^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG CLASS:

KDM4 inhibitor

Related drugs:
over1year
A Study to Assess the Safety, Pharmacokinetics, and Antitumor Activity of Oral TACH101 in Participants With Advanced or Metastatic Cancer (clinicaltrials.gov)
P1, N=30, Active, not recruiting, Tachyon Therapeutics, Inc. | Recruiting --> Active, not recruiting | N=70 --> 30
Enrollment closed • Enrollment change • Metastases
|
MSI (Microsatellite instability)
|
zavondemstat (TACH101)
almost2years
Phase classification • Metastases
|
MSI (Microsatellite instability)
|
MSI-H/dMMR
|
zavondemstat (TACH101)
almost3years
TACH101, a first-in-class pan-inhibitor of KDM4 histone demethylase. (PubMed, Anticancer Drugs)
A reduction in the population of tumor-initiating cells was observed following TACH101 treatment. Overall, these observations demonstrate the broad applicability of TACH101 as a potential anticancer agent and support its advancement into clinical trials.
Journal • Epigenetic controller
|
DRD (DNA Repair Deficiency)
|
DDR • DRD
|
zavondemstat (TACH101)
3years
A Study to Assess the Safety, Pharmacokinetics, and Antitumor Activity of Oral TACH101 in Participants With Advanced or Metastatic Cancer (clinicaltrials.gov)
P1a/1b, N=70, Recruiting, Tachyon Therapeutics, Inc. | Not yet recruiting --> Recruiting | Trial completion date: Mar 2024 --> Jul 2025 | Trial primary completion date: Jul 2023 --> Jul 2025
Enrollment open • Trial completion date • Trial primary completion date • Metastases
|
MSI (Microsatellite instability)
|
MSI-H/dMMR
|
zavondemstat (TACH101)
3years
A Study to Assess the Safety, Pharmacokinetics, and Antitumor Activity of Oral TACH101 in Participants With Advanced or Metastatic Cancer (clinicaltrials.gov)
P1a/1b, N=70, Not yet recruiting, Tachyon Therapeutics, Inc. | Phase classification: P1 --> P1a/1b | Trial primary completion date: Nov 2023 --> Jul 2023
Phase classification • Trial primary completion date • Metastases
|
MSI (Microsatellite instability)
|
MSI-H/dMMR
|
zavondemstat (TACH101)
over3years
Targeting KDM4 for treating PAX3-FOXO1-driven alveolar rhabdomyosarcoma. (PubMed, Sci Transl Med)
Combining KDM4 inhibition with cytotoxic chemotherapy led to tumor regression in preclinical PAX3-FOXO1 RMS subcutaneous xenograft models. In summary, we identified a targetable mechanism required for maintenance of the PAX3-FOXO1-related transcription factor network, which may translate to a therapeutic approach for fusion-positive RMS.
Journal
|
KDM4B (Lysine Demethylase 4B) • PAX3 (Paired Box 3)
|
PAX3-FOXO1 fusion
over3years
KDM4 inhibitor SD49-7 attenuates leukemia stem cell via KDM4A/MDM2/p21 axis. (PubMed, Theranostics)
Depletion of KDM4s activated the apoptosis signaling pathway by suppressing MDM2 expression via modulating H3K9me3 levels on the MDM2 promoter region. Our study demonstrates a unique KDM4 inhibitor for LSCs to overcome the resistance to traditional treatment and offers KDM4 inhibition as a promising strategy for resistant leukemia therapy.
Journal
|
MDM2 (E3 ubiquitin protein ligase)
almost4years
Natural product myricetin is a pan-KDM4 inhibitor which with poly lactic-co-glycolic acid formulation effectively targets castration-resistant prostate cancer. (PubMed, J Biomed Sci)
These results suggest that myricetin is a pan-KDM4 inhibitor and exhibited potent cell cytotoxicity toward CRPC cells. Importantly, the combination of PLGA-encapsulated myricetin with enzalutamide is potentially effective for CRPC.
Journal
|
KDM4B (Lysine Demethylase 4B)
|
AR mutation
|
Xtandi (enzalutamide)
4years
Inhibition of histone demethylase KDM4 by ML324 induces apoptosis through the unfolded protein response and Bim upregulation in hepatocellular carcinoma cells. (PubMed, Chem Biol Interact)
Physical binding of KDM4E to Bim and CHOP promoters decreased the response to ML324. Our findings suggest that KDM4 inhibition is a potent anti-tumor therapeutic strategy for human HCC, and further studies of UPR-induced apoptosis and the associated epigenetic functional mechanisms may lead to the discovery of novel target for future cancer therapy.
Journal • Epigenetic controller
|
TCF3 (Transcription Factor 3) • CASP3 (Caspase 3) • TNFRSF10B (TNF Receptor Superfamily Member 10b)
over4years
Enhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer. (PubMed, J Med Chem)
Furthermore, we provide evidence that the inhibitor's cytostatic properties arise from direct intracellular inhibition of KDM4 enzymes. PCa cells treated with the inhibitor exhibit reduced expression of genes regulated by the androgen receptor, an outcome accompanied by epigenetic maintenance of a heterochromatic state.
Journal
|
AR (Androgen receptor)
|
AR expression
over4years
Clinical • New P1 trial
|
MSI (Microsatellite instability)
|
MSI-H/dMMR
|
zavondemstat (TACH101)