Type | Private |
---|---|
Industry | Pharmaceutical |
Predecessor | Antalium and NeuroCeptor through merger |
Founded | 2004 |
Headquarters | Montreal, Quebec [1] , Canada |
Key people | Louis Lamontagne (President, 2004- ) [1] [2] |
Number of employees | 45 (2007) [1] |
PainCeptor Pharma is a private Canadian company focused on the development of drugs that act outside the central nervous system on nociceptors to treat pain. [3] The company was established in 2004 through the merger of two academic spinout firms: Antalium from McGill University and NeuroCeptor from Queens University. [4] [5] At its inception, the company's primary operations were in Montreal and Kingston, [5] and it established a partnership with the Danish company NeuroSearch as part of its birth. [2]
The company's strategic focus was on peripheral rather than central-acting therapeutics is an attempt to avoid the known side effects of existing central-acting agents. [6] The primary molecular targets addressed by PainCeptor are members of the ASIC ion channel family and nerve growth factor (NGF) and NGF receptors. [6] In 2006, the company secured funding from the Canadian Industrial Research Assistance Program. [7] In 2007, the company raised C$24.4 million in venture capital funding in anticipation of starting first-in-man clinical trials that year; an initial round of funding had been secured in 2004 in the amount of C$23 million. [1] [2] As of 2007, the company conducted research out of the Steacie Institute for Molecular Sciences, a facility of Canada's National Research Council located in Ottawa, Quebec. [1]
Although PainCeptor refers to itself as a biopharmaceutical company on its website, [3] its two primary publicly reported drug discovery projects aim to deliver small molecule therapeutics. [6] According to AdisInsight, a drug information platform published by Springer Nature, the small-molecule antagonists program discontinued in 2009; [8] while development of a separate drug, PPC-5650 (an ASIC channel antagonist) had been discontinued by 2016. [9]
According to one source, in 2006 the company was granted patent protection on antagonists of each of these receptor types. [10] Inspection of the patent applications, though, shows that no patents were, in fact, granted. In regard to US2005282840A1 "Methods of modulating neurotrophin-mediated activity", the application status was revised to 'abandoned' in 2009; [11] a second patent application, US2007123514A1, bearing the same title has also been noted to be 'abandoned' as of 2010. [12] Likewise, in regard to US2008004282A1 "Compositions and methods for modulating gated ion channels", the application status was revised to 'abandoned' in 2010. [13] Still another patent application was 'abandoned' in 2011, US2009082368A1 "Methods of Modulating Neurotrophin-mediated Activity". [14] One patent was actually granted to the firm, US2007191418A1 "Compositions and methods for modulating gated ion channels", in 2007; this patent transferred ownership to Aros Pharma in 2010, who subsequently did not keep up payment of maintenance fees, resulting in the status changing to 'lapsed' in 2018. [15]
Novartis AG is a Swiss multinational pharmaceutical corporation based in Basel, Switzerland. Consistently ranked in the global top five, Novartis is one of the largest pharmaceutical companies in the world and was the fourth largest by revenue in 2022.
Neurotrophins are a family of proteins that induce the survival, development, and function of neurons.
Montelukast, sold under the brand name Singulair among others, is a medication used in the maintenance treatment of asthma. It is generally less preferred for this use than inhaled corticosteroids. It is not useful for acute asthma attacks. Other uses include allergic rhinitis and hives of long duration. For allergic rhinitis it is a second-line treatment.
Tropomyosin receptor kinase A (TrkA), also known as high affinity nerve growth factor receptor, neurotrophic tyrosine kinase receptor type 1, or TRK1-transforming tyrosine kinase protein is a protein that in humans is encoded by the NTRK1 gene.
The transient receptor potential cation channel subfamily V member 1 (TRPV1), also known as the capsaicin receptor and the vanilloid receptor 1, is a protein that, in humans, is encoded by the TRPV1 gene. It was the first isolated member of the transient receptor potential vanilloid receptor proteins that in turn are a sub-family of the transient receptor potential protein group. This protein is a member of the TRPV group of transient receptor potential family of ion channels. And a receptor being clearly present in bacteria, the oldest organisms on Earth known to express phosphatidylethanolamine, the precursor to endocannabinoids, in their cytoplasmic membranes, and fatty acid metabolites with affinity for this CB receptor are produced by cyanobacteria, which diverged from eukaryotes at least 2000 million years ago (MYA).
Dezocine, sold under the brand name Dalgan, is an atypical opioid analgesic which is used in the treatment of pain. It is used by intravenous infusion and intramuscular injection.
Trk receptors are a family of tyrosine kinases that regulates synaptic strength and plasticity in the mammalian nervous system. Trk receptors affect neuronal survival and differentiation through several signaling cascades. However, the activation of these receptors also has significant effects on functional properties of neurons.
Acid-sensing ion channel 3 (ASIC3) also known as amiloride-sensitive cation channel 3 (ACCN3) or testis sodium channel 1 (TNaC1) is a protein that in humans is encoded by the ASIC3 gene. The ASIC3 gene is one of the five paralogous genes that encode proteins that form trimeric acid-sensing ion channels (ASICs) in mammals. The cDNA of this gene was first cloned in 1998. The ASIC genes have splicing variants that encode different proteins that are called isoforms.
Flupirtine is an aminopyridine that functions as a centrally acting non-opioid analgesic that was originally used as an analgesic for acute and chronic pain but in 2013 due to issues with liver toxicity, the European Medicines Agency restricted its use to acute pain, for no more than two weeks, and only for people who cannot use other painkillers. In March 2018, marketing authorisations for flupirtine were withdrawn following a European Medicines Agency recommendation based on the finding that the restrictions introduced in 2013 had not been sufficiently followed in clinical practice, and cases of serious liver injury still occurred including liver failure.
Kavain is the main kavalactone found mostly in the roots of the kava plant.
Acid-sensing ion channels (ASICs) are neuronal voltage-insensitive sodium channels activated by extracellular protons permeable to Na+. ASIC1 also shows low Ca2+ permeability. ASIC proteins are a subfamily of the ENaC/Deg superfamily of ion channels. These genes have splice variants that encode for several isoforms that are marked by a suffix. In mammals, acid-sensing ion channels (ASIC) are encoded by five genes that produce ASIC protein subunits: ASIC1, ASIC2, ASIC3, ASIC4, and ASIC5. Three of these protein subunits assemble to form the ASIC, which can combine into both homotrimeric and heterotrimeric channels typically found in both the central nervous system and peripheral nervous system. However, the most common ASICs are ASIC1a and ASIC1a/2a and ASIC3. ASIC2b is non-functional on its own but modulates channel activity when participating in heteromultimers and ASIC4 has no known function. On a broad scale, ASICs are potential drug targets due to their involvement in pathological states such as retinal damage, seizures, and ischemic brain injury.
Christian Karsten Hansen is a Danish biotechnology entrepreneur, investor and inventor, with work in new drugs, molecular biology and biochemistry.
Zucapsaicin (Civanex) is a medication used to treat osteoarthritis of the knee and other neuropathic pain. It is applied three times daily for a maximum of three months. Zucapsaicin is a member of phenols and a member of methoxybenzenes It is a modulator of transient receptor potential cation channel subfamily V member 1 (TRPV-1), also known as the vanilloid or capsaicin receptor 1 that reduces pain, and improves articular functions. It is the cis-isomer of capsaicin. Civamide, manufactured by Winston Pharmaceuticals, is produced in formulations for oral, nasal, and topical use.
Naldemedine is a medication that is used for the treatment of opioid-induced constipation in adults with chronic non-cancer pain. It is a peripherally acting μ-opioid receptor antagonist and was developed by Shionogi. Clinical studies have found it to possess statistically significant effectiveness for these indications and to be generally well tolerated, with predominantly mild to moderate gastrointestinal side effects. Effects indicative of central opioid withdrawal or impact on the analgesic or miotic effects of co-administered opioids have only been observed in a small number of patients.
Ospemifene is an oral medication indicated for the treatment of dyspareunia – pain during sexual intercourse – encountered by some women, more often in those who are post-menopausal. Ospemifene is a selective estrogen receptor modulator (SERM) acting similarly to an estrogen on the vaginal epithelium, building vaginal wall thickness which in turn reduces the pain associated with dyspareunia. Dyspareunia is most commonly caused by "vulvar and vaginal atrophy."
Funapide (INN) is a novel analgesic under development by Xenon Pharmaceuticals for the treatment of a variety of chronic pain conditions, including osteoarthritis, neuropathic pain, postherpetic neuralgia, and erythromelalgia, as well as dental pain. It acts as a small-molecule Nav1.7 and Nav1.8 voltage-gated sodium channel blocker. Funapide is being evaluated in humans in both oral and topical formulations, and as of July 2014, has reached phase IIb clinical trials.
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SB-366791 is a drug which acts as a potent and selective blocker of the TRPV1 ion channel. It has analgesic effects in animal studies, and is used in research into pain and inflammation.
Newly formed PainCeptor Pharma Corp. brings together two small Canadian pain companies, each of which was focused on a different target. NeuroCeptor Inc., a spinout from Queens University, was studying the role of neurotrophins, specifically nerve growth factor (NGF), in pain, Antalium Inc., a spinout from McGill University....
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