COMT

HANGZHOU, China, Aug. 15, 2024. Vimgreen Pharmaceuticals, a science-driven pharmaceutical company focused on the modulation of adenosine signaling, announced today the completion of enrollment of its Phase 2 clinical trial of VG081821AC, a novel adenosine A2A receptor (A2AR) antagonist that also functions as an inverse A2AR agonist, for the treatment of early-to-mid stage Parkinson's disease. A total of 150 participants have been enrolled and randomized into one of three cohorts, a high-dose VG081821 group, a low-dose VG081821 group, and a placebo group at a ratio of 1:1:1. The 12-week Phase 2 trial is a multicenter, randomized, placebo-controlled, double-blind study to investigate the safety and efficacy of VG081821 as monotherapy in early-to-mid stage PD patients. The primary endpoint was the difference of change from baseline in movement disorder society-unified Parkinson's disease rating scale (MDS-UPDRS) part III (motor symptoms) score between VG081821 and placebo over the 12 weeks of administration. For PD patients, current therapies are mainly dependent on dopamine replacement strategies with L-Dopa (top choice), dopamine agonists, MAO-B inhibitors and COMT inhibitors. These medicines either increase dopamine levels or mimic dopamine function. However, despite L-Dopa's efficacy in reducing the motor symptoms of PD, the onset of motor complications (wearing-off, ON–OFF, dyskinesia) is almost inevitable with long-term treatment. It is a well-known limit of the dopamine replacement therapy. In addition, the current therapies for PD are only symptomatic treatments. These therapies are unable to slow down the progression of PD. As an A2AR antagonist, which works non-dopaminergically, VG081821 has the potential to avoid, decrease or delay motor complications (wearing-off, ON–OFF, dyskinesia) if used early. What's special about VG081821 is that it is not only a highly potent A2A antagonist, but also a highly potent A2A receptor inverse agonist. More than a classical A2A antagonist, VG081821 may have extra therapeutic effect and greater efficacy on motor dysfunction in PD. Furthermore, VG081821 may provide not only symptomatic benefits, but also disease modifying benefits. VG081821 is expected to bring better treatment options and clinical benefits for PD patients. "In most previous trials of A2A antagonists for the treatment of Parkinson's Disease, A2A antagonists were used as an add-on treatment to alleviate off episodes in combination with L-Dopa for advanced PD patients. Although it has led to the approval of Istradefylline in US and Japan, it is not the best use of A2A antagonists for PD treatment," stated Sanxing Sun, President and Chief Executive Officer of Vimgreen. "VG081821 is to be used as monotherapy for improving movements in early-to-mid stage of PD. Later on, as the disease progresses, it can be used in combination with low doses of L-Dopa. This L-dopa sparing effect may minimize the problem of L-Dopa and prolong the quality of life of PD patients." It is known that A2AR gene expression in human peripheral blood mononuclear cells (PBMCs) are higher for PD patients. In the current Phase 2 trial of VG081821, the A2AR gene expression levels in PBMCs are to be analyzed. The potential correlation between drug efficacy and A2AR expression level may make VG081821 a precision medicine. The Phase 2 trial is to be completed in November. About VG081821AC VG081821AC/VG081821 is a potent, selective antagonist of adenosine A2A receptor (A2AR) developed by Vimgreen. Adenosine A2A receptors are distributed across basal ganglia, in particular in the striatum, and are believed to be involved in the regulation of motor functions. This makes A2AR an attractive non-dopaminergic target to treat the disease. VG081821 is an innovative A2AR antagonist that is not only a highly potent A2A antagonist, but also a highly potent A2A receptor inverse agonist. It is expected to bring better treatment options and clinical benefits for PD patients. About Vimgreen Pharmaceuticals Vimgreen is a science-driven pharmaceutical company located in the beautiful city of Hangzhou, China. At Vimgreen, the research programs are focused on the modulation of adenosine signaling. Adenosine is a major signaling molecule that is involved in a variety of critical physiological processes via activation of the adenosine receptors (A1, A2A, A2B or A3), including regulation of the nervous system, immune response, vascular function, and metabolism. In recent years, substantial progress has been made to understand the role of adenosine signaling in different pathologies during disease progression. These efforts have identified therapeutic possibilities for the treatment of various diseases, by either replenishing or inhibiting relevant adenosine signaling pathways. Currently Vimgreen has two compounds in clinical development. One is VG081821, an A2AR antagonist for the treatment of Parkinson's Disease. The other compound is VG290131, an A3 agonist for the treatment of NASH. Forward Looking Statements Certain statements in this press release may be considered forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995. Words such as "believes", "expects", "may", "will", "should", "potential" or the negative of these words or other comparable terminology (as well as other words or expressions referencing future events, conditions or circumstances) are intended to identify forward-looking statements. Forward-looking statements are predictions, projections and other statements about future events that are based on current expectations and assumptions and, as a result, are subject to risks and uncertainties. Many factors could cause actual future events to differ materially from the forward-looking statements in this press release, including, without limitation, those risks associated with Vimgreen's ability to execute on its commercial strategy. Forward-looking statements speak only as of the date when made. Vimgreen does not assume any obligation to publicly update or revise any forward-looking statements, whether as a result of new information, future events or otherwise, except as required by law. SOURCE Vimgreen Pharmaceuticals Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

HANGZHOU, China, Aug. 15, 2024 /PRNewswire/ -- Vimgreen Pharmaceuticals, a science-driven pharmaceutical company focused on the modulation of adenosine signaling, announced today the completion of enrollment of its Phase 2 clinical trial of VG081821AC, a novel adenosine A2A receptor (A2AR) antagonist that also functions as an inverse A2AR agonist, for the treatment of early-to-mid stage Parkinson's disease. A total of 150 participants have been enrolled and randomized into one of three cohorts, a high-dose VG081821 group, a low-dose VG081821 group, and a placebo group at a ratio of 1:1:1. The 12-week Phase 2 trial is a multicenter, randomized, placebo-controlled, double-blind study to investigate the safety and efficacy of VG081821 as monotherapy in early-to-mid stage PD patients. The primary endpoint was the difference of change from baseline in movement disorder society-unified Parkinson's disease rating scale (MDS-UPDRS) part III (motor symptoms) score between VG081821 and placebo over the 12 weeks of administration. For PD patients, current therapies are mainly dependent on dopamine replacement strategies with L-Dopa (top choice), dopamine agonists, MAO-B inhibitors and COMT inhibitors. These medicines either increase dopamine levels or mimic dopamine function. However, despite L-Dopa's efficacy in reducing the motor symptoms of PD, the onset of motor complications (wearing-off, ON–OFF, dyskinesia) is almost inevitable with long-term treatment. It is a well-known limit of the dopamine replacement therapy. In addition, the current therapies for PD are only symptomatic treatments. These therapies are unable to slow down the progression of PD. As an A2AR antagonist, which works non-dopaminergically, VG081821 has the potential to avoid, decrease or delay motor complications (wearing-off, ON–OFF, dyskinesia) if used early. What's special about VG081821 is that it is not only a highly potent A2A antagonist, but also a highly potent A2A receptor inverse agonist. More than a classical A2A antagonist, VG081821 may have extra therapeutic effect and greater efficacy on motor dysfunction in PD. Furthermore, VG081821 may provide not only symptomatic benefits, but also disease modifying benefits. VG081821 is expected to bring better treatment options and clinical benefits for PD patients. "In most previous trials of A2A antagonists for the treatment of Parkinson's Disease, A2A antagonists were used as an add-on treatment to alleviate off episodes in combination with L-Dopa for advanced PD patients. Although it has led to the approval of Istradefylline in US and Japan, it is not the best use of A2A antagonists for PD treatment," stated Sanxing Sun, President and Chief Executive Officer of Vimgreen. "VG081821 is to be used as monotherapy for improving movements in early-to-mid stage of PD. Later on, as the disease progresses, it can be used in combination with low doses of L-Dopa. This L-dopa sparing effect may minimize the problem of L-Dopa and prolong the quality of life of PD patients." It is known that A2AR gene expression in human peripheral blood mononuclear cells (PBMCs) are higher for PD patients. In the current Phase 2 trial of VG081821, the A2AR gene expression levels in PBMCs are to be analyzed. The potential correlation between drug efficacy and A2AR expression level may make VG081821 a precision medicine. The Phase 2 trial is to be completed in November. About VG081821AC VG081821AC/VG081821 is a potent, selective antagonist of adenosine A2A receptor (A2AR) developed by Vimgreen. Adenosine A2A receptors are distributed across basal ganglia, in particular in the striatum, and are believed to be involved in the regulation of motor functions. This makes A2AR an attractive non-dopaminergic target to treat the disease. VG081821 is an innovative A2AR antagonist that is not only a highly potent A2A antagonist, but also a highly potent A2A receptor inverse agonist. It is expected to bring better treatment options and clinical benefits for PD patients. About Vimgreen Pharmaceuticals Vimgreen is a science-driven pharmaceutical company located in the beautiful city of Hangzhou, China. At Vimgreen, the research programs are focused on the modulation of adenosine signaling. Adenosine is a major signaling molecule that is involved in a variety of critical physiological processes via activation of the adenosine receptors (A1, A2A, A2B or A3), including regulation of the nervous system, immune response, vascular function, and metabolism. In recent years, substantial progress has been made to understand the role of adenosine signaling in different pathologies during disease progression. These efforts have identified therapeutic possibilities for the treatment of various diseases, by either replenishing or inhibiting relevant adenosine signaling pathways. Currently Vimgreen has two compounds in clinical development. One is VG081821, an A2AR antagonist for the treatment of Parkinson's Disease. The other compound is VG290131, an A3 agonist for the treatment of NASH. Forward Looking Statements Certain statements in this press release may be considered forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995. Words such as "believes", "expects", "may", "will", "should", "potential" or the negative of these words or other comparable terminology (as well as other words or expressions referencing future events, conditions or circumstances) are intended to identify forward-looking statements. Forward-looking statements are predictions, projections and other statements about future events that are based on current expectations and assumptions and, as a result, are subject to risks and uncertainties. Many factors could cause actual future events to differ materially from the forward-looking statements in this press release, including, without limitation, those risks associated with Vimgreen's ability to execute on its commercial strategy. Forward-looking statements speak only as of the date when made. Vimgreen does not assume any obligation to publicly update or revise any forward-looking statements, whether as a result of new information, future events or otherwise, except as required by law. SOURCE Vimgreen Pharmaceuticals

Neurocrine has ongoing partnerships with the likes of Takeda, Idorsia, Voyager and Xenon, and has often been viewed as a hot M&A target. Soon, the firm will have a new CEO. Neurocrine Biosciences’ dealmaking prospects may soon get another round of attention with the installment of a new CEO.  More than three decades after founding Neurocrine in 1992, Kevin Gorman, Ph.D., will retire as the neuroscience specialist’s CEO, the company said Tuesday. Effective October 11, the biotech’s current chief business development and strategy officer, Kyle Gano, Ph.D., will take over the reins as the new CEO. Gorman, who has been Neurocrine’s CEO since 2008, worked the company to the commercial stage in 2017 with the FDA approval of Ingrezza. With indications in tardive dyskinesia and involuntary movements in Huntington’s disease, Ingrezza is today a fast-growing blockbuster with sales expected to surpass $2 billion this year. The paucity of commercial-stage neuroscience biotechs has made Neurocrine a regular name on Wall Street’s M&A watch lists. The revenue stream from Igrezza means Neurocrine has the firepower to buy things for itself, and a fast-growing product would give any larger buyer an immediate top-line boost. An IPO in 1996 helped Neurocrine raise $34 million, and today, the California biotech carries a market value of about $13.5 billion. The closest Neurocrine has come to being bought out likely happened in 2019. That year, Michel Vounatsos, then CEO at fellow neuroscience giant Biogen, planned to take over Neurocrine to ease the potential risk of what would later become the ill-fated Alzheimer’s disease drug Aduhelm, Stat reported earlier. Vounatsos rallied support from the entire Biogen exec team, but the plan was shot down by the company’s board. Biogen likely isn’t targeting any major neuroscience purchases these days, as new CEO Chris Viehbacher focuses more on immunology rather than the risky field of neurology. Neurocrine actually partnered up on its second commercial product, endometriosis therapy Orilissa, which it licensed to AbbVie in 2010. The following year, Gano, who originally joined in 2001 in a market research and analytics capacity, became Neurocrine’s chief business development officer. Business development has yielded success at Neurocrine but also brought the company’s most dramatic setback. Back in 2006, Neurocrine’s stock price crashed below its IPO price after Pfizer walked out on a partnership following an FDA rejection of the former partners’ investigational insomnia drug, indiplon. Last year, Neurocrine returned the North American rights to the struggling Parkinson’s disease med Ongentys to its licenser, Portuguese company Bial. Neurocrine paid $30 million upfront for the COMT inhibitor in 2017. And after an approval in April 2020, the drug couldn’t attract enough traction. Today, partnerships remain a key element in Neurocrine’s business. The company has a multi-candidate collaboration with Takeda. One of the programs failed in a phase 2 trial last year in patients with anhedonia in major depressive disorder (MDD), while another recently delivered a positive mid-stage trial readout in adjunctive MDD. Other than that, Neurocrine has tapped Mitsubishi Tanabe Pharma to run Ingrezza in Japan. It also boasts a sodium channel inhibitor pact with Xenon Pharmaceuticals and a gene therapy collaboration with Voyager Therapeutics. Further, the company bought a calcium channel blocker from Idorsia. Neurocrine is also working with Nxera Pharma, previously known as Sosei Heptares, to develop muscarinic receptor agonists for a range of neurological disorders. As Gorman put it in a Tuesday statement, now is “the right time to initiate this well-planned leadership transition.” He praised Gano for being instrumental in Neurocrine’s success and an “exceptional leader” of the organization. Gano is the lead inventor on the patent to the valbenazine molecule that forms Ingrezza. Besides the licensing deals mentioned above, Gano also oversaw the 2022 acquisition of Diurnal Group, which gave Neurocrine a pipeline targeting chronic endocrine conditions and a presence in Europe. A top priority at Neurocrine these days is crinecerfont, for which the company recently completed FDA submissions for the treatment of pediatric and adult patients with classic congenital adrenal hyperplasia. The company has already started building a commercial team around the drug, even though it expects the FDA will ask for an advisory committee meeting. Gorman will continue to serve on Neuroncrine’s board, on which Gano has been named a new member.