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kpg-818

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Overview

NCI Definition [1]:
An orally bioavailable modulator of the E3 ubiquitin ligase complex containing cereblon (CRL4-CRBN E3 ubiquitin ligase), with potential immunomodulating and antineoplastic activities. Upon oral administration, CRL4-CRBN modulator KPG-818 specifically targets and binds to cereblon (CRBN) of the E3 ubiquitin ligase (CRL4-CRBN) complex, thereby affecting the ubiquitin E3 ligase activity, and targeting certain substrate proteins for ubiquitination. This induces proteasome-mediated degradation of certain transcription factors, some of which are transcriptional repressors in T-cells. This leads to modulation of the immune system, including activation of T-lymphocytes, and downregulation of the activity of other proteins, some of which play key roles in the proliferation of certain cancer cell types. CRBN, the substrate recognition component of the CRL4-CRBN E3 ubiquitin ligase complex, plays a key role in the ubiquitination of certain proteins.

Clinical Trials

View Clinical Trials for kpg-818

Kpg-818 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating kpg-818, 1 is phase 1 (1 open).

Adult T-cell leukemia/lymphoma, chronic lymphocytic leukemia, and diffuse large B-cell lymphoma are the most common diseases being investigated in kpg-818 clinical trials [2].

Drug Details

Synonyms [2]:
kpg818, kpg 818, crbn e3 ubiquitin ligase complex crl4-crbn modulator kpg-818, crl4-crbn modulator kpg-818, cereblon e3 ubiquitin ligase modulating agent kpg-818
Drug Target(s) [2]:
CRBN
NCIT ID [1]:
C175979

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.