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DRUG:

BOLD-100

i
Other names: BOLD 100, KP-1339, BOLD100, BOLD-100, IT-139, NKP-1339
Associations
Trials
Company:
Bold Therap, Hana Pharm
Drug class:
Reactive oxygen species stimulant, GRP78 inhibitor
Associations
Trials
19d
Combinational studies of BOLD-100/KP1339 with established chemotherapeutics in gastrointestinal multicellular tumor spheroids. (PubMed, Cancer Chemother Pharmacol)
The purpose of this study was to assess in vitro the impact of BOLD-100 combinations with oxaliplatin, 5-FU, cisplatin or SN38 in multicellular tumor spheroids (MCTSs) compared to single-drug treatments...Apoptosis and necrosis were induced in the spheroid models by single-drug and combined treatment, with no hints at antagonism in the combination settings. In conclusion, these findings emphasize the potential of BOLD-100 for combination therapy of gastric and colorectal cancers.
Journal
|
HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5)
|
cisplatin • 5-fluorouracil • oxaliplatin • BOLD-100
3ms
New P1/2 trial
|
BRAF (B-raf proto-oncogene)
|
BRAF wild-type
|
5-fluorouracil • oxaliplatin • leucovorin calcium • BOLD-100
3ms
Enrollment change
|
BRAF (B-raf proto-oncogene)
|
BRAF wild-type
|
5-fluorouracil • oxaliplatin • leucovorin calcium • BOLD-100
6ms
BOLDSARC-01: BOLD-100 Plus Doxorubicin in Advanced Soft Tissue Sarcomas (clinicaltrials.gov)
P1, N=32, Not yet recruiting, University Health Network, Toronto | Initiation date: Jun 2025 --> Mar 2026
Trial initiation date
|
doxorubicin hydrochloride • BOLD-100
10ms
Ultrasound-Targeted Nanobubbles Codelivering NKP-1339 and miR-142-5p for Synergistic Mitochondrial Immunogenic Cell Death and PD-L1 Inhibition in Cancer Therapy. (PubMed, Biomater Res)
Moreover, the UTMD technique enhanced the tumoral accumulation and penetration of nanobubbles, improving delivery specificity and minimizing off-target effects. This combined treatment strategy, including UTMD, provides a promising translational potential for ESCC therapy.
Journal • PD(L)-1 Biomarker • IO biomarker
|
PD-L1 (Programmed death ligand 1) • CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • CALR (Calreticulin) • MIR142 (MicroRNA 142)
|
PD-L1 expression
|
BOLD-100
10ms
Machine Learning-Enhanced Calculation of Quantum-Classical Binding Free Energies. (PubMed, J Chem Theory Comput)
The ML potential approach takes electrostatic embedding and long-range electrostatics into account. We demonstrate the applicability of the workflow on the well-studied protein-ligand complex of myeloid cell leukemia 1 and the inhibitor 19G and on the anticancer drug NKP1339 acting on the glucose-regulated protein 78.
Journal
|
MCL1 (Myeloid cell leukemia 1)
|
BOLD-100
12ms
BOLD-100 Plus Doxorubicin in Advanced Soft Tissue Sarcomas (clinicaltrials.gov)
P1, N=32, Not yet recruiting, University Health Network, Toronto
New P1 trial
|
doxorubicin hydrochloride • BOLD-100
12ms
Therapeutic potential of BOLD-100, a GRP78 inhibitor, enhanced by ATR inhibition in pancreatic ductal adenocarcinoma. (PubMed, Cell Commun Signal)
BOLD-100 synergizes with AZD6738, an ATR inhibitor, to enhance anti-tumor efficacy compared to either agent alone in both in vitro and in vivo models. These findings suggest that BOLD-100, especially in combination with an ATR inhibitor, represents a promising therapeutic option for patients with PDAC.
Journal
|
CHEK1 (Checkpoint kinase 1) • HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5)
|
ceralasertib (AZD6738) • BOLD-100
1year
Unraveling BOLD-100 synergistic potential in pleural mesothelioma treatment: an in vitro study. (PubMed, Invest New Drugs)
Our aim is to investigate cellular responses of several PM cell lines to a regimen that includes BOLD-100 in addition to other commonly used treatments. BOLD-100 is a ruthenium-based anticancer therapeutic.
Preclinical • Journal
|
HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5)
|
BOLD-100
1year
Mechanical cues rewire lipid metabolism and support chemoresistance in epithelial ovarian cancer cell lines OVCAR3 and SKOV3. (PubMed, Cell Commun Signal)
This was associated with increased cholesterol uptake/biosynthesis and decreased sensitivity to the ruthenium-based anticancer drug BOLD-100. Overall, the present study contributes to shedding light on the molecular pathways connecting mechanical cues, tumor metabolism and drug responsiveness.
Preclinical • Journal
|
YAP1 (Yes associated protein 1)
|
BOLD-100
almost2years
BOLD-100-001: BOLD-100 in Combination With FOLFOX for the Treatment of Advanced Solid Tumours (clinicaltrials.gov)
P1/2, N=220, Recruiting, Bold Therapeutics, Inc. | Active, not recruiting --> Recruiting | Phase classification: P1b/2a --> P1/2 | N=117 --> 220 | Trial completion date: Sep 2024 --> Sep 2026 | Trial primary completion date: Dec 2023 --> Jun 2026
Enrollment open • Phase classification • Enrollment change • Trial completion date • Trial primary completion date • Combination therapy • Metastases
|
5-fluorouracil • leucovorin calcium • BOLD-100
almost2years
Ruthenium drug BOLD-100 regulates BRAFMT colorectal cancer cell apoptosis through AhR/ROS/ATR signaling axis modulation. (PubMed, Mol Cancer Res)
These results unveil possible novel therapeutic opportunity for BRAFMT CRC. Implications: BOLD-100 induces BRAFMT-dependent replication stress, and targeted strategies against replication stress (eg. by using ATR inhibitors) in combination with BOLD-100 may serve as a potential novel therapeutic strategy for clinically aggressive BRAFMT CRC.
Journal
|
CHEK1 (Checkpoint kinase 1) • CYP1A1 (Cytochrome P450 Family 1 Subfamily A Member 1)
|
BOLD-100