Phase 2, Multi-center, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Safety and Efficacy of EC-18 in Preventing the Progression of COVID-19 Infection to Severe Pneumonia or ARDS

A trial of EC-18 in patients with mild/moderate pneumonia due to COVID-19

Start Date30 Apr 2021

Sponsor / Collaborator

ENZYCHEM LIFESCIENCES Corp.

NCT04500132 / CompletedPhase 2

Phase 2, Multi-center, Randomized, Double-blind, Placebo- Controlled Study to Evaluate the Safety and Efficacy of EC-18 in COVID-19 Infection to Pneumonia

Prevention of COVID-19 infection to severe pneumonea or ARDS

Start Date28 May 2020

Sponsor / Collaborator

ENZYCHEM LIFESCIENCES Corp.

NCT03200340 / CompletedPhase 2

Phase 2, Multi-center, Randomized, Double-blind, Placebo-controlled Study to Evaluate EC-18 for Oral Mucositis in Patients With Concomitant Chemoirradiation for Cancers of the Mouth, Oropharynx, Hypopharynx and Nasopharynx

This is a Phase 2, randomized, double-blind, placebo-controlled, 2-stage trial in subjects with squamous cell cancers of the mouth, oropharynx, hypopharynx and nasopharynx planned to receive standard fractionated IMRT-delivered radiotherapy with concomitant chemotherapy (cisplatin). Informed consent will be obtained from each subject prior to enrollment.
The trial will be performed in 2 stages:
Stage 1 will consist of a blinded parallel group safety study of 4 cohorts in which 24 subjects will be randomized (1:1:1:1) into four equally sized groups to receive one of three doses of EC-18 (500 mg, 1000 mg, 2000 mg; unit dose of 500 mg) or placebo. Stage 2 of the study will evaluate both safety and efficacy.
Stage 2 will consist of eighty (80) subjects who will be randomized in a 1:1 scheme to receive either placebo or 2000 mg of EC-18 as determined by iDSMB in Stage 1.

Start Date03 Jul 2018

Sponsor / Collaborator

ENZYCHEM LIFESCIENCES Corp.

100 Clinical Results associated with Mosedipimod

100 Translational Medicine associated with Mosedipimod

100 Patents (Medical) associated with Mosedipimod

Literatures (Medical) associated with Mosedipimod

01 Jun 2023·Archiv der Pharmazie

Optimized synthesis and pharmacological evaluation of HCN channel inhibitor EC18

Article

Author: Budde, Thomas ; Disse, Paul ; Wiendl, Heinz ; Junker, Anna ; Meuth, Sven G. ; Vinnenberg, Laura ; Oniani, Tengiz ; Zobeiri, Mehrnoush ; Peischard, Stefan ; Seebohm, Guiscard ; Hundehege, Petra ; Patberg, Marius ; Epping, Lisa ; Romanelli, Maria N.

Abstract:

HCN4 channels are considered to be a promising target for cardiac pathologies, epilepsy, and multiple sclerosis. However, there are no subtype‐selective HCN channel blockers available, and only a few compounds are reported to display subtype preferences, one of which is EC18 (cis‐1). Herein, we report the optimized synthetic route for the preparation of EC18 and its evaluation in three different pharmacological models, allowing us to assess its activity on cardiac function, thalamocortical neurons, and immune cells.

01 Dec 2022·BMC cancer

Improving anticancer effect of aPD-L1 through lowering neutrophil infiltration by PLAG in tumor implanted with MB49 mouse urothelial carcinoma

Article

Author: Lee, Hyowon ; Lee, Se Hee ; Kim, Eun Young ; Sohn, Ki-Young ; Kim, Jae Wha ; Shin, Su-Hyun ; Kim, Guen Tae

Abstract:

Background:

The PD-L1 antibody is an immune checkpoint inhibitor (ICI) attracting attention. The third-generation anticancer drug has been proven to be very effective due to fewer side effects and higher tumor-specific reactions than conventional anticancer drugs. However, as tumors produce additional resistance in the host immune system, the effectiveness of ICI is gradually weakening. Therefore, it is very important to develop a combination therapy that increases the anticancer effect of ICI by removing anticancer resistance factors present around the tumor.

Methods :

The syngeneic model was used (n = 6) to investigate the enhanced anti-tumor effect of PD-L1 antibody with the addition of PLAG. MB49 murine urothelial cancer cells were implanted into the C57BL/6 mice subcutaneously. PLAG at different dosages (50/100 mpk) was daily administered orally for another 4 weeks with or without 5 mpk PD-L1 antibody (10F.9G2). PD-L1 antibody was delivered via IP injection once a week.

Results:

The aPD-L1 monotherapy group inhibited tumor growth of 56% compared to the positive group, while the PLAG and aPD-L1 co-treatment inhibited by 89%. PLAG treatment effectively reduced neutrophils infiltrating localized in tumor and converted to a tumor microenvironment with anti-tumor effective T-cells. PLAG increased tumor infiltration of CD8 positive cytotoxic T-cell populations while effectively inhibiting the infiltration of neoplastic T-cells such as CD4/FoxP3. Eventually, neutrophil-induced tumor ICI resistance was resolved by restoring the neutrophil-to-lymphocyte ratio to the normal range. In addition, regulation of cytokine and chemokine factors that inhibit neutrophil infiltration and increase the killing activity of cytotoxic T cells was observed in the tumors of mice treated with PLAG + aPD-L1.

Conclusions:

PLAG effectively turned the tumor-promoting microenvironment into a tumor-suppressing microenvironment. As a molecule that increases the anti-tumor effectiveness of aPD-L1, PLAG has the potential to be an essential and effective ICI co-therapeutic agent.

01 Sep 2022·Biochemical and biophysical research communications

PLAG co-treatment increases the anticancer effect of Adriamycin and cyclophosphamide in a triple-negative breast cancer xenograft mouse model

Article

Author: Lee, Hyowon ; Kim, Eun Young ; Lee, Se Hee ; Sohn, Ki-Young ; Kim, Jae Wha ; Shin, Su-Hyun ; Kim, Guen Tae

Chemotherapy induces tumor cell death and inhibits tumor progression, but the accompanying immune responses in the surrounding dying tissue cause significant inflammation. These responses, such as excessive neutrophil infiltration into tumor tissue, are the main causes of resistance to anticancer treatment. The development of drugs that reduce neutrophil infiltration into tumors is necessary to increase the anticancer effect of chemotherapy. Here, we show that the antitumor effect of the chemotherapy AC regimen (Adriamycin and cyclophosphamide) was increased by 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG) cotreatment in the MDA-MB-231 triple-negative breast cancer xenograft mouse model. Tumor growth was inhibited up to 56% in mice treated with AC and inhibited up to 94% in mice cotreated with AC and PLAG. Side effects of chemotherapy, such as a reduction in body weight, were alleviated in mice cotreated with AC and PLAG. Excessive neutrophil infiltration caused by the AC regimen was successfully cleared in mice cotreated with AC and PLAG. We conclude that PLAG inhibits excessive neutrophil infiltration that aids tumor growth. Reduced neutrophils and increased lymphocytes in PLAG-treated mice can maximize the antitumor effect of the AC regimen and inhibit tumor growth.

News (Medical) associated with Mosedipimod

28 Mar 2024

·www.pharmaceutical-technology.com

ReAlta signs deal with NIAID to develop drug for radiation poisoning

Acute radiation syndrome occurs when a person is exposed to high levels of ionising radiation, usually within a short period. Credit: Crystal Eye Studio via Shutterstock. US-based pharma company ReAlta Life Sciences has teamed up with the US National Institute of Allergy and Infectious Diseases (NIAID) to evaluate its acute radiation syndrome (ARS) drug RLS-0071 (PIC1-01). Scientists at the Armed Forces Radiobiology Research Institute (AFRRI), with support from the Radiation and Nuclear Countermeasures Program (RNCP) at NIAID, will assess RLS-0071’s effectiveness in reducing gastrointestinal damage from ARS using a mouse model in preclinical research collaboration. ARS is a severe condition that occurs when a person is exposed to high levels of ionising radiation, usually within a short period. Symptoms can vary depending on the dose and duration of exposure but typically include nausea, vomiting, diarrhoea, and in severe cases, damage to the gastrointestinal tract. Symptoms worsen as the radiation exposure increases. RLS-0071, ReAlta’s leading candidate, is a 15 amino acid peptide conjugated with polyethylene glycol (PEG) and acts by targeting the complement C1q. The drug has received investigational new drug (IND) clearance by the US Food and Drug Administration (FDA) for treating acute exacerbations of chronic obstructive pulmonary disease and acute graft-versus-host disease, and also holds IND clearance, orphan drug designation, and fast track designation for hypoxic-ischemic encephalopathy (HIE), as well as an orphan drug designation from the European Medicines Agency. In the announcement accompanying the collaboration, ReAlta’s chief scientific officer Neel Krishna said: “The anti-inflammatory, dual mechanism-of-action of RLS-0071 enables the rapid inhibition of both complement activation and neutrophil effectors that are key initiators of deadly inflammation in ARS.” See Also: Sorrento Therapeutics gets grant for transdermal drug delivery device with microneedle assembly and reservoir Eli Lilly and Co gets grant for patent granted for nasal drug delivery device In July 2023, Pluri signed a three-year contract worth $4.2m with the NIAID and the US Department of Defense (DoD) to develop its cell therapy avoplacel (PLX-R18) to treat haematopoietic ARS or radiation poisoning. The same month, RedHill Biopharma received additional funds worth $1.7m from the US Government to advance the development of Yeliva (opaganib) as a medical countermeasure for gastrointestinal ARS. Other drugs currently under development for acute radiation sickness include South Korea-based Enzychem Lifesciences’ Phase II mosedipimod (EC-18), and New Amsterdam Sciences’ Phase I small molecule NAS-150 (AEOL-10150).

Fast TrackOrphan DrugPhase 1Phase 2Radiation Therapy

12 Jul 2023

·www.pharmaceutical-technology.com

Israeli company bags $4.2m contract to develop cell therapy for radiation poisoning

The US FDA has approved avoplacel’s Investigational New Drug application (IND) and granted it an orphan drug designation for the treatment of radiation sickness in nuclear events. Image Credit: Bohdan Populov / Shutterstock. Israel-based Pluri has signed a three-year $4.2m contract with the US National Institute of Allergy and Infectious Diseases (NIAID) and the US Department of Defense (DoD) to develop its cell therapy avoplacel (PLX-R18) to treat haematopoietic acute radiation syndrome or radiation poisoning. The funding is expected to support avoplacel’s development until marketing approval has been granted by the US Food and Drug Administration (FDA), as per an 11 July announcement. Following that, there are plans to purchase avoplacel as a radiation exposure countermeasure for the US Strategic National Stockpile. Avoplacel is an intramuscular treatment composed of human placenta-derived stromal cells. It is intended to be administered 48 or more hours following exposure to radiation to help counteract radiation’s effect and boost bone marrow and blood cell recovery. The FDA has approved avoplacel’s investigational new drug (IND) application and granted it an orphan drug designation for the treatment of radiation sickness in nuclear events. Pluri CEO Yaky Yanay said: “The current time calls for us to accelerate the development and accessibility of radiation treatments, especially as geopolitical instability rises, and nuclear power plants face the threat of warfare. “Through this strategic contract with NIAID, we believe that we can realise our mission of making PLX-R18 (avoplacel) readily available for emergency preparedness.” Other drugs currently under development for acute radiation sickness include Enzychem Lifesciences’ mosedipimod, New Amsterdam Sciences’ NAS-150, and Statera Biopharma’s entolimod. Avoplacel’s study data In animal model studies, avoplacel showed a marked improvement in survival rates of 97% in the treatment group versus 29% in the control group following exposure to radiation. When used prophylactically, 24 hours to 72 hours before exposure, it resulted in survival rates of 74% and 4% in the treatment and control groups, respectively. There was also an increase in blood cell counts, including white blood cells, platelets, neutrophils, and lymphocytes, which are severely decreased because of radiation sickness. Human studies of avoplacel in patients with incomplete hematopoietic recovery following haematopoietic cell transplantation reported an increase in blood counts and a decreased need for repeated blood transfusions over a 12-month period.

Orphan DrugDrug ApprovalClinical ResultCell TherapyRadiation Therapy

25 Jul 2022

·www.biospace.com

Enzychem Lifesciences Announces Poster Presentation of EC-18 at the Radiation Research Society 2022 Annual Meeting

July 25, 2022 12:00 UTC ENGLEWOOD CLIFFS, N.J.--(BUSINESS WIRE)--Enzychem Lifesciences, Corp (KOSDAQ: 183490), a late-stage biopharmaceutical company, announced today the acceptance of a poster presentation at the Radiation Research Society (RRS) 2022 Annual Meeting, which will be held in Waikoloa, Hawaii on October 16-19, 2022. The abstract highlights the radio-mitigative potential of its lead investigational compound, EC-18 in gastrointestinal acute radiation syndrome. The details of the presentation are as follows: Presentation Title: “Mitigation of gastrointestinal acute radiation syndrome by 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol via inhibition of necroptosis in mice" Presenters: Drs. Yong Jae Kim and Jinseon Jeong Date/Time: Wednesday, October 19, 17:15-18:30 HAST (11:15-12:30 ET) Session: Radioprotection/Biodosimetry “We are excited to present our results at the 2022 RRS conference, that support EC-18’s unique mechanism of action to potentially treat gastrointestinal acute radiation syndrome,” said Ki Young Sohn, CEO & Chairman of Enzychem Lifesciences. Based on these results, EC-18 has shown an effect on histopathological improvement of intestinal tissues, leading to functional restoration of the gastrointestinal tract.” About Enzychem Lifesciences Enzychem Lifesciences (KOSDAQ: 183490) is a clinical-stage biopharmaceutical company focused on developing oral small molecule therapies for patients with unmet medical needs in oncology, metabolic and inflammatory diseases. EC-18 acts as an immunomodulator, facilitating the resolution of inflammation and early return to homeostasis. Enzychem is headquartered in South Korea, with an office in the United States. For more information, please visit

Small molecular drug

100 Deals associated with Mosedipimod

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Respiratory Distress Syndrome, Adult	Phase 2	US	ENZYCHEM LIFESCIENCES Corp.	30 Apr 2021
COVID-19	Phase 2	KR	ENZYCHEM LIFESCIENCES Corp.	28 May 2020
Mouth Neoplasms	Phase 2	US	ENZYCHEM LIFESCIENCES Corp.	03 Jul 2018
Stomatitis	Phase 2	US	ENZYCHEM LIFESCIENCES Corp.	03 Jul 2018
Advanced breast cancer	Phase 2	KR	ENZYCHEM LIFESCIENCES Corp.	30 Oct 2017
Advanced cancer	Phase 2	KR	ENZYCHEM LIFESCIENCES Corp.	30 Oct 2017
Chemotherapy-Induced Febrile Neutropenia	Phase 2	KR	ENZYCHEM LIFESCIENCES Corp.	30 Oct 2017
Nonalcoholic Steatohepatitis	Phase 1	-	ENZYCHEM LIFESCIENCES Corp.	-
Arthritis, Gouty	Preclinical	US	ENZYCHEM LIFESCIENCES Corp.	20 Apr 2020
Sepsis	Preclinical	KR	ENZYCHEM LIFESCIENCES Corp.	08 Jul 2015

Clinical Result

Indication

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Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03200340 (ASCO2022)	Phase 2	Head and Neck Neoplasms	105	EC-18 500 mg	xunczflihc(hkaqyijfwi) = rxmlcltauy avkaddwrlb (ftfemqcprc ) View more	-	02 Jun 2022
				EC-18 1000 mg	xunczflihc(hkaqyijfwi) = jewizopldt avkaddwrlb (ftfemqcprc ) View more
ASCO2015	Not Applicable	Uterine Cervical Dysplasia	48	PLAG	jyxstpjrqj(sokuqvrusx) = there was a tendency that the PLAG group was comprised of relatively mild CIN whereas the control group was comprised of those with more severe CIN gzlosumjyb (afmprgkufw )	-	20 May 2015
				1-Pamitoyl-2-Linoleoyl-3-Acetyl-rac-Glycerol (PLAG) (Control)

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