On January 10, HealZen Therapeutics/Shanghai Institute of Materia Medica jointly announced a global licensing agreement with Johnson & Johnson to develop a best-in-class BTK degrader for the treatment of various diseases.HealZen Therapeutics is a clinical-stage small molecule innovative drug discovery and development company driven by innovation technology, dedicated to addressing unmet clinical needs.DaTProD®The platform can be used to develop new protein degradation drugs with differentiated advantages, explore undruggable targets, and shorten the R&D time of TPD drugs through a mature and efficient workflow:- Proteomics+ engine: Based on multi-omics target and ligand discovery technology, accelerating the exploration of new targets and new ligands;
- DaELF+ engine: Based on multiple drug-like dimensions, several unique ELF (E3 ligand-linker) libraries have been established;
AI+ Engine: Based on artificial intelligence algorithms, predict the binding mode, degradation capability, and pharmacokinetic properties of TPD molecules.
The official website shows that HealZen Therapeutics focuses on drug development in the fields of oncology, autoimmune diseases, and central nervous system disorders. It has previously reached strategic cooperation with multiple companies in China. The BTK degrader in the company’s R&D pipeline is HZ-Q1070, a PROTAC molecule targeting BTK for the treatment of hematologic tumors and autoimmune diseases, currently in Phase I clinical trials.
HealZen Therapeutics' R&D Pipeline (Source: Company Website)
In April 2023, HealZen Therapeutics presented the preclinical data of HZ-Q1070 at AACR. HZ-Q1070 targets BTKWTDC in China50As low as picomolar level, it exhibits potent anti-tumor proliferation inhibitory activity against different lymphoma cells; demonstrates strong degradation activity against various mutant BTK proteins (C481S, C481Y, C481F, T474M) and effectively inhibits cell lines with the BTK-C481S mutation; completely suppresses tumor growth in multiple xenograft models (including the BTK-C481S mutation model); resolves the drug-likeness challenges of PROTAC molecules, showing good oral bioavailability across species and degrading >90% of BTK protein in vivo for over 24 hours; preclinical toxicology studies indicate good safety.In November 2024, HealZen Therapeutics presented the first-in-human Phase I study results of HZ-Q1070 in patients with relapsed or refractory B-cell malignancies at ASH. As of May 3, 2024, two patients were enrolled in the first 25mg dose cohort, and all treatment-related adverse events (TRAEs) were grade 1. No dose-limiting toxicity (DLT) was observed, and pharmacokinetic data showed satisfactory results. Pharmacodynamic results demonstrated that the degradation rate of BTK protein in peripheral blood mononuclear cells exceeded 95%.PharmaCube NextPharma®The database shows that more than ten companies have laid out BTK PROTAC, including representative companies such as BeiGene, Nurix Therapeutics, Haisco,HealZen Therapeuticsetc., HealZen Therapeutics' HZ-Q1070 ranks 4th out of 15 globally and 3rd out of 15 in China in this field.
Global R&D Status of BTK PROTAC Track (Source: PharmaCube NextPharma)®Database）
"HealZen Therapeutics CEO and co-founder Stella Zhou expressed: 'We are delighted to collaborate with Johnson & Johnson to accelerate the development of BTK degraders. We look forward to bringing new treatment options to patients and jointly achieving the goal of rapidly developing breakthrough therapies.'"References:
[1]http://cn.healzentx.com/
[2]https://ashpublications.org/blood/article/144/Supplement%201/6286/528082/Preclinical-and-First-in-Human-Phase-I-Study-of
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