Hezheng Pharma and Johnson & Johnson Enter Global License Agreement to Co-Develop Best-in-Class BTK Degrader HZ-Q1070
HealZen Therapeutics
Innovative Small-Molecule Drug Developer
Johnson & Johnson
Medical Device R&D and Manufacturer
On January 10, HealZen Therapeutics and Shanghai Institute of Materia Medica jointly announcedJohnson & JohnsonSign Global Licensing Agreement to DevelopPotential Best BTK Degrader, used to treat a variety of diseases.Currently, HealZen Therapeutics has 2 targeted therapiesPROTAC molecules for BTK under research, respectively HZ-Q1070(Phase I)And HZ-Q1060(Preclinical)。
2023At the AACR Annual MeetingHealZen TherapeuticsFirst Oral Presentation of the New BTKDegradantHZ-Q1070 Preclinical data.HZ-Q1070 isA Novel, Potent, High Bioavailability, and Highly Selective BTK Degrader:
To BTKWTDC in China50 As low as picomolar level, with potent anti-tumor proliferation inhibitory activity against different lymphoma cells; For multiple mutant BTK proteins（C481S、C481Y、C481F、T474M）HasPotent Degradation Activity, and strongly inhibit the BTK-C481S mutant cell line; Complete inhibition of tumor growth in multiple transplantable tumor models(Including BTK-C481S mutation model)； Solved the PROTAC molecule drug-likeness problem, with good oral bioavailability across species and in vivo.Degradation >90% BTK protein sustained for over 24 hours； Preclinical toxicology studies showed good safety.
At the 2024 ASH Conference,HealZen Therapeutics Co., Ltd. announcedHZ-Q1070 TheFirst-in-Human Phase I Study Data（CTR20240471）. The main objective of this study is to evaluateHZ-Q1070 in Patients with Relapsed or Refractory B-cell MalignanciesSafety and tolerability, and determine the maximum tolerated dose(MTD)And Phase II Clinical Recommended Dose(RP2D)。
As of May 3, 2024, there were 2 patients enrolled in the first 25 mg dose group, all treatment-related adverse events（TRAEs）All were grade 1. No dose-limiting toxicity was observed.（DLT）Pharmacokinetic data showed satisfactory results. Pharmacodynamic data showed that the degradation rate of BTK protein in peripheral blood mononuclear cells exceeded 95%.
Insight database shows that globally, there are 24 PROTAC molecules targeting BTK, with 12 produced in China, accounting for half. Three of them have entered the clinical stage, respectively.BeiGene BGB-16673（Phase I/II）、HealZen TherapeuticsHZ-Q1070 (Phase I) andHaiscoHSK29116 (Phase I).
