[Translation] Safety, pharmacokinetic and pharmacodynamic characteristics of single and multiple administrations of rasagiline mesylate transdermal patch in Chinese healthy subjects and comparison of PK/PD characteristics with rasagiline mesylate tablets

第一部分：PK/PD探索研究 1)评价甲磺酸雷沙吉兰透皮贴剂给药一周（4天/贴+3天/贴）的安全性。 2)评价甲磺酸雷沙吉兰透皮贴剂给药一周（4天/贴+3天/贴）的药代动力学和药效动力学特征。 3)比较甲磺酸雷沙吉兰透皮贴剂与甲磺酸雷沙吉兰片的药代动力学和药效动力学特征。 4)评价甲磺酸雷沙吉兰透皮贴剂给药后的黏附性、刺激性和致敏性。第二部分：多次给药生物利用度研究 1)比较甲磺酸雷沙吉兰透皮贴剂与甲磺酸雷沙吉兰片在健康人体内连续给药的相对生物利用度。 2)比较甲磺酸雷沙吉兰透皮贴剂与甲磺酸雷沙吉兰片多次给药的药效动力学特征。 3)评价甲磺酸雷沙吉兰透皮贴剂和甲磺酸雷沙吉兰片多次给药的安全性。 4)评价甲磺酸雷沙吉兰透皮贴剂多次给药的黏附性、刺激性和致敏性。第三部分：不同部位生物利用度研究 1)比较甲磺酸雷沙吉兰透皮贴剂不同部位给药的生物利用度。 2)评价甲磺酸雷沙吉兰透皮贴剂的安全性、黏附性、刺激性和致敏性。

[Translation]

Part I: PK/PD Exploratory Study 1) Evaluate the safety of rasagiline mesylate transdermal patch for one week (4 days/patch + 3 days/patch). 2) Evaluate the pharmacokinetic and pharmacodynamic characteristics of rasagiline mesylate transdermal patch for one week (4 days/patch + 3 days/patch). 3) Compare the pharmacokinetic and pharmacodynamic characteristics of rasagiline mesylate transdermal patch and rasagiline mesylate tablets. 4) Evaluate the adhesion, irritation and sensitization of rasagiline mesylate transdermal patch after administration. Part II: Multiple-dose bioavailability study 1) Compare the relative bioavailability of rasagiline mesylate transdermal patch and rasagiline mesylate tablets after continuous administration in healthy humans. 2) Compare the pharmacodynamic characteristics of rasagiline mesylate transdermal patch and rasagiline mesylate tablets after multiple administration. 3) Evaluate the safety of multiple administration of rasagiline mesylate transdermal patch and rasagiline mesylate tablets. 4) Evaluate the adhesion, irritation and sensitization of multiple administration of rasagiline mesylate transdermal patch. Part III: Bioavailability study at different sites 1) Compare the bioavailability of rasagiline mesylate transdermal patch at different sites. 2) Evaluate the safety, adhesion, irritation and sensitization of rasagiline mesylate transdermal patch.

Start Date05 Feb 2025

Sponsor / Collaborator

Shanghai Shiling Pharmaceutical Co., Ltd.

[+1]

CTR20243770

/ CompletedNot Applicable

甲磺酸雷沙吉兰片在健康受试者中空腹与餐后条件下开放、随机、单次给药、两制剂、两序列、四周期完全重复交叉设计生物等效性试验

[Translation] An open, randomized, single-dose, two-formulation, two-sequence, four-period fully repeated crossover bioequivalence study of rasagiline mesylate tablets in healthy subjects under fasting and fed conditions

研究空腹与餐后状态下单次口服受试制剂（甲磺酸雷沙吉兰片，规格1mg，浙江九洲生物医药有限公司持证）与参比制剂（甲磺酸雷沙吉兰片，规格1mg，商品名安齐来，Teva Pharmaceutical Industries Ltd.持证）在健康受试者体内的药代动力学特征，比较受试制剂与参比制剂的生物等效性，并研究药物在健康受试者体内的安全性。

[Translation]

To study the pharmacokinetic characteristics of the test preparation (Rasagiline Mesylate Tablets, specification 1 mg, licensed by Zhejiang Jiuzhou Biotechnology Co., Ltd.) and the reference preparation (Rasagiline Mesylate Tablets, specification 1 mg, trade name Anqilai, licensed by Teva Pharmaceutical Industries Ltd.) after a single oral dose in healthy subjects under fasting and fed conditions, compare the bioequivalence of the test preparation and the reference preparation, and study the safety of the drug in healthy subjects.

Start Date05 Nov 2024

Sponsor / Collaborator

Zhejiang Jiuzhou Pharmaceutical Technology Co Ltd.

CTIS2024-512311-41-00

/ Not yet recruitingPhase 1

- UECHUP-RAS/24-2

Start Date04 Jun 2024

Sponsor / Collaborator-

100 Clinical Results associated with Rasagiline mesylate

100 Translational Medicine associated with Rasagiline mesylate

100 Patents (Medical) associated with Rasagiline mesylate

1,062

Literatures (Medical) associated with Rasagiline mesylate

01 Dec 2025·MOLECULAR BIOLOGY REPORTS

Molecular pathways: the quest for effective MAO-B inhibitors in neurodegenerative therapy

Review

Author: Udi, Onoriode Andrew ; Ogbutor, Udoji Godsday ; Atere, Adedeji David ; Oyovwi, Mega Obukohwo ; Joseph, Gregory Uchechukwu

Neurodegenerative diseases like Parkinson's and Alzheimer's are a global health challenge due to their progressive degeneration, leading to cognitive decline and motor dysfunction. Monoamine oxidase B (MAO-B) enzyme is implicated in neurodegeneration, and developing inhibitors could be a promising therapeutic strategy. This review explores MAO-B activity molecular pathways, evaluates MAO-B inhibitors in neurodegenerative therapy, identifies challenges, and suggests future research directions. This review synthesizes findings from a range of scientific literature, including experimental studies, clinical trials, and biochemical analyses that focus on the role of MAO-B in neurodegeneration. Information was gathered from databases such as PubMed, Scopus, and Web of Science, ensuring a comprehensive overview of recent advancements in MAO-B inhibition strategies. The review reveals several promising MAO-B inhibitors that have demonstrated efficacy in preclinical models, as well as some that have progressed to clinical trials. Compounds such as rasagiline and selegiline have shown neuroprotective effects and benefits in symptom management in patients with Parkinson's disease. Furthermore, the review discusses novel inhibitors that target specific molecular pathways, enhancing the potential for improved therapeutic outcomes. However, several inhibitors also present challenges regarding their selectivity, side effects, and long-term efficacy. Research on MAO-B inhibitors for neurodegenerative diseases is crucial, with ongoing studies aiming for selective, potent molecules with fewer side effects and multimodal therapies.

01 May 2025·MOVEMENT DISORDERS

Update on Treatments for Parkinson's Disease Motor Fluctuations – An International Parkinson and Movement Disorder Society Evidence‐Based Medicine Review

Review

Author: Perez Lloret, Santiago ; Swinnen, Bart E.K.S. ; Mestre, Tiago A. ; de Bie, Rob M.A. ; Costa, João ; Aquino, Camila ; Katzenschlager, Regina ; Peball, Marina ; Dijk, Joke M. ; Kauppila, Linda Azevedo ; Coelho, Miguel ; Fox, Susan H. ; Bruno, Veronica ; Spijker, René ; Heim, Beatrice ; Seppi, Klaus ; Sampaio, Cristina ; Lin, Chin‐Hsien ; Litvan, Irene ; Lim, Shen‐Yang ; Tan, Ai Huey ; Silverdale, Monty A.

Abstract:

Objective:

To update evidence‐based medicine recommendations for treating motor fluctuations of Parkinson's disease (PD).

Background:

The International Parkinson and Movement Disorder Society (MDS) Evidence Based Medicine in Movement Disorders Committee recommendations for the treatments of PD were first published in 2002 and regularly updated. The current review uses a new methodology, including the Cochrane Risk of Bias tool and a modified version of GRADE (Grading of Recommendations, Assessment, Development, and Evaluations).

Methods:

On January 1, 2023, a literature search was conducted without date limit in the MEDLINE, Embase, and Cochrane databases using the following search terms: Parkinson disease, levodopa and, for the Embase database, randomized controlled trial (RCT). The inclusion criteria for studies were: patients with PD, on oral levodopa therapy, experiencing motor fluctuations, investigating an intervention that was (commercially) available in at least one country, study design RCT, and with a follow‐up duration of at least 3 months.

Results:

A total of 102 studies were included. Levodopa extended release, pramipexole immediate release and extended release, ropinirole immediate release, rotigotine, opicapone, safinamide, and bilateral subthalamic nucleus deep brain stimulation (DBS) were assessed as efficacious, and continuous intestinal levodopa infusion, continuous subcutaneous levodopa, continuous subcutaneous apomorphine, ropinirole prolonged release, ropinirole patch, entacapone, rasagiline, istradefylline, amantadine extended release, zonisamide, bilateral globus pallidus DBS, and pallidotomy were assessed as likely efficacious for the treatment of motor fluctuations in people with PD who are already being treated with levodopa.

Conclusions:

There are several treatment options that can improve motor fluctuations in PD. These recommendations will assist physicians and patients in determining which intervention to use. © 2025 The Author(s). Movement Disorders published by Wiley Periodicals LLC on behalf of International Parkinson and Movement Disorder Society.

11 Apr 2025·ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Integrating Circular Polarized Luminescence and Long Persistent Luminescence in Cu₈ Cage‐Like Clusters via Ligand Engineering

Article

Author: Zhan, Wen‐Wen ; Zhou, Jie ; Li, Yan ; Yang, Yang ; Zheng, Hao ; Wu, Guanyi ; Sun, Di ; Zhang, Chengkai

Abstract:

Copper clusters with diverse luminescent properties are of particular interest. In this study, a series of Cu8 clusters with cage‐like structures was synthesized and characterized. By employing a stepwise ligand engineering strategy that progressively introduced circularly polarized luminescence (CPL) and long persistent luminescence (LPL) properties, we successfully synthesized R/S‐Cu8−Cl, the first copper cluster to demonstrate both CPL and LPL. The CPL originates from the chiral metal core induced by the chiral alkynyl ligand, whereas the LPL is attributed to the inherent properties of chlorine‐modified triphenylphosphine, which is retained and modified after ligation. The polymethyl methacrylate (PMMA) film containing Cu8 clusters displays lifetimes of up to 75.18 ms at room temperature and an afterglow exceeding 1.5 s, marking the longest luminescent lifetime recorded for molecular copper‐cluster‐based materials known to date. Additionally, R/S‐Cu8−Cl shows excitation‐dependent luminescence and variations in luminescence when UV light is switched on and off, highlighting its potential for advanced anti‐counterfeiting applications. This work not only presents innovative cage‐like copper cluster structures but also offers new approaches for designing multifunctional clusters.

News (Medical) associated with Rasagiline mesylate

22 Apr 2025

·www.prnewswire.com

XADAGO/EQUFINA Set to Revolutionize Parkinson's Disease Treatment Landscape | DelveInsight

As a selective monoamine oxidase B (MAO-B) inhibitor, XADAGO offers a unique mechanism of action that complements traditional therapies, potentially improving motor function and reducing "off" time in patients. The increasing prevalence of Parkinson's disease and the growing demand for effective therapies create a substantial market opportunity for XADAGO, particularly in regions with aging populations. LAS VEGAS, April 22, 2025 /PRNewswire/ -- DelveInsight's " XADAGO/EQUFINA Market Size, Forecast, and Market Insight Report" highlights the details around XADAGO/EQUFINA, an inhibitor of monoamine oxidase B (MAO-B) indicated as an adjunctive treatment to levodopa/carbidopa in patients with Parkinson's disease experiencing "off" episodes. The report provides product descriptions, patent details, and competitor products (marketed and emerging therapies) of XADAGO/EQUFINA. The report also highlights the historical and forecasted sales from 2020 to 2034 segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan]. Newron Pharmaceuticals/Eisai/Meiji Seika Pharma's XADAGO/EQUFINA (safinamide) Overview XADAGO is a monoamine oxidase B (MAO-B) inhibitor used alongside levodopa/carbidopa to help manage "off" episodes in individuals with Parkinson's disease. While its exact mode of action in treating Parkinson's is not fully understood, it is thought to work by inhibiting MAO-B, thereby reducing dopamine breakdown. This leads to increased dopamine levels and enhanced dopaminergic activity in the brain. XADAGO contains the active ingredient safinamide in the form of a mesylate salt and is available in 50 mg and 100 mg film-coated oral tablets. Each tablet provides either 65.88 mg or 131.76 mg of safinamide mesylate, equivalent to 50 mg or 100 mg of the safinamide base. The medication is marketed as XADAGO in the United States and Europe and under the name EQUFINA in Japan. Learn more about XADAGO/EQUFINA projected market size for Parkinson's disease @ XADAGO/EQUFINA Market Potential Parkinson's disease is a progressive neurological disorder that mainly impairs movement control. It results from the slow degeneration of dopamine-producing neurons in the brain, especially in the substantia nigra, a region crucial for managing voluntary motor function. According to estimates by DelveInsight, there were 2.7 million diagnosed prevalent cases of Parkinson's disease in the 7MM in 2023, with the United States accounting for around 45% of these cases. While a cure for Parkinson's remains elusive, a combination of pharmacological and non-pharmacological therapies is used to manage symptoms. Physical, occupational, and speech therapies form key components of treatment, and surgical procedures may benefit select patients. Additionally, complementary therapies are sometimes employed to help address particular symptoms. Frequently prescribed medications for Parkinson's include levodopa, dopamine agonists, MAO-B inhibitors, COMT inhibitors, amantadine, anticholinergics, and adenosine A2A antagonists. These treatments primarily target motor symptoms, which are a major concern for those affected. DelveInsight reports that the Parkinson's disease market in the 7MM was valued at USD 3.2 billion in 2023. The market is expected to grow over the forecast period (2020–2034), fueled by the launch of new therapies, increasing prevalence, better access to healthcare, and rising demand for more advanced and effective treatment options. Discover more about the Parkinson's disease market in detail @ Parkinson's Disease Market Report Emerging Competitors of XADAGO/EQUFINA Some of the drugs in the pipeline include Solengepras (Cerevance), Minzasolmin (UCB Biopharma SRL/Novartis), Buntanetap (Annovis Bio), and others. Buntanetap has successfully completed Phase III trials for early-stage Parkinson's disease. Annovis Bio has scheduled a meeting with the FDA in Q1 2025 to determine the development path forward for Buntanetap in the treatment of Parkinson's disease. Buntanetap is also being developed for Alzheimer's disease, Lewy Body Dementia, and other neurodegenerative disorders. In November 2024, Cerevance announced the dosing of the first patient in its pivotal Phase III ARISE trial, evaluating solengepras as a potential adjunctive treatment for Parkinson's disease. Cerevance expects to report topline data in the first half of 2026. In December 2021, UCB partnered with Novartis to globally co-develop and co-commercialize UCB0599, a pioneering alpha-synuclein misfolding inhibitor currently in Phase II clinical trials for Parkinson's disease. To know more about the number of competing drugs in development, visit @ XADAGO/EQUFINA Market Positioning Compared to Other Drugs Key Milestones of XADAGO/EQUFINA In April 2020, Newron Pharmaceutical acknowledged that US WorldMeds, who held the US commercialization rights for the licensed drug, XADAGO, as a sub licensee of Zambon, had entered into a definitive agreement with Supernus Pharmaceuticals under which Supernus would acquire the CNS portfolio of US WorldMeds, including the US rights to XADAGO In November 2019, Eisai announced that it had launched the EQUFINA 50mg tablets for the indication of improvement of the wearing-off phenomenon in patients with Parkinson's disease under treatment with a drug containing levodopa in Japan. Manufacturing and marketing approval of EQUFINA was obtained in September 2019. In April 2017, Eisai Co., Ltd. and Meiji Seika Pharma announced entering into a license agreement for the commercialization of safinamide (development code: ME2125) to treat Parkinson's disease in Japan and Asia. In March 2017, Newron Pharmaceuticals announced the US FDA approval of XADAGO to treat Parkinson's disease as an add-on therapy to levodopa/carbidopa for patients experiencing "off" episodes. In March 2016, Zambon announced a strategic agreement with US WorldMeds to commercialize Newron's lead compound, XADAGO, to treat Parkinson's disease in the US. In February 2015, XADAGO was approved in the European Union as an add-on therapy to levodopa, alone or in combination with other Parkinson's medications, in mid-late stage PD patients with motor fluctuations. XADAGO/EQUFINA Patent Details XADAGO tablets are currently protected by three XADAGO patents with US patent numbers 8,076,515, 8,278,485, and 8,283,380, which expire between June 2027 and December 2028 and are listed in the FDA's publication, Approved Drug Products with Therapeutic Equivalence Evaluations, commonly referred to as the Orange Book. The company has a license agreement with Zambon S.p.A., Newron's partner, related to the XADAGO Patents, and as a new chemical entity, XADAGO is under the 5-year FDA exclusivity period that expires on March 21, 2022. In May 2017, Zambon filed a worldwide patent under the patent number WO2017207587A1. The invention relates to pharmaceutical compositions comprising safinamide and, more particularly, to taste-masked particles comprising said active ingredient or pharmaceutically acceptable salts thereof, oral dosage forms that include said particles, and a process for preparing them. Discover how XADAGO/EQUFINA is shaping the Parkinson's disease treatment landscape @ XADAGO 50mg XADAGO/EQUFINA Market Dynamics XADAGO, marketed as EQUFINA in some regions (notably in South Korea and Japan), is a once-daily oral selective MAO-B inhibitor used as an add-on treatment for Parkinson's disease patients experiencing "off" episodes while on a stable dose of levodopa. The drug's unique dual mechanism of action—MAO-B inhibition and modulation of glutamate release—offers both dopaminergic and non-dopaminergic effects, positioning it as a differentiated product in the PD adjunctive therapy landscape. This has helped it carve a niche in markets where patients are inadequately controlled by levodopa alone, particularly those in mid-to-late-stage PD. The global market dynamics for XADAGO/EQUFINA are shaped by a mix of competitive intensity, regional adoption trends, and payer dynamics. In the U.S. and Europe, the drug has faced stiff competition from generic MAO-B inhibitors (like selegiline and rasagiline) and newer Parkinson's disease therapies, including COMT inhibitors, dopamine agonists, and extended-release levodopa formulations. Despite this, its favorable safety profile and once-daily dosing have supported its uptake in certain patient segments, especially in Europe. Market penetration has been slower in the U.S. due to both reimbursement hurdles and physician preference for more established adjunctive treatments. In Asia, particularly Japan and South Korea, EQUFINA has demonstrated stronger market performance thanks to focused commercial strategies and a high unmet need for effective "off time" management. Meiji Seika Pharma and Eisai, the regional marketing partners, have successfully leveraged the drug's differentiated profile in clinician education, which has led to growing adoption among neurologists. In Japan, where the aging population is rapidly expanding and Parkinson's prevalence is rising, EQUFINA has benefited from both demographic tailwinds and formulary access. Looking ahead, the market outlook for XADAGO/EQUFINA depends on several strategic levers, including lifecycle management, regional partnerships, and real-world evidence generation. The manufacturer's ability to expand into new geographies, secure favorable reimbursement, and differentiate against both generics and newer entrants will be critical. Moreover, as Parkinson's disease treatment moves toward more personalized approaches, XADAGO/EQUFINA may find sustained relevance in specific subpopulations, particularly those requiring a balance of efficacy and tolerability. Dive deeper to get more insight into XADAGO/EQUFINA's strengths & weaknesses relative to competitors @ XADAGO/EQUFINA Market Drug Report Table of Contents Related Reports Parkinson's Disease Market Parkinson's Disease Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key Parkinson's disease companies, including UCB Biopharma SRL, Novartis, Annovis Bio, Supernus Pharmaceuticals, Inc., Britannia Pharmaceutical, Pharma Two B, Mitsubishi Tanabe Pharma (NeuroDerm), AbbVie, Cerevel Therapeutics, Cerevance, among others. Parkinson's Disease Pipeline Parkinson's Disease Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key Parkinson's disease companies, including Cerevel Therapeutics, Inhibikase Therapeutics, Neuraly, Peptron, Biogen, Roche, Brain Neurotherapy Bio, Inc., Modag, Annovis Bio Inc., BioVie Inc., United Neuroscience Ltd., Luye Pharma Group, AbbVie, UCB Biopharma SRL, InnoMedica Schweiz AG, Integrative Research Laboratories AB, H. Lundbeck A/S, Shanghai WD Pharmaceutical Co., Ltd., Cerevance Beta, Inc., Nobilis Therapeutics Inc., BlueRock Therapeutics, Taiwan Mitochondrion Applied Technology Co., Ltd., among others. Cell and Gene Therapy in Parkinson's Disease Market Cell and Gene Therapy in Parkinson's Disease Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key cell and gene therapy in Parkinson's disease companies including MeiraGTx, Hope Biosciences, Sumitomo Pharma, Prevail Therapeutics, BlueRock Therapeutics, Voyager Therapeutics, among others. Parkinson's Disease Psychosis Market Parkinson's Disease Psychosis Market Insights, Epidemiology, and Market Forecast – 2034 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key Parkinson's disease psychosis companies, including Sumitomo Pharma America Inc., Vanda Pharmaceuticals, Acadia Pharmaceuticals Inc., Otsuka America Pharmaceutical, Lundbeck LLC, Jazz Pharmaceuticals, Alkahest Inc., Sandoz, Sio Gene Therapies, Axovant Sciences Ltd, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Phase 3Drug ApprovalLicense out/inPhase 2

05 Dec 2024

·www.globenewswire.com

Pharma Two B Announces Poster Presentation on P2B001 at the Annual Meeting of the Parkinson’s Disease Study Group

Pooled data analysis of efficacy and safety from Phase 2b and Phase 3 data sets in patients with early-stage Parkinson’s disease (PD) support P2B001 as a first line, once-daily treatment choice for early PD KIRYAT ONO, Israel, Dec. 05, 2024 (GLOBE NEWSWIRE) -- Pharma Two B, a private, late-stage pharmaceutical company developing innovative combination drugs for neurological disorders, today announced a poster presentation of integrated safety and efficacy data on P2B001 from its Phase 2b and Phase 3 studies in early-stage Parkinson’s disease (PD) patients. P2B001 is a fixed, low-dose extended-release (ER) combination of pramipexole, 0.6 mg and rasagiline, 0.75 mg. The data are being presented today by Henry Moore, M.D., Associate Professor of Clinical Neurology, University of Miami, Miller School of Medicine, at the Parkinson’s Study Group (PSG) 33rd Annual Meeting in Nashville, TN. “The poster includes robust safety and efficacy data from two double-blind studies, which compared once-daily P2B001 to titrated pramipexole ER (PramiER) or placebo, over a 12-week period,” said Dr. Moore, Associate Professor of Clinical Neurology at the University of Miami and presenter of the study. “P2B001 consistently demonstrated a favorable risk-benefit profile in treating PD symptoms in early-stage patients, compared to the groups receiving other, commercially available therapies. It therefore could be a valuable potential first-line therapy for such patients who are often treated by general neurologists and primary care physicians.” The poster summarizes an integrated modified-ITT analysis of Unified Parkinson’s Disease Rating Scale (UPDRS) results in 196 early-stage PD patients, as follows: P2B001 had significantly greater effect on the UPDRS Part II (Activities of Daily Living, or ADL), Part III (Motor), and Total (Parts II and III) scores versus placebo.P2B001 had comparable efficacy to individually titrated PramiER.P2B001 had significantly less worsening in daytime-sleepiness compared to those treated with PramiER.P2B001 was well-tolerated with an adverse event profile that included fewer sleep-related and dopaminergic adverse events than titrated doses of PramiER. Dan Teleman, CEO of Pharma Two B, added, “These data provide further support for P2B001 as a first-line, once-daily combination pill treatment for people with early PD that requires no titration. Currently, we are focused on completing our merger with Hepion and thereafter look forward to moving P2B001 towards an NDA submission.” About the PSG Annual Conference The 2024 Annual Meeting of the Parkinson Study Group is being held December 5-8, 2024, in Nashville, TN. For over three decades, the PSG Annual Meeting has showcased the organization’s efforts in collaborative research and a commitment to education and mentorship. The meeting welcomes leading investigators, coordinators, trainees, advocates, and allied stakeholders to exchange the latest advances and practices in PD. About Pharma Two B Pharma Two B is a private, late-stage pharmaceutical company. Pharma Two B’s mission is to improve patients’ quality of life by developing innovative, value-added combination drugs for neurological disorders, with a clear unmet need, that are based on previously approved oral drugs and that may offer meaningful clinical benefits, as well as improved safety and enhanced convenience. Pharma Two B’s lead product candidate is P2B001. For more information, please visit: www.pharma2b.com. Pharma Two B plans to go public via a merger transaction (the “Merger”) with Hepion Pharmaceuticals, Inc. (Nasdaq: HEPA) (“Hepion”) in conjunction with the closing of a concurrent private placement. The proposed merger transaction was initially announced on July 22, 2024, and on November 11, 2024, the U.S. Securities and Exchange Commission (“SEC”) declared effective the Company’s registration statement on Form F-4, as amended (the “Registration Statement”) relating to the Merger. The Merger, which has been approved by the respective boards of directors of Pharma Two B and Hepion, is expected to close in the fourth quarter of 2024 and remains subject to approval by both Pharma Two B and Hepion’s respective stockholders, regulatory approval, listing of Pharma Two B’s ordinary shares on Nasdaq under the ticker symbol “PHTB” and other customary closing conditions. About P2B001 P2B001 is an investigational, novel, fixed-dose, extended-release combination of pramipexole and rasagiline (0.6 mg/0.75 mg), both at low doses that are not commercially available. Marketed pramipexole and rasagiline are currently indicated for the treatment of PD (as monotherapy and adjunct therapy for early and more advanced patients). P2B001 is being developed for potential use as a first-line therapy for people with PD. Extended release rasagiline is a new and proprietary formulation of rasagiline developed by Pharma Two B. In a Phase 3 clinical trial, P2B001 demonstrated that it provides benefits comparable with commercially used doses of marketed pramipexole-ER (PramiER) while minimizing associated daytime sleep-related and dopaminergic side effects. Pharma Two B owns worldwide-granted patents for both pharmaceutical composition and method of treatment with P2B001. About Hepion Pharmaceuticals Hepion is a biopharmaceutical company headquartered in Edison, New Jersey, previously focused on the development of drug therapy for treatment of chronic liver diseases. This therapeutic approach targets fibrosis, inflammation, and shows potential for the treatment of hepatocellular carcinoma (“HCC”) associated with non-alcoholic steatohepatitis (“NASH”), viral hepatitis, and other liver diseases. Hepion’s cyclophilin inhibitor, rencofilstat, was being developed to offer benefits to address multiple complex pathologies related to the progression of liver disease. In December 2023, Hepion’s board of directors approved a strategic restructuring plan to preserve capital by reducing operating costs. Additionally, Hepion initiated a process to explore a range of strategic and financing alternatives focused on maximizing stockholder value within the current financial environment and NASH drug development landscape. On April 19, 2024, Hepion announced that it has begun wind-down activities in its ASCEND- NASH clinical trial which wind-down activities have since been completed and the trial has been closed. Hepion is continuing efforts, to the extent that cash is available, to provide any value derived from rencofilstat to its shareholders. Forward-Looking Statements Certain statements in this press release may be considered “forward-looking statements”. Forward-looking statements generally relate to future events or Hepion’s or Pharma Two B’s future financial or operating performance. For example, express or implied statements regarding Hepion and Pharma Two B’s expectations with respect to the Merger, including the timing of the Special Meeting, listing Pharma Two B’s ordinary shares on Nasdaq, receipt of necessary shareholder approvals and the timing of closing of the Merger, and related matters, as well as all other statements other than statements of historical fact included in this press release, are forward-looking statements. When used in this press release, words such as “anticipate,” “believe,” “continue,” “could,” “estimate,” “expect,” “intend,” “may,” “might,” “plan,” “possible,” “potential,” “predict,” “project,” “should,” “would” and similar expressions, as they relate to Hepion or Pharma Two B, identify forward-looking statements. Such forward-looking statements are based on the beliefs of management, as well as assumptions made by, and information currently available to, Hepion’s and Pharma Two B’s management. Actual results could differ materially from those contemplated by the forward-looking statements as a result of certain factors detailed in Hepion’s and Pharma Two B’s filings with the SEC. Most of these factors are outside the control of Hepion and/or Pharma Two B and are difficult to predict. In addition to factors disclosed in Hepion’s and Pharma Two B’s filings with the SEC, the following factors, among others, could cause actual results and the timing of events to differ materially from the anticipated results or other expectations expressed in the forward-looking statements: the risk that the Merger may not be completed in the fourth quarter of 2024 or at all; the inability to meet the closing conditions to the Merger, including the failure of Pharma Two B to meet Nasdaq initial listing standards in connection with the consummation of the Merger; costs related to the Merger and the failure to realize anticipated benefits of the Merger or to realize estimated pro forma results with respect thereto as well as other risks associated with biopharmaceutical companies generally, including the risks of filing an NDA, obtaining regulatory approval for any product candidates, commercialization of any approved product, including P2B001 for PD, as well as the total addressable market and potential for success of P2B001, the presentation of financial information in U.S. GAAP, completion of a PCAOB audit of U.S. GAAP financials, as well as other risks set forth in more detail in the Registration Statement. The forward-looking statements are based upon management’s beliefs and assumptions; and other risks and uncertainties identified in the Registration Statement, including those under “Risk Factors” therein, and in other filings with the SEC made by Hepion. Each of Hepion and Pharma Two B undertake no obligation to update these statements for revisions or changes after the date of press release, except as required by law. No Offer or Solicitation This press release does not constitute an offer to sell or a solicitation of an offer to buy, or the solicitation of any vote or approval in any jurisdiction in connection with the Merger or any related transactions, nor shall there be any sale, issuance or transfer of securities in any jurisdiction where, or to any person to whom, such offer, solicitation or sale may be unlawful. Any offering of securities or solicitation of votes regarding the proposed transaction will be made only by means of a proxy statement/prospectus that complies with applicable rules and regulations promulgated under the Securities Act, and the Securities Exchange Act of 1934, as amended, or pursuant to an exemption from the Securities Act or in a transaction not subject to the registration requirements of the Securities Act. Additional Information and Where to Find It In connection with the Merger, Pharma Two B filed the Registration Statement with the SEC, which includes a prospectus with respect to its securities to be issued in connection with the Merger, and a definitive proxy statement with respect to Hepion’s stockholder meeting at which Hepion’s stockholders will be asked to vote on the Merger and related matters. The Registration Statement has been declared effective by the SEC and Hepion is mailing a definitive proxy statement and prospectus to its shareholders. Each of Hepion and Pharma Two B urge investors, stockholders, and other interested persons to read, when available, the Registration Statement including the proxy statement/prospectus, any amendments thereto, and any other documents filed with the SEC, before making any voting or investment decision because these documents will contain important information about the Merger. Investors and security holders will be able to obtain free copies of the Registration Statement, the proxy statement prospectus and all other relevant documents filed or that will be filed with the SEC by Pharma Two B or Hepion through the website maintained by the SEC at www.sec.gov. Participants in the Solicitation Pharma Two B and Hepion and their respective directors and executive officers may be deemed to be participants in the solicitation of proxies from Hepion’s stockholders in connection with the Merger. Information about Hepion’s directors and executive officers and their ownership of Hepion’s securities is set forth in Hepion’s filings with the SEC. To the extent that holdings of Hepion’s securities have changed since the amounts printed in Hepion’s Annual Report on Form 10-K/A, such changes have been or will be reflected on Statements of Change in Ownership on Form 4 filed with the SEC. A list of the names of such directors and executive officers and information regarding their interests in the Merger is contained in the proxy statement/prospectus in the Registration Statement. You may obtain free copies of these documents as described in the preceding paragraph. Contact: Pharma Two BDan TelemanCEOPharma Two B Ltd.Cell: + 972-54-550-0804Email: dan@pharma2b.comwww.pharma2b.com U.S. investors Chuck PadalaLifeSci Advisors, LLC+1-917-741-7792chuck@lifesciadvisors.com

Clinical ResultPhase 2Phase 3Acquisition

14 Nov 2024

·www.globenewswire.com

Pharma Two B and Hepion Pharmaceuticals, Inc. Announce Effectiveness of Registration Statement Related to Proposed Merger

Nov. 11, 2024 -- Pharma Two B Ltd. (“Pharma Two B”), a late-clinical stage company that is developing P2B001, an innovative combination product candidate for the treatment of Parkinson’s Disease (“PD”) and Hepion Pharmaceuticals, Inc. (Nasdaq: HEPA) (“Hepion”), a clinical stage biopharmaceutical company that had been developing a treatment for non-alcoholic steatohepatitis (“NASH”), hepatocellular carcinoma (“HCC”), and other chronic liver diseases, today jointly announced that the U.S. Securities and Exchange Commission ("SEC") has declared effective the registration statement on Form F-4 (as amended, the "Registration Statement") filed with the SEC related to Pharma Two B’s merger transaction with Hepion as previously announced on July 22, 2024 (the “Proposed Transaction”). The Proposed Transaction, which has been approved by the respective boards of directors of Pharma Two B and Hepion, is expected to close in the fourth quarter of 2024 and remains subject to approval by both Pharma Two B and Hepion’s respective stockholders, regulatory approval, listing of Pharma Two B’s ordinary shares on Nasdaq under the ticker symbol “PHTB” and other customary closing conditions. Upon the anticipated closing of the Proposed Transaction, the combined company will operate under the “Pharma Two B” name. Hepion also announced that a special meeting (the “Special Meeting”) of its stockholders will be held on December 12, 2024 to approve the Proposed Transaction. The Special Meeting will be held at 9:00 a.m. Eastern Time via live webcast at www.virtualshareholdermeeting.com/HEPA2024SM. Hepion stockholders of record at the close of business on the record date of November 6, 2024 are entitled to vote at the Special Meeting. Hepion filed its definitive proxy statement/prospectus relating to the Proposed Transaction with the SEC and will mail it to stockholders on or about November 8, 2024. More details about the Proposed Transaction and the resolutions to be voted upon at the Special Meeting can be found in the definitive proxy statement/prospectus, available at http://www.sec.gov. Hepion stockholders who need assistance in completing the proxy card, need additional copies of the proxy statement/prospectus, or have questions regarding the Special meeting may contact Hepion’s proxy solicitor, Campaign Management, by calling 1-855-422-1042 or emailing info@campaign-mgmt.com. A.G.P./Alliance Global Partners is serving as financial advisor to Hepion and Sheppard, Mullin, Richter & Hampton LLP is acting as U.S. legal advisor to Hepion and Lipa Meir & Co.is acting as Israeli legal advisor to Hepion. Sullivan & Worcester LLP is serving as legal advisor to A.G.P. Laidlaw & Company (UK) Ltd. is acting as financial advisor to Pharma Two B. and Meitar Law Offices and Goodwin Procter LLP are acting as legal advisors to Pharma Two B. Pharma Two B is a private, late-stage pharmaceutical company. Pharma Two B’s mission is to improve patients’ quality of life by developing innovative, value-added combination drugs for neurological disorders, with a clear unmet need, that are based on previously approved oral drugs and that may offer meaningful clinical benefits, as well as improved safety and enhanced convenience. Pharma Two B’s lead product candidate is P2B001. For more information, please visit: www.pharma2b.com. P2B001 is an investigational, novel, fixed-dose, extended-release combination of pramipexole and rasagiline (0.6 mg/0.75 mg), both at low doses that are not commercially available. Marketed pramipexole and rasagiline are currently indicated for the treatment of PD (as monotherapy and adjunct therapy for early and more advanced patients). P2B001 is being developed for potential use as a first-line therapy for people with PD. Extended release rasagiline is a new and proprietary formulation of rasagiline developed by Pharma Two B. In a Phase 3 clinical trial, P2B001 demonstrated that it provides benefits comparable with commercially used doses of marketed pramipexole-ER (PramiER) while minimizing associated daytime sleep-related and dopaminergic side effects. Pharma Two B owns worldwide-granted patents for both pharmaceutical composition and method of treatment with P2B001. Hepion is a biopharmaceutical company headquartered in Edison, New Jersey, previously focused on the development of drug therapy for treatment of chronic liver diseases. This therapeutic approach targets fibrosis, inflammation, and shows potential for the treatment of hepatocellular carcinoma (“HCC”) associated with non-alcoholic steatohepatitis (“NASH”), viral hepatitis, and other liver diseases. Hepion’s cyclophilin inhibitor, rencofilstat, was being developed to offer benefits to address multiple complex pathologies related to the progression of liver disease. In December 2023, Hepion’s board of directors approved a strategic restructuring plan to preserve capital by reducing operating costs. Additionally, Hepion initiated a process to explore a range of strategic and financing alternatives focused on maximizing stockholder value within the current financial environment and NASH drug development landscape. On April 19, 2024, Hepion announced that it has begun wind-down activities in its ASCEND- NASH clinical trial which wind-down activities have since been completed and the trial has been closed. Hepion is continuing efforts, to the extent that cash is available, to provide any value derived from rencofilstat to its shareholders. The content above comes from the network. if any infringement, please contact us to modify.

Acquisition

100 Deals associated with Rasagiline mesylate

External Link

KEGG	Wiki	ATC	Drug Bank
D02562	Rasagiline mesylate	N04BD02	DB01367

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Parkinson Disease	European Union	Teva Pharmaceuticals Europe BV	21 Feb 2005
Parkinson Disease	Iceland	Teva Pharmaceuticals Europe BV	21 Feb 2005
Parkinson Disease	Liechtenstein	Teva Pharmaceuticals Europe BV	21 Feb 2005
Parkinson Disease	Norway	Teva Pharmaceuticals Europe BV	21 Feb 2005

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Motor Disorders	Phase 3	-	H. Lundbeck A/S	01 Jan 2011
Restless Legs Syndrome	Phase 3	United States	Teva Neuroscience, Inc.	01 Sep 2010
Supranuclear Palsy, Progressive	Phase 3	Germany	Teva Branded Pharmaceutical Products R&D, Inc.	01 Jan 2010
Multiple System Atrophy	Phase 2	United States	H. Lundbeck A/S	01 Dec 2009
Multiple System Atrophy	Phase 2	Austria	H. Lundbeck A/S	01 Dec 2009
Multiple System Atrophy	Phase 2	Canada	H. Lundbeck A/S	01 Dec 2009
Multiple System Atrophy	Phase 2	France	H. Lundbeck A/S	01 Dec 2009
Multiple System Atrophy	Phase 2	Germany	H. Lundbeck A/S	01 Dec 2009
Multiple System Atrophy	Phase 2	Hungary	H. Lundbeck A/S	01 Dec 2009
Multiple System Atrophy	Phase 2	Israel	H. Lundbeck A/S	01 Dec 2009

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03727139 (JapicCTI-184181, Pubmed \| Expert Opin Drug Saf)	Not Applicable	Parkinson Disease	961	Rasagiline 1 mg once daily	rssasvjkxa(nohjelkmbm) = vttjpfxskm ntjkvgetrg (tgqtbzpbqe )	Positive	02 Jan 2024
NCT02789020 (CTgov)	Phase 2	Parkinson Disease	96	functional Magnetic Resonance Imaging+Rasagiline (Rasagiline)	qichkemmdf(uudpcddvvh) = zaryoqveke lbuwhgldod (xaejulsgpi, 0.01) View more	-	06 Sep 2023
				functional Magnetic Resonance Imaging (Placebo)	qichkemmdf(uudpcddvvh) = pblxyhtpnp lbuwhgldod (xaejulsgpi, 0.01) View more
NCT02359552 (R2, CTgov)	Phase 2	Alzheimer Disease	50	Placebo (Placebo)	pznjtqvszv(rzfvqbdzwi) = muwqsxqkvs yzphtckysz (opggxrcygh, 0.030) View more	-	20 Oct 2020
				Rasagiline (Rasagiline)	pznjtqvszv(rzfvqbdzwi) = tumnniyjbq yzphtckysz (opggxrcygh, 0.030) View more
NCT01786603 (CTgov)	Phase 2	Amyotrophic Lateral Sclerosis	80	Rasagiline (Rasagiline)	zyvtimvhyh(arpojdaguv) = ccrolhbxwo hvvjmenude (gljhbqcxet, ylnlkhbelp - cdnsidhjac) View more	-	27 Jan 2020
				Placebo (Placebo)	zyvtimvhyh(arpojdaguv) = xqqzccudql hvvjmenude (gljhbqcxet, pmzskdbqvq - rahuynepxc) View more
BIPARK-I and II (MDS2019)	Not Applicable	Parkinson Disease	-	Opicapone 50mg	cridttobkj(luvzqaapxy) = snvkqtrkdd mwbvxdtwmr (dbkhhflgic ) View more	-	22 Sep 2019
NCT02337764 (CTgov)	Phase 3	Parkinson Disease	222	TVP-1012	cssnvxajdu = sqrexvzxjq ttlkybphse (ypmfwygbnb, pjjutbjsmu - dshazwqano) View more	-	19 Apr 2019
NCT02337725 (Pubmed) Manual	Phase 3	Parkinson Disease	244	Rasagiline	ijltjdcsrx(qvdfejhtup): difference = -6.39 (95% CI, -8.530 to -4.250), P-Value = <0.0001 View more	Positive	01 Mar 2019
				Placebo
NCT02337751 (Pubmed \| J Neural Transm (Vienna))	Phase 3	Parkinson Disease	210	Placebo	zuulawzpcp(eapinrwelp) = fajlclrmny xyrggekhsc (qokpmwycpz ) View more	-	01 Mar 2019
				Rasagiline 1 mg/day	zuulawzpcp(eapinrwelp) = tbfkrsjnij xyrggekhsc (qokpmwycpz ) View more
NCT02337738 (CTgov)	Phase 2/3	Parkinson Disease	404	Placebo	oudhknsphe(oveltpkuof) = eilfnnpwgr jbeljccldg (ytgoxhyaar, 0.167) View more	-	28 Feb 2019
NCT02337751 (CTgov)	Phase 3	Parkinson Disease	198	Placebo+TVP-1012 (Placebo + TVP-1012 Group)	nhxajwlszr = cnxwzflqjr vajpdwxsnb (pjaazkaovo, qzutvjguek - glhpkpnagi) View more	-	28 Feb 2019
				TVP-1012 (TVP-1012 + TVP-1012 Group)	nhxajwlszr = ynwshmoill vajpdwxsnb (pjaazkaovo, dfasohcsht - hwyybcfrwn) View more

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