Circadin® 2mg prolonged-release melatonin formulation, approved for use (up to 13 weeks) in treatment of primary insomnia characterized by poor quality of sleep in patients aged 55 years or over.
Circadin® has been approved by several agencies globally, including the European Medicines Agency (EMA), the Australian Therapeutic Goods Administration (TGA), the Swiss Agency for Therapeutic Products (SwissMedic) and the Israeli Ministry of Health (MOH). The approval is based on clinical studies demonstrating positive effects on sleep quality, sleep induction, and most importantly next day alertness and functioning.
Products in Clinical Phase
Piromelatine is a novel compound under development for the treatment of insomnia associated with pain.
Piromelatine is a melatonin agonist, serotonin 5-HT-1A and 5-HT-1D agonist. The compound binds to the MT1, 2 and 3 receptors which govern the body’s sleep-wake cycle and circadian rhythm. The sleep promoting, analgesic, anti-diabetic, antihypertensive, anti-neurodegenerative, anxiolytic and antidepressant effects of Piromelatine have been demonstrated in a series of relevant animal models.
Piromelatine is a multi-facet drug addressing a wide range of potential indications including, but not limited to, insomnia, IBS, neuropathy and fibromyalgia.
Neurim has recently completed a phase-II clinical trial to assess the efficacy and safety of Piromelatine in patients with primary insomnia.
Neu-P11, a novel melatonin agonist, inhibits weight gain and improves insulin sensitivity in high-fat/high-sucrose-fed rats.
She M, Deng X, Guo Z, Laudon M, Hu Z, Liao D, Hu X, Luo Y, Shen Q, Su Z, Yin W. Pharmacol Res. 2009 Apr;59(4):248-53. Read more
Antidepressant- and anxiolytic effects of the novel melatonin agonist Neu-P11 in rodent models. Acta Pharmacol Sin.
Tian SW, Laudon M, Han L, Gao J, Huang FL, Yang YF, Deng HF. 2010 Jul;31(7):775-83. Read more
Cardiovascular effects of melatonin receptor agonists.
Paulis L, Simko F, Laudon M. Expert Opin Investig Drugs. 2012;21(11):1661-78. Read more
Neu-120 is a highly potent and selective uncompetitive NMDA receptor modulator aimed at reducing levodopa-induced dyskinesia. It also inhibits MAO-B and GSK-3B activities in vitro, but does not interact with other receptors, transporters or enzymes. Neu-120 has been developed as adjunct therapy to levodopa in Parkinson’s disease patients with motor fluctuations and in patients who do not tolerate optimal doses of levodopa. It has completed a Phase I study in healthy volunteers and Phase Ia in patients.
Products in Preclinical Phase
Neu-240 is a highly potent and selective uncompetitive NMDA receptor modulator aimed at improving motor control. Neu-240 is intended for use as adjunct therapy to levodopa in patients with Parkinson’s disease and is currently at the preclinical stage.
Neu-P12 is a multi-facetted new chemical entity with analgesic potential. It inhibits Nav1.7/1.3 (neuronal) sodium channels.
Neu-P12 does not interact with COX 1 or 2 or opioid receptors, suggesting a selective mode of action. It demonstrates a good potential for the treatment of inflammatory and neuropathic pain in three different and relevant animal pain models.
Neu-P12 is intended as a therapy for neuropathic pain and is currently in at the preclinical stage.
Neu-105 / Neu-164
Neurim Pharmaceuticals has developed several drug candidates intended for respiratory disease inhibitors.
Neu-164, our lead compound, is an inhibitor of 5-lipoxygenase, a strong antioxidant and myeloperoxidase inhibitor (an oxidizing neutrophiles enzyme.
Neu-164 is developed by the inhalation route to allow dose reduction and to minimize systemic side effects. Neu-164 has very low absorption rate and fast elimination, suggesting a very good safety profile.
In preclinical efficacy studies Neu-164 was found to reduce airways eosinophilia and hyperresponsiveness in ovalbumin-challenged in mice and rats asthma models. In addition, Neu-164 was tested in acute smoking model in mice and was found to reduce significantly the number of bronchoalveolar lavage fluid (BALF) neutrophils as well as IL-6 and IL-8 BALF levels. Neu-164 is well tolerated in inhalation toxicology studies.
Neu-164 shows a great potential as an asthma and COPD drug candidate in terms of both safety and efficacy.
Neu-164 and Neu-107, two novel anti-oxidant and anti-myeloperoxidase compounds, inhibit acute cigarette smoke-induced lung inflammation.
Thatcher TH, Hsiao HM, Pinner E, Laudon M, Pollock SJ, Sime PJ, Phipps RP. Am J Physiol Lung Cell Mol Physiol. 2013 May 17. Read more