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- | Acelarin (fosgemcitabine palabenamide) / NuCana, ubenimex (DFP-14323) - Delta / Fly Pharma, gemcitabine / Generic mfg.
Journal: Design, synthesis, and anti-cancer evaluation of the novel conjugate of gemcitabine's ProTide prodrug based on CD13. (Pubmed Central) - Mar 16, 2025
5f demonstrates significant in vivo anti-tumor activity in 22Rv1 xenograft tumor models. Our findings indicate that 5f shows strong potential for further development as a candidate for the treatment of prostate cancer.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Discovery of New Nanomolar Selective IRAP Inhibitors. (Pubmed Central) - Feb 27, 2025
A few series of inhibitors inspired either by angiotensin IV, one of IRAP substrates, or by bestatin a pan aminopeptidase inhibitor, have been disclosed...Several inhibitors in the series displayed IRAP-dependent inhibition of antigen cross-presentation. These results pave the way to the development of novel therapeutic agents targeting IRAP.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Synthesis and biological evaluation of new dual APN/NEP inhibitors as potent analgesics. (Pubmed Central) - Feb 13, 2025
These results pave the way to the development of novel therapeutic agents targeting IRAP. In in-vivo antinociceptive assays, SDUY816 and SDUY817 demonstrated superior analgesic efficacy compared to Thiorphan and Bestatin in mice models of acute, inflammatory and neuropathic pains with jumping latencies exceeding 100
- || 5-fluorouracil / Generic mfg., ubenimex (DFP-14323) - Delta / Fly Pharma
PK/PD data, Journal: Synthesis, biological and pharmacokinetic characterization of a novel leucine ureido derivative as a multi-target anticancer agent. (Pubmed Central) - Feb 11, 2025
Moreover, synergistic anti-proliferation effects against tumor cells were found when used in combination with 5-Fluorouracil (5-FU)...The biological activity evaluation showed that compound 3 exhibited more potent in vitro anti-proliferative, anti-metastatic, anti-angiogenic activities than the positive control bestatin...In vivo pharmacokinetic study displayed that compound 3 was absorbed quickly after oral administration in rats and maintained in vivo for a long time, but exhibited poor oral bioavailability. Generally speaking, compound 3 is a promising lead for further development of more potent analogs as anticancer agents.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Why Bestatin Prefers Human Carnosinase 2 (CN2) to Human Carnosinase 1 (CN1). (Pubmed Central) - Dec 5, 2024
In contrast, the high mobility of the aryl end and the complete loss of metal-BES interactions in CN1 cause a loose BES binding. Seemingly, polar termini were required for a good CN1 inhibitor.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal, Cytokine storm: The triple combination DBDx alleviates cytokine storm and related lung injury. (Pubmed Central) - Nov 27, 2024
All of these results demonstrate that DBDx, a triple combination of clinical orally-administered drugs, can alleviate cytokine storm and related lung injury. DBDx is beneficial for treating cytokine storm disorders.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: A Nanofluorescent Probe for Evaluating the Fluctuation of Aminopeptidase N in Nonalcoholic Fatty Liver Disease and Hepatic Fibrosis. (Pubmed Central) - Sep 1, 2024
Furthermore, we investigated the inhibitory effect of the APN inhibitor bestatin in nonalcoholic fatty liver and hepatic fibrosis disease models, confirming its regulatory effect on APN levels in cells and in vivo in both disease models. Therefore, this study may offer diagnostic possibilities for detecting NAFLD and hepatic fibrosis.
- STR-324 / ArchiMed
PSTR324. Astrocytes and Disease Mechanisms (MCP Hall A) - Aug 22, 2024 - Abstract #Neuroscience2024Neuroscience_739;
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Preclinical, Journal: Effect of X-ray irradiation on renal excretion of bestatin through down-regulating organic anion transporters via the vitamin D receptor in rats. (Pubmed Central) - Jul 31, 2024
Additionally, elevated plasma urea nitrogen levels and histopathological changes were observed in rats after exposure to irradiation. The "RT-PK" phenomenon of bestatin occurs in rats after exposure to irradiation, possibly resulting in the regulation of the expressions and activities of renal Oats via activation of the Vdr signalling pathway.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Crystal structure of a newly identified M61 family aminopeptidase with broad substrate specificity that is solely responsible for recycling acidic amino acids. (Pubmed Central) - Jul 18, 2024
The "RT-PK" phenomenon of bestatin occurs in rats after exposure to irradiation, possibly resulting in the regulation of the expressions and activities of renal Oats via activation of the Vdr signalling pathway. Further, we report the high-resolution crystal structure of M61xc in the apo form (2.1?
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Biomarker, Journal: Leukotriene B4: A Potential Mediator and Biomarker for Cardiac Allograft Vasculopathy. (Pubmed Central) - Jul 13, 2024
Further, we report the high-resolution crystal structure of M61xc in the apo form (2.1? This study provides key evidence supporting the role of the inflammatory cytokine LTB4 as an important mediator of CAV development
- || ubenimex (DFP-14323) - Delta / Fly Pharma
Review, Journal: State of the Art in the Development of Human Serum Carnosinase Inhibitors. (Pubmed Central) - Jun 19, 2024
Bestatin is the only inhibitor reported other than carnostatine, although its activity is not selective towards serum carnosinase. Herein, we present a review of the most critical findings on human serum carnosinase, including enzyme expression, localization and substrate selectivity, along with factors affecting the hydrolytic activity, its implication in human diseases and the properties of known inhibitors of the enzyme.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Preclinical, Journal: Novel paired CD13-negative (MT-50.1) and CD13-positive (MT-50.4) HTLV-1-infected T-cell lines with differential regulatory T cell-like activity. (Pubmed Central) - Jun 1, 2024
These findings suggest that CD13 expression may be involved in the increased Treg-like activity of MT-50.4 cells. Hence, MT-50.4 cells will be useful for in-depth studies of CD13+Foxp3+ HTLV-1-infected cells.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Bestatin attenuates breast cancer stemness by targeting puromycin-sensitive aminopeptidase. (Pubmed Central) - May 30, 2024
Puromycin-sensitive aminopeptidase is implicated in the process through the regulation of cell cycle, resulting in heightened cell apoptosis and diminished cell proliferation of BCSCs. Our study suggest that targeting cancer stem cell may offer a promising approach in breast cancer treatment, presenting noval therapeutic strategies for patients with breast cancer.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal, IO biomarker: Targeting the GPI transamidase subunit GPAA1 abrogates the CD24 immune checkpoint in ovarian cancer. (Pubmed Central) - Apr 26, 2024
Consequently, we show that bestatin, a clinically advanced aminopeptidase inhibitor, binds to GPAA1 and blocks GPI attachment, resulting in reduced CD24 cell surface expression, increased macrophage-mediated phagocytosis, and suppressed growth of ovarian tumors. Our study highlights the potential of targeting GPAA1 as an immunotherapeutic approach for CD24+ ovarian cancers.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Preclinical, Journal: Ubenimex combined with Albendazole for the treatment of Echinococcus multilocularis-induced alveolar echinococcosis in mice. (Pubmed Central) - Apr 8, 2024
The levels of ALT, AST, TBIL, DBIL, ALP, and ?-GT were reduced after the combined treatment, indicating that treatment with both Ubenimex and Albendazole could alleviate liver damage. This study suggests that the combined treatment with Ubenimex and Albendazole could be a potential therapeutic strategy for E. multilocularis infections.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Preclinical, Journal: CD13 expression affects glioma patient survival and influences key functions of human glioblastoma cell lines in vitro. (Pubmed Central) - Mar 27, 2024
Bestatin treatment reduced proliferation, migration and colony formation of glioma cells in a CD13-dependent manner while apoptosis was increased. In summary, CD13 has an impact on glioma patient survival and is important for the main function of specific glioma cells.
- | Natacyn (natamycin) / Novartis, ubenimex (DFP-14323) - Delta / Fly Pharma, SAL-003 (evolocumab biosimilar) / Shenzhen Salubris, Ligand
Journal: Targeting Allosteric Site of PCSK9 Enzyme for the Identification of Small Molecule Inhibitors: An In Silico Drug Repurposing Study. (Pubmed Central) - Feb 24, 2024
Moreover, the MM-GBSA calculations revealed binding free energy values ranging from -84.22 to -76.39 kcal/mol, which were found comparable to those obtained for the co-crystallized ligand structure. In conclusion, these identified drug molecules have the potential to serve as inhibitors PCSK9 enzyme and these finding could pave the way for the development of new PCSK9 inhibitory drugs in future in vitro research.
- | Keytruda (pembrolizumab) / Merck (MSD), ubenimex (DFP-14323) - Delta / Fly Pharma
Journal, Metastases: A Phase ? Study of Ubenimex Combined With Pembrolizumab, Nab-Paclitaxel, and Carboplatin for Previously Untreated Advanced Squamous Non-Small-Cell Lung Cancer: TORG2241 (UBE-Q). (Pubmed Central) - Jan 15, 2024
This is the first study to evaluate the efficacy and safety of ubenimex combined with pembrolizumab, nab-paclitaxel, and carboplatin in patients with previously untreated advanced squamous NSCLC. The results will help devise future treatment strategies.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: The triple-drug combination DBDx enhances the antitumor efficacy of PD-1 antibody associated with Treg modulation. (Pubmed Central) - Jan 6, 2024
The results will help devise future treatment strategies. The combination of PD-1 antibody and DBDx could achieve enhanced therapeutic antitumor efficacy than anti-PD-1 monotherapy, suggesting potential for using the triple-drug combination DBDx in cancer immunotherapy.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Expression, Characterisation, Homology Modelling and Molecular Docking of a Novel M17 Family Leucyl-Aminopeptidase from Bacillus cereus CZ. (Pubmed Central) - Nov 18, 2023
EDTA significantly inhibits the enzymatic activity, and bestatin and SDS also show strong inhibition...There may be two nucleophilic catalytic mechanisms in bcLAP, one involving His 437 or Arg346 and the other involving His437 and Arg346. The bcLAP can hydrolyse the peptide bonds in Leu-Trp, Asp-Trp and Ala-Ala-Gly.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Ubenimex suppresses glycolysis mediated by CD13/Hedgehog signaling to enhance the effect of cisplatin in liver cancer. (Pubmed Central) - Nov 16, 2023
The glycolysis inhibitor 2-deoxy-D-glucose enhanced the antiproliferative effect of ubenimex and CDDP...Moreover, ubenimex inhibited the production of lactic acid and adenosine triphosphate (ATP), as well as the expression of key proteins involved in glycolysis, which was similar to the effects caused by the Hh inhibitor cyclopamine...Ubenimex inhibits glycolysis by targeting the CD13/Hh pathway, thus playing an anti-tumor role together with CDDP. This study demonstrated the adjuvant effect of ubenimex from the perspective of Hh signal-dependent glycolysis regulation.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Statins markedly potentiate aminopeptidase inhibitor activity against (drug-resistant) human acute myeloid leukemia cells. (Pubmed Central) - Oct 16, 2023
Consistently, statin potentiation of CHR2863 activity was abrogated by co-administration of mevalonate and/or farnesyl pyrophosphate, suggesting the involvement of protein prenylation; this was experimentally confirmed by impaired Rheb prenylation by simvastatin. These novel findings suggest that the combined inhibitory effect of impaired Rheb prenylation and CHR2863-dependent mTOR inhibition instigates a potent synergistic inhibition of statins and APis on human AML cells.
- | Zolinza (vorinostat) / Merck (MSD), ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Design, synthesis, and biological evaluation of novel HDAC/CD13 dual inhibitors for the treatment of cancer. (Pubmed Central) - Sep 18, 2023
The representative compound 12 exhibited more potent inhibitory activity against human CD13, HDAC1-3, and antiproliferative activity than positive controls bestatin and SAHA. Compound 12 effectively induced apoptosis in MV4-11
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Discovery of a Novel Ubenimex Derivative as a First-in-Class Dual CD13/Proteasome Inhibitor for the Treatment of Cancer. (Pubmed Central) - Sep 13, 2023
Moreover, BC-05 showed more favorable safety profiles than those of ixazomib in preliminary toxicity studies. Overall, the results indicate that BC-05 is a promising drug candidate for the treatment of multiple myeloma.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: A promising new target to control fasciolosis: Fasciola hepatica leucine aminopeptidase 2. (Pubmed Central) - Jul 31, 2023
The activity was inhibited by bestatin, 1,10-phenanthroline, and EDTA, specific inhibitors of aminopeptidase and/or metalloproteases...The immunized group elicited total specific IgG and subclasses IgG1 and IgG2 antibody responses. This study highlights the potential of a new candidate vaccine formulation with potential applications in natural ruminant hosts, especially those targeting the juvenile stage.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Antiplasmodial Activity Evaluation of a Bestatin-Related Aminopeptidase Inhibitor, Phebestin. (Pubmed Central) - Jul 17, 2023
This study highlights the potential of a new candidate vaccine formulation with potential applications in natural ruminant hosts, especially those targeting the juvenile stage. Phebestin inhibited the in vitro multiplication of the P. falciparum 3D7 (chloroquine-sensitive) and K1 (chloroquine-resistant) strains at IC values of 157.90?
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Bestatin as a treatment modality in experimental periodontitis. (Pubmed Central) - Apr 6, 2023
We show that in a murine model of CP bestatin not only shifted the biofilm species composition from pathogenic to a commensal one, but also promoted bacteria clearance by immune cells and alleviated inflammation. Taken together, these results suggest that bestatin is a promising drug choice for the treatment and/or prevention of periodontitis and clinical trials are required to fully evaluate its potency.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Preclinical, Journal: Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies. (Pubmed Central) - Mar 15, 2023
In silico study was conducted to predict the possible binding of hybrid 1e with methionine aminopeptidases 1 and 2 of L. donovani. Molecular dynamic simulations verified the predicted binding modes and provide more in depth understanding of the impact of hybrid 1e on LdMetAP-1 and LdMetAP-2.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Development of Hydroxamate Derivatives Containing a Pyrazoline Moiety as APN Inhibitors to Overcome Angiogenesis. (Pubmed Central) - Dec 12, 2022
2,6-Dichloro substituted compound 14o with R = CH, showed the best capacity for inhibiting APN with an IC value of 0.0062 ± 0.0004 μM, which was three orders of magnitude better than that of the positive control bestatin...The hydroxamate moiety chelated the zinc ion and formed four hydrogen bonds with His, Glu and His. Meanwhile, the terminal phenyl group and another phenyl group of 14o interacted with S' and S pockets via hydrophobic effects, respectively.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal, PARP Biomarker: FASN inhibitors enhance bestatin-related tumor cell apoptosis through upregulating PEPT1. (Pubmed Central) - Nov 23, 2022
Meanwhile, the terminal phenyl group and another phenyl group of 14o interacted with S' and S pockets via hydrophobic effects, respectively. FASN inhibitors facilitate tumor cells susceptible to bestatin-induced apoptosis involving the up-regulation of PEPT1 at the mRNA translation level and the transport of bestatin by PEPT1, emerging as a promising strategy for tumor targeted therapy.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Therapeutic effect on Alveolar echinococcosis by targeting EM-Leucine aminopeptidase. (Pubmed Central) - Nov 1, 2022
In this study, the therapeutic effect of recombinant EM-LAP (rEM-LAP) on AE was evaluated and verified using Ubenimex, a broad-spectrum inhibitor of LAP...The indirect ELISA shows that rEM-LAP could induce specific immunity response and produce high levels of IgG, IgG1, IgG2a, IgM, and IgA, and the serum levels of IFN-γ and IL-4 are significantly increased compared to the control groups, indicating that treatment with rEM-LAP leads to a Th1 and Th2 mixed-type immune response. This study suggests that EM-LAP could be a potential therapeutic target of E. multilocularis infection.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: CD13 downregulation mediated by ubenimex inhibits autophagy to overcome 5-FU resistance by disturbing the EMP3/FAK/NF-κB pathway in gastric cancer cells. (Pubmed Central) - Sep 14, 2022
Ubenimex affects autophagy and apoptosis to reverse GC cell resistance by targeting the CD13/EMP3/FAK/NF-κB pathway. These results showed that ubenimex is a promising agent that may inhibit GC autophagy to improve chemotherapeutic drug sensitivity and thereby reverse drug resistance.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Preclinical, Journal: Exploring ex vivo peptideolysis of thymopentin and lipid-based nanocarriers towards oral formulations. (Pubmed Central) - Sep 14, 2022
Inhibition of TP5 enzymatic peptidolysis was screened in the presence or absence of EDTA, trypsin and chymotrypsin inhibitors from soybean (SBTCI), and bestatin...TP5 and SBTCI were loaded into three lipid-based delivery systems, displaying superior protection under ex vivo intestinal luminal contents and mucosal homogenates for 6 hours compared with the pure drug solution. These findings suggest that using select inhibitors and lipid-based nanocarriers can decrease peptide degradation and may improve oral bioavailability of TP5 following oral administration.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Melanoma Mediated Disruption of Brain Endothelial Barrier Integrity Is Not Prevented by the Inhibition of Matrix Metalloproteinases and Proteases. (Pubmed Central) - Aug 26, 2022
The inhibitors batimastat, Pefabloc SC, antipain and bestatin alone decreased the barrier strength. These results suggest that although some MMPs and proteases are released by melanoma cells, there is no direct evidence that they are substantially involved in the initial melanoma-mediated disruption of the brain endothelium.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Nav1.6 promotes the progression of human follicular thyroid carcinoma cells via JAK-STAT signaling pathway. (Pubmed Central) - Aug 6, 2022
Furthermore, downregulating the expression of Nav1.6 improve the susceptibility of FTC cells to ubenimex in vitro. These results suggest Nav1.6 accelerates FTC progression through JAK/STAT signaling and may be a potential target for FTC therapy.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Thymidine kinase 1 mediates the synergistic antitumor activity of ubenimex and celecoxib via regulation of cell cycle in colorectal cancer. (Pubmed Central) - Aug 4, 2022
In summary, this research demonstrates that celecoxib combined with ubenimex inhibit the development of colorectal cancer in vitro and in vivo, making them a viable combination regimen. Significance Statement In this study, our data reveal the great potential of celecoxib combined with ubenimex in the treatment of colorectal cancer, providing new ideas for clinical antitumor drug regimens and theoretical reference for drug development.
- || Rituxan (rituximab) / Roche
Trial completion: INGRID: RCHOP Chemoimmunotherapy Preceded BY BBB Permeabilization by t-NGR Necrosis Factor (clinicaltrials.gov) - Aug 3, 2022
P2, N=28, Completed, Sponsor: Andres J. M. Ferreri
Significance Statement In this study, our data reveal the great potential of celecoxib combined with ubenimex in the treatment of colorectal cancer, providing new ideas for clinical antitumor drug regimens and theoretical reference for drug development. Unknown status --> Completed
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Discovery of Selective Nanomolar Inhibitors for Insulin-Regulated Aminopeptidase Based on α-Hydroxy-β-amino Acid Derivatives of Bestatin. (Pubmed Central) - Jul 31, 2022
X-ray crystallographic analysis of IRAP in complex with this inhibitor suggest that interactions with the GAMEN loop is an unappreciated key determinant for potency and selectivity. Overall, our results suggest that α-hydroxy-β-amino acid derivatives may constitute useful chemical tools and drug leads for this group of aminopeptidases.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Clinical efficacy of intravesical gemcitabine combined with ubenimex in patients with non-muscle-invasive bladder carcinoma after transurethral resection of bladder tumor. (Pubmed Central) - Jul 10, 2022
For NMIBC patients receiving bladder-preserving surgery, intravesical gemcitabine combined with immunotherapy can reduce the recurrence rate, relieve lower urinary tract symptoms, increase the tolerance of patients to intravesical chemotherapy and significantly improve the function of T lymphocytes, without obvious increase in adverse drug reactions. Therefore, it is safe and effective, and has certain clinical value.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Ubenimex Combined with Pemetrexed Upregulates SOCS1 to Inhibit Lung Adenocarcinoma Progression via the JAK2-STAT3 Signaling Pathway. (Pubmed Central) - Jul 8, 2022
In addition, UBE combined with PEM therapy was associated with increased SOCS1 expression in patients' serum and knocking down SOCS1 reversed the antitumor effects of UBE and PEM. Overall, combination therapy with UBE and PEM could inhibit the JAK2-STAT3 signaling pathway by upregulating SOCS1 expression to hinder the progression of lung adenocarcinoma cells.
- || ubenimex (DFP-14323) - Delta / Fly Pharma, tosedostat (CHR-2797) / CTI BioPharma
Review, Journal: Review: Aminopeptidases in Cancer, Biology and Prospects for Pharmacological Intervention. (Pubmed Central) - Jun 25, 2022
While there are agents that directly target aminopeptidases which demonstrate potential as cancer therapies, such as bestatin and tosedostat, more selective and more targeted therapeutic approaches are needed. This article specifically looks at the biological role of aminopeptidases in both normal and cancer processes, and their potential as a biological target for future therapeutic strategies.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Discovery of Novel Tetrahydro-β-carboline Containing Aminopeptidase N Inhibitors as Cancer Chemosensitizers. (Pubmed Central) - Jun 10, 2022
In the in vivo study, the selected APN inhibitors, especially D12, exhibited improved anticancer activity in combination with Paclitaxel compared with Bestatin. Collectively, potent APN inhibitors were discovered, which could be used as lead compounds for tumor chemo-sensitization and cancer stem cell-based therapies.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Development of pyrazoline-based derivatives as aminopeptidase N inhibitors to overcome cancer invasion and metastasis. (Pubmed Central) - Apr 29, 2022
At the same concentration of 100 μM, the in vitro anti-invasion activity of compound 2k was also significantly better than that of bestatin. Moreover, compound 2k could effectively prevent the pulmonary metastasis of mice H22 hepatoma cells in vivo, supporting its further research and development as an antitumor agent.
- ubenimex (DFP-14323) - Delta / Fly Pharma, Gilotrif (afatinib) / Boehringer Ingelheim
Final progression-free survival analysis of phase II study with the combination therapy of DFP-14323, protease inhibitor, and low-dose afatinib as first-line therapy for common EGFR mutation–positive NSCLC. (Available On Demand; 97) - Apr 28, 2022 - Abstract #ASCO2022ASCO_2875;
Combination of DFP-14323 and low-dose afatinib has shown comparable potential as a first-line treatment for EGFR mutation positive NSCLC with feasible efficacy and good safety profile. We are planning a phase III study to evaluate this combination therapy as compared with other EGFR-TKIs.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Preclinical, Journal: Bradykinin induces peripheral antinociception in PGE-induced hyperalgesia in mice. (Pubmed Central) - Apr 26, 2022
We are planning a phase III study to evaluate this combination therapy as compared with other EGFR-TKIs. The present study is the first to demonstrate BK-induced antinociception in peripheral tissues against PGE-induced nociception in mice and the involvement of κ-opioid and CB cannabinoid receptors in this effect.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Curcumin induces peripheral antinociception by opioidergic and cannabinoidergic mechanism: Pharmacological evidence. (Pubmed Central) - Feb 22, 2022
The present study is the first to demonstrate BK-induced antinociception in peripheral tissues against PGE-induced nociception in mice and the involvement of κ-opioid and CB cannabinoid receptors in this effect. These results suggest that curcumin possibly peripheral antinociception induced by opioid and cannabinoid systems activation and possibly for endocannabinoids and opioids release.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Intracellular Aminopeptidase Activity Determination from the Fungus Sporisorium reilianum: Purification and Biochemical Characterization of psrAPEi Enzyme. (Pubmed Central) - Feb 15, 2022
Enzymatic activity was optimal at pH 7.0 and 35 °C and was inhibited by EDTA-Na2, 1,10-phenanthroline, bestatin, and PMSF...The K and V values were 3.72 μM and 188.0 μmol/min, respectively, for L-lysyl-4-nitroanilide. This is the first study to report on intracellular aminopeptidase activity in S. reilianum and the purification and characterization of an intracellular metallo-serine-aminopeptidase (psrAPEi).
- || Nexavar (sorafenib) / Bayer, Amgen
Biomarker, Review, Journal: New frontiers against sorafenib resistance in renal cell carcinoma: From molecular mechanisms to predictive biomarkers. (Pubmed Central) - Feb 10, 2022
Herein, we comprehensively summarize the underlying mechanisms of sorafenib resistance and molecular biomarkers for predicting sorafenib responsiveness. Moreover, we outline strategies suitable for overcoming sorafenib resistance and prospect potential approaches for identifying biomarkers associated with sorafenib resistance in RCC, which contributes to guide individualized and precision drug therapy.
- | ubenimex (DFP-14323) - Delta / Fly Pharma
Journal: Synthesis and Molecular Simulation Studies of Mandelic Acid Peptidomimetic Derivatives as Aminopeptidase N Inhibitors. (Pubmed Central) - Jan 14, 2022
Moreover, we outline strategies suitable for overcoming sorafenib resistance and prospect potential approaches for identifying biomarkers associated with sorafenib resistance in RCC, which contributes to guide individualized and precision drug therapy. The compound 9m might represent a promising scaffold for the further development of novel anti-cancer drugs.