- |||||||||| Azixa (verubulin) / Immune Pharma
Trial primary completion date: Exploratory Evaluation of [11C]MPC6827 (clinicaltrials.gov) - Oct 26, 2023 P1, N=40, Recruiting, The hit compound (N-(4-methoxyphenyl)-N,2-dimethyl-5,6,7,8-tetrahydroquinazolin-4-amine) was encapsulated in biocompatible nanocontainers based on Ca or Mg cross-linked alginate and it was demonstrated that its cytotoxic activity was preserved after encapsulation. Trial primary completion date: Sep 2023 --> Sep 2024
- |||||||||| NanomAbs / Immune Pharma, STC Biologics
Anti-ETX Nanobodies: Innovative Tools for MS Research, Diagnosis and Therapy (Gold) - Jul 21, 2023 - Abstract #MSMilan2023MSMilan_991; With this study we have successfully developed innovative nanobody-based biologics that can both sensitively detect and neutralize ETX, a potential triggering factor in RRMS. Our findings pave the way for a deeper understanding of the ETX-MS connection and open new avenues for targeted diagnostic and therapeutic interventions.
- |||||||||| Azixa (verubulin) / Immune Pharma
Dual PET imaging of microtubules and synaptic density in a mouse model of Alzheimer's Disease (In-Person) - Jul 6, 2023 - Abstract #AAIC2023AAIC_2034; In vivo PET, ex vivo biodistribution, and in vitro autoradiography data corroborated each other. Preliminary [ 11 C]MPC-6827 and [ 18 F]UCB-H PET evaluations showed negative correlations (* r = -0.778), suggesting MT destabilization and synaptic loss happen concurrently.
- |||||||||| Azixa (verubulin) / Immune Pharma
Dual PET imaging of microtubules and synaptic density in a mouse model of Alzheimer's Disease (Hall 2 (RAI Amsterdam Convention Centre)) - Jul 6, 2023 - Abstract #AAIC2023AAIC_434; In vivo PET, ex vivo biodistribution, and in vitro autoradiography data corroborated each other. Preliminary [11C]MPC-6827 and [18F]UCB-H PET evaluations showed negative correlations (*r= -0.778), suggesting MT destabilization and synaptic loss happen concurrently.
- |||||||||| crolibulin (EPC2407) / Immune Pharma
Journal: Study of FGFR2 status in gastric cancer by immunohistochemistry and fluorescent in situ hybridization (Pubmed Central) - Jun 9, 2023 Clone EPR24075-418 showed the best result in assessing the expression of FGFR2: the correlation with FISH results in reaction 3+ was 100%. Due to the high heterogeneity of FGFR2 expression, it is recommended to either examine the material of the primary tumor and metastasis, or evaluate a large volume of the primary tumor.
- |||||||||| Azixa (verubulin) / Immune Pharma
Preclinical, Journal: Antitumor Activity of Tubulin-Binding Agent MPC-6827 on Different Types of Cancer Cell Lines. (Pubmed Central) - Aug 24, 2022 These parameters showed that 4 nM was the optimum concentration for HeLa and A549 cells, while 2 nM was the optimum concentration for MCF-7 cells. The use of optimum concentrations for each cell line has shown that while there was a significant decrease in mitotic index, BrdU labelling index, there was a significant increase in apoptotic index.
- |||||||||| Azixa (verubulin) / Immune Pharma
Preclinical, Journal: Preliminary mechanistic insights of a brain-penetrant microtubule imaging PET ligand in a tau-knockout mouse model. (Pubmed Central) - Jul 27, 2022 Given the radiotracer binding does not require the presence of aggregated tau, we hypothesize that [C]MPC-6827 may be particularly useful in preclinical stages of AD prior to tau deposition. Our study provides immediate clarity on high uptake of the MT-based radiotracer in AD brains, which directly informs clinical utility in MT/tau-based PET imaging studies.
- |||||||||| Azixa (verubulin) / Immune Pharma
Preclinical, Journal: Preclinical evaluation of a microtubule PET ligand [C]MPC-6827 in tau and amyotrophic lateral sclerosis animal models. (Pubmed Central) - May 29, 2022 S. Dileep Kumar, Andrei Molotkov, Jongho Kim, Patrick Carberry, Sidney Idumonyi, John Castrillon, Karen Duff, Neil A. Shneider, Akiva Mintz.
- |||||||||| Azixa (verubulin) / Immune Pharma
Preclinical, Journal: Initial Evaluations of the Microtubule-Based PET Radiotracer, [C]MPC-6827 in a Rodent Model of Cocaine Abuse. (Pubmed Central) - Mar 18, 2022 Our initial observations suggest that [C]MPC-6827 uptake decreases in cocaine self-administered rats and that it may selectively bind to destabilized tubulin units in the brain. Further longitudinal studies correlating cocaine intake with [C]MPC-6827 PET brain measures could potentially establish the MT scaffold as an imaging biomarker for CUD, providing researchers and clinicians with a sensitive tool to better understand the biological underpinnings of CUD and tailor new treatments.
- |||||||||| Ceplene (histamine) / Immune Pharma
Review, Journal: MP-AzeFlu in Moderate-to-Severe Allergic Rhinitis: A Literature Review. (Pubmed Central) - Nov 16, 2021 Treatment of AR with MP-AzeFlu results in effective, sustained relief of nasal and ocular symptoms, and faster onset and time to control compared with intranasal azelastine or fluticasone propionate...Furthermore, MP-AzeFlu significantly improves patient quality of life. MP-AzeFlu is a currently available combination that may satisfy all these patient needs and expectations.
- |||||||||| Azixa (verubulin) / Immune Pharma
Journal: Preliminary Evaluations of [C]Verubulin: Implications for Microtubule Imaging With PET. (Pubmed Central) - Sep 28, 2021 We also conducted the first comparative in vivo PET imaging study with [C]verubulin, [C]HD-800 and [C]colchicine in a non-human primate. [C]Verubulin and [C]HD-800 require pharmacokinetic modeling and quantification studies to understand the role of how these radiotracers bind to MTs before translation to human use.
- |||||||||| Azixa (verubulin) / Immune Pharma
Journal: Effect of ethanol and cocaine on [C]MPC-6827 uptake in SH-SY5Y cells. (Pubmed Central) - Jun 10, 2021 Consistent with this mechanism of action, we observed lower [C]MPC-6827 uptake in SH-SY5Y cells after EtOH and cocaine treatments (e.g., fewer free tubulin units). We are currently performing in vivo PET imaging and ex vivo biodistribution studies in rodent and nonhuman primate models of AUD and SUDs and Alzheimer's disease.
- |||||||||| Ceplene (histamine) / Immune Pharma
Clinical, Journal: Allergic Rhinitis Therapy Decisions During a Routine Consultation: A Multicenter, Cross-Sectional Survey. (Pubmed Central) - Apr 16, 2021 Many patients suffering from acute AR symptoms consulted with their physician because of insufficient medications. Not all patients with uncontrolled symptoms received a step-up in treatment, underscoring the need for improved physician education to enhance AR management and control in accordance with consensus treatment guidelines.
- |||||||||| Azixa (verubulin) / Immune Pharma
Journal: PET Imaging of [C]MPC-6827, a Microtubule-Based Radiotracer in Non-Human Primate Brains. (Pubmed Central) - Feb 12, 2021 [C]MPC-6827 showed excellent brain uptake with good pharmacokinetics in non-human primate brains, with significant correlation between the test and retest scan data (r = 0.77, p = 0.023). These initial evaluations demonstrate the high translational potential of [C]MPC-6827 to image microtubules in the brain in vivo in monkey models of neurological and psychiatric diseases.
- |||||||||| Azixa (verubulin) / Immune Pharma
Preclinical, Journal: In vivo comparison of N-CH vs O-CH radiolabeled microtubule targeted PET ligands. (Pubmed Central) - Jan 23, 2021 Both O-CH and N-CH labeled MT tracers exhibit high specific binding and brain. The N-CH labeled PET ligands demonstrated similar in vivo binding characteristics compared with the corresponding O-CH labeled tracers, [C]MPC-6827 and [C]HD-800 respectively.
- |||||||||| CKD-702 / Chong Kun Dang
The novel bi-specific antibody CKD-702 is a potential agent for NSCLC patients with aberrant cMET and EGFR signaling (Virtual Meeting II: E-Posters) - May 16, 2020 - Abstract #AACRII2020AACR-II_1037; Interestingly, unlike other previously developed EGFR-targeting agents, CKD-702 showed limited skin rash in GLP toxicity study.In summary, CKD-702 is confirmed to inhibit tumors with activated cMET pathway such as cMET amplification and exon 14 skipping as well as with EGFR-activating mutations. This profile of preclinical data supports the clinical trial of CKD-702 as monotherapy in selected lung cancer patients with aberrant cMET and EGFR signaling.A Phase I study of CKD-702 is planned to initiate in 2020.
- |||||||||| EP1013 / Immune Pharma, Enbrel (etanercept) / Pfizer, Amgen
Preclinical, Journal: Pan-caspase inhibitor F573 mitigates liver ischemia reperfusion injury in a murine model. (Pubmed Central) - Apr 3, 2020 Anakinra with etanercept, and BMX-001 did not demonstrate convincing efficacy at reducing IRI in this model, and likely need further optimization. The positive findings set rational groundwork for future translational studies of applying F573 during normothermic ex situ liver perfusion, with the aim of improving the quality of marginal grafts.
- |||||||||| crolibulin (EPC2407) / Immune Pharma
Journal: Molecular mechanism of crolibulin in complex with tubulin provides a rationale for drug design. (Pubmed Central) - Dec 20, 2019 Here we report a 2.5 Å crystal structure of tubulin complexed with crolibulin. This complex structure reveals the interactions between crolibulin and tubulin, helps explain the results of the structure-activity-relationship (SAR) studies and provides a solid structural basis for the design and development of new 4-Aryl-4H-chromenes derivatives as MTAs.
- |||||||||| LidoPain (lidocaine) / Immune Pharma
Clinical, Journal: Is burning mouth syndrome a neuropathic pain condition? (Pubmed Central) - Apr 3, 2019 The central type does not respond to local treatments and associates often with psychiatric comorbidity (depression or anxiety), whereas the peripheral type responds to peripheral lidocaine blocks and topical clonazepam. Burning mouth syndrome is most prevalent in postmenopausal women, having led to a hypothesis that BMS is triggered as a consequence of nervous system damage caused by neurotoxic factors affecting especially vulnerable small fibers and basal ganglia in a setting of decrease in neuroprotective gonadal hormones and increase in stress hormone levels, typical for menopause.
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