HBW-3210 / Hyperway Pharma - LARVOL DELTA

A Multi-Center Phase I/II Study to Investigate the Safety, Tolerability, Efficacy and Pharmacokinetic of HBW-3210 Capsules in Chinese patients with mature B cell lymphoma (ChiCTR) - P1/2 | N=80 | Recruiting | Sponsor: Beijing Tiantan Hospital, Capital Medical University; Hyperway Pharmaceutical Co.,Ltd.

New P1/2 trial • B Cell Lymphoma • Chronic Lymphocytic Leukemia • Follicular Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology

Phase I clinical study of Bruton's tyrosine kinase inhibitor (BTKi) HBW-3220 capsules in patients with relapsed/refractory (R/R) B-cell non-Hodgkin lymphoma (B-NHL) (AACR 2024) - "Purpose: This clinical study is to evaluate HBW-3220, a novel reversible BTK inhibitor (BTKi) with an improved in vitro profile than the existing non-covalent drugs pirtobrutinib (LOXO-305, approved) and MK-1026 (Phase III). HBW-3220 shows superior inhibition against BTK wild-type and several common mutants, such as C481S, C481R, T474I, T316A, and L528W (the one predominantly enriched in patients resistant to the newer-generation BTKis), and hematopoietic cell kinase (HCK), a key contributor to the development of ibrutinib resistance associated with kinase-defective BTK. This phase I clinical study was conducted in R/R B-NHL patients who had received two or more prior lines of treatments... The current data show that HBW-3220 is well tolerated, showing no DLT occurred at daily doses up to 150 mg, and has good efficacy in patients with CLL/SLL, MZL, and MCL."

Clinical • IO biomarker • P1 data • Chronic Lymphocytic Leukemia • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Leukemia • Lymphoma • Mantle Cell Lymphoma • Marginal Zone Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Small Lymphocytic Lymphoma • HCK

Phase I clinical study of orally-dosed HBW-3220 in patients with relapsed/refractory B-cell lymphoma. (ASCO 2023) - "The current data show that HBW-3220 is well tolerated and of efficacy in patients with B-cell lymphoma. Its clinical PK characteristics support once-a-day administration. Clinical trial information: ChiCTR20221130."

Clinical • P1 data • Chronic Lymphocytic Leukemia • Diffuse Large B Cell Lymphoma • Follicular Lymphoma • Hematological Disorders • Hematological Malignancies • Immunology • Infectious Disease • Leukemia • Lymphoma • Lymphoplasmacytic Lymphoma • Mantle Cell Lymphoma • Marginal Zone Lymphoma • Neutropenia • Non-Hodgkin’s Lymphoma • Oncology • Respiratory Diseases • Small Lymphocytic Lymphoma • Waldenstrom Macroglobulinemia

[VIRTUAL] DISCOVERY OF HBW-3-20, THE FIRST REVERSIBLE INHIBITOR OF BRUTON’S TYROSINE KINASE (BTK) WITH HIGH BRAIN EXPOSURE (EHA 2021) - "Compound tirabrutinib PRN-2246 HBW-3-20 BTK IC50 (nM) 22 2.1 2.5 BTKC481S IC50 (nM) na na 3.8 TMD8 IC50 (nM) 158 29 72 Plasma concentration（ng/mL） 713 387 3457 Brain tissue concentration（ng/mL） 84 16.5 2009 Brain/Plasma Ratio（%） 11.8 4.2 58 Conclusion HBW-3-20 is the first potent reversible BTK inhibitor with superior brain permeability. HBW-3-20 provides a very valuable clinical candidate for treating B-cell malignancies in brain and autoimmune disorders!"

Brain Cancer • CNS Disorders • CNS Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Immunology • Lymphoma • Multiple Sclerosis • Non-Hodgkin’s Lymphoma • Oncology

[VIRTUAL] Discovery of HBW-3-20, the first potent reversible inhibitor of Bruton’s tyrosine kinase (BTK) with high brain exposure. (ASCO 2021) - "In a head-to-head direct comparison of brain exposure experiment, HBW-3-20, tirabrutinib and PRN2246 were all dosed at 10mg/kg orally . HBW-3-20 is the first potent reversible BTK inhibitor that shows promisingly high brain permeability . HBW-3-20 provides a very valuable clinical candidate for treating B-cell malignancies in brain and autoimmune disorders!"

Brain Cancer • CNS Disorders • CNS Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Immunology • Lymphoma • Multiple Sclerosis • Non-Hodgkin’s Lymphoma • Oncology

"Live at #EHA2021 Hyperway's reversible BTK inhibitors HBW-3-20 and HBW-3-10 show superior PK and antitumor effects to comparator compounds in mouse models" (@Cortellis)

Preclinical • Oncology