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DRUG CLASS:

HDAC2 inhibitor

3d
Venetoclax and Azacitidine Combined With Chidamide (VAC) for the Treatment of Newly Diagnosed Acute Monocytic Leukemia (clinicaltrials.gov)
P2, N=92, Recruiting, The First Affiliated Hospital of Soochow University | Trial primary completion date: Sep 2024 --> Sep 2025
Trial primary completion date
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BCL2 (B-cell CLL/lymphoma 2)
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Venclexta (venetoclax) • azacitidine • Epidaza (chidamide)
4d
Entinostat treatment causes hypophosphatemia and hypocalcemia by increasing Fgf23 in mice. (PubMed, Biochem Biophys Res Commun)
Meanwhile, Entinostat treatment increased the serum level of the active form (intact) Fgf23 and reduced that of Pi and calcium (Ca) as well. This study raised a concern about the anabolic effects of Entinostat in bone, and demonstrated that Entinostat treatment causes hypophosphatemia and hypocalcemia by upregulating Fgf23 mRNA and increasing intact Fgf23 protein in serum.
Preclinical • Journal
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CTSK (Cathepsin K) • FGF23 (Fibroblast Growth Factor 23) • RUNX2 (RUNX Family Transcription Factor 2)
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Jingzhuda (entinostat)
4d
RLC Followed by CR-CHOP in Elderly Patients with Newly-diagnosed DEL (clinicaltrials.gov)
P2, N=44, Recruiting, Zhejiang Cancer Hospital | Not yet recruiting --> Recruiting
Enrollment open
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Rituxan (rituximab) • lenalidomide • cyclophosphamide • epirubicin • Epidaza (chidamide) • vindesine
5d
Discovery of Novel 5-Cyano-3-phenylindole-Based LSD1/HDAC Dual Inhibitors for Colorectal Cancer Treatment. (PubMed, J Med Chem)
Compound 20c effectively modulated the expression of biomarkers associated with LSD1 and HDAC inhibition and demonstrated superior antiproliferative activity compared to SAHA and 4SC-202 across multiple colorectal cancer cell lines...It demonstrated significantly enhanced antitumor efficacy compared to SAHA, without causing observable toxicity. These findings highlight the potential of LSD1/HDAC dual inhibitors for the treatment of malignant cancers.
Journal
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HDAC1 (Histone Deacetylase 1)
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Zolinza (vorinostat) • domatinostat (4SC-202)
10d
Sincerely20: Sintilimab Combined With Chidamide in Treating Peripheral T Cell Lymphoma (clinicaltrials.gov)
P2, N=51, Recruiting, Fudan University | Trial completion date: Sep 2025 --> Dec 2026 | Trial primary completion date: Dec 2023 --> Dec 2026
Trial completion date • Trial primary completion date • IO biomarker • Epigenetic controller
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PD-L1 expression
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Tyvyt (sintilimab) • Epidaza (chidamide)
12d
Prospective, open-label, phase II clinical study of the combination of Chidamide and Anlotinib ± PD-1/PD-L1 inhibitors in patients with SWI/SNF complex-deficient mutations (ChiCTR2400090522)
P2, N=57, Recruiting, Cancer Hospital Chinese Academy of Medical Sciences; Cancer Hospital Chinese Academy of Medical Sciences
New P2 trial • IO biomarker
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ARID1A (AT-rich interaction domain 1A) • SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1) • SMARCA2 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily A, Member 2)
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Focus V (anlotinib) • Epidaza (chidamide)
12d
New P2 trial • Combination therapy • Metastases
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EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase)
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EGFR mutation • ALK fusion
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gemcitabine • Epidaza (chidamide) • Ariely (adebrelimab)
12d
New P2 trial • Combination therapy • Metastases
|
Focus V (anlotinib) • Loqtorzi (toripalimab-tpzi) • Epidaza (chidamide)
12d
New P2 trial • Combination therapy • Metastases
|
HER-2 (Human epidermal growth factor receptor 2)
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HER-2 negative
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capecitabine • vinorelbine tartrate • Epidaza (chidamide)
17d
New P2 trial
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Rituxan (rituximab) • lenalidomide • cyclophosphamide • epirubicin • Epidaza (chidamide) • vindesine
18d
Real-world efficacy of chidamide plus R-CHOP in newly diagnosed double-expressor diffuse large B-cell lymphoma. (PubMed, Ther Adv Hematol)
To evaluate the efficacy of a novel histone deacetylase inhibitor, chidamide, in combination with rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisone (CR-CHOP) in the treatment of DEL. The most common grades 3-4 hematologic and nonhematologic toxicity were leukopenia (46.7%) and infection (21%), respectively. This long-term follow-up study indicates that CR-CHOP in untreated DLBCL with the DEL phenotype demonstrates high short-term efficacy and safety as well as promising survival outcomes.
Journal • Real-world evidence • IO biomarker • Real-world effectiveness • Real-world
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • BCL2 (B-cell CLL/lymphoma 2)
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BCL2 expression • MYC expression
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Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • vincristine • prednisone • Epidaza (chidamide)
18d
New trial
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Epidaza (chidamide) • Folotyn (pralatrexate)
22d
Chidamide Combined with (+) -JQ-1 to Kill MLL-Rearrangement Acute Myeloid Leukemia Cells by Disrupting the DNA Damage Response Pathway (PubMed, Zhongguo Shi Yan Xue Ye Xue Za Zhi)
Chidamide combined with (+)-JQ-1 can inhibit the proliferation of MLL-r AML cells, inhibit the initiation of protective self-repair of these leukemia cells by inhibiting the DNA damage response pathway, and ultimately increase the apoptosis of these cells, but non- MLL-r AML cells have no similar results.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • KMT2A (Lysine Methyltransferase 2A) • CHEK2 (Checkpoint kinase 2) • RAD51 (RAD51 Homolog A) • CHEK1 (Checkpoint kinase 1) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • BRD4 (Bromodomain Containing 4) • TP53BP1 (Tumor Protein P53 Binding Protein 1)
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MLL rearrangement • MLL rearrangement • BCL2 expression • BAX expression
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JQ-1 • Epidaza (chidamide)
22d
Phase I Study of WJ47156 Monotherarpy and in Combination With Other Therapy in Advanced Solid Tumors (clinicaltrials.gov)
P1, N=93, Recruiting, Shanghai Junshi Bioscience Co., Ltd. | Not yet recruiting --> Recruiting
Enrollment open • Combination therapy • Metastases
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Avastin (bevacizumab) • Loqtorzi (toripalimab-tpzi)
29d
Chidamide triggers pyroptosis in T-cell lymphoblastic lymphoma/leukemia via the FOXO1/GSDME axis. (PubMed, Chin Med J (Engl))
Our study suggested that chidamide exerts an antitumor effect on T-LBL/ALL and promotes a more inflammatory form of cell death via the FOXO1/GSDME axis, which provides a novel choice of targeted therapy for patients with T-LBL/ALL.
Journal
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CASP3 (Caspase 3) • FOXO1 (Forkhead box O1) • HDAC2 (Histone deacetylase 2) • HDAC1 (Histone Deacetylase 1) • GSDME (Gasdermin E) • HDAC3 (Histone Deacetylase 3)
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Epidaza (chidamide)
30d
Combining ERAP1 silencing and entinostat therapy to overcome resistance to cancer immunotherapy in neuroblastoma. (PubMed, J Exp Clin Cancer Res)
These findings demonstrate that ERAP1 inhibition combined with HDACi entinostat treatment and PD-1 blockade remodels the immune landscape of a non-immunogenic tumor such as NB, making it responsive to checkpoint immunotherapy.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • CD8 (cluster of differentiation 8) • MYCN (MYCN Proto-Oncogene BHLH Transcription Factor) • CD4 (CD4 Molecule) • CASP3 (Caspase 3) • ERAP1 (Endoplasmic Reticulum Aminopeptidase 1) • CASP7 (Caspase 7)
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Jingzhuda (entinostat)
30d
R-ICE+X: Novel Targeted Drugs Combined With R-ICE Regimen in Relapsed and Refractory Diffuse Large B-cell Lymphoma (clinicaltrials.gov)
P2, N=76, Recruiting, Ruijin Hospital | Trial primary completion date: Jun 2024 --> Jun 2025
Trial primary completion date
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carboplatin • Brukinsa (zanubrutinib) • decitabine • Epidaza (chidamide) • pomalidomide • tofacitinib
1m
New trial
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BCL2 (B-cell CLL/lymphoma 2)
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Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • vincristine • prednisone • Epidaza (chidamide)
1m
NUSAP1 is Upregulated by Estrogen to Promote Lung Adenocarcinoma Growth and Serves as a Therapeutic Target. (PubMed, Int J Biol Sci)
In this study, by conducting bioinformatics analyses as well as in vitro and in vivo experiments, we identified that NUSAP1 was significantly upregulated in LUAD, with a notable correlation with poorer overall survival, higher scores for immunogenicity and immune infiltration, as well as increased sensitivity to conventional chemotherapeutic drugs such as paclitaxel, docetaxel and vinorelbine in LUAD. Furthermore, we identified entinostat as a novel inhibitor of NUSAP1. Pharmacological targeting ERβ/NUSAP1 axis with fulvestrant (ERβ antagonist) or entinostat (novel NUSAP1 inhibitor) significantly reduced LUAD growth both in vitro and in vivo, which may represent effective alternative therapeutic strategies for patients with LUAD.
Journal
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NUSAP1 (Nucleolar and Spindle Associated Protein 1)
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NUSAP1 overexpression
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paclitaxel • docetaxel • fulvestrant • vinorelbine tartrate • Jingzhuda (entinostat)
1m
Triple Combination of Entinostat, a Bromodomain Inhibitor, and Cisplatin Is a Promising Treatment Option for Bladder Cancer. (PubMed, Cancers (Basel))
The triple combination of entinostat, a BETi, and cisplatin is highly synergistic, reverses cisplatin resistance, and may thus serve as a novel therapeutic approach for bladder cancer.
Journal
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CDKN1A (Cyclin-dependent kinase inhibitor 1A)
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cisplatin • JQ-1 • birabresib (OTX015) • Jingzhuda (entinostat)
1m
Design, Synthesis, and Biological Evaluation of HDAC Inhibitors Containing Natural Product-Inspired N-Linked 2-Acetylpyrrole Cap. (PubMed, Molecules)
Among them, compound 20 exhibited potential inhibitory activity on HDAC1, and demonstrated notable potency against RPMI-8226 cells with an IC50 value of 2.89 ± 0.43 μM, which was better than chidamide (IC50 = 10.23 ± 1.02 μM)...The ADME parameters calculation showed that 20 possesses remarkable theoretical drug-likeness properties. Taken together, these results suggested that 20 is worthy of further exploration as a potential HDAC-targeted anticancer drug candidate.
Journal
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HDAC1 (Histone Deacetylase 1) • ANXA5 (Annexin A5)
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Epidaza (chidamide)
1m
New P2 trial • Metastases
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Epidaza (chidamide) • Yidafan (ivonescimab)
1m
Novel dual inhibitor targeting CDC25 and HDAC for treating triple-negative breast cancer. (PubMed, Apoptosis)
18A possessed similar HDAC inhibitory activity as MS-275 and potently suppressed CDC25 activity in vitro and the CDK1 dephosphorylation in cells. Additionally, 18A hindered the progression of S and G2/M phases, triggered DNA damage, and induced apoptosis. These findings underscore the potential of 18A as a targeted therapy for TNBC and warrants further preclinical development.
Journal
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CDK1 (Cyclin-dependent kinase 1) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1)
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Jingzhuda (entinostat)
1m
Transcriptional repression by HDAC3 mediates T cell exclusion from Kras mutant lung tumors. (PubMed, Proc Natl Acad Sci U S A)
Finally, we showed that T cells contribute to in vivo tumor growth control in the presence of entinostat and trametinib combination treatment. Together, our findings reveal that HDAC3 is a druggable endogenous repressor of T cell recruitment into Kras mutant lung tumors.
Journal
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KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • STK11 (Serine/threonine kinase 11) • CXCL10 (Chemokine (C-X-C motif) ligand 10) • HDAC3 (Histone Deacetylase 3)
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KRAS mutation • CXCL10 expression
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Mekinist (trametinib) • Jingzhuda (entinostat)
1m
Developing new drugs for adult T-cell leukemia/lymphoma by targeting hypoxia: insights from toxicity of MS-275 and its analogs. (PubMed, J Chemother)
Results of alamarBlue assay demonstrated that MS-275 and analogs significantly (p < 0.001) reduced viability of MT-2 cells in hypoxic condition. Findings of the present study hold promise for developing new drugs targeting hypoxia-induced changes in ATL.
Journal
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PD-L1 (Programmed death ligand 1) • HIF1A (Hypoxia inducible factor 1, alpha subunit)
|
HIF1A overexpression • HIF1A expression
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Jingzhuda (entinostat)
2ms
Hydrazide-Based Class I Selective HDAC Inhibitors Completely Reverse Chemoresistance Synergistically in Platinum-Resistant Solid Cancer Cells. (PubMed, J Med Chem)
Moreover, the hydrazide derivatives 5 and 6 showed strong synergism with cisplatin (combination indices <0.2), again outperforming entinostat, and increased DNA damage, p21, and pro-apoptotic BIM expression, leading to caspase-mediated apoptosis and cell death. Thus, compounds 5 and 6 represent promising lead structures for developing new HDACi capable of reversing chemoresistance in cisplatin resistant cancer cells.
Journal
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BCL2L11 (BCL2 Like 11) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
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cisplatin • Jingzhuda (entinostat)
2ms
Venetoclax Combining Chidamide and Azacitidine (VCA) in the Treatment of R/R AML (clinicaltrials.gov)
P2, N=30, Recruiting, The First Affiliated Hospital of Xiamen University | Trial completion date: Jan 2026 --> Jun 2027 | Trial primary completion date: Jan 2024 --> Jan 2026
Trial completion date • Trial primary completion date
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Venclexta (venetoclax) • azacitidine • Epidaza (chidamide)
2ms
Efficacy and Safety of Oral HBI-8000 in Patients With Relapsed or Refractory Peripheral T-cell Lymphoma (PTCL) (clinicaltrials.gov)
P2, N=55, Completed, HUYABIO International, LLC. | Phase classification: P2b --> P2 | N=40 --> 55
Phase classification • Enrollment change
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Epidaza (chidamide)
2ms
Chidamide, Venetoclax, and Azacitidine for Newly Diagnosed Acute Myeloid Leukemia (clinicaltrials.gov)
P=N/A, N=184, Recruiting, Institute of Hematology & Blood Diseases Hospital, China | Not yet recruiting --> Recruiting
Enrollment open
|
Venclexta (venetoclax) • azacitidine • Epidaza (chidamide)
2ms
New trial • Metastases
|
AiRuiKa (camrelizumab) • albumin-bound paclitaxel • Epidaza (chidamide) • Teysuno (gimeracil/oteracil/tegafur)
2ms
New P2 trial • Metastases
|
gemcitabine • oxaliplatin • Epidaza (chidamide) • Kaitanni (cadonilimab)
2ms
Adebrelimab and Chidamide plus Gemcitabine as first-line treatment for advanced and metastatic pancreatic cancer patients (P-reCise/SCOG-P001): An exploratory, phase 2 trial. (ChiCTR2400079609)
P2, N=32, Recruiting, First affiliated hospital of Soochow university; First affiliated hospital of Soochow university | Not yet recruiting --> Recruiting | Phase classification: PN/A --> P2 | N=90 --> 32 | Initiation date: Jan 2024 --> Aug 2024
Enrollment open • Phase classification • Enrollment change • Trial initiation date • Metastases
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gemcitabine • Epidaza (chidamide) • Ariely (adebrelimab)
2ms
Identification of Entinostat as a Novel Modifier of STAT3 Pre-mRNA Alternative Splicing. (PubMed, Biol Pharm Bull)
Our findings demonstrate that alternative splicing of STAT3 can be regulated by a compound, providing an important clue for understanding the regulation mechanisms of the expression balance of STAT3 isoforms in a chemical biology approach. Entinostat is likely to be a promising seed compound for elucidating how the higher ratio of STAT3β expression impacts on biological responses associated with Janus kinase (JAK)/STAT3 signaling pathway.
Journal
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STAT3 (Signal Transducer And Activator Of Transcription 3)
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STAT3 expression
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Jingzhuda (entinostat)
2ms
Trial completion date • IO biomarker • Surgery • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • CD86 (CD86 Molecule)
|
HR positive • HER-2 negative
|
Opdivo (nivolumab) • Yervoy (ipilimumab) • Jingzhuda (entinostat) • ABP 206 (nivolumab biosimilar)
2ms
Efficacy and Safety of Oral HBI-8000 in Patients With Relapsed or Refractory Adult T Cell Lymphoma (ATL) (clinicaltrials.gov)
P2, N=23, Completed, HUYABIO International, LLC. | Phase classification: P2b --> P2
Phase classification
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Epidaza (chidamide)
2ms
Cancer-Associated Fibroblasts Expressing Sulfatase 1 Facilitate VEGFA-Dependent Microenvironmental Remodeling to Support Colorectal Cancer. (PubMed, Cancer Res)
Importantly, tumor growth inhibition by HDAC inhibition was dependent on SULF1 expression in CAFs, and CRC patients with more SULF1+ CAFs were more responsive to treatment with the HDAC inhibitor chidamide. Collectively, these findings unveil the critical role of SULF1+ CAFs in CRC and provide a strategy to stratify CRC patients for HDAC inhibitor treatment.
Journal
|
VEGFA (Vascular endothelial growth factor A)
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Epidaza (chidamide)
3ms
Alteration in folate carrier expression via histone deacetylase inhibition in BeWo human placental choriocarcinoma cells. (PubMed, Toxicol In Vitro)
FOLR1 expression was upregulated by VPA, apicidin, and trichostatin A, but downregulated by MS-275 after 24 h treatment. By contrast, HDAC inhibitors exert different regulatory effects on folate carriers. Moreover, HDAC1/2 inhibition may be a potential mechanism involved in altering FOLR1 and SLC46A1 levels.
Journal • Epigenetic controller
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FOLR1 ( Folate receptor alpha ) • SLC19A1 (Solute Carrier Family 19 Member 1)
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FOLR1 expression
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Jingzhuda (entinostat) • trichostatin A (VTR-297)
3ms
Chidamide maintenance therapy after allo-HSCT in SET-NUP214 fusion positive T-ALL patients: A report of two cases. (PubMed, Transpl Immunol)
Here we report chidamide maintenance therapy after allo-HSCT in patients with SET-NUP214 fusion positive T-ALL. Both patients improved effectively during follow-up, confirming the efficacy of chidamide in improving the condition of these patients and may provide valuable clinical information for the treatment of this rare and understudied disease.
Journal
|
NUP214 (Nucleoporin 214)
|
SET-NUP214 fusion
|
Epidaza (chidamide)
3ms
Study of Entinostat With Nivolumab Plus Ipilimumab in Previously Treated Renal Cell Carcinoma (clinicaltrials.gov)
P2, N=12, Terminated, Roberto Pili | N=18 --> 12 | Trial completion date: Aug 2023 --> Feb 2024 | Active, not recruiting --> Terminated; Funder halted development of compound in this disease
Enrollment change • Trial completion date • Trial termination • Combination therapy
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Opdivo (nivolumab) • Yervoy (ipilimumab) • Jingzhuda (entinostat)
3ms
Entinostat in Combination With Aldesleukin in Treating Patients With Metastatic Kidney Cancer (clinicaltrials.gov)
P1/2, N=47, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Jul 2024 --> Jul 2025
Trial completion date • Combination therapy • Epigenetic controller • Metastases
|
mTOR (Mechanistic target of rapamycin kinase)
|
Jingzhuda (entinostat) • Proleukin (aldesleukin)
3ms
Glofitamab Combination With Chidamide in Patients With Recurrent/Refractory DLBCL (clinicaltrials.gov)
P2, N=22, Not yet recruiting, Tianjin Medical University Cancer Institute and Hospital
New P2 trial
|
Epidaza (chidamide) • Columvi (glofitamab-gxbm)
3ms
Enrollment change • IO biomarker
|
PD-1 (Programmed cell death 1)
|
decitabine • Adcetris (brentuximab vedotin) • Epidaza (chidamide)