2024 ASH： TransThera Reports Phase I Results for TT-01488, a New BTK Inhibitor, in Relapsed-Refractory B-cell Malignancies

NANJING, China and GAITHERSBURG, Md., Dec. 10, 2024 /PRNewswire/ -- TransThera Sciences (Nanjing), Inc. ("TransThera"), a company in the clinical registrational stage that centers on creating innovative small molecule drugs for cancer, inflammation, and heart-related metabolic disorders, has announced its poster presentation at the 2024 American Society of Hematology (ASH) Annual Meeting. This presentation will address the phase I research findings of TT-01488, a groundbreaking reversible BTK inhibitor aimed at patients with relapsed or refractory B-cell cancers.

 

Bruton's tyrosine kinase (BTK) is integral to the B-cell receptor signaling pathway and acts as a key regulator in cell growth and survival across various B-cell cancers. Presently, five irreversible BTK inhibitors (BTKis) have received approval globally. However, mutations at the covalent binding site (C481S) of these inhibitors necessitate the development of next-gen BTKi to counter resistance.

 

TT-01488 is a cutting-edge, reversible BTKi with non-covalent binding properties designed to tackle resistance seen in irreversible BTKis. Preclinical trials demonstrate TT-01488's strong capability to inhibit both the wildtype BTK and the C481S mutation.

 

The Phase I trial for TT-01488 shared at the ASH meeting was an open-label, multi-site, dose-escalation study. By the cut-off date on October 2, 2024, 18 individuals previously treated for B-cell malignancies were part of the study, having undergone a median of three prior therapies. TT-01488 was well accepted across all trial participants, showing no dose-limiting toxicities (DLT) or reports of bleeding, atrial flutter, or atrial fibrillation. In the pharmacokinetic and pharmacodynamic evaluations, persistent inhibition of pBTK C481S-mutant beyond IC­90 was seen with regular dosing at 150 mg once daily (QD) and 100 mg twice daily (BID). Of the 14 participants whose efficacy was assessable, the objective response rate (ORR) was 57% (8/14), including three complete remissions (CR) and five partial remissions (PR). A 100% ORR rate (7/7) was noted in mantle cell lymphoma (MCL), Waldenström macroglobulinemia (WM), and marginal zone lymphoma (MZL). Overall, TT-01488 provided promising results in B-cell non-Hodgkin lymphoma (B-NHL) patients, independently of C481S mutation status and prior cBTKi treatment.

 

About TT-01488
TT-01488 is a self-developed, non-covalent, reversible BTK inhibitor designed to counter acquired resistance to approved covalent BTK inhibitors in a range of relapsed or refractory blood cancers. Its potent action against both wild type and mutated BTK, coupled with high selectivity over EGFR and Tec, indicates substantial potential for efficacy and safety.

 

About TransThera
TransThera is a biopharmaceutical company focused on clinical needs, operating in the registrational clinical stage, committed to discovering and developing innovative small molecule therapies for oncological, inflammatory, and cardiometabolic conditions. With deep insights from translational medicine and drug design, TransThera aims to develop pioneering or superior drug candidates strategically designed to meet urgent global clinical demands. For more details, please visit

 

Forward-looking statements
This announcement includes forward-looking statements that involve risks, uncertainties, and assumptions. If such risks or uncertainties arise or assumptions prove incorrect, actual outcomes could differ significantly from those anticipated or implied by the forward-looking statements. All statements aside from historical facts may be considered forward-looking, including, but not limited to, management’s future operational plans, strategies, objectives, potential markets, product developments, and other related items or assumptions mentioned.

 

SOURCE TransThera Sciences (Nanjing) Inc.

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