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DRUG CLASS:

MAPK inhibitor

2d
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)
4d
New P2 trial • Combination therapy • Metastases
|
EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase)
|
EGFR mutation • ALK fusion
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gemcitabine • Epidaza (chidamide) • Ariely (adebrelimab)
4d
New P2 trial • Combination therapy • Metastases
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 negative
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capecitabine • vinorelbine tartrate • Epidaza (chidamide)
4d
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)
4d
New P2 trial • Combination therapy • Metastases
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Focus V (anlotinib) • Loqtorzi (toripalimab-tpzi) • Epidaza (chidamide)
10d
New P2 trial
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Rituxan (rituximab) • lenalidomide • cyclophosphamide • epirubicin • Epidaza (chidamide) • vindesine
10d
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)
10d
New trial
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Epidaza (chidamide) • Folotyn (pralatrexate)
14d
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)
19d
EXPRESS: Combined treatment with ruxolitinib and MK-2206 inhibits ERα activity by inhibiting MAPK signaling in BT474 breast cancer cells. (PubMed, J Investig Med)
Our results revealed the relationships among the ERα, PI3K/AKT, and MAPK signaling pathways in ER+ breast cancer cells. Understanding the interactions among ERα, PI3K-AKT-mTOR, and MAPK could lead to novel combination therapies.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • JAK1 (Janus Kinase 1)
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Jakafi (ruxolitinib) • MK-2206
21d
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)
22d
Stromal reprogramming overcomes resistance to RAS-MAPK inhibition to improve pancreas cancer responses to cytotoxic and immune therapy. (PubMed, Sci Transl Med)
Concomitant inhibition of both FAK (with VS-4718) and rapidly accelerated fibrosarcoma and MAPK kinase (RAF-MEK) (with avutometinib) induced tumor growth inhibition and increased survival across multiple PDAC mouse models. Combination of FAK and RAF-MEK inhibition alone improved antitumor immunity and priming of T cell responses in response to chemotherapy. These findings provided the rationale for an ongoing clinical trial evaluating the efficacy of avutometinib and defactinib in combination with gemcitabine and nab-paclitaxel in patients with PDAC and may suggest further paths for combined stromal and tumor-targeting therapies.
Journal • Stroma
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KRAS (KRAS proto-oncogene GTPase) • MYC (V-myc avian myelocytomatosis viral oncogene homolog)
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KRAS mutation
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gemcitabine • albumin-bound paclitaxel • avutometinib (VS-6766) • defactinib (VS-6063) • VS-4718
23d
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
24d
New trial
|
BCL2 (B-cell CLL/lymphoma 2)
|
Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • vincristine • prednisone • Epidaza (chidamide)
28d
Dual MAPK Inhibition Triggers Pro-inflammatory Signals and Sensitizes BRAF V600E Glioma to T Cell-Mediated Checkpoint Therapy. (PubMed, bioRxiv)
Using patient tumor tissue before and after BRAFi+MEKi, two novel syngeneic murine models of BRAF V600E HGG, and patient-derived cell lines, we examined the effects of clinically relevant BRAFi+MEKi with dabrafenib and trametinib on tumor growth, cell states, and tumor-infiltrating T cells. The quadruple treatment overcame BRAFi+MEKi resistance by invigorating T cell-mediated anti-tumor immunity in murine BRAF V600E HGG. PD-L1 expression was elevated in human BRAF-mutant versus BRAF-wildtype glioblastoma clinical specimen, complementing experimental findings and suggesting translational relevance for patient care.
Journal • PD(L)-1 Biomarker • IO biomarker
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BRAF (B-raf proto-oncogene) • IFNG (Interferon, gamma) • CTLA4 (Cytotoxic T-Lymphocyte Associated Protein 4) • IL23A (Interleukin 23 Subunit Alpha) • IL32 (Interleukin 32)
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PD-L1 expression • BRAF V600E • BRAF V600 • BRAF wild-type
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Mekinist (trametinib) • Tafinlar (dabrafenib)
29d
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
Transglutaminase 2 promotes epithelial-to-mesenchymal transition by regulating the expression of matrix metalloproteinase 7 in colorectal cancer cells via the MEK/ERK signaling pathway. (PubMed, Biochim Biophys Acta Mol Basis Dis)
The ERK-inhibitor GDC-0994 blocked phosphorylation of MEK/ERK and suppressed TGM2 and MMP7. TGM2 communicates with MMP7 in colon cancer cells forces cell migration and invasion by the MEK/ERK signaling pathway and triggers EMT. Inhibiting TGM2 could thus offer new therapeutic options to treat patients with colon cancer, particularly to prevent metastatic progression.
Journal
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CDH1 (Cadherin 1) • TGM2 (Transglutaminase 2) • CDH2 (Cadherin 2) • SNAI1 (Snail Family Transcriptional Repressor 1) • SNAI2 (Snail Family Transcriptional Repressor 2) • MMP7 (Matrix metallopeptidase 7)
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CDH1 expression • TGM2 overexpression • TGM2 expression
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ravoxertinib (RG7842)
1m
Regulation of voltage-gated sodium channels by TNF-α during herpes simplex virus latency establishment. (PubMed, J Neurovirol)
Latency establishment was mimicked by culturing HSV-1 infected ND7/23 cells in the presence of acyclovir (ACV) for 3 days...There were no changes in the pharmacological and biophysical properties of sodium currents promoted by TNF-α, including sensitivity to tetrodotoxin and the current-voltage relationship...Inhibition of p38 signaling with SB203580 or SB202190 eliminates the stimulatory effect of TNF-α on sodium currents. These results indicate that TNF-α signaling in sensory neurons during latency establishment upregulates the expression of voltage-gated Na+ channels in order to maintain the transmission of pain information.
Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha)
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SB202190
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
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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
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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
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
Parecoxib Enhances Resveratrol against Human Colorectal Cancer Cells through Akt and TXNDC5 Inhibition and MAPK Regulation. (PubMed, Nutrients)
This study presents evidence that parecoxib enhances the anti-cancer power of resveratrol in DLD-1 colorectal cancer cells via the inhibition of TXNDC5 and Akt signaling and enhancement of JNK/p38 MAPK pathways. Parecoxib may be provided as an efficient drug to sensitize colorectal cancer by resveratrol.
Journal
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TXN (Thioredoxin) • MAPK8 (Mitogen-activated protein kinase 8)
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Dynastat (parecoxib)
2ms
AIBP promotes cell proliferation and migration through the ERK1/2-MAPK signaling pathway in hepatocellular carcinoma. (PubMed, Transl Cancer Res)
Finally, we discovered that AIBP could control the MAPK signaling pathway-involved genes expression, including P-MEK, MEK, c-Myc, P-ERK1/2, and ERK1/2, and that GDC-0994, a specific ERK1/2 inhibitor, could suppress the AIBP overexpression induced cell migration and proliferation abilities. These findings demonstrated that the ERK/MAPK signaling pathway might be stimulated by AIBP in HCC tissues, leading to increased cell invasion, migration, and proliferation. It was hypothesized that AIBP might act as a useful prognostic and diagnostic marker for HCC.
Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • APOA1 (Apolipoprotein A-I)
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MYC expression
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ravoxertinib (RG7842)
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
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VEGFA (Vascular endothelial growth factor A)
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Epidaza (chidamide)
2ms
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
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NUP214 (Nucleoporin 214)
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SET-NUP214 fusion
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Epidaza (chidamide)
2ms
Belamcanda chinensis extract inhibits non-small cell lung cancer proliferation and induces apoptosis via inhibiting the MAPK (Ras/Raf) and Akt pathways. (PubMed, Heliyon)
Furthermore, BCE significantly inhibited the growth of NSCLC cells SPC-A1 in nude mice and downregulated Ras, Raf, Akt, and p-Akt expression in vivo. The antitumor effects of BCE suggest its potential clinical application in patients with NSCLC, especially in those bearing Ras or Raf mutations.
Journal • PARP Biomarker
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PARP1 (Poly(ADP-Ribose) Polymerase 1) • CASP3 (Caspase 3) • CASP8 (Caspase 8) • CASP9 (Caspase 9)
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RAS mutation
2ms
Single-cell RNA sequencing reveals melanoma cell state-dependent heterogeneity of response to MAPK inhibitors. (PubMed, EBioMedicine)
Nonresponding melanoma cells are identified in all transcriptional cell states and are predisposed to BRAF/MEK inhibitor resistance due to pro-inflammatory IL6 and TNFɑ signalling. Our study provides a framework to study treatment response within distinct melanoma cell states and indicate that tumour-intrinsic pro-inflammatory signalling contributes to BRAF/MEK inhibitor resistance.
Journal
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IL6 (Interleukin 6)
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)
3ms
Targeted agents plus CHOP compared with CHOP as the first-line treatment for newly diagnosed patients with peripheral T-cell lymphoma (GUIDANCE-03): an open-label, multicentre phase 2 clinical trial. (PubMed, Lancet Reg Health West Pac)
We conducted an open-label, phase 2 nonrandomised, externally controlled study to evaluate the efficacy and safety of targeted agents plus CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisolone) (CHOPX) for PTCL in the front-line setting...Specific targeted agents were added from Cycle 2, decitabine if TP53 mut, azacytidine if TET2/KMT2D mut, tucidinostat if CREBBP/EP300 mut, and lenalidomide if without mutations above...Biomarker-driven therapeutic strategy is feasible and may lead to promising efficacy specifically toward molecular features in PTCL. This study was supported by the National Key Research and Development Program (2022YFC2502600) and the General Program of the Shanghai Municipal Health Commission (202040400).
P2 data • Journal
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TP53 (Tumor protein P53) • TET2 (Tet Methylcytosine Dioxygenase 2) • KMT2D (Lysine Methyltransferase 2D) • CREBBP (CREB binding protein) • EP300 (E1A binding protein p300)
|
lenalidomide • doxorubicin hydrochloride • azacitidine • cyclophosphamide • decitabine • vincristine • Epidaza (chidamide)
3ms
New P2 trial • IO biomarker
|
PD-1 (Programmed cell death 1)
|
decitabine • Adcetris (brentuximab vedotin) • Epidaza (chidamide) • bendamustine
3ms
New P2 trial • Metastases
|
Epidaza (chidamide) • AiRuiKang (dalpiciclib)
3ms
New P2 trial
|
Epidaza (chidamide)
3ms
Chidamide induces cell cycle arrest via NR4A3/P21 axis upregulation to suppress relapsed and refractory acute myeloid leukemia. (PubMed, Biochem Biophys Res Commun)
We have discovered a novel epigenetic regulatory mechanism of chidamide in the treatment of relapsed and refractory acute myeloid leukemia (R/R AML).
Journal
|
NR4A3 (Nuclear receptor subfamily 4 group A member 3) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
|
Epidaza (chidamide)
3ms
New P2 trial • Metastases
|
Focus V (anlotinib) • Tevimbra (tislelizumab-jsgr) • Epidaza (chidamide)
3ms
Trial of Chidamide in Combination With Envafolimab in Patients With PD-1 Inhibitor Resistant Advanced NSCLC. (clinicaltrials.gov)
P2, N=34, Completed, Chipscreen Biosciences, Ltd. | Active, not recruiting --> Completed | Trial completion date: Dec 2023 --> May 2024
Trial completion • Trial completion date • Combination therapy • Metastases
|
Epidaza (chidamide) • Enweida (envafolimab)
3ms
A Study of Tucidinostat Combined With Tislelizumab as First-line Treatment in Advanced NSCLC (clinicaltrials.gov)
P2, N=118, Active, not recruiting, Chipscreen Biosciences, Ltd. | Recruiting --> Active, not recruiting | Trial primary completion date: Oct 2023 --> Oct 2024
Enrollment closed • Trial primary completion date • Metastases
|
PD-L1 (Programmed death ligand 1)
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Tevimbra (tislelizumab-jsgr) • Epidaza (chidamide)