Chalcones and Mannich bases are a group of compounds known for their cytotoxicities. In this study restricted chalcone analogue, compound 2-(4-hydroxybenzylidene)-2,3-dihydroinden-1-one MT1, was used as a starting compound to synthesize new mono Mannich bases since Mannich bases may induce more cytotoxicity than chalcone analogue that they are derived from by producing additional alkylating center for cellular thiols. In this study, cyclic and acyclic amines were used to synthesize Mannich bases. All compounds were tested against Ca9-22 (gingival carcinoma), HSC-2, HSC-3 and HSC-4 (oral squamous cell carcinoma) as tumour cell lines and HGF (gingival fibroblasts), HPC (pulp cells) and HPLF (periodontal ligament fibroblasts) human normal oral cells as non tumour cell lines. Cytotoxicity, selectivity index (SI) values and potency selectivity expression (PSE) values expressed as a percentage were determined for the compounds. According to data obtained, the compound MT8 with the highest PSE value bearing N-methylpiperazine moiety seems to be a good candidate to develop new cytotoxic compounds and is suited for further investigation.

Pharmaceutics

Novel Transethosomal Gel Containing Miconazole Nitrate; Development, Characterization, and Enhanced Antifungal Activity

Article

Author: Gad, Heba A. ; Sajid-ur-Rehman, Muhammad ; Asghar, Zara ; Jamshaid, Usama ; Jamshaid, Talha

Miconazole nitrate (MCNR) is a BCS class II antifungal drug with poor water solubility. Although numerous attempts have been made to increase its solubility, formulation researchers struggle with this significant issue. Transethosomes are promising novel nanocarriers for improving the solubility and penetration of drugs that are inadequately soluble and permeable. Thus, the objective of this study was to develop MCNR-loaded transethosomal gel in order to enhance skin permeation and antifungal activity. MCNR-loaded transethosomes (MCNR-TEs) were generated using the thin film hydration method and evaluated for their zeta potential, particle size, polydispersity index, and entrapment efficiency (EE%). SEM, FTIR, and DSC analyses were also done to characterize the optimized formulation of MCNR-TEs (MT-8). The optimized formulation of MCNR-TEs was incorporated into a carbopol 934 gel base to form transethosomal gel (MNTG) that was subjected to ex vivo permeation and drug release studies. In vitro antifungal activity was carried out against Candida albicans through the cup plate technique. An in vivo skin irritation test was also performed on Wistar albino rats. MT-8 displayed smooth spherical transethosomal nanoparticles with the highest EE% (89.93 ± 1.32%), lowest particle size (139.3 ± 1.14 nm), polydispersity index (0.188 ± 0.05), and zeta potential (−18.1 ± 0.10 mV). The release profile of MT-8 displayed an initial burst followed by sustained release, and the release data were best fitted with the Korsmeyer-Peppas model. MCNR-loaded transethosomal gel was stable and showed a non-Newtonian flow. It was found that ex vivo drug permeation of MNTG was 48.76%, which was significantly higher than that of MNPG (plain gel) (p ≤ 0.05) following a 24-h permeation study. The prepared MCNR transethosomal gel exhibited increased antifungal activity, and its safety was proven by the results of an in vivo skin irritation test. Therefore, the developed transethosomal gel can be a proficient drug delivery system via a topical route with enhanced antifungal activity and skin permeability.

News (Medical) associated with REC-0559

27 Jan 2022

·mimetech.eu

“Udonitrectag” receives orphan drug designation from the European Commission as treatment in solid organ transplantation

On 15/11/2021, orphan designation (EU/3/21/2521) was granted by the European Commission to MIMETECH S.r.l., Italy, for Udonitrectag as treatment in solid organ transplantation. When organs are transplanted, the period in which they are cut off from their normal blood supply can lead to damage and death of cells that means they work less well after transplantation and are prone to inflammation that increases the risk of rejection. The medicine acts in the same way as natural growth factors that help to protect cells from this type of damage. This is expected to improve the function of the transplanted organ and reduce the risk of rejection. At the time of submission of the application for orphan designation the effects of the medicine had been evaluated in experimental models and no clinical trials in patients undergoing solid organ transplantation had been started.

Orphan Drug

05 Dec 2018

·mimetech.eu

Recordati receives Orphan Drug Designation for its investigational treatment for neurotrophic keratitis

Recordati today announced that the FDA has granted Orphan Drug Designation to Recordati Rare Disease’s investigational product REC 0559 for the treatment of neurotrophic keratitis. REC 0559 is a low molecular weight non-peptidic human nerve growth factor (NGF) mimetic currently under global development by Recordati. REC 0559 was licensed in 2017 from MimeTech, an Italian based company focused on the development of pharmaceutical applications for synthetic neurotrophin mimetics. Neurotrophic keratitis is a rare degenerative corneal disease, which in its more severe forms affects less than one person out of 10,000 worldwide, and it results from a deficiency of the trigeminal nerve or its branches, usually caused by surgery, neoplasia, aneurysm or facial trauma. Impairment or loss of corneal sensory innervation is responsible for corneal epithelial defects, ulcer, and perforation, with a progression of the disease leading to dramatic impairment to patients’ sight. Orphan drug designation applies to drugs that seek to treat rare diseases or conditions affecting fewer than 200,000 patients in the U.S. while providing a significant therapeutic advantage over existing therapies. The designation can provide development and commercial incentives for designated compounds and medicines, including eligibility for a seven-year period of market exclusivity in the U.S. after product approval, FDA assistance in clinical trial design and an exemption from FDA user fees. “Orphan drug designation is a key regulatory achievement in the global development of REC 0559. We are very pleased to receive the designation from US FDA, which confirms our continuous commitment to innovative treatments to address the needs of patients suffering from rare diseases”, stated Andrea Recordati, CEO. “This represents another significant step in the development of our business dedicated to the treatment of diseases with unmet medical needs.”

Orphan Drug

01 Feb 2015

·mimetech.eu

“Udonitrectag” receives orphan drug designation from the European Commission for the treatment of neurotrophic keratitis

On 16/12/2014, orphan designation (EU/3/14/1400) was granted by the European Commission to MIMETECH S.r.l., Italy, for (1S,4R,5R,7S)-3,4-dibenzyl-2-oxo-6,8-dioxa-3-azabyciclo[3.2.1]octane-7-carboxylic acid-L-lysine for the treatment of neurotrophic keratitis. Patients with neurotrophic keratitis have lower than normal levels of growth factors that are normally supplied by the trigeminal nerve and which play an important role in the growth and survival of the cells of the cornea. The medicine is a compound that can mimic the action of a growth factor called nerve growth factor. When given as eye drops to patients with neurotrophic keratitis, the medicine is expected to help restore some of the normal growth processes in the eye and reduce the damage to the cornea associated with the condition. The effects of the medicine have been evaluated in experimental models.

Orphan Drug

100 Deals associated with REC-0559

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Keratitis	Phase 2	United States	Recordati Rare Diseases, Inc.	13 Oct 2020
Keratitis	Phase 2	France	Recordati Rare Diseases, Inc.	13 Oct 2020
Keratitis	Phase 2	Germany	Recordati Rare Diseases, Inc.	13 Oct 2020
Keratitis	Phase 2	Hungary	Recordati Rare Diseases, Inc.	13 Oct 2020
Keratitis	Phase 2	Italy	Recordati Rare Diseases, Inc.	13 Oct 2020
Keratitis	Phase 2	Spain	Recordati Rare Diseases, Inc.	13 Oct 2020
Keratitis	Phase 2	United Kingdom	Recordati Rare Diseases, Inc.	13 Oct 2020
Neurotrophic keratitis	Phase 2	-	MimeTech SRL	-
Anemia, Sickle Cell	IND Application	-	MimeTech SRL	-
Dry Eye Syndromes	IND Application	-	MimeTech SRL	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Biosimilar

Competitive landscape of biosimilars in different countries/locations. Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

AI Agents Built for Biopharma Breakthroughs

Accelerate discovery. Empower decisions. Transform outcomes.

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis