IIa study (NAPISTAR 1-01, NCT06303505) that aims to evaluate the safety, tolerability, pharmacokinetics and efficacy of TUB-040 as a monotherapy in patients with platinum-resistant high-grade ovarian cancer (PROC) or relapsed/refractory adenocarcinoma non-small cell lung cancer (NSCLC), who have exhausted other available treatment options. In June 2024, the U.S. Food
and Drug Administration (“FDA”) granted Fast Track designation to TUB-040 for the treatment of patients with platinum-resistant ovarian cancer.

Tubulis’ antibody-drug conjugate (ADC) candidate TUB-030 is directed against 5T4, a cancer-associated antigen expressed in a wide range of solid tumor indications. It consists of an IgG1 antibody targeting 5T4 connected to the topoisomerase I inhibitor Exatecan through a cleavable linker system based on the company’s proprietary P5 conjugation technology with a homogeneous drug-to-antibody-ratio (DAR) of 8. P5 conjugation is a novel chemistry for cysteine-selective conjugation that enables ADC generation with unprecedented linker stability and superior biophysical properties.

Preclinical pharmacokinetic analysis showed that TUB-030 efficiently delivers its payload to the tumor while reducing off-site toxicities. The candidate demonstrated effective and durable responses, even at lower target expression levels, as well as an excellent safety profile in a range of preclinical solid tumor models.

TUB-030 is currently being investigated in a multicenter Phase I/IIa study (5-STAR 1-01, NCT06657222) that aims to evaluate the safety, tolerability, pharmacokinetics and efficacy of TUB-030 as a monotherapy in patients with advanced solid tumors.