TT-01488 / TransThera Biosci - LARVOL DELTA

Preliminary efficacy and safety of TT-01488, a novel, non-covalent, reversible BTK inhibitor, in patients with relapsed/refractory mantle cell lymphoma (ASH 2025) - P1 | "One pt whopreviously received Orelabrutinib and had a BTK C481S mutation achieved CR lasting for over 22 months.Pharmacokinetics (PK) data among MCL pts showed that TT-01488 was rapidly absorbed in plasma with amedian Tmax of 1 h post-dose. TT-01488, a novel, non-covalent, reversible BTK inhibitor, demonstrated promising antitumoractivity and a manageable safety profile in heavily pretreated patients with r/r MCL, including thosepreviously treated with covalent BTK inhibitors and those harboring BTK C481S mutations. The observedoverall response rate of 70% supports its potential clinical benefit in this difficult-to-treat population. PKanalyses showed rapid absorption and sustained BTK inhibition at steady state, indicating favorableexposure and targe engagement."

Clinical • Dyslipidemia • Hematological Malignancies • Hypertriglyceridemia • Lymphoma • Mantle Cell Lymphoma • Non-Hodgkin’s Lymphoma

Phase 1 Study of TT-01488, a Novel, Non-Covalent, Reversible BTK Inhibitor, in Patients with Relapsed or Refractory B-Cell Malignancies (ASH 2024) - P1 | "One pt with MCL who previously received Orelabrutinib and had a BTK C481S mutation achieved CR lasting for over 13 months. Another pt with WM who previously received Ibrutinib achieved PR lasting for over 11 months...Further evaluation of dose and dosing schedule is to provide the DRDE. Clinical trial information : NCT05683717"

Clinical • P1 data • Anemia • B Cell Lymphoma • B Cell Non-Hodgkin Lymphoma • Chronic Lymphocytic Leukemia • Diffuse Large B Cell Lymphoma • Dyslipidemia • Follicular Lymphoma • Hematological Disorders • Hematological Malignancies • Hypertriglyceridemia • Leukemia • Lymphoma • Lymphoplasmacytic Lymphoma • Mantle Cell Lymphoma • Marginal Zone Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Waldenstrom Macroglobulinemia

2024 ASH | TransThera Announces the Phase I Study Results of TT-01488, a Novel Non-Covalent BTK Inhibitor, in Patients with Relapsed or Refractory B-cell Malignancies (PRNewswire) - P1 | N=37 | NCT05683717 | Sponsor: TransThera Sciences (Nanjing), Inc. | "The Phase I study of TT-01488 presented at ASH Annual Meeting was an open, multi-center, dose escalation study. As of the data cut-off date on October 2, 2024, 18 patients with pre-treated B-cell malignancies were enrolled, with the median 3 lines of prior therapies. TT-01488 was well-tolerated in all patients. Neither dose limiting toxicity (DLT) occurred nor any bleeding, atrial flutter or atrial fibrillation was reported. In pharmacokinetics and pharmacodynamics study, sustained pBTK C481S-mutant inhibition covering IC­90 was observed at steady state following multiple dosing at both 150 mg (QD) and 100 mg (BID) dose levels. Among 14 efficacy evaluable patients, objective response rate (ORR) was 57% (8/14), including 3 complete remission (CR) and 5 partial remission (PR). 100% (7/7) of ORR was achieved in mantle cell lymphoma (MCL), Waldenström macroglobulinemia (WM) and marginal zone lymphoma (MZL)."

P1 data • Mantle Cell Lymphoma • Marginal Zone Lymphoma • Waldenstrom Macroglobulinemia

A Phase 1 Study to Evaluate the Safety and Tolerability of TT-01488 in Patients With B-Cell Malignancies (clinicaltrials.gov) - P1 | N=37 | Recruiting | Sponsor: TransThera Sciences (Nanjing), Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Hematological Malignancies • Oncology • CD20

A Phase 1 Study to Evaluate the Safety and Tolerability of TT-01488 in Patients With B-Cell Malignancies (clinicaltrials.gov) - P1 | N=37 | Not yet recruiting | Sponsor: TransThera Sciences (Nanjing), Inc.

New P1 trial • Hematological Malignancies • Oncology • CD20

Study to Evaluate the Safety and Tolerability of TT-01488 in Patients With B-Cell Malignancies (clinicaltrials.gov) - P1 | N=37 | Recruiting | Sponsor: TransThera Sciences (Nanjing), Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Hematological Malignancies • Oncology

Study to Evaluate the Safety and Tolerability of TT-01488 in Patients With B-Cell Malignancies (clinicaltrials.gov) - P1 | N=37 | Not yet recruiting | Sponsor: TransThera Sciences (Nanjing), Inc.

New P1 trial • Hematological Malignancies • Oncology

TransThera Announces that the IND Application of TT-01488, a Non-covalent Reversible BTK Inhibitor, for the Treatment of B-Cell Lymphomas has been Approved by the FDA in the US and Officially Accepted by the NMPA in China (PRNewswire) - "TransThera Sciences...announced that the U.S. Food and Drug Administration ('FDA') approved the Investigational New Drug ('IND') application of TT-01488, a non-covalent reversible Bruton's Tyrosine Kinase ('BTK') inhibitor, for the treatment of B-cell lymphomas on January 24, 2022, and TransThera will initiate the Phase I clinical trials in the U.S. soon. TransThera also announced that China National Medical Products Administration ('NMPA') officially accepted the IND application of TT-01488 for the treatment of B-cell lymphomas on February 14, 2022....'We will actively cooperate with the regulatory authorities to initiate the clinical trials of TT-01488 globally as soon as possible'."

IND • New trial • Hematological Malignancies • Lymphoma • Oncology