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Finishingrainbow
Today, the latest announcement by CDE shows that the clinical trial application of BeiGene BTK protein degradation agent BGB-16673 film-coated tablets has been accepted
.
Screenshot from CDE official website
As early as August of this year, China Baiji in the American Society of Clinical Network (ClinicalTrials.
gov) Registration targeting BTK degradation agent BGB-16673, indications include B-cell lymphoma, marginal zone lymphoma, follicular lymphoma
.
This is BeiGene's first product under development based on its protein-degrading CDAC (innovative PROTAC) platform and entering the clinical stage.
CDAC technology platform (Source: BeiGene)
PROTAC technology is an emerging direction for drug research and development.
Unlike traditional drugs that block proteins, PROTAC combines two ligands with the target protein and ubiquitin E3 ligase simultaneously to form a stable target protein-PROTAC-E3 ligase ternary The complex, which induces ubiquitination and degradation by the proteasome, is expected to break through the non-drugable protein target
.
In addition to BTK targets, Baekje also targets tyrosine kinase receptors (for lung cancer), cyclins (for hematoma), apoptosis-related proteins (hematoma and solid tumors), and TLR signaling pathways (hematoma and tumor immunity) Therapeutics), cytokines (hematoma and tumor immunotherapy), epigenetics (hematoma) and other targets are deployed in a wide range of early CDAC projects, and follow-up progress can be expected
.
BeiGene CDAC technology platform project layout (Source: BeiGene)
Arvinas is a cutting-edge company in PROTAC technology worldwide
.
At present, the company has two PROTAC drugs into clinical phase II, namely ARV-110 targeting the androgen receptor (AR) and ARV-471 targeting the estrogen receptor (ER)
ARV-110 and ARV-471 (Source: Arvinas)
In addition to BeiGene, Fendi Technology, Hejing Pharmaceutical, Haichuang Pharmaceutical, and Lingke Pharmaceutical, besides BeiGene, the current domestic deployment of PROTAC technology
.
Among them, the PROTAC drugs with the highest clinical progress include HSK29116 from Haisco and GT20029 from Kaifeng Pharmaceutical
Haisco’s HSK29116 is an oral BTK-PROTAC small molecule anti-tumor drug screened based on the PROTAC R&D platform.
On the one hand, it can directly inhibit BKT activity by specifically binding BTK; on the other hand, it can induce BTK ubiquitination labeling through the proteasome pathway.
It is degraded, thereby blocking the transmission of the BCR signal pathway, inhibiting the growth and proliferation of B-cell lymphoma cells, and exerting a dual anti-tumor effect
.
In April 2021, HSK29116 has launched an international multi-center phase I clinical trial.
The GT20029 of Kaifeng Pharmaceutical is an AR degradation agent that degrades AR protein.
It is the world's first external AR-PROTAC.
Its indications are androgenetic alopecia and acne
.
The mechanism of action of GT20029 is to recruit AR protein to E3 ubiquitin ligase for degradation.
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